Literature for peptidase S08.039: PCSK9 peptidase

Summary Gene structure Alignment Tree Sequences Sequence features Distribution Structure Literature Substrates Pharma

(Topics flags: A Assay, S Structure, T Target, P Specificity, K Knockout, V Review, M Mutation, R Splicing, I Inhibitor. To select only the references relevant to a single topic, click the link above. See explanation.)

2026

Alanazi,M., Al-Kuraishy,H.M., Hussain,N.R., Waheed,H.J., Al-Gareeb,A.I., Albuhadily,A.K., Waheeb,T.S. and Batiha,G.E. Targeting of PCSK9 in the Management of Alzheimer's Disease: Expanding the New Potential Key Player Drug Dev Res (2026) 87, e70231-e70231. PubMed Europe PubMed DOI
Kaur,S., Panjwani,D., Singh,S., Banerjee,S., Wadehra,S., Kaur,A. and Singh,T.G. Molecular mechanisms of PCSK9 in cardiology: therapeutic implications and clinical impacts on the cardiorenal axis Mol Cell Biochem (2026) PubMed Europe PubMed DOI
Kulshreshtha,A. and Bhatnagar,S. Impact of loss-of-function variations of PCSK9 on LDLR interaction and dynamics: Implications for heart function Biochem Biophys Res Commun (2026) 799, 153224-153224. PubMed Europe PubMed DOI
Lim,G.B. PCSK9 inhibition for primary prevention of cardiovascular events Nat Rev Cardiol (2026) 23, 6-6. PubMed Europe PubMed DOI

2025

Chen,X., Sun,M., Ma,X., Ma,Y. and Chen,B. Silencing hepatic PCSK9 via novel chimeric AAV8 mitigates the progression of atherosclerosis by inhibiting inflammation in ApoE(-/-) mice Mol Ther Methods Clin Dev (2025) 33, 101390-101390. PubMed Europe PubMed DOI PMC EPMC
Cui,Y.F., Chen,X.C., Mijiti,T., Abudurusuli,A., Deng,L.H., Ma,X. and Chen,B. PCSK9 with a gain of function D374Y mutation aggravates atherosclerosis by inhibiting PPARalpha expression Sci Rep (2025) 15, 6941-6941. PubMed Europe PubMed DOI PMC EPMC
Duddu,S., Katakia,Y.T., Suresh,N., Chakrabarti,R., Majumder,S. and Shukla,P.C. Vitamin D attenuates PCSK9-driven phenotypic switch of vascular smooth muscle cells and neointimal hyperplasia via SIRT6 activation Biochim Biophys Acta Mol Basis Dis (2025) 1872, 168135-168135. PubMed Europe PubMed DOI K
Fan,G., Guo,W., Lu,J., He,Y., Zha,J., Zhang,Q., Chen,Y., Tan,D., Tang,Z., Yang,J., Yu,Z. and Liu,M. CADD-engineered peptide protacs efficiently target PCSK9 for hypercholesterolemia in vivo Metabolism (2025) 176, 156485-156485. PubMed Europe PubMed DOI
Gu,B., Li,M., Li,D. and Huang,K. CRISPR-Cas9 Targeting PCSK9: A Promising Therapeutic Approach for Atherosclerosis J Cardiovasc Transl Res (2025) PubMed Europe PubMed DOI
Jaafar,A.K., Paulo-Ramos,A., Rastoldo,G., Veeren,B., Planesse,C., Bringart,M., Rondeau,P., Chemello,K., Meilhac,O., Lambert,G.C. and Bourane,S. PCSK9 deficiency promotes the development of peripheral neuropathy JCI Insight (2025) PubMed Europe PubMed DOI
Koren,M.J., Vega,R.B., Agrawal,N., Xu,Y., Barbour,A.M., Yu,H., Wallerstedt,E., Carter,D., Middlemiss,J., Twaddle,L., McCarthy,M.C. and Rosenmeier,J.B. An Oral PCSK9 Inhibitor for Treatment of Hypercholesterolemia: The PURSUIT Randomized Trial J Am Coll Cardiol (2025) PubMed Europe PubMed DOI I
Martini,E. Epigenetic silencing of PCSK9 enables durable reduction of low-density lipoprotein cholesterol Nat Cardiovasc Res (2025) 4, 347-347. PubMed Europe PubMed DOI
Nowacka,A., Sniegocki,M. and Ziolkowska,E.A. PCSK9 Regulation of Lipid Metabolism in the Nervous System: Implications for Schwann Cell Function and Peripheral Neuropathy Cells (2025) 14 PubMed Europe PubMed DOI PMC EPMC V
Sun,P., Han,F., Li,X., Wu,C., Deng,T., He,J., Zhang,C. and Kuai,R. Silencing PCSK9 reshapes the spatiotemporal activation of STING for safe and effective cancer immunotherapy Nat Commun (2025) PubMed Europe PubMed DOI K
Suswidiantoro,V., Puteri,M.U., Kato,M., Ariestanti,D.M., James,R.J. and Saputri,F.C. The Roles of PCSK9 in Alzheimer's Disease: A Systematic Review of Clinical, Genetic, and Preclinical Evidence Life (Basel) (2025) 15 PubMed Europe PubMed DOI PMC EPMC
Tremblay,F., Xiong,Q., Shah,S.S., Ko,C.W., Kelly,K., Morrison,M.S., Giancarlo,C., Ramirez,R.N., Hildebrand,E.M., Voytek,S.B., El Sebae,G.K., Wright,S.H., Lofgren,L., Clarkson,S., Waters,C., Linder,S.J., Liu,S., Eom,T., Parikh,S., Weber,Y., Martinez,S., Malyala,P., Abubucker,S., Friedland,A.E., Maeder,M.L., Lombardo,A., Myer,V.E. and Jaffe,A.B. A potent epigenetic editor targeting human PCSK9 for durable reduction of low-density lipoprotein cholesterol levels Nat Med (2025) PubMed Europe PubMed DOI
Wang,D., Yang,X., Chen,Y., Gong,K., Yu,M., Gao,Y., Wu,X., Hu,H., Liao,C., Han,J. and Duan,Y. Correction: Ascorbic acid enhances low-density lipoprotein receptor expression by suppressing proprotein convertase subtilisin/kexin 9 expression J Biol Chem (2025) 301, 108269-108269. PubMed Europe PubMed DOI
Wang,Y., Cao,S., Wang,Z., Li,C., Ye,J., Liu,Y., Jin,T., Zhou,Y., Su,W. and Zong,G. PCSK9 affects vascular senescence through the SIRT1 pathway Exp Gerontol (2025) 201, 112701-112701. PubMed Europe PubMed DOI
Wang,Z., Yu,X., Ma,H., Yao,S., Li,Z., Zhang,R., Liang,H. and Jiao,J. Proprotein convertase subtilisin/kexin type 9 contributes to cisplatin-induced acute kidney injury by interacting with cyclase-associated protein 1 to promote megalin lysosomal degradation Biochim Biophys Acta Mol Cell Res (2025) 1872, 119984-119984. PubMed Europe PubMed DOI
Zhang,Y., Su,W., Ji,X., Yang,Z., Guan,Q., Pang,Y., Zhong,L., Wang,Y. and Xiang,J. PCSK9 promotes progression of anaplastic thyroid cancer through E-cadherin endocytosis Cell Death Dis (2025) 16, 362-362. PubMed Europe PubMed DOI PMC EPMC

2024

Agarwala,A., Asim,R. and Ballantyne,C.M. Oral PCSK9 Inhibitors Curr Atheroscler Rep (2024) 26, 147-152. PubMed Europe PubMed DOI V I
Aldworth,H. and Hooper,N.M. Post-translational regulation of the low-density lipoprotein receptor provides new targets for cholesterol regulation Biochem Soc Trans (2024) 52, 431-440. PubMed Europe PubMed DOI PMC EPMC
Arsh,H., Manoj Kumar,F., Simran,F., Tamang,S., Rehman,M.U., Ahmed,G., Khan,M., Malik,J. and Mehmoodi,A. Role of PCSK9 inhibition during the inflammatory stage of SARS-COV-2: an updated review Ann Med Surg (Lond) (2024) 86, 899-908. PubMed Europe PubMed DOI PMC EPMC
Azar,Y., Ludwig,T.E., Le Bon,H., Strom,T.B., Bluteau,O., Di-Filippo,M., Carrie,A., Chtioui,H., Beliard,S., Marmontel,O., Fonteille,A., Gebhart,M., Peretti,N., Moulin,P., Ferrieres,J., Pradignac,A., Farnier,M., Gallo,A., Yelnik,C., Blom,D., Genin,E., Bogsrud,M.P., Leren,T.P., Boileau,C., Abifadel,M., Rabes,J.P. and Varret,M. The singular French PCSK9-p.Ser127Arg gain-of-function variant: A significant player in cholesterol levels from a 775-year-old common ancestor Atherosclerosis (2024) 399, 118596-118596. PubMed Europe PubMed DOI
Bao,H., Wang,X., Zhou,H., Zhou,W., Liao,F., Wei,F., Yang,S., Luo,Z. and Li,W. PCSK9 regulates myofibroblast transformation through the JAK2/STAT3 pathway to regulate fibrosis after myocardial infarction Biochem Pharmacol (2024) 220, 115996-115996. PubMed Europe PubMed DOI
Bao,X., Liang,Y., Chang,H., Cai,T., Feng,B., Gordon,K., Zhu,Y., Shi,H., He,Y. and Xie,L. Targeting proprotein convertase subtilisin/kexin type 9 (PCSK9): from bench to bedside Signal Transduct Target Ther (2024) 9, 13-13. PubMed Europe PubMed DOI PMC EPMC V
Cappelluti,M.A., Mollica Poeta,V., Valsoni,S., Quarato,P., Merlin,S., Merelli,I. and Lombardo,A. Durable and efficient gene silencing in vivo by hit-and-run epigenome editing Nature (2024) 627, 416-423. PubMed Europe PubMed DOI PMC EPMC
Chackerian,B. and Remaley,A.T. PCSK9 vaccines: a promising new strategy for the treatment of hypercholesterolemia? J Lipid Res (2024) 65, 100524-100524. PubMed Europe PubMed DOI PMC EPMC
Charbe,N.B., Zacconi,F.C., Kowthavarapu,V.K., Gupta,C., Palakurthi,S.S., Satheeshkumar,R., Lokwani,D.K., Tambuwala,M.M. and Palakurthi,S. Targeting Allosteric Site of PCSK9 Enzyme for the Identification of Small Molecule Inhibitors: An In Silico Drug Repurposing Study Biomedicines (2024) 12 PubMed Europe PubMed DOI PMC EPMC
Chong,S., Mu,G., Cen,X., Xiang,Q. and Cui,Y. Effects of PCSK9 on thrombosis and haemostasis in a variety of metabolic states: Lipids and beyond (Review) Int J Mol Med (2024) 53 PubMed Europe PubMed DOI PMC EPMC V
Coppinger,C., Pomales,B., Movahed,M.R., Marefat,M. and Hashemzadeh,M. Berberine: A Multi-Target Natural PCSK9 Inhibitor with the Potential to Treat Diabetes, Alzheimer's, Cancer and Cardiovascular Disease Curr Rev Clin Exp Pharmacol (2024) 19, 312-326. PubMed Europe PubMed DOI
Duddu,S., Katakia,Y.T., Chakrabarti,R., Sharma,P. and Shukla,P.C. New Epigenome Players in the Regulation of PCSK9 - H3K4me3 and H3K9ac Alteration by Statins in hypercholesterolemia J Lipid Res (2024) , 100699-100699. PubMed Europe PubMed DOI
Fassi,E.M.A., Citarella,A., Albani,M., Milano,E.G., Legnani,L., Lammi,C., Silvani,A. and Grazioso,G. PCSK9 inhibitors: a patent review 2018-2023 Expert Opin Ther Pat (2024) , 1-17. PubMed Europe PubMed DOI K
Fernandez-Ruiz,I. An epigenome editing approach induces durable silencing of Pcsk9 Nat Rev Cardiol (2024) 21, 279-279. PubMed Europe PubMed DOI
Giannessi,L., Lupo,M.G., Rossi,I., Martina,M.G., Vilella,A., Bodria,M., Giuliani,D., Zimetti,F., Zanotti,I., Poti,F., Bernini,F., Ferri,N. and Radi,M. Identification of 4-amino-2-Pyridones as new potent PCSK9 inhibitors: From phenotypic hit discovery to in vivo tolerability Eur J Med Chem (2024) 265, 116063-116063. PubMed Europe PubMed DOI
Grejtakova,D., Boronova,I., Bernasovska,J. and Bellosta,S. PCSK9 and Lipid Metabolism: Genetic Variants, Current Therapies, and Cardiovascular Outcomes Cardiovasc Drugs Ther (2024) PubMed Europe PubMed DOI V
Grosche,P., Flyer,A.N., Gattlen,R., Xu,M., Golosov,A.A., Vera,V., Pickett,S., Brousseau,M.E., Chopra,R., Clairmont,K.B., Koch,A., Liu,E., Reid,P., Perry,L., Yang,L., Yang,Q. and Monovich,L.G. Discovery of Truncated Cyclic Peptides Targeting an Induced-Fit Pocket on PCSK9 ChemMedChem (2024) , e202400208-e202400208. PubMed Europe PubMed DOI
Hassandokht Mashhadi,M., Taheri,F., Irani,S., Mesbah Mousavi,A., Mehri,A. and Javid,H. Current Understanding of PCSK9 and Its Relevance to Cancer Prognosis and Immune Therapy: A Review Iran J Pathol (2024) 19, 1-9. PubMed Europe PubMed DOI PMC EPMC V
Hoekstra,M. and Van Eck,M. Gene Editing for the Treatment of Hypercholesterolemia Curr Atheroscler Rep (2024) PubMed Europe PubMed DOI V
Hsu,C.Y., Abdulrahim,M.N., Mustafa,M.A., Omar,T.M., Balto,F., Pineda,I., Khudair,T.T., Ubaid,M. and Ali,M.S. The multifaceted role of PCSK9 in cancer pathogenesis, tumor immunity, and immunotherapy Med Oncol (2024) 41, 202-202. PubMed Europe PubMed DOI V
Huang,P., Ran,J., Zhu,W., Dai,W., Tang,Y., Lian,P., Huang,X. and Li,R. PCSK9 dysregulates cholesterol homeostasis and triglyceride metabolism in olanzapine-induced hepatic steatosis via both receptor-dependent and receptor-independent pathways FASEB J (2024) 38, e23464-e23464. PubMed Europe PubMed DOI
Imaralu,O.E., Aluganti Narasimhulu,C., Singal,P.K. and Singla,D.K. Role of proprotein convertase subtilisin/kexin type 9 (PCSK9) in diabetic complications Can J Physiol Pharmacol (2024) 102, 14-25. PubMed Europe PubMed DOI V
Katsuki,S., Jha,P.K., Aikawa,E. and Aikawa,M. The role of proprotein convertase subtilisin/kexin 9 (PCSK9) in macrophage activation: a focus on its LDL receptor-independent mechanisms Front Cardiovasc Med (2024) 11, 1431398-1431398. PubMed Europe PubMed DOI PMC EPMC
Kozan,D.W. and Farber,S.A. Is It Ever Wise to Edit Wild-Type Alleles? Engineered CRISPR Alleles Versus Millions of Years of Human Evolution Arterioscler Thromb Vasc Biol (2024) 44, 328-333. PubMed Europe PubMed DOI PMC EPMC
Liu,S., Wan,J., Wang,D., Yang,Y., Fang,J., Luo,T., Liang,D., Hu,J., Hou,J. and Wang,P. Effect of the PCSK9 R46L genetic variant on plasma insulin and glucose levels, risk of diabetes mellitus and cardiovascular disease: A meta-analysis Nutr Metab Cardiovasc Dis (2024) 34, 1339-1351. PubMed Europe PubMed DOI
Ma,Z., Liu,H., Jiang,S., Li,W., Li,Y., Liu,Y., Wang,L. and Li,W. Identification of benzothiazoles as novel PCSK9 inhibitors Bioorg Med Chem Lett (2024) 97, 129542-129542. PubMed Europe PubMed DOI
Macvanin,M., Gluvic,Z., Klisic,A., Manojlovic,M., Suri,J., Rizzo,M. and Isenovic,E. The Link between miRNAs and PCKS9 in Atherosclerosis Curr Med Chem (2024) 31, 6926-6956. PubMed Europe PubMed DOI V
Mahjoubin-Tehran,M., Rezaei,S., Santos,R.D., Jamialahmadi,T., AlMahmeed,W. and Sahebkar,A. Targeting PCSK9 as a key player in lipid metabolism: exploiting the therapeutic and biosensing potential of aptamers Lipids Health Dis (2024) 23, 156-156. PubMed Europe PubMed DOI PMC EPMC V
Mei,W., Faraj Tabrizi,S., Godina,C., Lovisa,A.F., Isaksson,K., Jernstrom,H. and Tavazoie,S.F. A commonly inherited human PCSK9 germline variant drives breast cancer metastasis via LRP1 receptor Cell (2024) PubMed Europe PubMed DOI
Ndoj,K., Meurs,A., Papaioannou,D., Bjune,K. and Zelcer,N. The low-density lipoprotein receptor: Emerging post-transcriptional regulatory mechanisms Atherosclerosis (2024) 401, 119082-119082. PubMed Europe PubMed DOI V
Park,J.H., Oh,S.Y., Jung,S.C., Song,T.J. and Jo,I. Far-infrared irradiation increases the uptake of LDL cholesterol by downregulating PCSK9 through the activation of TRPV4 calcium channels in HepG2 cells Biochem Biophys Res Commun (2024) 723, 150187-150187. PubMed Europe PubMed DOI
Pott,J., Kheirkhah,A., Gadin,J.R., Kleber,M.E., Delgado,G.E., Kirsten,H., Forer,L., Hauck,S.M., Burkhardt,R., Scharnagl,H., Loeffler,M., Marz,W., Thiery,J., Gieger,C., Peters,A., Silveira,A., Hooft,F.V., Kronenberg,F. and Scholz,M. Sex and statin-related genetic associations at the PCSK9 gene locus: results of genome-wide association meta-analysis Biol Sex Differ (2024) 15, 26-26. PubMed Europe PubMed DOI PMC EPMC
Sabnis,R.W. Novel PCSK9 Inhibitors for Treating Cardiovascular Diseases ACS Med Chem Lett (2024) 15, 443-444. PubMed Europe PubMed DOI PMC EPMC
Siddiqui,Z. and Frishman,W. New Oral PCSK9 Inhibitor: "MK-0616" Cardiol Rev (2024) PubMed Europe PubMed DOI K I
Testa,G., Giannelli,S., Staurenghi,E., Cecci,R., Floro,L., Gamba,P., Sottero,B. and Leonarduzzi,G. The Emerging Role of PCSK9 in the Pathogenesis of Alzheimer's Disease: A Possible Target for the Disease Treatment Int J Mol Sci (2024) 25 PubMed Europe PubMed DOI PMC EPMC V
Vilella,A., Bodria,M., Papotti,B., Zanotti,I., Zimetti,F., Remaggi,G., Elviri,L., Poti,F., Ferri,N., Lupo,M.G., Panighel,G., Daini,E., Vandini,E., Zoli,M., Giuliani,D. and Bernini,F. PCSK9 ablation attenuates Abeta pathology, neuroinflammation and cognitive dysfunctions in 5XFAD mice Brain Behav Immun (2024) 115, 517-534. PubMed Europe PubMed DOI
Wang,W.Z., Liu,C., Luo,J.Q., Lei,L.J., Chen,M.H., Zhang,Y.Y., Sheng,R., Li,Y.N., Wang,L., Jiang,X.H., Xiao,T.M., Zhang,Y.H., Li,S.W., Wu,Y.X., Xu,Y., Xu,Y.N. and Si,S.Y. A novel small-molecule PCSK9 inhibitor E28362 ameliorates hyperlipidemia and atherosclerosis Acta Pharmacol Sin (2024) 45, 2119-2133. PubMed Europe PubMed DOI I
Wang,Y., Chen,Y., Yang,J., Sun,W. and Zhang,X. Histone demethylase JMJD1C advances macrophage foam cell formation and atherosclerosis progression by promoting the transcription of PCSK9 J Physiol Biochem (2024) PubMed Europe PubMed DOI K
Zendjebil,S. and Steg,P.G. PCSK9 Monoclonal Antibodies Have Come a Long Way Curr Atheroscler Rep (2024) 26, 721-732. PubMed Europe PubMed DOI V
Zhang,Q., Miao,M., Cao,S., Liu,D., Cao,Z., Bai,X., Yin,Y., Jin,S., Dong,L. and Zheng,M. PCSK9 promotes vascular neointimal hyperplasia through non-lipid regulation of vascular smooth muscle cell proliferation, migration, and autophagy Biochem Biophys Res Commun (2024) 742, 151081-151081. PubMed Europe PubMed DOI I
Zhu,X.B., Xu,Y.Y., Li,L.C., Sun,J.B., Wang,Y.Z., Chen,J., Wang,C., Zhang,S. and Jin,L.Y. Function of proprotein convertase subtilisin/kexin type 9 and its role in central nervous system diseases: An update on clinical evidence Drug Dev Res (2024) 85, e22131-e22131. PubMed Europe PubMed DOI V

2023

Aspnes,G.E., Coffey,S.B., Darout,E., Dechert-Schmitt,A.M., Dullea,R.G., Kamlet,A.S., Limberakis,C., Londregan,A.T., McClure,K.F., Menhaji-Klotz,E., Piotrowski,D.W., Polivkova,J., Raymer,B., Ruggeri,R.B., Salatto,C.T., Tu,M., Wei,L. and Xiao,J. Small molecule inhibitors of PCSK9. SAR investigations of head and amine groups Bioorg Med Chem Lett (2023) 92, 129394-129394. PubMed Europe PubMed DOI
Ballantyne,C.M., Banka,P., Mendez,G., Garcia,R., Rosenstock,J., Rodgers,A., Mendizabal,G., Mitchel,Y. and Catapano,A.L. Phase 2b Randomized Trial of the Oral PCSK9 Inhibitor MK-0616 J Am Coll Cardiol (2023) 81, 1553-1564. PubMed Europe PubMed DOI I
Bell,A.S., Wagner,J., Rosoff,D.B. and Lohoff,F.W. Proprotein convertase subtilisin/kexin type 9 (PCSK9) in the central nervous system Neurosci Biobehav Rev (2023) 149, 105155-105155. PubMed Europe PubMed DOI V
Burnett,J.R. and Hooper,A.J. MK-0616: an oral PCSK9 inhibitor for hypercholesterolemia treatment Expert Opin Investig Drugs (2023) 32, 873-878. PubMed Europe PubMed DOI I
Cale,J.M., Ham,K.A., Li,D., McIntosh,C.S., Watts,G.F., Wilton,S.D. and Aung-Htut,M.T. Induced alternative splicing an opportunity to study PCSK9 protein isoforms at physiologically relevant concentrations Sci Rep (2023) 13, 19725-19725. PubMed Europe PubMed DOI PMC EPMC K
Cendron,L., Rothenberger,S., Cassari,L., Dettin,M. and Pasquato,A. Proprotein convertases regulate trafficking and maturation of key proteins within the secretory pathway Adv Protein Chem Struct Biol (2023) 133, 1-54. PubMed Europe PubMed DOI V
Chan,D.C. and Watts,G.F. The Promise of PCSK9 and Lipoprotein(a) as Targets for Gene Silencing Therapies Clin Ther (2023) 45, 1034-1046. PubMed Europe PubMed DOI K V
Chang,Y.C., Hsu,L.A. and Ko,Y.L. Exploring PCSK9 Genetic Impact on Lipoprotein(a) via Dual Approaches: Association and Mendelian Randomization Int J Mol Sci (2023) 24 PubMed Europe PubMed DOI PMC EPMC
Di Fusco,S.A., Scicchitano,P., Spinelli,A., Conte,E., Aquilani,S., Aiello,A., Nardi,F., Riccio,C., Caldarola,P., De Luca,L., Roncon,L., Valente,S., Gulizia,M.M., Gabrielli,D., Oliva,F. and Colivicchi,F. [ANMCO Position paper: Inclisiran: an innovative therapeutic approach for the clinical management of hypercholesterolemia] G Ital Cardiol (Rome) (2023) 24, 581-588. PubMed Europe PubMed DOI
Fruchart Gaillard,C., Ouadda,A.B.D., Ciccone,L., Girard,E., Mikaeeli,S., Evagelidis,A., Le Devehat,M., Susan-Resiga,D., Lajeunesse,E.C., Nozach,H., Ramos,O.H.P., Thureau,A., Legrand,P., Prat,A., Dive,V. and Seidah,N.G. Molecular interactions of PCSK9 with an inhibitory nanobody, CAP1 and HLA-C: Functional regulation of LDLR levels Mol Metab (2023) 67, 101662-101662. PubMed Europe PubMed DOI PMC EPMC K
Gianazza,E., Macchi,C., Banfi,C. and Ruscica,M. Proteomics and Lipidomics to unveil the contribution of PCSK9 beyond cholesterol lowering: a narrative review Front Cardiovasc Med (2023) 10, 1191303-1191303. PubMed Europe PubMed DOI PMC EPMC
Hummelgaard,S., Vilstrup,J.P., Gustafsen,C., Glerup,S. and Weyer,K. Targeting PCSK9 to tackle cardiovascular disease Pharmacol Ther (2023) 249, 108480-108480. PubMed Europe PubMed DOI V
Iqbal,M., Hasanah,N., Arianto,A.D., Aryati,W.D., Puteri,M.U. and Saputri,F.C. Brazilin from Caesalpinia sappan L. as a Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitor: Pharmacophore-Based Virtual Screening, In Silico Molecular Docking, and In Vitro Studies Adv Pharmacol Pharm Sci (2023) 2023, 5932315-5932315. PubMed Europe PubMed DOI PMC EPMC I
Irfan,N., Vaithyanathan,P., Anandaram,H., Mohammed Zaidh,S., Priya Varshini,S. and Puratchikody,A. Active and allosteric site binding MM-QM studies of Methylidene tetracyclo derivative in PCSK9 protein intended to make a safe antilipidemic agent J Biomol Struct Dyn (2023) , 1-10. PubMed Europe PubMed DOI
Jaafar,A.K., Techer,R., Chemello,K., Lambert,G. and Bourane,S. PCSK9 and the nervous system: a no-brainer? J Lipid Res (2023) 64, 100426-100426. PubMed Europe PubMed DOI PMC EPMC V
[YEAR:11-7-2023]Johns,D.G., Campeau,L.C., Banka,P., Bautmans,A., Bueters,T., Bianchi,E., Branca,D., Bulger,P.G., Crevecoeur,I., Ding,F.X., Garbaccio,R.M., Guetschow,E.D., Guo,Y., Ha,S.N., Johnston,J.M., Josien,H., Kauh,E.A., Koeplinger,K.A., Kuethe,J.T., Lai,E., Lanning,C.L., Lee,A.Y.H., Li,L., Nair,A.G., O'Neill,E.A., Stoch,S.A., Thaisrivongs,D.A., Tucker,T.J., Vachal,P., van,D.K., Vanhoutte,F.P., Volckaert,B., Wolford,D.G., Xu,A., Zhao,T., Zhou,D., Zhou,S., Zhu,X., Zokian,H.J., Walji,A.M. and Wood,H.B. Orally Bioavailable Macrocyclic Peptide That Inhibits Binding of PCSK9 to the Low Density Lipoprotein Receptor Circulation (11-7-2023) 148, 144-158. PubMed Europe PubMed I
Kuethe,J.T., Lee,J., Thaisrivongs,D., Yasuda,N., Pollack,S.R., Leone,J., DaSilva,J., Biba,M., Tsay,F.R., Regalado,E.L., Qi,J., Li,H., Poggetto,G.D. and Cohen,R. Synthesis of a Complex and Highly Potent PCSK9 Inhibitor Org Lett (2023) 25, 5001-5005. PubMed Europe PubMed DOI I
Laufs,U., Bluher,M. and Isermann,B. Third generation PCSK9-inhibitors Eur Heart J (2023) 44, 4281-4283. PubMed Europe PubMed DOI
Lee,J.H., Shores,K.L., Breithaupt,J.J., Lee,C.S., Fodera,D.M., Kwon,J.B., Ettyreddy,A.R., Myers,K.M., Evison,B.J., Suchowerska,A.K., Gersbach,C.A., Leong,K.W. and Truskey,G.A. PCSK9 activation promotes early atherosclerosis in a vascular microphysiological system APL Bioeng (2023) 7, 046103-046103. PubMed Europe PubMed DOI PMC EPMC
Luan,C., He,Y., Liu,W., Rong,Y., Gao,J., Xu,K., Yu,H., Hu,Y., Zhang,J., Chen,K. and Guo,W. PCSK9 inhibition interrupts the cross-talk between keratinocytes and macrophages and prevents UVB-induced skin damage J Biol Chem (2023) 299, 104895-104895. PubMed Europe PubMed DOI PMC EPMC K
Meng,F.H., Liu,S., Xiao,J., Zhou,Y.X., Dong,L.W., Li,Y.F., Zhang,Y.Q., Li,W.H., Wang,J.Q., Wang,Y., Song,B.L., Ma,Y.T., Fu,Z.Y. and Luo,J. New Loss-of-Function Mutations in PCSK9 Reduce Plasma LDL Cholesterol Arterioscler Thromb Vasc Biol (2023) 43, 1219-1233. PubMed Europe PubMed DOI
Mohamed,F., Mansfield,B. and Raal,F.J. Targeting PCSK9 and Beyond for the Management of Low-Density Lipoprotein Cholesterol J Clin Med (2023) 12 PubMed Europe PubMed DOI PMC EPMC V
Newman,C.B. and Tobert,J.A. Targeting PCSK9 With Antibodies and Gene Silencing to Reduce LDL Cholesterol J Clin Endocrinol Metab (2023) 108, 784-790. PubMed Europe PubMed DOI
Oostveen,R.F., Khera,A.V., Kathiresan,S., Stroes,E.S.G., Fitzgerald,K., Harms,M.J., Oakes,B.L. and Kastelein,J.J.P. New Approaches for Targeting PCSK9: Small-Interfering Ribonucleic Acid and Genome Editing Arterioscler Thromb Vasc Biol (2023) 43, 1081-1092. PubMed Europe PubMed DOI V
Qiao,M.Q., Li,Y., Yang,Y.X., Pang,C.X., Liu,Y.T., Bian,C., Wang,L., Chen,X.F. and Hong,B. Structure-activity relationship and biological evaluation of xanthine derivatives as PCSK9 inhibitors for the treatment of atherosclerosis Eur J Med Chem (2023) 247, 115047-115047. PubMed Europe PubMed DOI
Rikhi,R. and Shapiro,M.D. Proprotein Convertase Subtilisin/Kexin Type 9 Inhibition: The Big Step Forward in Lipid Control Eur Cardiol (2023) 18, e45-e45. PubMed Europe PubMed DOI PMC EPMC V
Roychowdhury,T., Klarin,D., Levin,M.G., Spin,J.M., Rhee,Y.H., Deng,A., Headley,C.A., Tsao,N.L., Gellatly,C., Zuber,V., Shen,F., Hornsby,W.E., Laursen,I.H., Verma,S.S., Locke,A.E., Einarsson,G., Thorleifsson,G., Graham,S.E., Dikilitas,O., Pattee,J.W., Judy,R.L., Pauls-Verges,F., Nielsen,J.B., Wolford,B.N., Brumpton,B.M., Dilme,J., Peypoch,O., Juscafresa,L.C., Edwards,T.L., Li,D., Banasik,K., Brunak,S., Jacobsen,R.L., Garcia-Barrio,M.T., Zhang,J., Rasmussen,L.M., Lee,R., Handa,A., Wanhainen,A., Mani,K., Lindholt,J.S., Obel,L.M., Strauss,E., Oszkinis,G., Nelson,C.P., Saxby,K.L., van Herwaarden,J.A., van der Laan,S.W., van Setten,J., Camacho,M., Davis,F.M., Wasikowski,R., Tsoi,L.C., Gudjonsson,J.E., Eliason,J.L., Coleman,D.M., Henke,P.K., Ganesh,S.K., Chen,Y.E., Guan,W., Pankow,J.S., Pankratz,N., Pedersen,O.B., Erikstrup,C., Tang,W., Hveem,K., Gudbjartsson,D., Gretarsdottir,S., Thorsteinsdottir,U., Holm,H., Stefansson,K., Ferreira,M.A., Baras,A., Kullo,I.J., Ritchie,M.D., Christensen,A.H., Iversen,K.K., Eldrup,N., Sillesen,H., Ostrowski,S.R., Bundgaard,H., Ullum,H., Burgess,S., Gill,D., Gallagher,K., Sabater-Lleal,M., Surakka,I., Jones,G.T., Bown,M.J., Tsao,P.S., Willer,C.J. and Damrauer,S.M. Genome-wide association meta-analysis identifies risk loci for abdominal aortic aneurysm and highlights PCSK9 as a therapeutic target Nat Genet (2023) 55, 1831-1842. PubMed Europe PubMed DOI PMC EPMC
Sener,Y.Z. and Tokgozoglu,L. Pleiotropy of PCSK9: Functions in Extrahepatic Tissues Curr Cardiol Rep (2023) 25, 979-985. PubMed Europe PubMed DOI V
Singh,S., Sharma,H., Ramankutty,R., Ramaswamy,S. and Agrawal,N. Natural Proprotein Convertase Subtilisin/Kexin Type 9 Inhibitors: A Review Comb Chem High Throughput Screen (2023) 26, 2668-2678. PubMed Europe PubMed DOI V
Wang,Y., Fang,D., Yang,Q., You,J., Wang,L., Wu,J., Zeng,M. and Luo,M. Interactions between PCSK9 and NLRP3 inflammasome signaling in atherosclerosis Front Immunol (2023) 14, 1126823-1126823. PubMed Europe PubMed DOI PMC EPMC V
Xu,J.N., Wang,T.T., Shu,H., Shi,S.Y., Tao,L.C. and Li,J.J. Insight into the role of PCSK9 in glucose metabolism Clin Chim Acta (2023) 547, 117444-117444. PubMed Europe PubMed DOI V

2022

Ahamad,S., Mathew,S., Khan,W.A. and Mohanan,K. Development of small-molecule PCSK9 inhibitors for the treatment of hypercholesterolemia Drug Discov Today (2022) 27, 1332-1349. PubMed Europe PubMed DOI V
Byun,J.H., Lebeau,P.F., Platko,K., Carlisle,R.E., Faiyaz,M., Chen,J., MacDonald,M.E., Makda,Y., Yousof,T., Lynn,E.G., Dickhout,J.G., Krepinsky,J.C., Weaver,F., Igdoura,S.A., Seidah,N.G. and Austin,R.C. Inhibitory Antibodies against PCSK9 Reduce Surface CD36 and Mitigate Diet-Induced Renal Lipotoxicity Kidney360 (2022) 3, 1394-1410. PubMed Europe PubMed DOI PMC EPMC
Cai,Y.J., Li,P.H., Wang,X.A., Xu,Y.M., Yang,S., Tang,Y.N., Zhu,Z., Yang,X.Y., He,J.Y., Luo,H., Zhang,T., Qi,H., Chen,X., Qin,Q.W. and Sun,H.Y. Epinephelus coioides PCSK9 affect the infection of SGIV by regulating the innate immune response Fish Shellfish Immunol (2022) 126, 113-121. PubMed Europe PubMed DOI
Cammisotto,V., Baratta,F., Simeone,P.G., Barale,C., Lupia,E., Galardo,G., Santilli,F., Russo,I. and Pignatelli,P. Proprotein Convertase Subtilisin Kexin Type 9 (PCSK9) Beyond Lipids: The Role in Oxidative Stress and Thrombosis Antioxidants (Basel) (2022) 11 PubMed Europe PubMed DOI PMC EPMC V
Coppinger,C., Movahed,M.R., Azemawah,V., Peyton,L., Gregory,J. and Hashemzadeh,M. A Comprehensive Review of PCSK9 Inhibitors J Cardiovasc Pharmacol Ther (2022) 27, 10742484221100107-10742484221100107. PubMed Europe PubMed DOI
Hay,R., Cullen,B., Graham,N., Lyall,D.M., Aman,A., Pell,J.P., Ward,J., Smith,D.J. and Strawbridge,R.J. Genetic analysis of the PCSK9 locus in psychological, psychiatric, metabolic and cardiovascular traits in UK Biobank Eur J Hum Genet (2022) 30, 1380-1390. PubMed Europe PubMed DOI
Huang,G., Lu,X., Duan,Z., Zhang,K., Xu,L., Bao,H., Xiong,X., Lin,M., Li,C., Li,Y., Zhou,H., Luo,Z. and Li,W. PCSK9 Knockdown Can Improve Myocardial Ischemia/Reperfusion Injury by Inhibiting Autophagy Cardiovasc Toxicol (2022) 22, 951-961. PubMed Europe PubMed DOI K
Huang,G., Lu,X., Zhou,H., Li,R., Huang,Q., Xiong,X., Luo,Z. and Li,W. PCSK9 inhibition protects against myocardial ischemia-reperfusion injury via suppressing autophagy Microvasc Res (2022) 142, 104371-104371. PubMed Europe PubMed DOI
Katzmann,J.L., Cupido,A.J. and Laufs,U. Gene Therapy Targeting PCSK9 Metabolites (2022) 12 PubMed Europe PubMed DOI PMC EPMC K V
Katzmann,J.L., Custodis,F., Schirmer,S.H. and Laufs,U. [Update on PCSK9 inhibition] Herz (2022) 47, 196-203. PubMed Europe PubMed DOI
Kuzmich,N., Andresyuk,E., Porozov,Y., Tarasov,V., Samsonov,M., Preferanskaya,N., Veselov,V. and Alyautdin,R. PCSK9 as a Target for Development of a New Generation of Hypolipidemic Drugs Molecules (2022) 27 PubMed Europe PubMed DOI PMC EPMC V
Liu,C., Xu,H., Yuan,F., Chen,W., Chen,H., Sheng,L., Wu,Y. and Li,X. Identification of dominant conformational epitopes from the whole structure of the proprotein convertase subtilisin/kexin type 9 Biochem Biophys Res Commun (2022) 606, 55-60. PubMed Europe PubMed DOI
Liu,C., Chen,J., Chen,H., Zhang,T., He,D., Luo,Q., Chi,J., Hong,Z., Liao,Y., Zhang,S., Wu,Q., Cen,H., Chen,G., Li,J. and Wang,L. PCSK9 Inhibition: From Current Advances to Evolving Future Cells (2022) 11 PubMed Europe PubMed DOI PMC EPMC V
Maliglowka,M., Kosowski,M., Hachula,M., Cyrnek,M., Buldak,L., Basiak,M., Boldys,A., Machnik,G., Buldak,R.J. and Okopien,B. Insight into the Evolving Role of PCSK9 Metabolites (2022) 12 PubMed Europe PubMed DOI PMC EPMC
Mbikay,M. and Chretien,M. The Biological Relevance of PCSK9: When Less Is Better. Biochem Cell Biol (2022) 100, 189-198. PubMed Europe PubMed DOI V
Puccini,M., Landmesser,U. and Rauch,U. Pleiotropic Effects of PCSK9: Focus on Thrombosis and Haemostasis Metabolites (2022) 12 PubMed Europe PubMed DOI PMC EPMC
Puteri,M.U., Azmi,N.U., Ridwan,S., Iqbal,M., Fatimah,T., Rini,T.D.P., Kato,M. and Saputri,F.C. Recent Update on PCSK9 and Platelet Activation Experimental Research Methods: In Vitro and In Vivo Studies J Cardiovasc Dev Dis (2022) 9 PubMed Europe PubMed DOI PMC EPMC V
Puteri,M.U., Azmi,N.U., Kato,M. and Saputri,F.C. PCSK9 Promotes Cardiovascular Diseases: Recent Evidence about Its Association with Platelet Activation-Induced Myocardial Infarction Life (Basel) (2022) 12 PubMed Europe PubMed DOI PMC EPMC
Saitoski,K., Ryaboshapkina,M., Hamza,G.M., Jarnuczak,A.F., Berthault,C., Carlotti,F., Armanet,M., Sengupta,K., Underwood,C.R., Andersson,S., Guillas,I., Le Goff,W. and Scharfmann,R. Proprotein convertase PCSK9 affects expression of key surface proteins in human pancreatic beta cells via intracellular and extracellular regulatory circuits J Biol Chem (2022) 298, 102096-102096. PubMed Europe PubMed DOI PMC EPMC K
Seidah,N.G. and Prat,A. The Multifaceted Biology of PCSK9 Endocr Rev (2022) 43, 558-582. PubMed Europe PubMed DOI PMC EPMC
Seidah,N.G. and Garcon,D. Expanding Biology of PCSK9: Roles in Atherosclerosis and Beyond Curr Atheroscler Rep (2022) 24, 821-830. PubMed Europe PubMed DOI PMC EPMC K V
Wong,C.C., Wu,J.L., Ji,F., Kang,W., Bian,X., Chen,H., Chan,L.S., Luk,S.T.Y., Tong,S., Xu,J., Zhou,Q., Liu,D., Su,H., Gou,H., Cheung,A.H., To,K.F., Cai,Z., Shay,J.W. and Yu,J. The cholesterol uptake regulator PCSK9 promotes and is a therapeutic target in APC/KRAS-mutant colorectal cancer Nat Commun (2022) 13, 3971-3971. PubMed Europe PubMed DOI PMC EPMC
Zulkapli,R., Yusof,M.Y.P.M., Abd Muid,S., Wang,S.M., Firus Khan,A.Y. and Nawawi,H. A Systematic Review on Attenuation of PCSK9 in Relation to Atherogenesis Biomarkers Associated with Natural Products or Plant Bioactive Compounds in In Vitro Studies: A Critique on the Quality and Imprecision of Studies Int J Environ Res Public Health (2022) 19 PubMed Europe PubMed DOI PMC EPMC V

2021

Almeida,C.R., Ferreira,B.H. and Duarte,I.F. Targeting PCSK9: a promising adjuvant strategy in cancer immunotherapy Signal Transduct Target Ther (2021) 6, 111-111. PubMed Europe PubMed DOI PMC EPMC
Banerjee,Y., Pantea Stoian,A., Cicero,A.F.G., Fogacci,F., Nikolic,D., Sachinidis,A., Rizvi,A.A., Janez,A. and Rizzo,M. Inclisiran: a small interfering RNA strategy targeting PCSK9 to treat hypercholesterolemia Expert Opin Drug Saf (2021) , 1-12. PubMed Europe PubMed DOI V
Bhattacharya,A., Chowdhury,A., Chaudhury,K. and Shukla,P.C. Proprotein convertase subtilisin/kexin type 9 (PCSK9): A potential multifaceted player in cancer Biochim Biophys Acta Rev Cancer (2021) 1876, 188581-188581. PubMed Europe PubMed DOI V
Fan,T.Y., Yang,Y.X., Zeng,Q.X., Wang,X.L., Wei,W., Guo,X.X., Zhao,L.P., Song,D.Q., Wang,Y.X., Wang,L. and Hong,B. Structure-activity relationship and biological evaluation of berberine derivatives as PCSK9 down-regulating agents Bioorg Chem (2021) 113, 104994-104994. PubMed Europe PubMed DOI
Frostegard,J. The role of PCSK9 in inflammation, immunity, and autoimmune diseases Expert Rev Clin Immunol (2021) , 1-8. PubMed Europe PubMed DOI
Furuhashi,M., Kataoka,Y., Nishikawa,R., Koyama,M., Sakai,A., Higashiura,Y., Tanaka,M., Saitoh,S., Shimamoto,K. and Ohnishi,H. Circulating PCSK7 Level is Independently Associated with Obesity, Triglycerides Level and Fatty Liver Index in a General Population without Medication J Atheroscler Thromb (2021) PubMed Europe PubMed DOI
Gencer,B. and Mach,F. PCSK9 inhibition could be effective for acute myocardial infarction Curr Med Chem (2021) PubMed Europe PubMed DOI V
Hamasaki,M., Hosaka,N., Freeman,L.A., Sato,M., Hara,K., Remaley,A.T. and Kotani,K. A novel loop-mediated isothermal amplification-based genotyping method and its application for identifying proprotein convertase subtilisin/kexin type 9 variants in familial hypercholesterolemia Biochim Biophys Acta Gen Subj (2021) 1866, 130063-130063. PubMed Europe PubMed DOI
Ioannou,G.N., Lee,S.P., Linsley,P.S., Gersuk,V., Yeh,M.M., Chen,Y.Y., Peng,Y.J., Dutta,M., Mascarinas,G., Molla,B., Cui,J.Y. and Savard,C. Pcsk9 Deletion Promotes Murine Nonalcoholic Steatohepatitis and Hepatic Carcinogenesis: Role of Cholesterol Hepatol Commun (2021) PubMed Europe PubMed DOI
Kingwell,K. Pushing the envelope with PCSK9 Nat Rev Drug Discov (2021) PubMed Europe PubMed DOI
Ma,N., Fan,L., Dong,Y., Xu,X., Yu,C., Chen,J. and Ren,J. New PCSK9 inhibitor miR-552-3p reduces LDL-C via enhancing LDLR in high fat diet-fed mice Pharmacol Res (2021) 167, 105562-105562. PubMed Europe PubMed DOI K
Mahboobnia,K., Pirro,M., Marini,E., Grignani,F., Bezsonov,E.E., Jamialahmadi,T. and Sahebkar,A. PCSK9 and cancer: Rethinking the link Biomed Pharmacother (2021) 140, 111758-111758. PubMed Europe PubMed DOI K V
Masagalli,J.N., BasavanaGowda,M.K., Chae,H.S. and Choi,W.J. Synthesis of Moracin C and Its Derivatives with a 2-arylbenzofuran Motif and Evaluation of Their PCSK9 Inhibitory Effects in HepG2 Cells Molecules (2021) 26 DOI I
Masagalli,J.N., BasavanaGowda,M.K., Chae,H.S. and Choi,W.J. Synthesis of Moracin C and Its Derivatives with a 2-arylbenzofuran Motif and Evaluation of Their PCSK9 Inhibitory Effects in HepG2 Cells Molecules (2021) 26 PubMed Europe PubMed DOI PMC EPMC I
Momtazi-Borojeni,A.A., Pirro,M., Xu,S. and Sahebkar,A. PCSK9 inhibition-based therapeutic approaches: an immunotherapy perspective Curr Med Chem (2021) PubMed Europe PubMed DOI
Musunuru,K., Chadwick,A.C., Mizoguchi,T., Garcia,S.P., DeNizio,J.E., Reiss,C.W., Wang,K., Iyer,S., Dutta,C., Clendaniel,V., Amaonye,M., Beach,A., Berth,K., Biswas,S., Braun,M.C., Chen,H.M., Colace,T.V., Ganey,J.D., Gangopadhyay,S.A., Garrity,R., Kasiewicz,L.N., Lavoie,J., Madsen,J.A., Matsumoto,Y., Mazzola,A.M., Nasrullah,Y.S., Nneji,J., Ren,H., Sanjeev,A., Shay,M., Stahley,M.R., Fan,S.H.Y., Tam,Y.K., Gaudelli,N.M., Ciaramella,G., Stolz,L.E., Malyala,P., Cheng,C.J., Rajeev,K.G., Rohde,E., Bellinger,A.M. and Kathiresan,S. In vivo CRISPR base editing of PCSK9 durably lowers cholesterol in primates Nature (2021) 593, 429-434. PubMed Europe PubMed DOI K
Nhoek,P., Chae,H.S., Kim,Y.M., Pel,P., Huh,J., Kim,H.W., Choi,Y.H., Lee,K. and Chin,Y.W. Sesquiterpenoids from the Aerial Parts of Salvia plebeia with Inhibitory Activities on Proprotein Convertase Subtilisin/Kexin Type 9 Expression J Nat Prod (2021) 84, 220-229. PubMed Europe PubMed DOI
Petersen-Uribe,A., Kremser,M., Rohlfing,A.K., Castor,T., Kolb,K., Dicenta,V., Emschermann,F., Li,B., Borst,O., Rath,D., Muller,K.A.L. and Gawaz,M.P. Platelet-Derived PCSK9 Is Associated with LDL Metabolism and Modulates Atherothrombotic Mechanisms in Coronary Artery Disease Int J Mol Sci (2021) 22 PubMed Europe PubMed DOI PMC EPMC
Peyot,M.L., Roubtsova,A., Lussier,R., Chamberland,A., Essalmani,R., Murthy Madiraju,S.R., Seidah,N.G., Prentki,M. and Prat,A. Substantial PCSK9 inactivation in beta-cells does not modify glucose homeostasis or insulin secretion in mice Biochim Biophys Acta Mol Cell Biol Lipids (2021) 1866, 158968-158968. PubMed Europe PubMed DOI K
Rifai,M.A. and Ballantyne,C.M. PCSK9-targeted therapies: present and future approaches Nat Rev Cardiol (2021) 18, 805-806. PubMed Europe PubMed DOI
Robson,A. Three different therapies to target PCSK9 Nat Rev Cardiol (2021) PubMed Europe PubMed DOI
Rothgangl,T., Dennis,M.K., Lin,P.J.C., Oka,R., Witzigmann,D., Villiger,L., Qi,W., Hruzova,M., Kissling,L., Lenggenhager,D., Borrelli,C., Egli,S., Frey,N., Bakker,N., Walker,J.A., Kadina,A.P., Victorov,D.V., Pacesa,M., Kreutzer,S., Kontarakis,Z., Moor,A., Jinek,M., Weissman,D., Stoffel,M., van Boxtel,R., Holden,K., Pardi,N., Thony,B., Haberle,J., Tam,Y.K., Semple,S.C. and Schwank,G. In vivo adenine base editing of PCSK9 in macaques reduces LDL cholesterol levels Nat Biotechnol (2021) PubMed Europe PubMed DOI
Roudaut,M., Idriss,S., Caillaud,A., Girardeau,A., Rimbert,A., Champon,B., David,A., Leveque,A., Arnaud,L., Pichelin,M., Prieur,X., Prat,A., Seidah,N.G., Zibara,K., Le May,C., Cariou,B. and Si-Tayeb,K. PCSK9 regulates the NODAL signaling pathway and cellular proliferation in hiPSCs Stem Cell Reports (2021) 16, 2958-2972. PubMed Europe PubMed DOI
Ruotsalainen,A.K., Makinen,P. and Yla-Herttuala,S. Novel RNAi-Based Therapies for Atherosclerosis Curr Atheroscler Rep (2021) 23, 45-45. PubMed Europe PubMed DOI PMC EPMC V
Schulz,R., Andreadou,I. and Ferdinandy,P. Editorial: PCSK9: Importance in Physiology and Pathophysiology Front Physiol (2021) 12, 706115-706115. PubMed Europe PubMed DOI PMC EPMC
Seidah,N.G. and Prat,A. The multifaceted biology of PCSK9 Endocr Rev (2021) PubMed Europe PubMed DOI K
Singh,A., Kumar,P., Sonkar,A.B., Gautam,A.K., Verma,A., Maity,B., Tiwari,H., Sahoo,N.G., Keshari,A.K., Yadav,S.K. and Saha,S. A Comprehensive Review on PCSK9 as Mechanistic Target Approach in Cancer Therapy Mini Rev Med Chem (2021) PubMed Europe PubMed DOI
Stulz,R., Milligan,F., Stovold,C., Love,I., Stromberg,R., Andersson,S. and Dahlen,A. (34)S-SIL of PCSK9-Active Oligonucleotide as Tools for Accurate Quantification by Mass Spectrometry Nucleic Acid Ther (2021) PubMed Europe PubMed DOI K
Sun,H., Wang,J., Liu,S., Zhou,X., Dai,L., Chen,C., Xu,Q., Wen,X., Cheng,K., Sun,H. and Yuan,H. Discovery of Novel Small Molecule Inhibitors Disrupting the PCSK9-LDLR Interaction J Chem Inf Model (2021) PubMed Europe PubMed DOI
Sundararaman,S.S., Doring,Y. and van der Vorst,E.P.C. PCSK9: A Multi-Faceted Protein That Is Involved in Cardiovascular Biology Biomedicines (2021) 9 PubMed Europe PubMed DOI PMC EPMC V
Tombling,B.J., Lammi,C., Bollati,C., Anoldi,A., Craik,D.J. and Wang,C.K. Increased Valency Improves Inhibitory Activity of Peptides Targeting Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Chembiochem (2021) PubMed Europe PubMed DOI
Tombling,B.J., Lammi,C., Lawrence,N., Gilding,E.K., Grazioso,G., Craik,D.J. and Wang,C.K. Bioactive Cyclization Optimizes the Affinity of a Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Peptide Inhibitor J Med Chem (2021) 64, 2523-2533. PubMed Europe PubMed DOI
Tucker,T.J., Embrey,M.W., Alleyne,C., Amin,R.P., Bass,A., Bhatt,B., Bianchi,E., Branca,D., Bueters,T., Buist,N., Ha,S.N., Hafey,M., He,H., Higgins,J., Johns,D.G., Kerekes,A.D., Koeplinger,K.A., Kuethe,J.T., Li,N., Murphy,B., Orth,P., Salowe,S., Shahripour,A., Tracy,R., Wang,W., Wu,C., Xiong,Y., Zokian,H.J., Wood,H.B. and Walji,A. A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors J Med Chem (2021) 64, 16770-16800. PubMed Europe PubMed DOI
Xiang,Q., Liu,W., Zeng,J., Deng,Y., Peng,J., Liu,H., Ren,Z., Jiang,Z., Liu,L. and Tang,Z. Effect of PCSK9 on Vascular Smooth Muscle Cell Functions: A New Player in Atherosclerosis Curr Med Chem (2021) 28, 7446-7460. PubMed Europe PubMed DOI V
Yasuda,D., Hiraoka,Y., Ohno,M., Nishi,K., Iwasaki,H., Kita,T., Nishi,E. and Kume,N. Deficiency of Nardilysin in the Liver Reduces Serum Cholesterol Levels Biol Pharm Bull (2021) 44, 363-371. PubMed Europe PubMed DOI
Zainab,R., Kaleem,A., Ponczek,M.B., Abdullah,R., Iqtedar,M. and Hoessli,D.C. Finding inhibitors for PCSK9 using computational methods PLoS ONE (2021) 16, e0255523-e0255523. PubMed Europe PubMed DOI PMC EPMC
Zamarron-Licona,E., Rodriguez-Perez,J.M., Posadas-Sanchez,R., Vargas-Alarcon,G., Banos-Gonzalez,M.A., Borgonio-Cuadra,V.M. and Perez-Hernandez,N. Variants of PCSK9 Gene Are Associated with Subclinical Atherosclerosis and Cardiometabolic Parameters in Mexicans. The GEA Project Diagnostics (Basel) (2021) 11 PubMed Europe PubMed DOI

2020

Adorni,M.P., Zimetti,F., Lupo,M.G., Ruscica,M. and Ferri,N. Naturally occurring PCSK9 inhibitors Nutrients (2020) 12 PubMed Europe PubMed DOI I
Alleyne,C., Amin,R.P., Bhatt,B., Bianchi,E., Blain,J.C., Boyer,N., Branca,D., Embrey,M.W., Ha,S.N., Jette,K., Johns,D.G., Kerekes,A.D., Koeplinger,K.A., LaPlaca,D., Li,N., Murphy,B., Orth,P., Ricardo,A., Salowe,S., Seyb,K., Shahripour,A., Stringer,J.R., Sun,Y., Tracy,R., Wu,C., Xiong,Y., Youm,H., Zokian,H.J. and Tucker,T.J. Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based Design J Med Chem (2020) 63, 13796-13824. PubMed Europe PubMed DOI
Andreadou,I., Tsoumani,M., Vilahur,G., Ikonomidis,I., Badimon,L., Varga,Z.V., Ferdinandy,P. and Schulz,R. PCSK9 in Myocardial Infarction and Cardioprotection: Importance of Lipid Metabolism and Inflammation Front Physiol (2020) 11, 602497-602497. PubMed Europe PubMed DOI PMC EPMC V
Atreya,M.R., Whitacre,B.E., Cvijanovich,N.Z., Bigham,M.T., Thomas,N.J., Schwarz,A.J., Weiss,S.L., Fitzgerald,J.C., Allen,G.L., Lutfi,R., Nowak,J.E., Quasney,M.W., Shah,A.S. and Wong,H.R. Proprotein Convertase Subtilisin/Kexin Type 9 Loss-of-Function Is Detrimental to the Juvenile Host With Septic Shock Crit Care Med (2020) PubMed Europe PubMed DOI
Barkas,F., Milionis,H., Anastasiou,G. and Liberopoulos,E. Statins and PCSK9 inhibitors: What is their role in coronavirus disease 2019? Med Hypotheses (2020) 146, 110452-110452. PubMed Europe PubMed DOI PMC EPMC
Bayona,A., Arrieta,F., Rodriguez-Jimenez,C., Cerrato,F., Rodriguez-Novoa,S., Fernandez-Lucas,M., Gomez-Coronado,D. and Mata,P. Loss-of-function mutation of PCSK9 as a protective factor in the clinical expression of familial hypercholesterolemia: A case report Medicine (Baltimore) (2020) 99, e21754-e21754. PubMed Europe PubMed DOI PMC EPMC
Burdick,D.J., Skelton,N.J., Ultsch,M., Beresini,M.H., Eigenbrot,C., Li,W., Zhang,Y., Nguyen,H., Kong-Beltran,M., Quinn,J.G. and Kirchhofer,D. Design of organo-peptides as bipartite PCSK9 antagonists ACS Chem Biol (2020) 15, 425-436. PubMed Europe PubMed DOI
Cesaro,A., Bianconi,V., Gragnano,F., Moscarella,E., Fimiani,F., Monda,E., Scudiero,O., Limongelli,G., Pirro,M. and Calabro,P. Beyond cholesterol metabolism: the pleiotropic effects of proprotein convertase subtilisin/kexin type 9 (PCSK9). Genetics, mutations, expression, and perspective for long-term inhibition Biofactors (2020) PubMed Europe PubMed DOI
Choi,H.S., Kim,C.S., Ma,S.K., Kim,S.W. and Bae,E.H. Treatment of hyperlipidemia with proprotein convertase subtilisin/kexin type 9 inhibitor in a patient with nephrotic syndrome: a case report Ann Palliat Med (2020) 9, 2357-2360. PubMed Europe PubMed DOI
Crunkhorn,S. Blocking PCSK9 enhances immune checkpoint therapy Nat Rev Drug Discov (2020) PubMed Europe PubMed DOI
Ding,Z., Wang,X., Liu,S., Zhou,S., Kore,R.A., Mu,S., Deng,X., Fan,Y. and Mehta,J.L. NLRP3 inflammasome via IL-1beta regulates PCSK9 secretion Theranostics (2020) 10, 7100-7110. PubMed Europe PubMed DOI PMC EPMC
Dong,J., He,M., Li,J., Pessentheiner,A.R., Wang,C., Zhang,J., Sun,Y., Wang,W.T., Zhang,Y., Liu,J., Wang,S.C., Huang,P.H., Gordts,P.L., Yuan,Z.Y., Tsimikas,S. and Shyy,J.Y. MicroRNA-483 ameliorates hypercholesterolemia by inhibiting PCSK9 production JCI Insight (2020) PubMed Europe PubMed DOI
Emma,M.R., Giannitrapani,L., Cabibi,D., Porcasi,R., Pantuso,G., Augello,G., Giglio,R.V., Re,N.L., Capitano,A.R., Montalto,G., Soresi,M. and Cervello,M. Hepatic and circulating levels of PCSK9 in morbidly obese patients: Relation with severity of liver steatosis Biochim Biophys Acta Mol Cell Biol Lipids (2020) 1865, 158792-158792. PubMed Europe PubMed DOI
Evison,B.J., Palmer,J.T., Lambert,G., Treutlein,H., Zeng,J., Nativel,B., Chemello,K., Zhu,Q., Wang,J., Teng,Y., Tang,W., Xu,Y., Rathi,A.K., Kumar,S., Suchowerska,A.K., Parmar,J., Dixon,I., Kelly,G.E. and Bonnar,J. A small molecule inhibitor of PCSK9 that antagonizes LDL receptor binding via interaction with a cryptic PCSK9 binding groove Bioorg Med Chem (2020) 28, 115344-115344. PubMed Europe PubMed DOI I
Felekos,I., Karamasis,G.V. and Pavlidis,A.N. PCSK9 inhibitors for the management of dyslipidemia in people with Type 2 Diabetes: How low is too low? Curr Pharm Des (2020) PubMed Europe PubMed DOI
Furtado,R.H.M. and Giugliano,R.P. What lessons have we learned and what remains to be clarified for PCSK9 inhibitors? A review of FOURIER and ODYSSEY outcomes trials Cardiol Ther (2020) 9, 59-73. PubMed Europe PubMed DOI V
Gan,E.S., Tan,H.C., Duyen,H.L.T., Trieu,H.T., Wills,B., Ooi,E.E., Seidah,N.G. and Yacoub,S. Dengue virus induces PCSK9 expression to alter antiviral responses and disease outcomes J Clin Invest (2020) PubMed Europe PubMed DOI
Garcon,D., Moreau,F., Ayer,A., Dijk,W., Prieur,X., Arnaud,L., Roubtsova,A., Seidah,N., Prat,A., Cariou,B. and Le May,C. Circulating Rather Than Intestinal PCSK9 (Proprotein Convertase Subtilisin Kexin Type 9) Regulates Postprandial Lipemia in Mice Arterioscler Thromb Vasc Biol (2020) , ATVBAHA120314194-ATVBAHA120314194. PubMed Europe PubMed DOI
German,C.A. and Shapiro,M.D. Small interfering RNA therapeutic Inclisiran: a new approach to targeting PCSK9 BioDrugs (2020) 34, 1-9. PubMed Europe PubMed DOI
Guo,S., Xia,X.D., Gu,H.M. and Zhang,D.W. Proprotein Convertase Subtilisin/Kexin-Type 9 and Lipid Metabolism Adv Exp Med Biol (2020) 1276, 137-156. PubMed Europe PubMed DOI
Guo,Y., Yan,B., Tai,S., Zhou,S. and Zheng,X.L. PCSK9: Associated with cardiac diseases and their risk factors? Arch Biochem Biophys (2020) , 108717-108717. PubMed Europe PubMed DOI V
Hamamura,H., Adachi,H., Enomoto,M., Fukami,A., Nakamura,S., Nohara,Y., Morikawa,N., Sakaue,A., Toyomasu,K., Yamamoto,M. and Fukumoto,Y. Serum Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) is Independently Associated with Insulin Resistance, Triglycerides, Lipoprotein(a) Levels but not Low-Density Lipoprotein Cholesterol Levels in a General Population J Atheroscler Thromb (2020) PubMed Europe PubMed DOI
Han,J., Bilgrami,S., Ross,S., Broadhead,H. and Attar,N. Real-world lipid lowering effects of proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors: A single-centre study Int J Cardiol (2020) PubMed Europe PubMed DOI
Kim,E.J. and Wierzbicki,A.S. The history of proprotein convertase subtilisin kexin-9 inhibitors and their role in the treatment of cardiovascular disease Ther Adv Chronic Dis (2020) 11, 2040622320924569-2040622320924569. PubMed Europe PubMed DOI PMC EPMC
Kirchhofer,D., Burdick,D.J., Skelton,N.J., Zhang,Y. and Ultsch,M. Regions of conformational flexibility in the proprotein convertase PCSK9 and design of antagonists for LDL cholesterol lowering Biochem Soc Trans (2020) 48, 1323-1336. PubMed Europe PubMed DOI
Kolovou,V., Katsiki,N., Makrygiannis,S., Mavrogieni,S., Karampetsou,N., Manolis,A., Melidonis,A., Mikhailidis,D.P. and Kolovou,G.D. Lipoprotein Apheresis and Proprotein Convertase Subtilisin/Kexin Type 9 Inhibitors in Patients With Heterozygous Familial Hypercholesterolemia: A One Center Study J Cardiovasc Pharmacol Ther (2020) , 1074248420943079-1074248420943079. PubMed Europe PubMed DOI
Kuo,W.C., Stevens,J.M., Ersig,A.L., Johnson,H.M., Tung,T.H. and Bratzke,L.C. Does 24-h Activity Cycle Influence Plasma PCSK9 Concentration? A Systematic Review and Meta-Analysis Curr Atheroscler Rep (2020) 22, 30-30. PubMed Europe PubMed DOI
Liberopoulos,E. Lipoprotein(a) reduction with proprotein convertase subtilisin/kexin type 9 inhibitors: an unsolved mystery Eur J Prev Cardiol (2020) , 2047487320926777-2047487320926777. PubMed Europe PubMed DOI
Liu,X., Bao,X., Hu,M., Chang,H., Jiao,M., Cheng,J., Xie,L., Huang,Q., Li,F. and Li,C.Y. Inhibition of PCSK9 potentiates immune checkpoint therapy for cancer Nature (2020) PubMed Europe PubMed DOI
Macchi,C., Favero,C., Ceresa,A., Vigna,L., Conti,D.M., Pesatori,A.C., Racagni,G., Corsini,A., Ferri,N., Sirtori,C.R., Buoli,M., Bollati,V. and Ruscica,M. Depression and cardiovascular risk-association among Beck Depression Inventory, PCSK9 levels and insulin resistance Cardiovasc Diabetol (2020) 19, 187-187. PubMed Europe PubMed DOI PMC EPMC
Mikaeeli,S., Susan-Resiga,D., Girard,E., Ben Djoudi Ouadda,A., Day,R., Prost,S. and Seidah,N.G. Functional analysis of natural PCSK9 mutants in modern and archaic humans FEBS J (2020) 287, 515-528. PubMed Europe PubMed DOI M
Nergiz-Unal,R., Ulug,E., Kisioglu,B., Tamer,F., Bodur,M., Yalcimin,H. and Yuruk,A.A. Basi Hepatic cholesterol synthesis and lipoprotein levels impaired by dietary fructose and saturated fatty acids in mice: Insight on PCSK9 and CD36 Nutrition (2020) 79-80, 110954-110954. PubMed Europe PubMed DOI
O'Connell,E.M. and Lohoff,F.W. Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) in the Brain and Relevance for Neuropsychiatric Disorders Front Neurosci (2020) 14, 609-609. PubMed Europe PubMed DOI PMC EPMC V
Oleaga,C., Hay,J., Gurcan,E., David,L.L., Mueller,P.A., Tavori,H., Shapiro,M.D., Pamir,N. and Fazio,S. Insights on the kinetics and dynamics of the furin-cleaved form of PCSK9 J Lipid Res (2020) PubMed Europe PubMed DOI
Peng,J., Liu,M.M., Jin,J.L., Cao,Y.X., Guo,Y.L., Wu,N.Q., Zhu,C.G., Dong,Q., Sun,J., Xu,R.X. and Li,J.J. Association of circulating PCSK9 concentration with cardiovascular metabolic markers and outcomes in stable coronary artery disease patients with or without diabetes: a prospective, observational cohort study Cardiovasc Diabetol (2020) 19, 167-167. PubMed Europe PubMed DOI PMC EPMC
Petrilli,W.L., Adam,G.C., Erdmann,R.S., Abeywickrema,P., Agnani,V., Ai,X., Baysarowich,J., Byrne,N., Caldwell,J.P., Chang,W., DiNunzio,E., Feng,Z., Ford,R., Ha,S., Huang,Y., Hubbard,B., Johnston,J.M., Kavana,M., Lisnock,J.M., Liang,R., Lu,J., Lu,Z., Meng,J., Orth,P., Palyha,O., Parthasarathy,G., Salowe,S.P., Sharma,S., Shipman,J., Soisson,S.M., Strack,A.M., Youm,H., Zhao,K., Zink,D.L., Zokian,H., Addona,G.H., Akinsanya,K., Tata,J.R., Xiong,Y. and Imbriglio,J.E. From screening to targeted degradation: strategies for the discovery and optimization of small molecule ligands for PCSK9 Cell Chem Biol (2020) 27, 32-40. PubMed Europe PubMed DOI S I
Qi,Z., Hu,L., Zhang,J., Yang,W., Liu,X., Jia,D., Yao,Z., Chang,L., Pan,G., Zhong,H., Luo,X., Yao,K., Sun,A., Qian,J., Ding,Z. and Ge,J. PCSK9 Enhances Platelet Activation, Thrombosis, and Myocardial Infarct Expansion by Binding to Platelet CD36 Circulation (2020) PubMed Europe PubMed DOI
Raal,F.J., Chilton,R., Ranjith,N., Rambiritch,V., Leisegang,R.F., Ebrahim,I.O., Tonder,A.V., Shunmoogam,N., Bouharati,C., Musa,M.G., Karamchand,S., Naidoo,P. and Blom,D.J. PCSK9 Inhibitors: from Nature's lessons to clinical utility Endocr Metab Immune Disord Drug Targets (2020) PubMed Europe PubMed DOI
Rakipovski,G., Hovingh,G.K. and Nyberg,M. Proprotein convertase subtilisin/kexin type 9 inhibition as the next statin? Curr Opin Lipidol (2020) PubMed Europe PubMed DOI V
Sabnis,R.W. Novel Cyclic Tetramer Compounds as PCSK9 Inhibitors for Treating Metabolic Disorders ACS Med Chem Lett (2020) 11, 1671-1673. PubMed Europe PubMed DOI PMC EPMC
Sarkar,S.K., Foo,A.C.Y., Matyas,A., Asikhia,I., Kosenko,T., Goto,N.K., Vergara-Jaque,A. and Lagace,T.A. A transient amphipathic helix in the prodomain of PCSK9 facilitates binding to low-density lipoprotein particles J Biol Chem (2020) 295, 2285-2298. PubMed Europe PubMed DOI
Schluter,K.D., Wolf,A. and Schreckenberg,R. Coming Back to Physiology: Extra Hepatic Functions of Proprotein Convertase Subtilisin/Kexin Type 9 Front Physiol (2020) 11, 598649-598649. PubMed Europe PubMed DOI PMC EPMC V
Sgrignani,J., Fassi,E.M.A., Lammi,C., Roda,G. and Grazioso,G. Exploring Proprotein Convertase Subtilisin/Kexin 9 (PCSK9) Autoproteolysis Process by Molecular Simulations: Hints for Drug Design ChemMedChem (2020) 15, 1601-1607. PubMed Europe PubMed DOI
Shingai,Y., Kimura,N., Doijiri,R., Takahashi,K., Yokosawa,M., Kanoke,A., Kikuchi,T., Sugawara,T. and Tominaga,T. Effect of preoperative administration of proprotein convertase subtilisin/kexin type 9 inhibitor on carotid artery stenting World Neurosurg (2020) 135, e36-e36. PubMed Europe PubMed DOI I
Sinning,D. and Landmesser,U. Low-density Lipoprotein-Cholesterol Lowering Strategies for Prevention of Atherosclerotic Cardiovascular Disease: Focus on siRNA Treatment Targeting PCSK9 (Inclisiran) Curr Cardiol Rep (2020) 22, 176-176. PubMed Europe PubMed DOI PMC EPMC V
Small,A.M., Huffman,J.E., Klarin,D., Lynch,J.A., Assimes,T., DuVall,S., Sun,Y.V., Shere,L., Natarajan,P., Gaziano,M., Rader,D.J., Wilson,P.W.F., Tsao,P.S., Chang,K.M., Cho,K., O'Donnell,C.J., Casas,J.P. and Damrauer,S.M. PCSK9 loss of function is protective against extra-coronary atherosclerotic cardiovascular disease in a large multi-ethnic cohort PLoS ONE (2020) 15, e0239752-e0239752. PubMed Europe PubMed DOI PMC EPMC
Sparks,R.P., Arango,A.S., Jenkins,J.L., Guida,W.C., Tajkhorshid,E., Sparks,C.E., Sparks,J.D. and Fratti,R.A. An Allosteric Binding Site on Sortilin Regulates the Trafficking of VLDL, PCSK9, and LDLR in Hepatocytes Biochemistry (2020) 59, 4321-4335. PubMed Europe PubMed DOI PMC EPMC
Tada,H., Okada,H., Nomura,A., Nohara,A., Takamura,M. and Kawashiri,M.A. A healthy family of familial hypobetalipoproteinemia caused by a protein-truncating variant in the PCSK9 gene Intern Med (2020) 59, 783-787. PubMed Europe PubMed DOI M
Venugopal,J., Wang,J., Guo,C., Lu,H., Chen,Y.E. and Eitzman,D.T. Non-hematopoietic deficiency of proprotein convertase subtilisin/kexin type 9 deficiency leads to more severe anemia in a murine model of sickle cell disease Sci Rep (2020) 10, 16514-16514. PubMed Europe PubMed DOI PMC EPMC
Wang,D., Yang,X., Chen,Y., Gong,K., Yu,M., Gao,Y., Wu,X., Hu,H., Liao,C., Han,J. and Duan,Y. Ascorbic acid enhances low-density lipoprotein receptor expression by suppressing proprotein convertase subtilisin/kexin 9 expression J Biol Chem (2020) 295, 15870-15882. PubMed Europe PubMed DOI
Wang,X., Chen,X., Zhang,X., Su,C., Yang,M., He,W., Du,Y., Si,S., Wang,L. and Hong,B. A small-molecule inhibitor of PCSK9 transcription ameliorates atherosclerosis through the modulation of FoxO1/3 and HNF1alpha EBioMedicine (2020) 52, 102650-102650. PubMed Europe PubMed DOI PMC EPMC
Wang,X., Li,X., Liu,S., Brickell,A.N., Zhang,J., Wu,Z., Zhou,S. and Ding,Z. PCSK9 regulates pyroptosis via mtDNA damage in chronic myocardial ischemia Basic Res Cardiol (2020) 115, 66-66. PubMed Europe PubMed DOI
Wu,Y.X. and Wang,Y. [Progress on the molecular mechanisms of PCSK9-mediated degradation of low density lipoprotein receptor] Yi Chuan (2020) 42, 965-978. PubMed Europe PubMed DOI V
Ye,Q., Svatikova,A., Meeusen,J.W., Kludtke,E.L. and Kopecky,S.L. Effect of Proprotein Convertase Subtilisin/Kexin Type 9 Inhibitors on Plasma Ceramide Levels Am J Cardiol (2020) 128, 163-167. PubMed Europe PubMed DOI V
Yuan,Y., Wu,W., Sun,S., Zhang,Y. and Chen,Z. PCSK9: A Potential Therapeutic Target for Sepsis J Immunol Res (2020) 2020, 2687692-2687692. PubMed Europe PubMed DOI PMC EPMC V
Yurtseven,E., Ural,D., Baysal,K. and Tokgozoglu,L. An Update on the Role of PCSK9 in Atherosclerosis J Atheroscler Thromb (2020) 27, 909-918. PubMed Europe PubMed DOI V
Zenti,M.G., Lupo,M.G., De Martin,S., Altomari,A., Galvan,S., Aventaggiato,M., Maneschi,C., Sandri,D., Paiola,E., Battistoni,M., Eccher,A., Targher,G., Bonora,E., Ruscica,M. and Ferri,N. Impact of bariatric surgery-induced weight loss on circulating PCSK9 levels in obese patients Nutr Metab Cardiovasc Dis (2020) 30, 2372-2378. PubMed Europe PubMed DOI

2019

Adorni,M.P., Ruscica,M., Ferri,N., Bernini,F. and Zimetti,F. Proprotein convertase subtilisin/kexin type 9, brain cholesterol homeostasis and potential implication for Alzheimer's disease Front Aging Neurosci (2019) 11, 120-120. PubMed Europe PubMed DOI PMC EPMC
Elamin,A.F.M., Grafton-Clarke,C., Wen Chen,K., Obafemi,T., Luvai,A., Katira,R. and Davis,G. Potential use of PCSK9 inhibitors as a secondary preventative measure for cardiovascular disease following acute coronary syndrome: a UK real-world study Postgrad Med J (2019) 95, 61-66. PubMed Europe PubMed DOI
Ferrari,F., Stein,R., Motta,M.T. and Moriguchi,E.H. PCSK9 Inhibitors: clinical relevance, molecular mechanisms, and safety in clinical practice Arq Bras Cardiol (2019) 112, 453-460. PubMed Europe PubMed DOI I
Guarnieri,F., Kulp JL Jr, Kulp JL 3rd and Cloudsdale,I.S. Fragment-based design of small molecule PCSK9 inhibitors using simulated annealing of chemical potential simulations PLoS ONE (2019) 14, e0225780-e0225780. PubMed Europe PubMed DOI I
Iqbal,Z., Dhage,S., Mohamad,J.B., Abdel-Razik,A., Donn,R., Malik,R., Ho,J.H., Liu,Y., Adam,S., Isa,B., Stefanutti,C. and Soran,H. Efficacy and safety of PCSK9 monoclonal antibodies Expert Opin Drug Saf (2019) 18, 1191-1201. PubMed Europe PubMed DOI
Khoshnejad,M., Patel,A., Wojtak,K., Kudchodkar,S.B., Humeau,L., Lyssenko,N.N., Rader,D.J., Muthumani,K. and Weiner,D.B. Development of novel DNA-encoded PCSK9 monoclonal antibodies as lipid-lowering therapeutics Mol Ther (2019) 27, 188-199. PubMed Europe PubMed DOI
Lammi,C., Sgrignani,J., Arnoldi,A. and Grazioso,G. Biological characterization of computationally designed analogs of peptide TVFTSWEEYLDWV (Pep2-8) with increased PCSK9 antagonistic activity Sci Rep (2019) 9, 2343-2343. PubMed Europe PubMed DOI PMC EPMC I
Lammi,C., Sgrignani,J., Arnoldi,A., Lesma,G., Spatti,C., Silvani,A. and Grazioso,G. Computationally driven structure optimization, synthesis, and biological evaluation of imidazole-based proprotein convertase subtilisin/kexin 9 (PCSK9) inhibitors J Med Chem (2019) 62, 6163-6174. PubMed Europe PubMed DOI I
Lavecchia,A. and Cerchia,C. Recent advances in developing PCSK9 inhibitors for lipid-lowering therapy Future Med Chem (2019) 11, 423-441. PubMed Europe PubMed DOI
Mahmood,T. and Shapiro,M.D. Future role of proprotein convertase subtilisin/kexin type 9 inhibitors in preventive cardiology Curr Opin Cardiol (2019) 34, 519-525. PubMed Europe PubMed DOI
Momtazi-Borojeni,A.A., Jaafari,M.R., Badiee,A. and Sahebkar,A. Long-term generation of antiPCSK9 antibody using a nanoliposome-based vaccine delivery system Atherosclerosis (2019) 283, 69-78. PubMed Europe PubMed DOI
Palee,S., McSweeney,C.M., Maneechote,C., Moisescu,D.M., Jaiwongkam,T., Kerdphoo,S., Chattipakorn,S.C. and Chattipakorn,N. PCSK9 inhibitor improves cardiac function and reduces infarct size in rats with ischaemia/reperfusion injury: benefits beyond lipid-lowering effects J Cell Mol Med (2019) 23, 7310-7319. PubMed Europe PubMed DOI I
Sanchez-Hernandez,R.M., Di Taranto,M.D., Benito-Vicente,A., Uribe,K.B., Lamiquiz-Moneo,I., Larrea-Sebal,A., Jebari,S., Galicia-Garcia,U., Novoa,F.J., Boronat,M., Wagner,A.M., Civeira,F., Martin,C. and Fortunato,G. The Arg499His gain-of-function mutation in the C-terminal domain of PCSK9 Atherosclerosis (2019) 289, 162-172. PubMed Europe PubMed DOI M
Seidah,N.G. The elusive inhibitory function of the acidic N-terminal segment of the prodomain of PCSK9: the plot thickens J Mol Biol (2019) 431, 904-907. PubMed Europe PubMed DOI
Sheridan,C. PCSK9-gene-silencing, cholesterol-lowering drug impresses Nat Biotechnol (2019) 37, 1385-1387. PubMed Europe PubMed DOI
Ultsch,M., Li,W., Eigenbrot,C., Di Lello,P., Lipari,M.T., Gerhardy,S., AhYoung,A.P., Quinn,J., Franke,Y., Chen,Y., Kong Beltran,M., Peterson,A. and Kirchhofer,D. Identification of a helical segment within the intrinsically disordered region of the PCSK9 prodomain J Mol Biol (2019) 431, 885-903. PubMed Europe PubMed DOI
Wang,Y. and Liu,Z.P. PCSK9 inhibitors: novel therapeutic strategies for lowering LDL-cholesterol Mini Rev Med Chem (2019) 19, 165-176. PubMed Europe PubMed DOI
Ward,N.C., Page,M.M. and Watts,G.F. PCSK9 inhibition 2018: riding a new wave of coronary prevention Clin Sci (Lond) (2019) 133, 205-224. PubMed Europe PubMed DOI
Zhang,C., He,J., Li,J., Zhou,Y., Fu,X., Zhao,Y., Chen,J., Mao,W. and Yu,C. A novel light-electricity sensing method for PCSK9 detection based on s-PdNFs with multifunctional property Biosens Bioelectron (2019) 144, 111575-111575. PubMed Europe PubMed DOI A

2018

Bai,X.Q., Peng,J., Wang,M.M., Xiao,J., Xiang,Q., Ren,Z., Wen,H.Y., Jiang,Z.S., Tang,Z.H. and Liu,L.S. PCSK9: A potential regulator of apoE/apoER2 against inflammation in atherosclerosis? Clin Chim Acta (2018) 483, 192-196. PubMed Europe PubMed DOI
Bajaj,N.S., Patel,N., Kalra,R., Ahmad,A., Venkatraman,A., Arora,G. and Arora,P. Neurological effects of proprotein convertase subtilisin/kexin type 9 inhibitors: direct comparisons Eur Heart J Qual Care Clin Outcomes (2018) 4, 132-141. PubMed Europe PubMed DOI
Baum,S.J. and Cannon,C.P. PCSK9 inhibitor valuation: a science-based review of the two recent models Clin Cardiol (2018) 41, 544-550. PubMed Europe PubMed DOI
Chorba,J.S., Galvan,A.M. and Shokat,K.M. Stepwise processing analyses of the single-turnover PCSK9 protease reveal its substrate sequence specificity and link clinical genotype to lipid phenotype J Biol Chem (2018) 293, 1875-1886. PubMed Europe PubMed DOI P
Chorba,J.S., Galvan,A.M. and Shokat,K.M. A high-throughput luciferase assay to evaluate proteolysis of the single-turnover protease PCSK9 J Vis Exp (2018) , 58265-58265. PubMed Europe PubMed DOI A
Eroglu,Z., Tetik Vardarli,A., Duzgun,Z., Gunduz,C., Bozok Cetintas,V. and Kayikcioglu,M. Case-control study on PCSK9 R496W (rs374603772) and D374Y (rs137852912) mutations in Turkish patients with primary dyslipidemia Anatol J Cardiol (2018) 19, 334-340. PubMed Europe PubMed DOI M
Essalmani,R., Weider,E., Marcinkiewicz,J., Chamberland,A., Susan-Resiga,D., Roubtsova,A., Seidah,N.G. and Prat,A. A single domain antibody against the Cys- and His-rich domain of PCSK9 and evolocumab exhibit different inhibition mechanisms in humanized PCSK9 mice Biol Chem (2018) 399, 1363-1374. PubMed Europe PubMed DOI
Genga,K.R., Lo,C., Cirstea,M.S., Leitao Filho,F.S., Walley,K.R., Russell,J.A., Linder,A., Francis,G.A. and Boyd,J.H. Impact of PCSK9 loss-of-function genotype on 1-year mortality and recurrent infection in sepsis survivors EBioMedicine (2018) 38, 257-264. PubMed Europe PubMed DOI M
Hedayat,A.F., Park,K.H., Kwon,T.G., Woollard,J.R., Jiang,K., Carlson,D.F., Lerman,A. and Lerman,L.O. Peripheral vascular atherosclerosis in a novel PCSK9 gain-of-function mutant Ossabaw miniature pig model Transl Res (2018) 192, 30-45. PubMed Europe PubMed DOI M
Hess,C.N., Low Wang,C.C. and Hiatt,W.R. PCSK9 inhibitors: mechanisms of action, metabolic effects, and clinical outcomes Annu Rev Med (2018) 69, 133-145. PubMed Europe PubMed DOI
Iacocca,M.A., Wang,J., Sarkar,S., Dron,J.S., Lagace,T., McIntyre,A.D., Lau,P., Robinson,J.F., Yang,P., Knoll,J.H., Cao,H., McPherson,R. and Hegele,R.A. Whole-gene duplication of PCSK9 as a novel genetic mechanism for severe familial hypercholesterolemia Can J Cardiol (2018) 34, 1316-1324. PubMed Europe PubMed DOI M
Jiang,C., Nischal,H., Sun,H., Li,L., Cao,Y., Wei,P., Chang,J.Y. and Teng,B.B. Non-native conformational isomers of the catalytic domain of PCSK9 induce an immune response, reduce lipids and increase LDL receptor levels Int J Mol Sci (2018) 19 PubMed Europe PubMed DOI
Karagiannis,A.D., Liu,M., Toth,P.P., Zhao,S., Agrawal,D.K., Libby,P. and Chatzizisis,Y.S. Pleiotropic anti-atherosclerotic effects of PCSK9 inhibitors from molecular biology to clinical translation Curr Atheroscler Rep (2018) 20, 20-20. PubMed Europe PubMed DOI V
Kosmas,C.E., Munoz Estrella,A., Sourlas,A., Silverio,D., Hilario,E., Montan,P.D. and Guzman,E. Inclisiran: a new promising agent in the management of hypercholesterolemia Diseases (2018) 6 PubMed Europe PubMed DOI
Li,Z. and Liu,Q. Proprotein convertase subtilisin/kexin type 9 inhibits hepatitis C virus replication through interacting with NS5A J Gen Virol (2018) 99, 44-61. PubMed Europe PubMed DOI
Londregan,A.T., Aspnes,G., Limberakis,C., Loria,P.M., McClure,K.F., Petersen,D.N., Raymer,B., Ruggeri,R.B., Wei,L., Xiao,J. and Piotrowski,D.W. Discovery of N-(piperidin-3-yl)-N-(pyridin-2-yl)piperidine/piperazine-1-carboxamides as small molecule inhibitors of PCSK9 Bioorg Med Chem Lett (2018) 28, 3685-3688. PubMed Europe PubMed DOI
Masuda,Y., Yamaguchi,S., Suzuki,C., Aburatani,T., Nagano,Y., Miyauchi,R., Suzuki,E., Yamamura,N., Nagatomo,K., Ishihara,H., Okuno,K., Nara,F., Matschiner,G., Hashimoto,R., Takahashi,T. and Nishizawa,T. Generation and characterization of a novel small biologic alternative to proprotein convertase subtilisin/kexin type 9 (PCSK9) antibodies, DS-9001a, albumin binding domain-fused anticalin protein J Pharmacol Exp Ther (2018) 365, 368-378. PubMed Europe PubMed DOI
Nishikido,T. and Ray,K.K. Non-antibody approaches to proprotein convertase subtilisin kexin 9 inhibition: siRNA, antisense oligonucleotides, adnectins, vaccination, and new attempts at small-molecule inhibitors based on new discoveries Front Cardiovasc Med (2018) 5, 199-199. PubMed Europe PubMed DOI PMC EPMC I
Paquette,M. and Baass,A. A novel cause of familial hypercholesterolemia: PCSK9 gene duplication Can J Cardiol (2018) 34, 1259-1260. PubMed Europe PubMed DOI M
Paquette,M., Hegele,R.A. and Baass,A. PCSK9 inhibitors in familial hypercholesterolemia: what is the evidence? J Clin Lipidol (2018) 12, 1106-1108. PubMed Europe PubMed DOI
Pettersen,D. and Fjellstrom,O. Small molecule modulators of PCSK9 - a literature and patent overview Bioorg Med Chem Lett (2018) 28, 1155-1160. PubMed Europe PubMed DOI V I
Roth,E.M. and Davidson,M.H. PCSK9 inhibitors: mechanism of action, efficacy, and safety Rev Cardiovasc Med (2018) 19, S31-S31. PubMed Europe PubMed
Stoekenbroek,R.M. and Kastelein,J.J.P. Proprotein convertase subtilisin/kexin type 9: from genetics to clinical trials Curr Opin Cardiol (2018) 33, 269-275. PubMed Europe PubMed DOI V
Stoekenbroek,R.M., Lambert,G., Cariou,B. and Hovingh,G.K. Inhibiting PCSK9 - biology beyond LDL control Nat Rev Endocrinol (2018) 15, 52-62. PubMed Europe PubMed DOI
Taechalertpaisarn,J., Zhao,B., Liang,X. and Burgess,K. Small molecule inhibitors of the PCSK9.LDLR interaction J Am Chem Soc (2018) 140, 3242-3249. PubMed Europe PubMed DOI
Yuan,F., Guo,L., Park,K.H., Woollard,J.R., Taek-Geun,K., Jiang,K., Melkamu,T., Zang,B., Smith,S.L., Fahrenkrug,S.C., Kolodgie,F.D., Lerman,A., Virmani,R., Lerman,L.O. and Carlson,D.F. Ossabaw pigs with a PCSK9 gain-of-function mutation develop accelerated coronary atherosclerotic lesions: a novel model for preclinical studies J Am Heart Assoc (2018) 7 PubMed Europe PubMed DOI M

2017

Baruch,A., Mosesova,S., Davis,J.D., Budha,N., Vilimovskij,A., Kahn,R., Peng,K., Cowan,K.J., Harris,L.P., Gelzleichter,T., Lehrer,J., Davis,J.C., Jr. and Tingley,W.G. Effects of RG7652, a monoclonal antibody against PCSK9, on LDL-C, LDL-C subfractions, and inflammatory biomarkers in patients at high risk of or with established coronary heart disease (from the Phase 2 EQUATOR Study) Am J Cardiol (2017) 119, 1576-1583. PubMed Europe PubMed DOI
Baruch,A., Luca,D., Kahn,R.S., Cowan,K.J., Leabman,M., Budha,N.R., Chiu,C.P.C., Wu,Y., Kirchhofer,D., Peterson,A., Davis,J.C., Jr. and Tingley,W.G. A phase 1 study to evaluate the safety and LDL cholesterol-lowering effects of RG7652, a fully human monoclonal antibody against proprotein convertase subtilisin/kexin type 9 Clin Cardiol (2017) 40, 503-511. PubMed Europe PubMed DOI
Chaudhary,R., Garg,J., Shah,N. and Sumner,A. PCSK9 inhibitors: a new era of lipid lowering therapy World J Cardiol (2017) 9, 76-91. PubMed Europe PubMed DOI PMC EPMC
Cirulli,E.T. and Ginsburg,G.S. Studying genetic resilience to improve human health Oral Dis (2017) 23, 685-688. PubMed Europe PubMed DOI M
Civeira,F. and Jarauta,E. Vaccine against PCSK9: the natural strategy from passive to active immunization for the prevention of atherosclerosis J Thorac Dis (2017) 9, 4291-4294. PubMed Europe PubMed DOI PMC EPMC
Di Taranto,M.D., Benito-Vicente,A., Giacobbe,C., Uribe,K.B., Rubba,P., Etxebarria,A., Guardamagna,O., Gentile,M., Martin,C. and Fortunato,G. Identification and in vitro characterization of two new PCSK9 gain of function variants found in patients with familial hypercholesterolemia Sci Rep (2017) 7, 15282-15282. PubMed Europe PubMed DOI PMC EPMC M
Dron,J.S. and Hegele,R.A. Complexity of mechanisms among human proprotein convertase subtilisin-kexin type 9 variants Curr Opin Lipidol (2017) 28, 161-169. PubMed Europe PubMed DOI M
El Khoury,P., Elbitar,S., Ghaleb,Y., Khalil,Y.A., Varret,M., Boileau,C. and Abifadel,M. PCSK9 Mutations in familial hypercholesterolemia: from a groundbreaking discovery to anti-PCSK9 therapies Curr Atheroscler Rep (2017) 19, 49-49. PubMed Europe PubMed DOI M V
Fitzgerald,K., White,S., Borodovsky,A., Bettencourt,B.R., Strahs,A., Clausen,V., Wijngaard,P., Horton,J.D., Taubel,J., Brooks,A., Fernando,C., Kauffman,R.S., Kallend,D., Vaishnaw,A. and Simon,A. A highly durable RNAi therapeutic inhibitor of PCSK9 N Engl J Med (2017) 376, 41-51. PubMed Europe PubMed DOI
Gibbs,J.P., Slatter,J.G., Egbuna,O., Geller,M., Hamilton,L., Dias,C.S., Xu,R.Y., Johnson,J., Wasserman,S.M. and Emery,M.G. Evaluation of evolocumab (AMG 145), a fully human anti-PCSK9 IgG2 monoclonal antibody, in subjects with hepatic impairment J Clin Pharmacol (2017) 57, 513-523. PubMed Europe PubMed DOI
Gielen,S. PCSK9 deficiency: a double-edged sword? Eur J Prev Cardiol (2017) 24, 1867-1869. PubMed Europe PubMed DOI M
Gouni-Berthold,I. The efficacy of anti-PCSK9 antibodies: results from recent trials Atheroscler Suppl (2017) 30, 9-18. PubMed Europe PubMed DOI
Gumbiner,B., Joh,T., Liang,H., Wan,H., Levisetti,M., Vana,A.M., Shelton,D.L., Forgues,P., Billotte,S., Pons,J., Baum,C.M. and Garzone,P.D. The effects of single- and multiple-dose administration of bococizumab (RN316/PF-04950615), a humanized IgG2Deltaa monoclonal antibody binding proprotein convertase subtilisin/kexin type 9, in hypercholesterolemic subjects treated with and without atorvastatin: Results from four phase I studies Cardiovasc Ther (2017) 36 PubMed Europe PubMed DOI
Gustafsen,C., Olsen,D., Vilstrup,J., Lund,S., Reinhardt,A., Wellner,N., Larsen,T., Andersen,C.B.F., Weyer,K., Li,J.P., Seeberger,P.H., Thirup,S., Madsen,P. and Glerup,S. Heparan sulfate proteoglycans present PCSK9 to the LDL receptor Nat Commun (2017) 8, 503-503. PubMed Europe PubMed DOI PMC EPMC
Hansen,R.J., Berna,M.J., Sperry,A.E., Beyer,T.P., Wroblewski,V.J., Schroeder,K.M. and Eacho,P.I. Quantitative characterization of the mechanism of action and impact of a 'proteolysis-permitting' anti-PCSK9 antibody MAbs (2017) 9, 285-296. PubMed Europe PubMed DOI
Higgins,C.A. and Rees,A. The onward march of PCSK9 inhibition Curr Opin Lipidol (2017) 28, 222-223. PubMed Europe PubMed DOI
Ito,M.K. and Santos,R.D. PCSK9 inhibition with monoclonal antibodies: modern management of hypercholesterolemia J Clin Pharmacol (2017) 57, 7-32. PubMed Europe PubMed DOI
Lambert,G., Thedrez,A., Croyal,M., Ramin-Mangata,S., Couret,D., Diotel,N., Nobecourt-Dupuy,E., Krempf,M., LeBail,J.C., Poirier,B., Blankenstein,J., Villard,E.F. and Guillot,E. The complexity of lipoprotein (a) lowering by PCSK9 monoclonal antibodies Clin Sci (Lond) (2017) 131, 261-268. PubMed Europe PubMed DOI
Landlinger,C., Pouwer,M.G., Juno,C., van der Hoorn,J.W.A., Pieterman,E.J., Jukema,J.W., Staffler,G., Princen,H.M.G. and Galabova,G. The AT04A vaccine against proprotein convertase subtilisin/kexin type 9 reduces total cholesterol, vascular inflammation, and atherosclerosis in APOE*3Leiden.CETP mice Eur Heart J (2017) 38, 2499-2507. PubMed Europe PubMed DOI
Li,Y., He,J., Chen,J., Niu,Y., Zhao,Y., Zhang,Y. and Yu,C. A dual-type responsive electrochemical immunosensor for quantitative detection of PCSK9 based on n-C60-PdPt/N-GNRs and Pt-poly (methylene blue) nanocomposites Biosens Bioelectron (2017) 101, 7-13. PubMed Europe PubMed DOI A
Liberale,L., Montecucco,F., Camici,G.G., Dallegri,F., Vecchie,A., Carbone,F. and Bonaventura,A. Treatment with proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors to reduce cardiovascular inflammation and outcomes Curr Med Chem (2017) 24, 1403-1416. PubMed Europe PubMed DOI
Lintner,N.G., McClure,K.F., Petersen,D., Londregan,A.T., Piotrowski,D.W., Wei,L., Xiao,J., Bolt,M., Loria,P.M., Maguire,B., Geoghegan,K.F., Huang,A., Rolph,T., Liras,S., Doudna,J.A., Dullea,R.G. and Cate,J.H. Selective stalling of human translation through small-molecule engagement of the ribosome nascent chain PLoS Biol (2017) 15, e2001882-e2001882. PubMed Europe PubMed DOI K
McClure,K.F., Piotrowski,D.W., Petersen,D., Wei,L., Xiao,J., Londregan,A.T., Kamlet,A.S., Dechert-Schmitt,A.M., Raymer,B., Ruggeri,R.B., Canterbury,D., Limberakis,C., Liras,S., DaSilva-Jardine,P., Dullea,R.G., Loria,P.M., Reidich,B., Salatto,C.T., Eng,H., Kimoto,E., Atkinson,K., King-Ahmad,A., Scott,D., Beaumont,K., Chabot,J.R., Bolt,M.W., Maresca,K., Dahl,K., Arakawa,R., Takano,A. and Halldin,C. Liver-targeted small-molecule inhibitors of proprotein convertase subtilisin/kexin type 9 synthesis Angew Chem Int Ed Engl (2017) 56, 16218-16222. PubMed Europe PubMed DOI
Mullard,A. Nine paths to PCSK9 inhibition Nat Rev Drug Discov (2017) 16, 299-301. PubMed Europe PubMed DOI
Naeli,P., Mirzadeh Azad,F., Malakootian,M., Seidah,N.G. and Mowla,S.J. Post-transcriptional regulation of PCSK9 by miR-191, miR-222, and miR-224 Front Genet (2017) 8, 189-189. PubMed Europe PubMed DOI PMC EPMC
Pan,Y., Zhou,Y., Wu,H., Chen,X., Hu,X., Zhang,H., Zhou,Z., Qiu,Z. and Liao,Y. A therapeutic peptide vaccine against PCSK9 Sci Rep (2017) 7, 12534-12534. PubMed Europe PubMed DOI PMC EPMC
Preiss,D. and Mafham,M. PCSK9 inhibition: the dawn of a new age in cholesterol lowering? Diabetologia (2017) 60, 381-389. PubMed Europe PubMed DOI V
Scherer,D.J., Nelson,A.J., Psaltis,P.J. and Nicholls,S.J. Targeting low-density lipoprotein cholesterol with PCSK9 inhibitors Intern Med J (2017) 47, 856-865. PubMed Europe PubMed DOI V
Schmitz,J. and Gouni-Berthold,I. Anti-PCSK9 antibodies: a new era in the treatment of dyslipidemia Curr Pharm Des (2017) 23, 1484-1494. PubMed Europe PubMed
Seidah,N.G. The PCSK9 revolution and the potential of PCSK9-based therapies to reduce LDL-cholesterol Glob Cardiol Sci Pract (2017) 2017, e201702-e201702. PubMed Europe PubMed DOI PMC EPMC
Seidah,N.G. Insights into a PCSK9 structural groove: a harbinger of new drugs to reduce LDL-cholesterol Nat Struct Mol Biol (2017) 24, 785-786. PubMed Europe PubMed DOI
Shen,T., James,D.E. and Krueger,K.A. Population pharmacokinetics (PK) and pharmacodynamics (PD) analysis of LY3015014, a monoclonal antibody to protein convertase subtilisin/kexin type 9 (PCSK9) in healthy subjects and hypercholesterolemia patients Pharm Res (2017) 34, 185-192. PubMed Europe PubMed DOI
Varret,M., Abifadel,M., Despina Kalopissis,A., Fatoumata Maiga,S., Lambert,G., Seidah,N.G., Boileau,C. and Chabert,M. Effect of the p.Arg357His mutation of PCSK9 on basal and postprandial lipoprotein metabolism Atherosclerosis (2017) 263, e2-e2. PubMed Europe PubMed DOI M
Wang,L., Hong,B. and Wang,X. Identification of novel human proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors using a cell-based high-throughput screening assay Atherosclerosis (2017) 263, e220-e220. PubMed Europe PubMed DOI
Zhang,Y., Ultsch,M., Skelton,N.J., Burdick,D.J., Beresini,M.H., Li,W., Kong-Beltran,M., Peterson,A., Quinn,J., Chiu,C., Wu,Y., Shia,S., Moran,P., Di Lello,P., Eigenbrot,C. and Kirchhofer,D. Discovery of a cryptic peptide-binding site on PCSK9 and design of antagonists Nat Struct Mol Biol (2017) 24, 848-856. PubMed Europe PubMed DOI I

2016

Achimastos,A., Alexandrides,T., Alexopoulos,D., Athyros,V., Bargiota,A., Bilianou,E., Chrysochoou,C., Drogari,E., Elisaf,M., Ganotakis,E., Goudevenos,I., Ioannidis,I., Kolovou,G., Kotsis,V., Lekakis,I., Liberopoulos,E., Melidonis,A., Nikolaou,V., Ntaios,G., Papanas,N., Pappas,S., Pitsavos,C., Rallidis,L., Richter,D., Skoumas,I., Tentolouris,N., Tousoulis,D., Tselepis,A., Tsioufis,K., Tziakas,D., Tziomalos,K., Vardas,P., Vlachopoulos,C. and Vlahakos,D. Expert consensus on the rational clinical use of proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors Hormones (Athens) (2016) 15, 8-14. PubMed Europe PubMed DOI
Alkindi,M., Siminovitch,K.A., Gupta,M. and Genest,J. Monoclonal antibodies for the treatment of hypercholesterolemia: targeting PCSK9 Can J Cardiol (2016) 32, 1552-1560. PubMed Europe PubMed DOI
Banerjee,Y., Santos,R.D., Al-Rasadi,K. and Rizzo,M. Targeting PCSK9 for therapeutic gains: have we addressed all the concerns? Atherosclerosis (2016) 248, 62-75. PubMed Europe PubMed DOI
Chackerian,B. and Remaley,A. Vaccine strategies for lowering LDL by immunization against proprotein convertase subtilisin/kexin type 9 Curr Opin Lipidol (2016) 27, 345-350. PubMed Europe PubMed DOI
Della Badia,L.A., Elshourbagy,N.A. and Mousa,S.A. Targeting PCSK9 as a promising new mechanism for lowering low-density lipoprotein cholesterol Pharmacol Ther (2016) 164, 183-194. PubMed Europe PubMed DOI
Denegri,A., Petrova-Slater,I., Pasotti,E., Rossi,M.G., Pedrazzini,G.B., Moccetti,T. and Moccetti,M. PCSK9 inhibitors: an overview on a new promising lipid-lowering therapy J Cardiovasc Med (Hagerstown) (2016) 17, 237-244. PubMed Europe PubMed DOI
Dixon,D.L., Trankle,C., Buckley,L., Parod,E., Carbone,S., Van Tassell,B.W. and Abbate,A. A review of PCSK9 inhibition and its effects beyond LDL receptors J Clin Lipidol (2016) 10, 1073-1080. PubMed Europe PubMed DOI
Eisen,A. and Giugliano,R.P. Advances in the field of proprotein convertase subtilisin kexin type 9 inhibitors Curr Opin Cardiol (2016) 31, 644-653. PubMed Europe PubMed DOI
Elbitar,S., Khoury,P.E., Ghaleb,Y., Rabes,J.P., Varret,M., Seidah,N.G., Boileau,C. and Abifadel,M. Proprotein convertase subtilisin / kexin 9 (PCSK9) inhibitors and the future of dyslipidemia therapy: an updated patent review (2011-2015) Expert Opin Ther Pat (2016) 26, 1377-1392. PubMed Europe PubMed DOI
Fala,L. Repatha (Evolocumab): second PCSK9 inhibitor approved by the FDA for patients with familial hypercholesterolemia Am Health Drug Benefits (2016) 9, 136-139. PubMed Europe PubMed PMC EPMC
Feinstein,M.J. and Lloyd-Jones,D.M. Monoclonal antibodies for lipid management Curr Atheroscler Rep (2016) 18, 39-39. PubMed Europe PubMed DOI
Ferri,N., Marchiano,S., Tibolla,G., Baetta,R., Dhyani,A., Ruscica,M., Uboldi,P., Catapano,A.L. and Corsini,A. PCSK9 knock-out mice are protected from neointimal formation in response to perivascular carotid collar placement Atherosclerosis (2016) 253, 214-224. PubMed Europe PubMed DOI K
Garvie,C.W., Fraley,C.V., Elowe,N.H., Culyba,E.K., Lemke,C.T., Hubbard,B.K., Kaushik,V.K. and Daniels,D.S. Point mutations at the catalytic site of PCSK9 inhibit folding, autoprocessing, and interaction with the LDL receptor Protein Sci (2016) 25, 2018-2027. PubMed Europe PubMed DOI M
He,X.M., Chen,L., Wang,T.S., Zhang,Y.B., Luo,J.B. and Feng,X.X. E670G polymorphism of PCSK9 gene of patients with coronary heart disease among Han population in Hainan and three provinces in the northeast of China Asian Pac J Trop Med (2016) 9, 172-176. PubMed Europe PubMed DOI M
Jones,P.H., Bays,H.E., Chaudhari,U., Pordy,R., Lorenzato,C., Miller,K. and Robinson,J.G. Safety of alirocumab (a PCSK9 monoclonal antibody) from 14 randomized trials Am J Cardiol (2016) 118, 1805-1811. PubMed Europe PubMed DOI
Kastelein,J.J., Nissen,S.E., Rader,D.J., Hovingh,G.K., Wang,M.D., Shen,T. and Krueger,K.A. Safety and efficacy of LY3015014, a monoclonal antibody to proprotein convertase subtilisin/kexin type 9 (PCSK9): a randomized, placebo-controlled phase 2 study Eur Heart J (2016) 37, 1360-1369. PubMed Europe PubMed DOI
Klose,G. [Introduction of PCSK9 inhibitors : new perspectives in treatment and practical implementation] Herz (2016) 41, 307-312. PubMed Europe PubMed DOI
Langsted,A., Nordestgaard,B.G., Benn,M., Tybjaerg-Hansen,A. and Kamstrup,P.R. PCSK9 R46L loss-of-function mutation reduces lipoprotein(a), LDL cholesterol, and risk of aortic valve stenosis J Clin Endocrinol Metab (2016) 101, 3281-3287. PubMed Europe PubMed DOI M
Lauer,M.S. PCSK9 inhibitors: lots of work done, lots more to do Ann Intern Med (2016) 164, 624-625. PubMed Europe PubMed DOI
Laufs,U., Custodis,F. and Werner,C. [PCSK9 inhibitors : recommendations for patient selection] Herz (2016) 41, 296-306. PubMed Europe PubMed DOI
Lu,H., Howatt,D.A., Balakrishnan,A., Graham,M.J., Mullick,A.E. and Daugherty,A. Hypercholesterolemia induced by a PCSK9 gain-of-function mutation augments angiotensin II-induced abdominal aortic aneurysms in C57BL/6 mice-brief report Arterioscler Thromb Vasc Biol (2016) 36, 1753-1757. PubMed Europe PubMed DOI M
Maluch,I., Walewska,A., Sikorska,E. and Prahl,A. [Proprotein convertases - family of serine proteases with a broad spectrum of physiological functions] Postepy Biochem (2016) 62, 472-481. PubMed Europe PubMed V
Manniello,M. and Pisano,M. Alirocumab (Praluent): first in the new class of PCSK9 inhibitors P T (2016) 41, 28-53. PubMed Europe PubMed PMC EPMC
Mazhar,F. and Haider,N. Proprotein convertase subtilisin/kexin type 9 enzyme inhibitors: an emerging new therapeutic option for the treatment of dyslipidemia J Pharmacol Pharmacother (2016) 7, 190-193. PubMed Europe PubMed DOI PMC EPMC
McDonagh,M., Peterson,K., Holzhammer,B. and Fazio,S. A systematic review of PCSK9 inhibitors alirocumab and evolocumab J Manag Care Spec Pharm (2016) 22, 641-653. PubMed Europe PubMed DOI V
Moore,K.J. and Goldberg,I.J. Emerging roles of PCSK9: more than a one-trick pony Arterioscler Thromb Vasc Biol (2016) 36, 211-212. PubMed Europe PubMed DOI PMC EPMC
Neumann,C.L., Schettler,E. and Schettler,V.J. Significance of monoclonal PCSK9-antibodies - new approaches to the therapy of hypercholesterolemia Blood Purif (2016) 41, 270-276. PubMed Europe PubMed DOI
Norata,G.D., Tavori,H., Pirillo,A., Fazio,S. and Catapano,A.L. Biology of proprotein convertase subtilisin kexin 9: beyond low-density lipoprotein cholesterol lowering Cardiovasc Res (2016) 112, 429-442. PubMed Europe PubMed DOI
Ohta,N., Hori,M., Takahashi,A., Ogura,M., Makino,H., Tamanaha,T., Fujiyama,H., Miyamoto,Y. and Harada-Shiba,M. Proprotein convertase subtilisin/kexin 9 V4I variant with LDLR mutations modifies the phenotype of familial hypercholesterolemia J Clin Lipidol (2016) 10, 547-555. PubMed Europe PubMed DOI M
Paton,D.M. PCSK9 inhibitors: monoclonal antibodies for the treatment of hypercholesterolemia Drugs Today (Barc) (2016) 52, 183-192. PubMed Europe PubMed DOI
Pedro-Botet,J. and Badimon,L. [PCSK9: Structure and function. PCSK9 and low-density lipoprotein receptor. Mutations and their effects] Clin Investig Arterioscler (2016) 28 Suppl 2, 3-8. PubMed Europe PubMed DOI M
Petersen,D.N., Hawkins,J., Ruangsiriluk,W., Stevens,K.A., Maguire,B.A., O'Connell,T.N., Rocke,B.N., Boehm,M., Ruggeri,R.B., Rolph,T., Hepworth,D., Loria,P.M. and Carpino,P.A. A small-molecule anti-secretagogue of PCSK9 targets the 80S ribosome to inhibit PCSK9 protein translation Cell Chem Biol (2016) 23, 1362-1371. PubMed Europe PubMed DOI
Poirier,S., Hamouda,H.A., Villeneuve,L., Demers,A. and Mayer,G. Trafficking dynamics of PCSK9-induced LDLR degradation: focus on human PCSK9 mutations and C-terminal domain PLoS ONE (2016) 11, e0157230-e0157230. PubMed Europe PubMed DOI M
Raal,F.J., Giugliano,R.P., Sabatine,M.S., Koren,M.J., Blom,D., Seidah,N.G., Honarpour,N., Lira,A., Xue,A., Chiruvolu,P., Jackson,S., Di,M., Peach,M., Somaratne,R., Wasserman,S.M., Scott,R. and Stein,E.A. PCSK9 inhibition-mediated reduction in Lp(a) with evolocumab: an analysis of 10 clinical trials and the LDL receptor's role J Lipid Res (2016) 57, 1086-1096. PubMed Europe PubMed DOI
Raedler,L.A. Praluent (alirocumab): first PCSK9 inhibitor approved by the FDA for hypercholesterolemia Am Health Drug Benefits (2016) 9, 123-126. PubMed Europe PubMed PMC EPMC
Rey,J., Poitiers,F., Paehler,T., Brunet,A., DiCioccio,A.T., Cannon,C.P., Surks,H.K., Pinquier,J.L., Hanotin,C. and Sasiela,W.J. Relationship between low-density lipoprotein cholesterol, free proprotein convertase subtilisin/kexin type 9, and alirocumab levels after different lipid-lowering strategies J Am Heart Assoc (2016) 5 PubMed Europe PubMed DOI
Rosenson,R.S., Jacobson,T.A., Preiss,D., Djedjos,C.S., Dent,R., Bridges,I. and Miller,M. Efficacy and safety of the PCSK9 inhibitor evolocumab in patients with mixed hyperlipidemia Cardiovasc Drugs Ther (2016) 30, 305-313. PubMed Europe PubMed DOI
Roth,E.M. Alirocumab for hyperlipidemia: ODYSSEY phase III clinical trial results and US FDA approval indications Future Cardiol (2016) 12, 115-128. PubMed Europe PubMed DOI
Salowe,S.P., Zhang,L., Zokian,H.J., Gesell,J.J., Zink,D.L., Wiltsie,J., Ai,X., Kavana,M. and Pinto,S. In vitro assays for the discovery of PCSK9 autoprocessing inhibitors J Biomol Screen (2016) 21, 1034-1041. PubMed Europe PubMed DOI I
Schmidli,R. PCSK9 inhibitors - clinical applications Aust Prescr (2016) 39, 168-170. PubMed Europe PubMed DOI PMC EPMC
Seidah,N.G. New developments in proprotein convertase subtilisin-kexin 9's biology and clinical implications Curr Opin Lipidol (2016) 27, 274-281. PubMed Europe PubMed DOI
Stein,E.A. What role will proprotein convertase subtilisin/kexin type 9 inhibitors play in hyperlipidemia management? Curr Opin Endocrinol Diabetes Obes (2016) 23, 97-105. PubMed Europe PubMed DOI
Stein,E.A. PCSK9: the critical role of familial hypercholesterolemia from discovery to benefit for all : Editorial to: "Efficacy and safety of alirocumab in patients with heterozygous familial hypercholesterolemia and LDL-C of 160 mg/Dl or higher" by Henry N. Ginsberg et Al Cardiovasc Drugs Ther (2016) 30, 427-431. PubMed Europe PubMed DOI
Strat,A.L., Ghiciuc,C.M., Lupusoru,C.E. and Mitu,F. New class of drugs: therapeutic RNAi inhibition of PCSK9 as a specific LDL-C lowering therapy Rev Med Chir Soc Med Nat Iasi (2016) 120, 228-232. PubMed Europe PubMed
Stroes,E., Guyton,J.R., Lepor,N., Civeira,F., Gaudet,D., Watts,G.F., Baccara-Dinet,M.T., Lecorps,G., Manvelian,G. and Farnier,M. Efficacy and safety of alirocumab 150 mg every 4 weeks in patients with hypercholesterolemia not on statin therapy: the ODYSSEY CHOICE II study J Am Heart Assoc (2016) 5 PubMed Europe PubMed DOI
Stucchi,M., Grazioso,G., Lammi,C., Manara,S., Zanoni,C., Arnoldi,A., Lesma,G. and Silvani,A. Disrupting the PCSK9/LDLR protein-protein interaction by an imidazole-based minimalist peptidomimetic Org Biomol Chem (2016) 14, 9736-9740. PubMed Europe PubMed DOI
Thedrez,A., Sjouke,B., Passard,M., Prampart-Fauvet,S., Guedon,A., Croyal,M., Dallinga-Thie,G., Peter,J., Blom,D., Ciccarese,M., Cefalu,A.B., Pisciotta,L., Santos,R.D., Averna,M., Raal,F., Pintus,P., Cossu,M., Hovingh,K. and Lambert,G. Proprotein convertase subtilisin kexin type 9 inhibition for autosomal recessive hypercholesterolemia-brief report Arterioscler Thromb Vasc Biol (2016) 36, 1647-1650. PubMed Europe PubMed DOI
Wang,X., Raghavan,A., Chen,T., Qiao,L., Zhang,Y., Ding,Q. and Musunuru,K. CRISPR-Cas9 targeting of PCSK9 in human hepatocytes in vivo - brief report Arterioscler Thromb Vasc Biol (2016) 36, 783-786. PubMed Europe PubMed DOI K
Whayne,T.F., Jr. Defining the role of PCSK9 inhibitors in the treatment of hyperlipidemia Am J Cardiovasc Drugs (2016) 16, 83-92. PubMed Europe PubMed DOI
Wierod,L., Cameron,J., Strom,T.B. and Leren,T.P. Studies of the autoinhibitory segment comprising residues 31-60 of the prodomain of PCSK9: possible implications for the mechanism underlying gain-of-function mutations Mol Genet Metab Rep (2016) 9, 86-93. PubMed Europe PubMed DOI PMC EPMC M
Yadav,K., Sharma,M. and Ferdinand,K.C. Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors: present perspectives and future horizons Nutr Metab Cardiovasc Dis (2016) 26, 853-862. PubMed Europe PubMed DOI
Zhang,L., Song,K., Zhu,M., Shi,J., Zhang,H., Xu,L. and Chen,Y. Proprotein convertase subtilisin/kexin type 9 (PCSK9) in lipid metabolism, atherosclerosis and ischemic stroke Int J Neurosci (2016) 126, 675-680. PubMed Europe PubMed DOI V

2015

Alghamdi,R.H., O'Reilly,P., Lu,C., Gomes,J., Lagace,T.A. and Basak,A. LDL-R promoting activity of peptides derived from human PCSK9 catalytic domain (153-421): design, synthesis and biochemical evaluation Eur J Med Chem (2015) 92, 890-907. PubMed Europe PubMed DOI
Alves,A.C., Etxebarria,A., Medeiros,A.M., Benito-Vicente,A., Thedrez,A., Passard,M., Croyal,M., Martin,C., Lambert,G. and Bourbon,M. Characterization of the first PCSK9 gain of function homozygote J Am Coll Cardiol (2015) 66, 2152-2154. PubMed Europe PubMed DOI M
Ballantyne,C.M., Neutel,J., Cropp,A., Duggan,W., Wang,E.Q., Plowchalk,D., Sweeney,K., Kaila,N., Vincent,J. and Bays,H. Results of bococizumab, a monoclonal antibody against proprotein convertase subtilisin/kexin type 9, from a randomized, placebo-controlled, dose-ranging study in statin-treated subjects with hypercholesterolemia Am J Cardiol (2015) 115, 1212-1221. PubMed Europe PubMed DOI
Berger,J.M., Vaillant,N., Le May,C., Calderon,C., Bregeon,J., Prieur,X., Hadchouel,J., Loirand,G. and Cariou,B. PCSK9-deficiency does not alter blood pressure and sodium balance in mouse models of hypertension Atherosclerosis (2015) 239, 252-259. PubMed Europe PubMed DOI K
Bergeron,N., Phan,B.A., Ding,Y., Fong,A. and Krauss,R.M. Proprotein convertase subtilisin/kexin type 9 inhibition: a new therapeutic mechanism for reducing cardiovascular disease risk Circulation (2015) 132, 1648-1666. PubMed Europe PubMed DOI
Bonnefond,A., Yengo,L., Le May,C., Fumeron,F., Marre,M., Balkau,B., Charpentier,G., Franc,S., Froguel,P. and Cariou,B. The loss-of-function PCSK9 p.R46L genetic variant does not alter glucose homeostasis Diabetologia (2015) 58, 2051-2055. PubMed Europe PubMed DOI M
Budha,N.R., Leabman,M., Jin,J.Y., Wada,D.R., Baruch,A., Peng,K., Tingley,W.G. and Davis,J.D. Modeling and simulation to support phase 2 dose selection for RG7652, a fully human monoclonal antibody against proprotein convertase subtilisin/kexin type 9 AAPS J (2015) 17, 881-890. PubMed Europe PubMed DOI
Bulum,T. and Duvnjak,L. Proprotein convertase subtilisin kexin 9 inhibitors: new class of lipid-lowering therapy Diabetol Croat (2015) 44, 21-30.
Cao,Y., Yang,H., Zhou,X., Mao,H., Gao,T., Hu,Z., He,L., Pan,F. and Guo,Z. Selection and characterization of human PCSK9 antibody from phage displayed antibody library Biochem Biophys Res Commun (2015) 463, 712-718. PubMed Europe PubMed DOI
Chapman,M.J., Stock,J.K. and Ginsberg,H.N. PCSK9 inhibitors and cardiovascular disease: heralding a new therapeutic era Curr Opin Lipidol (2015) 26, 511-520. PubMed Europe PubMed DOI
Cicero,A.F., Colletti,A. and Borghi,C. Profile of evolocumab and its potential in the treatment of hyperlipidemia Drug Des Devel Ther (2015) 9, 3073-3082. PubMed Europe PubMed DOI PMC EPMC
Crossey,E., Amar,M.J., Sampson,M., Peabody,J., Schiller,J.T., Chackerian,B. and Remaley,A.T. A cholesterol-lowering VLP vaccine that targets PCSK9 Vaccine (2015) 33, 5747-5755. PubMed Europe PubMed DOI
Dragan,S., Serban,M.C. and Banach,M. Proprotein convertase subtilisin/kexin 9 inhibitors: an emerging lipid-lowering therapy? J Cardiovasc Pharmacol Ther (2015) 20, 157-168. PubMed Europe PubMed DOI I
EBioMedicine PCSK9 inhibitors: what lies beyond monoclonal antibodies? EBioMedicine (2015) 2, 1835-1835. PubMed Europe PubMed DOI PMC EPMC I
Ferdinand,K.C. and Nasser,S.A. PCSK9 inhibition: discovery, current evidence, and potential effects on LDL-C and Lp(a) Cardiovasc Drugs Ther (2015) 29, 295-308. PubMed Europe PubMed DOI
Gencer,B., Lambert,G. and Mach,F. PCSK9 inhibitors Swiss Med Wkly (2015) 145, w14094-w14094. PubMed Europe PubMed DOI
Geschwindner,S., Andersson,G.M., Beisel,H.G., Breuer,S., Hallberg,C., Kihlberg,B.M., Lindqvist,A.M., O'Mahony,G., Plowright,A.T., Raubacher,F. and Knecht,W. Characterisation of de novo mutations in the C-terminal domain of proprotein convertase subtilisin/kexin type 9 Protein Eng Des Sel (2015) 28, 117-125. PubMed Europe PubMed DOI M
Giugliano,R.P. and Sabatine,M.S. Are PCSK9 inhibitors the next breakthrough in the cardiovascular field? J Am Coll Cardiol (2015) 65, 2638-2651. PubMed Europe PubMed DOI
Giunzioni,I. and Tavori,H. New developments in atherosclerosis: clinical potential of PCSK9 inhibition Vasc Health Risk Manag (2015) 11, 493-501. PubMed Europe PubMed DOI PMC EPMC
Gouni-Berthold,I. PCSK9 antibodies: a new class of lipid-lowering drugs Atheroscler Suppl (2015) 18, 21-27. PubMed Europe PubMed DOI
Hopkins,P.N., Defesche,J., Fouchier,S.W., Bruckert,E., Luc,G., Cariou,B., Sjouke,B., Leren,T.P., Harada-Shiba,M., Mabuchi,H., Rabes,J.P., Carrie,A., van Heyningen,C., Carreau,V., Farnier,M., Teoh,Y.P., Bourbon,M., Kawashiri,M.A., Nohara,A., Soran,H., Marais,A.D., Tada,H., Abifadel,M., Boileau,C., Chanu,B., Katsuda,S., Kishimoto,I., Lambert,G., Makino,H., Miyamoto,Y., Pichelin,M., Yagi,K., Yamagishi,M., Zair,Y., Mellis,S., Yancopoulos,G.D., Stahl,N., Mendoza,J., Du,Y., Hamon,S., Krempf,M. and Swergold,G.D. Characterization of autosomal dominant hypercholesterolemia caused by PCSK9 gain of function mutations and its specific treatment with alirocumab, a PCSK9 monoclonal antibody Circ Cardiovasc Genet (2015) 8, 823-831. PubMed Europe PubMed DOI
Jialal,I. and Patel,S.B. PCSK9 inhibitors: the next frontier in low-density lipoprotein lowering Metab Syndr Relat Disord (2015) 13, 99-101. PubMed Europe PubMed DOI V
Joseph,L. and Robinson,J.G. Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibition and the future of lipid lowering therapy Prog Cardiovasc Dis (2015) 58, 19-31. PubMed Europe PubMed DOI
Kereiakes,D.J., Robinson,J.G., Cannon,C.P., Lorenzato,C., Pordy,R., Chaudhari,U. and Colhoun,H.M. Efficacy and safety of the proprotein convertase subtilisin/kexin type 9 inhibitor alirocumab among high cardiovascular risk patients on maximally tolerated statin therapy: The ODYSSEY COMBO I study Am Heart J (2015) 169, 906-915. PubMed Europe PubMed DOI
Koren,M.J., Roth,E.M., McKenney,J.M., Gipe,D., Hanotin,C., Ferrand,A.C., Wu,R. and Dufour,R. Safety and efficacy of alirocumab 150 mg every 2 weeks, a fully human proprotein convertase subtilisin/kexin type 9 monoclonal antibody: a Phase II pooled analysis Postgrad Med (2015) 127, 125-132. PubMed Europe PubMed DOI
Langslet,G., Emery,M. and Wasserman,S.M. Evolocumab (AMG 145) for primary hypercholesterolemia Expert Rev Cardiovasc Ther (2015) 13, 477-488. PubMed Europe PubMed DOI
Lepor,N.E. and Kereiakes,D.J. The PCSK9 inhibitors: a novel therapeutic target enters clinical practice Am Health Drug Benefits (2015) 8, 483-489. PubMed Europe PubMed PMC EPMC
Lettino,M. [PCSK9 monoclonal antibody inhibition: current evidence and future perspectives of lipid-lowering therapy according to the available results from the ODYSSEY program] G Ital Cardiol (Rome) (2015) 16, 211-216. PubMed Europe PubMed DOI
Li,C., Lin,L., Zhang,W., Zhou,L., Wang,H., Luo,X., Luo,H., Cai,Y. and Zeng,C. Efficiency and safety of proprotein convertase subtilisin/kexin 9 monoclonal antibody on hypercholesterolemia: a meta-analysis of 20 randomized controlled trials J Am Heart Assoc (2015) 4, e001937-e001937. PubMed Europe PubMed DOI
Mabuchi,H. and Nohara,A. Therapy: PCSK9 inhibitors for treating familial hypercholesterolaemia Nat Rev Endocrinol (2015) 11, 8-9. PubMed Europe PubMed DOI T
Markham,A. Evolocumab: first global approval Drugs (2015) 75, 1567-1573. PubMed Europe PubMed DOI
McKenney,J.M. Understanding PCSK9 and anti-PCSK9 therapies J Clin Lipidol (2015) 9, 170-186. PubMed Europe PubMed DOI
Milionis,H., Liamis,G. and Elisaf,M. Proprotein convertase subtilisin kexin 9 inhibitors: next generation in lipid-lowering therapy Expert Opin Biol Ther (2015) 15, 287-298. PubMed Europe PubMed DOI
Navarese,E.P., Kolodziejczak,M., Schulze,V., Gurbel,P.A., Tantry,U., Lin,Y., Brockmeyer,M., Kandzari,D.E., Kubica,J.M., D'Agostino,R.B., Sr., Kubica,J., Volpe,M., Agewall,S., Kereiakes,D.J. and Kelm,M. Effects of proprotein convertase subtilisin/kexin type 9 antibodies in adults with hypercholesterolemia: a systematic review and meta-analysis Ann Intern Med (2015) 163, 40-51. PubMed Europe PubMed DOI
Pecin,I. and Reiner,Z. Alirocumab: targeting PCSK9 to treat hypercholesterolemia Drugs Today (Barc) (2015) 51, 681-687. PubMed Europe PubMed DOI
Pokharel,Y., Virani,S.S. and Ballantyne,C.M. The promise of proprotein convertase subtilisin/kexin 9 inhibitors for the treatment of familial hypercholesterolemia Curr Atheroscler Rep (2015) 17, 508-508. PubMed Europe PubMed DOI I
Reiner,Z. PCSK9 inhibitors - past, present and future Expert Opin Drug Metab Toxicol (2015) 11, 1517-1521. PubMed Europe PubMed DOI
Rocha,C.S., Wiklander,O.P., Larsson,L., Moreno,P.M., Parini,P., Lundin,K.E. and Smith,C.I. RNA therapeutics inactivate PCSK9 by inducing a unique intracellular retention form J Mol Cell Cardiol (2015) 82, 186-193. PubMed Europe PubMed DOI
Sabatine,M.S., Giugliano,R.P., Wiviott,S.D., Raal,F.J., Blom,D.J., Robinson,J., Ballantyne,C.M., Somaratne,R., Legg,J., Wasserman,S.M., Scott,R., Koren,M.J. and Stein,E.A. Efficacy and safety of evolocumab in reducing lipids and cardiovascular events N Engl J Med (2015) 372, 1500-1509. PubMed Europe PubMed DOI
Schulz,R., Schluter,K.D. and Laufs,U. Molecular and cellular function of the proprotein convertase subtilisin/kexin type 9 (PCSK9) Basic Res Cardiol (2015) 110, 4-4. PubMed Europe PubMed DOI PMC EPMC V
Stawowy,P. Proprotein convertases in atherogenesis Curr Opin Lipidol (2015) 26, 338-344. PubMed Europe PubMed DOI V
Tavori,H., Giunzioni,I. and Fazio,S. PCSK9 inhibition to reduce cardiovascular disease risk: recent findings from the biology of PCSK9 Curr Opin Endocrinol Diabetes Obes (2015) 22, 126-132. PubMed Europe PubMed DOI V
van Poelgeest,E.P., Hodges,M.R., Moerland,M., Tessier,Y., Levin,A.A., Persson,R., Lindholm,M.W., Dumong Erichsen,K., Orum,H., Cohen,A.F. and Burggraaf,J. Antisense-mediated reduction of proprotein convertase subtilisin/kexin type 9 (PCSK9): a first-in-human randomized, placebo-controlled trial Br J Clin Pharmacol (2015) 80, 1350-1361. PubMed Europe PubMed DOI K
Wu,N.Q., Li,S. and Li,J.J. Update of clinical trials of anti-PCSK9 antibodies Cardiovasc Drugs Ther (2015) 29, 159-169. PubMed Europe PubMed DOI
Xu,H.-M. and Cai,H.-W. Clinical research progress of anti-proprotein convertase subtilisin/kexin type 9 (PCSK9) monoclonal antibodies Chin Pharm J (China) (2015) 50, 1375-1379. DOI
Zhang,X.L., Zhu,Q.Q., Zhu,L., Chen,J.Z., Chen,Q.H., Li,G.N., Xie,J., Kang,L.N. and Xu,B. Safety and efficacy of anti-PCSK9 antibodies: a meta-analysis of 25 randomized, controlled trials BMC Med (2015) 13, 123-123. PubMed Europe PubMed DOI PMC EPMC V

2014

Abifadel,M., Elbitar,S., El Khoury,P., Ghaleb,Y., Chemaly,M., Moussalli,M.L., Rabes,J.P., Varret,M. and Boileau,C. Living the PCSK9 adventure: from the identification of a new gene in familial hypercholesterolemia towards a potential new class of anticholesterol drugs Curr Atheroscler Rep (2014) 16, 439-439. PubMed Europe PubMed DOI V
Blom,D.J., Hala,T., Bolognese,M., Lillestol,M.J., Toth,P.D., Burgess,L., Ceska,R., Roth,E., Koren,M.J., Ballantyne,C.M., Monsalvo,M.L., Tsirtsonis,K., Kim,J.B., Scott,R., Wasserman,S.M. and Stein,E.A. A 52-week placebo-controlled trial of evolocumab in hyperlipidemia N Engl J Med (2014) 370, 1809-1819. PubMed Europe PubMed DOI
Bray,N. Sepsis: PCSK9 blockade helps clear pathogenic lipids Nat Rev Drug Discov (2014) 13, 886-886. PubMed Europe PubMed DOI T
Cariou,B., Benoit,I. and Le May,C. Preserved adrenal function in fully PCSK9-deficient subject Int J Cardiol (2014) 176, 499-500. PubMed Europe PubMed DOI M
Chorba,J.S. and Shokat,K.M. The proprotein convertase subtilisin/kexin type 9 (PCSK9) active site and cleavage sequence differentially regulate protein secretion from proteolysis J Biol Chem (2014) 289, 29030-29043. PubMed Europe PubMed DOI M I
Cicero,A.F., Tartagni,E. and Ertek,S. Efficacy and safety profile of evolocumab (AMG145), an injectable inhibitor of the proprotein convertase subtilisin/kexin type 9: the available clinical evidence Expert Opin Biol Ther (2014) 14, 863-868. PubMed Europe PubMed DOI
Colbert,A., Umble-Romero,A., Prokop,S., Xu,R., Gibbs,J. and Pederson,S. Characterization of a quantitative method to measure free proprotein convertase subtilisin/kexin type 9 in human serum MAbs (2014) 6, 1103-1113. PubMed Europe PubMed DOI A
Colhoun,H.M., Robinson,J.G., Farnier,M., Cariou,B., Blom,D., Kereiakes,D.J., Lorenzato,C., Pordy,R. and Chaudhari,U. Efficacy and safety of alirocumab, a fully human PCSK9 monoclonal antibody, in high cardiovascular risk patients with poorly controlled hypercholesterolemia on maximally tolerated doses of statins: rationale and design of the ODYSSEY COMBO I and II trials BMC Cardiovasc Disord (2014) 14, 121-121. PubMed Europe PubMed DOI
Galabova,G., Brunner,S., Winsauer,G., Juno,C., Wanko,B., Mairhofer,A., Luhrs,P., Schneeberger,A., von Bonin,A., Mattner,F., Schmidt,W. and Staffler,G. Peptide-based anti-PCSK9 vaccines - an approach for long-term LDLc management PLoS ONE (2014) 9, e114469-e114469. PubMed Europe PubMed DOI
Gouni-Berthold,I. and Berthold,H.K. PCSK9 antibodies for the treatment of hypercholesterolemia Nutrients (2014) 6, 5517-5533. PubMed Europe PubMed DOI
Han,B., Eacho,P.I., Knierman,M.D., Troutt,J.S., Konrad,R.J., Yu,X. and Schroeder,K.M. Isolation and characterization of the circulating truncated form of PCSK9 J Lipid Res (2014) 55, 1505-1514. PubMed Europe PubMed DOI
Hirayama,A., Honarpour,N., Yoshida,M., Yamashita,S., Huang,F., Wasserman,S.M. and Teramoto,T. Effects of evolocumab (AMG 145), a monoclonal antibody to PCSK9, in hypercholesterolemic, statin-treated Japanese patients at high cardiovascular risk - primary results from the phase 2 YUKAWA study Circ J (2014) 78, 1073-1082. PubMed Europe PubMed DOI
Kastelein,J.J., Robinson,J.G., Farnier,M., Krempf,M., Langslet,G., Lorenzato,C., Gipe,D.A. and Baccara-Dinet,M.T. Efficacy and safety of alirocumab in patients with heterozygous familial hypercholesterolemia not adequately controlled with current lipid-lowering therapy: design and rationale of the ODYSSEY FH studies Cardiovasc Drugs Ther (2014) 28, 281-289. PubMed Europe PubMed DOI
Koren,M.J., Lundqvist,P., Bolognese,M., Neutel,J.M., Monsalvo,M.L., Yang,J., Kim,J.B., Scott,R., Wasserman,S.M. and Bays,H. Anti-PCSK9 monotherapy for hypercholesterolemia: the MENDEL-2 randomized, controlled phase III clinical trial of evolocumab J Am Coll Cardiol (2014) 63, 2531-2540. PubMed Europe PubMed DOI
Lepor,N.E., Contreras,L., Desai,C. and Kereiakes,D.J. The potential role of anti-PCSK9 monoclonal antibodies in the management of hypercholesterolemia Rev Cardiovasc Med (2014) 15, 290-307. PubMed Europe PubMed DOI
Ling,H., Burns,T.L. and Hilleman,D.E. An update on the clinical development of proprotein convertase subtilisin kexin 9 inhibitors, novel therapeutic agents for lowering low-density lipoprotein cholesterol Cardiovasc Ther (2014) 32, 82-88. PubMed Europe PubMed DOI
Moriarty,P.M., Jacobson,T.A., Bruckert,E., Thompson,P.D., Guyton,J.R., Baccara-Dinet,M.T. and Gipe,D. Efficacy and safety of alirocumab, a monoclonal antibody to PCSK9, in statin-intolerant patients: design and rationale of ODYSSEY ALTERNATIVE, a randomized phase 3 trial J Clin Lipidol (2014) 8, 554-561. PubMed Europe PubMed DOI
Norata,G.D. [PCSK9 inhibitors and dyslipidemias: an update on clinical evidence] G Ital Cardiol (Rome) (2014) 15, 301-305. PubMed Europe PubMed DOI
Roth,E.M., Taskinen,M.R., Ginsberg,H.N., Kastelein,J.J., Colhoun,H.M., Robinson,J.G., Merlet,L., Pordy,R. and Baccara-Dinet,M.T. Monotherapy with the PCSK9 inhibitor alirocumab versus ezetimibe in patients with hypercholesterolemia: Results of a 24week, double-blind, randomized Phase 3 trial Int J Cardiol (2014) 176, 55-61. PubMed Europe PubMed DOI
Schwartz,G.G., Bessac,L., Berdan,L.G., Bhatt,D.L., Bittner,V., Diaz,R., Goodman,S.G., Hanotin,C., Harrington,R.A., Jukema,J.W., Mahaffey,K.W., Moryusef,A., Pordy,R., Roe,M.T., Rorick,T., Sasiela,W.J., Shirodaria,C., Szarek,M., Tamby,J.F., Tricoci,P., White,H., Zeiher,A. and Steg,P.G. Effect of alirocumab, a monoclonal antibody to PCSK9, on long-term cardiovascular outcomes following acute coronary syndromes: Rationale and design of the ODYSSEY Outcomes trial Am Heart J (2014) 168, 682-689. PubMed Europe PubMed DOI
Stawowy,P., Just,I.A. and Kaschina,E. Inhibition of PCSK9: a novel approach for the treatment of dyslipidemia Coron Artery Dis (2014) 25, 353-359. PubMed Europe PubMed DOI
Stein,E.A., Giugliano,R.P., Koren,M.J., Raal,F.J., Roth,E.M., Weiss,R., Sullivan,D., Wasserman,S.M., Somaratne,R., Kim,J.B., Yang,J., Liu,T., Albizem,M., Scott,R. and Sabatine,M.S. Efficacy and safety of evolocumab (AMG 145), a fully human monoclonal antibody to PCSK9, in hyperlipidaemic patients on various background lipid therapies: pooled analysis of 1359 patients in four phase 2 trials Eur Heart J (2014) 35, 2249-2259. PubMed Europe PubMed DOI
Tavori,H., Melone,M. and Rashid,S. Alirocumab: PCSK9 inhibitor for LDL cholesterol reduction Expert Rev Cardiovasc Ther (2014) 12, 1137-1144. PubMed Europe PubMed DOI
Weinreich,M. and Frishman,W.H. Antihyperlipidemic therapies targeting PCSK9 Cardiol Rev (2014) 22, 140-146. PubMed Europe PubMed DOI
Wu,N.Q. and Li,J.J. PCSK9 gene mutations and low-density lipoprotein cholesterol Clin Chim Acta (2014) 431, 148-153. PubMed Europe PubMed DOI M
Wu,Q., Tang,Z.H., Peng,J., Liao,L., Pan,L.H., Wu,C.Y., Jiang,Z.S., Wang,G.X. and Liu,L.S. The dual behavior of PCSK9 in the regulation of apoptosis is crucial in Alzheimer's disease progression (Review) Biomed Rep (2014) 2, 167-171. PubMed Europe PubMed DOI PMC EPMC V
Zhang,Y., Eigenbrot,C., Zhou,L., Shia,S., Li,W., Quan,C., Tom,J., Moran,P., Di Lello,P., Skelton,N.J., Kong-Beltran,M., Peterson,A. and Kirchhofer,D. Identification of a small peptide that inhibits PCSK9 protein binding to the low density lipoprotein receptor J Biol Chem (2014) 289, 942-955. PubMed Europe PubMed DOI PMC EPMC S I

2013

Al-Mashhadi,R.H., Sorensen,C.B., Kragh,P.M., Christoffersen,C., Mortensen,M.B., Tolbod,L.P., Thim,T., Du,Y., Li,J., Liu,Y., Moldt,B., Schmidt,M., Vajta,G., Larsen,T., Purup,S., Bolund,L., Nielsen,L.B., Callesen,H., Falk,E., Mikkelsen,J.G. and Bentzon,J.F. Familial hypercholesterolemia and atherosclerosis in cloned minipigs created by DNA transposition of a human PCSK9 gain-of-function mutant Sci Transl Med (2013) 5, 166ra1-166ra1. PubMed Europe PubMed DOI M
Banach,M., Rizzo,M., Obradovic,M., Montalto,G., Rysz,J., Mikhailidis,D.P. and Isenovic,E.R. PCSK9 inhibition - a novel mechanism to treat lipid disorders? Curr Pharm Des (2013) 19, 3869-3877. PubMed Europe PubMed T
Canuel,M., Sun,X., Asselin,M.C., Paramithiotis,E., Prat,A. and Seidah,N.G. Proprotein convertase subtilisin/kexin type 9 (PCSK9) can mediate degradation of the low density lipoprotein receptor-related protein 1 (LRP-1) PLoS ONE (2013) 8, e64145-e64145. PubMed Europe PubMed DOI PMC EPMC
Davidson,M.H. Dyslipidaemia: PCSK9 antibodies: a dividend of the genomics revolution Nat Rev Cardiol (2013) 10, 618-619. PubMed Europe PubMed DOI
Do,R.Q., Vogel,R.A. and Schwartz,G.G. PCSK9 inhibitors: potential in cardiovascular therapeutics Curr Cardiol Rep (2013) 15, 345-345. PubMed Europe PubMed DOI T I
Farnier,M. PCSK9 inhibitors Curr Opin Lipidol (2013) 24, 251-258. PubMed Europe PubMed DOI I
Hooper,A.J. and Burnett,J.R. Anti-PCSK9 therapies for the treatment of hypercholesterolemia Expert Opin Biol Ther (2013) 13, 429-435. PubMed Europe PubMed DOI I
Kosenko,T., Golder,M., Leblond,G., Weng,W. and Lagace,T.A. Low density lipoprotein binds to proprotein convertase subtilisin/kexin type-9 (PCSK9) in human plasma and inhibits PCSK9-mediated low density lipoprotein receptor degradation J Biol Chem (2013) 288, 8279-8288. PubMed Europe PubMed DOI
Lee,P. and Hegele,R.A. Current phase II proprotein convertase subtilisin/kexin 9 inhibitor therapies for dyslipidemia Expert Opin Investig Drugs (2013) 22, 1411-1423. PubMed Europe PubMed DOI I
Li,C.Y., Bai,Y. and Qin,Y.W. Research advances in proprotein convertase subtilisin/kexin type 9 inhibitors Pharm Care Res (2013) 13, 241-244. DOI I
Luna Saavedra,Y.G., Zhang,J. and Seidah,N.G. PCSK9 prosegment chimera as novel inhibitors of LDLR degradation PLoS ONE (2013) 8, e72113-e72113. PubMed Europe PubMed DOI PMC EPMC
Poirier,S. and Mayer,G. The biology of PCSK9 from the endoplasmic reticulum to lysosomes: new and emerging therapeutics to control low-density lipoprotein cholesterol Drug Des Devel Ther (2013) 7, 1135-1148. PubMed Europe PubMed DOI PMC EPMC V
Postmus,I., Trompet,S., de Craen,A.J., Buckley,B.M., Ford,I., Stott,D.J., Sattar,N., Slagboom,P.E., Westendorp,R.G. and Jukema,J.W. PCSK9 SNP rs11591147 is associated with low cholesterol levels but not with cognitive performance or noncardiovascular clinical events in an elderly population J Lipid Res (2013) 54, 561-566. PubMed Europe PubMed DOI M
Seidah,N.G. Proprotein convertase subtilisin kexin 9 (PCSK9) inhibitors in the treatment of hypercholesterolemia and other pathologies Curr Pharm Des (2013) 19, 3161-3172. PubMed Europe PubMed DOI T
Seidah,N.G., Sadr,M.S., Chretien,M. and Mbikay,M. The multifaceted proprotein convertases: their unique, redundant, complementary, and opposite functions J Biol Chem (2013) 288, 21473-21481. PubMed Europe PubMed DOI V
Shen,L., Peng,H.C., Nees,S.N., Zhao,S.P. and Xu,D.Y. Proprotein convertase subtilisin/kexin type 9 potentially influences cholesterol uptake in macrophages and reverse cholesterol transport FEBS Lett (2013) 587, 1271-1274. PubMed Europe PubMed DOI
Shen,L., Peng,H., Xu,D. and Zhao,S. The next generation of novel low-density lipoprotein cholesterol-lowering agents: proprotein convertase subtilisin/kexin 9 inhibitors Pharmacol Res (2013) 73, 27-34. PubMed Europe PubMed DOI I
Sheridan,C. Phase 3 data for PCSK9 inhibitor wows Nat Biotechnol (2013) 31, 1057-1058. PubMed Europe PubMed DOI
Stein,E.A. and Swergold,G.D. Potential of proprotein convertase subtilisin/kexin type 9 based therapeutics Curr Atheroscler Rep (2013) 15, 310-310. PubMed Europe PubMed DOI
Tveten,K., Strom,T.B., Berge,K.E. and Leren,T.P. PCSK9-mediated degradation of the LDL receptor generates a 17 kDa C-terminal LDL receptor fragment J Lipid Res (2013) 54, 1560-1566. PubMed Europe PubMed DOI
Willrich,M.A. and Baudhuin,L.M. PCSK9 and the road less traveled: how an unconventional approach led to a major discovery Clin Chem (2013) 59, 1283-1284. PubMed Europe PubMed V

2012

Banaszewska,A., Piechota,M. and Plewa,R. Proprotein convertase subtilisin/kexin type 9: a new target molecule for gene therapy Cell Mol Biol Lett (2012) 17, 228-239. PubMed Europe PubMed DOI
Basak,A., Palmer-Smith,H. and Mishra,P. Proprotein convertase subtilisin kexin9 (pcsk9): A novel target for cholesterol regulation Protein Pept Lett (2012) 19, 575-585. PubMed Europe PubMed T
Benjannet,S., Hamelin,J., Chretien,M. and Seidah,N.G. Loss- and gain-of-function PCSK9 variants: cleavage specificity, dominant negative effects, and low density lipoprotein receptor (LDLR) degradation J Biol Chem (2012) 287, 33745-33755. PubMed Europe PubMed DOI M P
Chretien,M. My road to Damascus: how I converted to the prohormone theory and the proprotein convertases Biochem Cell Biol (2012) 90, 750-768. PubMed Europe PubMed DOI M
Denis,M., Marcinkiewicz,J., Zaid,A., Gauthier,D., Poirier,S., Lazure,C., Seidah,N.G. and Prat,A. Gene inactivation of proprotein convertase subtilisin/kexin type 9 reduces atherosclerosis in mice Circulation (2012) 125, 894-901. PubMed Europe PubMed DOI K
Dias,C.S., Shaywitz,A.J., Wasserman,S.M., Smith,B.P., Gao,B., Stolman,D.S., Crispino,C.P., Smirnakis,K.V., Emery,M.G., Colbert,A., Gibbs,J.P., Retter,M.W., Cooke,B.P., Uy,S.T., Matson,M. and Stein,E.A. Effects of AMG 145 on low-density lipoprotein cholesterol levels: results from 2 randomized, double-blind, placebo-controlled, ascending-dose phase 1 studies in healthy volunteers and hypercholesterolemic subjects on statins J Am Coll Cardiol (2012) 60, 1888-1898. PubMed Europe PubMed DOI
Koren,M.J., Scott,R., Kim,J.B., Knusel,B., Liu,T., Lei,L., Bolognese,M. and Wasserman,S.M. Efficacy, safety, and tolerability of a monoclonal antibody to proprotein convertase subtilisin/kexin type 9 as monotherapy in patients with hypercholesterolaemia (MENDEL): a randomised, double-blind, placebo-controlled, phase 2 study Lancet (2012) 380, 1995-2006. PubMed Europe PubMed DOI
Lambert,G., Sjouke,B., Choque,B., Kastelein,J.J. and Hovingh,G.K. The PCSK9 decade J Lipid Res (2012) 53, 2515-2524. PubMed Europe PubMed DOI V
Lipari,M.T., Li,W., Moran,P., Kong-Beltran,M., Sai,T., Lai,J., Lin,S.J., Kolumam,G., Zavala-Solorio,J., Izrael-Tomasevic,A., Arnott,D., Wang,J., Peterson,A.S. and Kirchhofer,D. Furin-cleaved proprotein convertase subtilisin/kexin type 9 (PCSK9) is active and modulates low density lipoprotein receptor and serum cholesterol levels J Biol Chem (2012) 287, 43482-43491. PubMed Europe PubMed DOI
Marais,D.A., Blom,D.J., Petrides,F., Goueffic,Y. and Lambert,G. Proprotein convertase subtilisin/kexin type 9 inhibition Curr Opin Lipidol (2012) 23, 511-517. PubMed Europe PubMed DOI
Seidah,N.G. and Prat,A. The biology and therapeutic targeting of the proprotein convertases Nat Rev Drug Discov (2012) 11, 367-383. PubMed Europe PubMed DOI V
Seidah,N.G. Proprotein convertase PCSK9 [ISSN:978-0-12-407742-3] (2012) 3, 3315-3322. DOI
Seidah,N.G., Poirier,S., Denis,M., Parker,R., Miao,B., Mapelli,C., Prat,A., Wassef,H., Davignon,J., Hajjar,K.A. and Mayer,G. Annexin A2 Is a Natural Extrahepatic Inhibitor of the PCSK9-Induced LDL Receptor Degradation PLoS ONE (2012) 7, e41865-e41865. PubMed Europe PubMed DOI PMC EPMC
Sun,X., Essalmani,R., Day,R., Khatib,A.M., Seidah,N.G. and Prat,A. Proprotein convertase subtilisin/kexin type 9 deficiency reduces melanoma metastasis in liver Neoplasia (2012) 14, 1122-1131. PubMed Europe PubMed DOI K
Vogel,R.A. PCSK9 inhibition: the next statin? J Am Coll Cardiol (2012) 59, 2354-2355. PubMed Europe PubMed DOI T I

2011

Basak,A., Chen,A., Majumdar,S. and Smith,H.P. In vitro assay for protease activity of proprotein convertase subtilisin kexins (PCSKs): an overall review of existing and new methodologies Methods Mol Biol (2011) 768, 127-153. PubMed Europe PubMed DOI A
Brouwers,M.C., van Greevenbroek,M.M., Troutt,J.S., Bonner Freeman,A., Lu,A., Schaper,N.C., Konrad,R.J. and Stehouwer,C.D. Plasma proprotein convertase subtilisin kexin type 9 is a heritable trait of familial combined hyperlipidaemia Clin Sci (Lond) (2011) 121, 397-403. PubMed Europe PubMed DOI
Cariou,B., Le May,C. and Costet,P. Clinical aspects of PCSK9 Atherosclerosis (2011) 216, 258-265. PubMed Europe PubMed DOI M V
Dewpura,T. and Mayne,J. Analyses of PCSK9 post-translational modifications using time-of-flight mass spectrometry Methods Mol Biol (2011) 768, 167-187. PubMed Europe PubMed DOI
Du,F., Hui,Y., Zhang,M., Linton,M.F., Fazio,S. and Fan,D. Novel domain interaction regulates secretion of proprotein convertase subtilisin/kexin type 9 (PCSK9) protein J Biol Chem (2011) 286, 43054-43061. PubMed Europe PubMed DOI
Duff,C.J. and Hooper,N.M. PCSK9: an emerging target for treatment of hypercholesterolemia Expert Opin Ther Targets (2011) 15, 157-168. PubMed Europe PubMed DOI T I
Essalmani,R., Susan-Resiga,D., Chamberland,A., Abifadel,M., Creemers,J.W., Boileau,C., Seidah,N.G. and Prat,A. In vivo evidence that furin from hepatocytes inactivates PCSK9 J Biol Chem (2011) 286, 4257-4263. PubMed Europe PubMed DOI
Farnier,M. The role of proprotein convertase subtilisin/kexin type 9 in hyperlipidemia: focus on therapeutic implications Am J Cardiovasc Drugs (2011) 11, 145-152. PubMed Europe PubMed DOI T
Holla,O.L., Laerdahl,J.K., Strom,T.B., Tveten,K., Cameron,J., Berge,K.E. and Leren,T.P. Removal of acidic residues of the prodomain of PCSK9 increases its activity towards the LDL receptor Biochem Biophys Res Commun (2011) 406, 234-238. PubMed Europe PubMed DOI
Holla,O.L., Cameron,J., Tveten,K., Strom,T.B., Berge,K.E., Laerdahl,J.K. and Leren,T.P. Role of the C-terminal domain of PCSK9 in degradation of the LDL receptors J Lipid Res (2011) 52, 1787-1794. PubMed Europe PubMed DOI
Mayne,J., Dewpura,T., Raymond,A., Bernier,L., Cousins,M., Ooi,T.C., Davignon,J., Seidah,N.G., Mbikay,M. and Chretien,M. Novel loss-of-function PCSK9 variant is associated with low plasma LDL cholesterol in a French-Canadian family and with impaired processing and secretion in cell culture Clin Chem (2011) 57, 1415-1423. PubMed Europe PubMed DOI M
Seidah,N.G. What lies ahead for the proprotein convertases? Ann N Y Acad Sci (2011) 1220, 149-161. PubMed Europe PubMed DOI V
Seidah,N.G. The proprotein convertases, 20 years later Methods Mol Biol (2011) 768, 23-57. PubMed Europe PubMed DOI V
Soutar,A.K. Unexpected roles for PCSK9 in lipid metabolism Curr Opin Lipidol (2011) 22, 192-196. PubMed Europe PubMed DOI
Surdo,P.L., Bottomley,M.J., Calzetta,A., Settembre,E.C., Cirillo,A., Pandit,S., Ni,Y.G., Hubbard,B., Sitlani,A. and Carfi,A. Mechanistic implications for LDL receptor degradation from the PCSK9/LDLR structure at neutral pH EMBO Rep (2011) 12, 1300-1305. PubMed Europe PubMed DOI S
Tibolla,G., Norata,G.D., Artali,R., Meneghetti,F. and Catapano,A.L. Proprotein convertase subtilisin/kexin type 9 (PCSK9): from structure-function relation to therapeutic inhibition Nutr Metab Cardiovasc Dis (2011) 21, 835-843. PubMed Europe PubMed DOI V I

2010

Abifadel,M., Pakradouni,J., Collin,M., Samson-Bouma,M.E., Varret,M., Rabes,J.P. and Boileau,C. Strategies for proprotein convertase subtilisin kexin 9 modulation: a perspective on recent patents Expert Opin Ther Pat (2010) 20, 1547-1571. PubMed Europe PubMed DOI
Akram,O.N., Bernier,A., Petrides,F., Wong,G. and Lambert,G. Beyond LDL cholesterol, a new role for PCSK9 Arterioscler Thromb Vasc Biol (2010) 30, 1279-1281. PubMed Europe PubMed DOI
Benjannet,S., Luna Saavedra,Y.G., Hamelin,J., Asselin,M.C., Essalmani,R., Pasquato,A., Lemaire,P., Duke,G., Miao,B., Duclos,F., Parker,R., Mayer,G. and Seidah,N.G. Effects of the prosegment and pH on the activity of PCSK9: evidence for additional processing events J Biol Chem (2010) 285, 40965-40978. PubMed Europe PubMed DOI
Benn,M., Nordestgaard,B.G., Grande,P., Schnohr,P. and Tybjaerg-Hansen,A. PCSK9 R46L, low-density lipoprotein cholesterol levels, and risk of ischemic heart disease: 3 independent studies and meta-analyses J Am Coll Cardiol (2010) 55, 2833-2842. PubMed Europe PubMed DOI M
Dubuc,G., Tremblay,M., Pare,G., Jacques,H., Hamelin,J., Benjannet,S., Boulet,L., Genest,J., Bernier,L., Seidah,N.G. and Davignon,J. A new method for measurement of total plasma PCSK9: clinical applications J Lipid Res (2010) 51, 140-149. PubMed Europe PubMed DOI
Gupta,N., Fisker,N., Asselin,M.C., Lindholm,M., Rosenbohm,C., Orum,H., Elmen,J., Seidah,N.G. and Straarup,E.M. A locked nucleic acid antisense oligonucleotide (LNA) silences PCSK9 and enhances LDLR expression in vitro and in vivo PLoS ONE (2010) 5, e10682-e10682. PubMed Europe PubMed DOI PMC EPMC K
Lin,J., Wang,L.Y., Liu,S., Wang,X.M., Yong,Q., Yang,Y., Du,L.P., Pan,X.D., Wang,X. and Jiang,Z.S. A novel mutation in proprotein convertase subtilisin/kexin type 9 gene leads to familial hypercholesterolemia in a Chinese family Chin Med J (Engl) (2010) 123, 1133-1138. PubMed Europe PubMed DOI M
Liu,M., Wu,G., Baysarowich,J., Kavana,M., Addona,G.H., Bierilo,K.K., Mudgett,J.S., Pavlovic,G., Sitlani,A., Renger,J.J., Hubbard,B.K., Fisher,T.S. and Zerbinatti,C.V. PCSK9 is not involved in the degradation of LDL receptors and BACE1 in the adult mouse brain J Lipid Res (2010) 51, 2611-2618. PubMed Europe PubMed DOI
Mbikay,M., Sirois,F., Mayne,J., Wang,G.S., Chen,A., Dewpura,T., Prat,A., Seidah,N.G., Chretien,M. and Scott,F.W. PCSK9-deficient mice exhibit impaired glucose tolerance and pancreatic islet abnormalities FEBS Lett (2010) 584, 701-706. PubMed Europe PubMed DOI K
Noguchi,T., Katsuda,S., Kawashiri,M.A., Tada,H., Nohara,A., Inazu,A., Yamagishi,M., Kobayashi,J. and Mabuchi,H. The E32K variant of PCSK9 exacerbates the phenotype of familial hypercholesterolaemia by increasing PCSK9 function and concentration in the circulation Atherosclerosis (2010) 210, 166-172. PubMed Europe PubMed DOI M
Norata,G.D., Garlaschelli,K., Grigore,L., Raselli,S., Tramontana,S., Meneghetti,F., Artali,R., Noto,D., Cefalu,A.B., Buccianti,G., Averna,M. and Catapano,A.L. Effects of PCSK9 variants on common carotid artery intima media thickness and relation to ApoE alleles Atherosclerosis (2010) 208, 177-182. PubMed Europe PubMed DOI M
Pearlstein,R.A., Hu,Q.Y., Zhou,J., Yowe,D., Levell,J., Dale,B., Kaushik,V.K., Daniels,D., Hanrahan,S., Sherman,W. and Abel,R. New hypotheses about the structure-function of proprotein convertase subtilisin/kexin type 9: analysis of the epidermal growth factor-like repeat A docking site using WaterMap Proteins (2010) 78, 2571-2586. PubMed Europe PubMed DOI
Strom,T.B., Holla,O.L., Cameron,J., Berge,K.E. and Leren,T.P. Loss-of-function mutation R46L in the PCSK9 gene has little impact on the levels of total serum cholesterol in familial hypercholesterolemia heterozygotes Clin Chim Acta (2010) 411, 229-233. PubMed Europe PubMed DOI M

2009

Abifadel,M., Rabes,J.P., Devillers,M., Munnich,A., Erlich,D., Junien,C., Varret,M. and Boileau,C. Mutations and polymorphisms in the proprotein convertase subtilisin kexin 9 (PCSK9) gene in cholesterol metabolism and disease Hum Mutat (2009) 30, 520-529. PubMed Europe PubMed DOI M
Cameron,J., Holla,O.L., Laerdahl,J.K., Kulseth,M.A., Berge,K.E. and Leren,T.P. Mutation S462P in the PCSK9 gene reduces secretion of mutant PCSK9 without affecting the autocatalytic cleavage Atherosclerosis (2009) 203, 161-165. PubMed Europe PubMed DOI
Cariou,B., Ouguerram,K., Zair,Y., Guerois,R., Langhi,C., Kourimate,S., Benoit,I., Le May,C., Gayet,C., Belabbas,K., Dufernez,F., Chetiveaux,M., Tarugi,P., Krempf,M., Benlian,P. and Costet,P. PCSK9 dominant negative mutant results in increased LDL catabolic rate and familial hypobetalipoproteinemia Arterioscler Thromb Vasc Biol (2009) 29, 2191-2197. PubMed Europe PubMed DOI M
Chan,J.C., Piper,D.E., Cao,Q., Liu,D., King,C., Wang,W., Tang,J., Liu,Q., Higbee,J., Xia,Z., Di,Y., Shetterly,S., Arimura,Z., Salomonis,H., Romanow,W.G., Thibault,S.T., Zhang,R., Cao,P., Yang,X.P., Yu,T., Lu,M., Retter,M.W., Kwon,G., Henne,K., Pan,O., Tsai,M.M., Fuchslocher,B., Yang,E., Zhou,L., Lee,K.J., Daris,M., Sheng,J., Wang,Y., Shen,W.D., Yeh,W.C., Emery,M., Walker,N.P., Shan,B., Schwarz,M. and Jackson,S.M. A proprotein convertase subtilisin/kexin type 9 neutralizing antibody reduces serum cholesterol in mice and nonhuman primates Proc Natl Acad Sci U S A (2009) 106, 9820-9825. PubMed Europe PubMed DOI PMC EPMC
Duff,C.J., Scott,M.J., Kirby,I.T., Hutchinson,S.E., Martin,S.L. and Hooper,N.M. Antibody-mediated disruption of the interaction between PCSK9 and the low-density lipoprotein receptor Biochem J (2009) 419, 577-584. PubMed Europe PubMed DOI PMC EPMC
Fasano,T., Sun,X.M., Patel,D.D. and Soutar,A.K. Degradation of LDLR protein mediated by 'gain of function' PCSK9 mutants in normal and ARH cells Atherosclerosis (2009) 203, 166-171. PubMed Europe PubMed DOI
Geoghegan,K.F., Hoth,L.R., Varghese,A.H., Lin,W., Boyd,J.G. and Griffor,M.C. Binding to the low-density lipoprotein receptor accelerates futile catalytic cycling in PCSK9 and raises the equilibrium level of intramolecular acylenzyme Biochemistry (2009) 48, 2941-2949. PubMed Europe PubMed DOI
Hedrick,J.A. Targeting PCSK9 for the treatment of hypercholesterolemia Curr Opin Investig Drugs (2009) 10, 938-946. PubMed Europe PubMed V
Horton,J.D., Cohen,J.C. and Hobbs,H.H. PCSK9: a convertase that coordinates LDL catabolism J Lipid Res (2009) 50 Suppl, S172-S177. PubMed Europe PubMed DOI PMC EPMC T
Humphries,S.E., Neely,R.D., Whittall,R.A., Troutt,J.S., Konrad,R.J., Scartezini,M., Li,K.W., Cooper,J.A., Acharya,J. and Neil,A. Healthy individuals carrying the PCSK9 p.R46L variant and familial hypercholesterolemia patients carrying PCSK9 p.D374Y exhibit lower plasma concentrations of PCSK9 Clin Chem (2009) 55, 2153-2161. PubMed Europe PubMed DOI M
Kourimate,S., Chetiveaux,M., Jarnoux,A.L., Lalanne,F. and Costet,P. Cellular and secreted pro-protein convertase subtilisin/kexin type 9 catalytic activity in hepatocytes Atherosclerosis (2009) 206, 134-140. PubMed Europe PubMed DOI
Labonte,P., Begley,S., Guevin,C., Asselin,M.C., Nassoury,N., Mayer,G., Prat,A. and Seidah,N.G. PCSK9 impedes hepatitis C virus infection in vitro and modulates liver CD81 expression Hepatology (2009) 50, 17-24. PubMed Europe PubMed DOI
Lambert,G., Charlton,F., Rye,K.A. and Piper,D.E. Molecular basis of PCSK9 function Atherosclerosis (2009) 203, 1-7. PubMed Europe PubMed DOI V T
Le May,C., Kourimate,S., Langhi,C., Chetiveaux,M., Jarry,A., Comera,C., Collet,X., Kuipers,F., Krempf,M., Cariou,B. and Costet,P. Proprotein convertase subtilisin kexin type 9 null mice are protected from postprandial triglyceridemia Arterioscler Thromb Vasc Biol (2009) 29, 684-690. PubMed Europe PubMed DOI K
Leblond,F., Seidah,N.G., Precourt,L.P., Delvin,E., Dominguez,M. and Levy,E. Regulation of the proprotein convertase subtilisin/kexin type 9 in intestinal epithelial cells Am J Physiol Gastrointest Liver Physiol (2009) 296, G805-G815. PubMed Europe PubMed DOI
Leigh,S.E., Leren,T.P. and Humphries,S.E. Commentary PCSK9 variants: a new database Atherosclerosis (2009) 203, 32-33. PubMed Europe PubMed DOI M
Li,H., Li,H., Ziegler,N., Cui,R. and Liu,J. Recent patents on PCSK9: a new target for treating hypercholesterolemia Recent Pat DNA Gene Seq (2009) 3, 201-212. PubMed Europe PubMed DOI V
Luo,Y., Warren,L., Xia,D., Jensen,H., Sand,T., Petras,S., Qin,W., Miller,K.S. and Hawkins,J. Function and distribution of circulating human PCSK9 expressed extrahepatically in transgenic mice J Lipid Res (2009) 50, 1581-1588. PubMed Europe PubMed DOI PMC EPMC
McNutt,M.C., Kwon,H.J., Chen,C., Chen,J.R., Horton,J.D. and Lagace,T.A. Antagonism of secreted PCSK9 increases low density lipoprotein receptor expression in HepG2 cells J Biol Chem (2009) 284, 10561-10570. PubMed Europe PubMed DOI PMC EPMC
Mousavi,S.A., Berge,K.E. and Leren,T.P. The unique role of proprotein convertase subtilisin/kexin 9 in cholesterol homeostasis J Intern Med (2009) 266, 507-519. PubMed Europe PubMed DOI
Persson,L., Galman,C., Angelin,B. and Rudling,M. Importance of proprotein convertase subtilisin/kexin type 9 in the hormonal and dietary regulation of rat liver low-density lipoprotein receptors Endocrinology (2009) 150, 1140-1146. PubMed Europe PubMed DOI
Seidah,N.G. PCSK9 as a therapeutic target of dyslipidemia Expert Opin Ther Targets (2009) 13, 19-28. PubMed Europe PubMed DOI V
Steinberg,D. and Witztum,J.L. Inhibition of PCSK9: a powerful weapon for achieving ideal LDL cholesterol levels Proc Natl Acad Sci U S A (2009) 106, 9546-9547. PubMed Europe PubMed DOI PMC EPMC T

2008

Calandra,S. and Tarugi,P. Genetics and molecular biology: proprotein convertase subtilisin/kexin type 9 and LDL receptor - an intriguing story Curr Opin Lipidol (2008) 19, 208-211. PubMed Europe PubMed DOI V
Cameron,J., Holla,O.L., Laerdahl,J.K., Kulseth,M.A., Ranheim,T., Rognes,T., Berge,K.E. and Leren,T.P. Characterization of novel mutations in the catalytic domain of the PCSK9 gene J Intern Med (2008) 263, 420-431. PubMed Europe PubMed DOI M
Cameron,J., Holla,O.L., Berge,K.E., Kulseth,M.A., Ranheim,T., Leren,T.P. and Laerdahl,J.K. Investigations on the evolutionary conservation of PCSK9 reveal a functionally important protrusion FEBS J (2008) 275, 4121-4133. PubMed Europe PubMed DOI
Careskey,H.E., Davis,R.A., Alborn,W.E., Troutt,J.S., Cao,G. and Konrad,R.J. Atorvastatin increases human serum levels of proprotein convertase subtilisin/kexin type 9 J Lipid Res (2008) 49, 394-398. PubMed Europe PubMed DOI
Costet,P., Krempf,M. and Cariou,B. PCSK9 and LDL cholesterol: unravelling the target to design the bullet Trends Biochem Sci (2008) 33, 426-434. PubMed Europe PubMed DOI V
Dewpura,T., Raymond,A., Hamelin,J., Seidah,N.G., Mbikay,M., Chretien,M. and Mayne,J. PCSK9 is phosphorylated by a Golgi casein kinase-like kinase ex vivo and circulates as a phosphoprotein in humans FEBS J (2008) 275, 3480-3493. PubMed Europe PubMed DOI
Ding,K. and Kullo,I.J. Molecular population genetics of PCSK9: a signature of recent positive selection Pharmacogenet Genomics (2008) 18, 169-179. PubMed Europe PubMed DOI M
Fan,D., Yancey,P.G., Qiu,S., Ding,L., Weeber,E.J., Linton,M.F. and Fazio,S. Self-association of human PCSK9 correlates with its LDLR-degrading activity Biochemistry (2008) 47, 1631-1639. PubMed Europe PubMed DOI PMC EPMC
Frank-Kamenetsky,M., Grefhorst,A., Anderson,N.N., Racie,T.S., Bramlage,B., Akinc,A., Butler,D., Charisse,K., Dorkin,R., Fan,Y., Gamba-Vitalo,C., Hadwiger,P., Jayaraman,M., John,M., Jayaprakash,K.N., Maier,M., Nechev,L., Rajeev,K.G., Read,T., Rohl,I., Soutschek,J., Tan,P., Wong,J., Wang,G., Zimmermann,T., de Fougerolles,A., Vornlocher,H.P., Langer,R., Anderson,D.G., Manoharan,M., Koteliansky,V., Horton,J.D. and Fitzgerald,K. Therapeutic RNAi targeting PCSK9 acutely lowers plasma cholesterol in rodents and LDL cholesterol in nonhuman primates Proc Natl Acad Sci U S A (2008) 105, 11915-11920. PubMed Europe PubMed DOI PMC EPMC
Grefhorst,A., McNutt,M.C., Lagace,T.A. and Horton,J.D. Plasma PCSK9 preferentially reduces liver LDL receptors in mice J Lipid Res (2008) 49, 1303-1311. PubMed Europe PubMed DOI PMC EPMC
Jonas,M.C., Costantini,C. and Puglielli,L. PCSK9 is required for the disposal of non-acetylated intermediates of the nascent membrane protein BACE1 EMBO Rep (2008) 9, 916-922. PubMed Europe PubMed DOI PMC EPMC
Kostrzewa,G., Broda,G., Kurjata,P., Piotrowski,W. and Ploski,R. Effect of protein convertase subtilisin/kexin type 9 (PCSK9) 46L gene polymorphism on LDL cholesterol concentration in a Polish adult population Mol Genet Metab (2008) 94, 259-262. PubMed Europe PubMed DOI M
Kwon,H.J., Lagace,T.A., McNutt,M.C., Horton,J.D. and Deisenhofer,J. Molecular basis for LDL receptor recognition by PCSK9 Proc Natl Acad Sci U S A (2008) 105, 1820-1825. PubMed Europe PubMed DOI PMC EPMC S
Leren,T.P. and Berge,K.E. Identification of mutations in the apolipoprotein B-100 gene and in the PCSK9 gene as the cause of hypocholesterolemia Clin Chim Acta (2008) 397, 92-95. PubMed Europe PubMed DOI M
Lopez,D. PCSK9: an enigmatic protease Biochim Biophys Acta (2008) 1781, 184-191. PubMed Europe PubMed DOI V
Pandit,S., Wisniewski,D., Santoro,J.C., Ha,S., Ramakrishnan,V., Cubbon,R.M., Cummings,R.T., Wright,S.D., Sparrow,C.P., Sitlani,A. and Fisher,T.S. Functional analysis of sites within PCSK9 responsible for hypercholesterolemia J Lipid Res (2008) 49, 1333-1343. PubMed Europe PubMed DOI M
Poirier,S., Mayer,G., Benjannet,S., Bergeron,E., Marcinkiewicz,J., Nassoury,N., Mayer,H., Nimpf,J., Prat,A. and Seidah,N.G. The proprotein convertase PCSK9 induces the degradation of low density lipoprotein receptor (LDLR) and its closest family members VLDLR and ApoER2 J Biol Chem (2008) 283, 2363-2372. PubMed Europe PubMed DOI
Polisecki,E., Peter,I., Robertson,M., McMahon,A.D., Ford,I., Packard,C., Shepherd,J., Jukema,J.W., Blauw,G.J., Westendorp,R.G., de Craen,A.J., Trompet,S., Buckley,B.M., Murphy,M.B., Ordovas,J.M. and Schaefer,E.J. Genetic variation at the PCSK9 locus moderately lowers low-density lipoprotein cholesterol levels, but does not significantly lower vascular disease risk in an elderly population Atherosclerosis (2008) 200, 95-101. PubMed Europe PubMed DOI M
Ranheim,T., Mattingsdal,M., Lindvall,J.M., Holla,O.L., Berge,K.E., Kulseth,M.A. and Leren,T.P. Genome-wide expression analysis of cells expressing gain of function mutant D374Y-PCSK9 J Cell Physiol (2008) 217, 459-467. PubMed Europe PubMed DOI M
Schmidt,R.J., Zhang,Y., Zhao,Y., Qian,Y.W., Wang,H., Lin,A., Ehsani,M.E., Yu,X., Wang,G., Singh,J., Su,E.W., Li,S., Konrad,R.J. and Cao,G. A novel splicing variant of proprotein convertase subtilisin/kexin type 9 DNA Cell Biol (2008) 27, 183-189. PubMed Europe PubMed DOI R
Schmidt,R.J., Beyer,T.P., Bensch,W.R., Qian,Y.W., Lin,A., Kowala,M., Alborn,W.E., Konrad,R.J. and Cao,G. Secreted proprotein convertase subtilisin/kexin type 9 reduces both hepatic and extrahepatic low-density lipoprotein receptors in vivo Biochem Biophys Res Commun (2008) 370, 634-640. PubMed Europe PubMed DOI
Seidah,N.G., Mayer,G., Zaid,A., Rousselet,E., Nassoury,N., Poirier,S., Essalmani,R. and Prat,A. The activation and physiological functions of the proprotein convertases Int J Biochem Cell Biol (2008) 40, 1111-1125. PubMed Europe PubMed DOI
Shan,L., Pang,L., Zhang,R., Murgolo,N.J., Lan,H. and Hedrick,J.A. PCSK9 binds to multiple receptors and can be functionally inhibited by an EGF-A peptide Biochem Biophys Res Commun (2008) 375, 69-73. PubMed Europe PubMed DOI
Sirois,F., Gbeha,E., Sanni,A., Chretien,M., Labuda,D. and Mbikay,M. Ethnic differences in the frequency of the cardioprotective C679X PCSK9 mutation in a West African population Genet Test (2008) 12, 377-380. PubMed Europe PubMed DOI M
Varret,M., Abifadel,M., Rabes,J.P. and Boileau,C. Genetic heterogeneity of autosomal dominant hypercholesterolemia Clin Genet (2008) 73, 1-13. PubMed Europe PubMed DOI M
Zaid,A., Roubtsova,A., Essalmani,R., Marcinkiewicz,J., Chamberland,A., Hamelin,J., Tremblay,M., Jacques,H., Jin,W., Davignon,J., Seidah,N.G. and Prat,A. Proprotein convertase subtilisin/kexin type 9 (PCSK9): hepatocyte-specific low-density lipoprotein receptor degradation and critical role in mouse liver regeneration Hepatology (2008) 48, 646-654. PubMed Europe PubMed DOI
Zhang,D.W., Garuti,R., Tang,W.J., Cohen,J.C. and Hobbs,H.H. Structural requirements for PCSK9-mediated degradation of the low-density lipoprotein receptor Proc Natl Acad Sci U S A (2008) 105, 13045-13050. PubMed Europe PubMed DOI PMC EPMC

2007

Abboud,S., Karhunen,P.J., Lutjohann,D., Goebeler,S., Luoto,T., Friedrichs,S., Lehtimaki,T., Pandolfo,M. and Laaksonen,R. Proprotein convertase subtilisin/kexin type 9 (PCSK9) gene is a risk factor of large-vessel atherosclerosis stroke PLoS ONE (2007) 2, e1043-e1043. PubMed Europe PubMed DOI PMC EPMC M
Cunningham,D., Danley,D.E., Geoghegan,K.F., Griffor,M.C., Hawkins,J.L., Subashi,T.A., Varghese,A.H., Ammirati,M.J., Culp,J.S., Hoth,L.R., Mansour,M.N., McGrath,K.M., Seddon,A.P., Shenolikar,S., Stutzman-Engwall,K.J., Warren,L.C., Xia,D. and Qiu,X. Structural and biophysical studies of PCSK9 and its mutants linked to familial hypercholesterolemia Nat Struct Mol Biol (2007) 14, 413-419. PubMed Europe PubMed DOI M
Ding,K., McDonough,S.J. and Kullo,I.J. Evidence for positive selection in the C-terminal domain of the cholesterol metabolism gene PCSK9 based on phylogenetic analysis in 14 primate species PLoS ONE (2007) 2, e1098-e1098. PubMed Europe PubMed DOI PMC EPMC
Folsom,A.R., Peacock,J.M. and Boerwinkle,E. Sequence variation in proprotein convertase subtilisin/kexin type 9 serine protease gene, low LDL cholesterol, and cancer incidence Cancer Epidemiol Biomarkers Prev (2007) 16, 2455-2458. PubMed Europe PubMed DOI M
Graham,M.J., Lemonidis,K.M., Whipple,C.P., Subramaniam,A., Monia,B.P., Crooke,S.T. and Crooke,R.M. Antisense inhibition of proprotein convertase subtilisin/kexin type 9 reduces serum LDL in hyperlipidemic mice J Lipid Res (2007) 48, 763-767. PubMed Europe PubMed DOI
Hampton,E.N., Knuth,M.W., Li,J., Harris,J.L., Lesley,S.A. and Spraggon,G. The self-inhibited structure of full-length PCSK9 at 1.9 A reveals structural homology with resistin within the C-terminal domain Proc Natl Acad Sci U S A (2007) 104, 14604-14609. PubMed Europe PubMed DOI PMC EPMC S
Hooper,A.J., Marais,A.D., Tanyanyiwa,D.M. and Burnett,J.R. The C679X mutation in PCSK9 is present and lowers blood cholesterol in a Southern African population Atherosclerosis (2007) 193, 445-448. PubMed Europe PubMed DOI M
Horton,J.D., Cohen,J.C. and Hobbs,H.H. Molecular biology of PCSK9: its role in LDL metabolism Trends Biochem Sci (2007) 32, 71-77. PubMed Europe PubMed DOI PMC EPMC V
Lambert,G. Unravelling the functional significance of PCSK9 Curr Opin Lipidol (2007) 18, 304-309. PubMed Europe PubMed DOI V
Li,J., Tumanut,C., Gavigan,J.A., Huang,W.J., Hampton,E.N., Tumanut,R., Suen,K.F., Trauger,J.W., Spraggon,G., Lesley,S.A., Liau,G., Yowe,D. and Harris,J.L. Secreted PCSK9 promotes LDL receptor degradation independently of proteolytic activity Biochem J (2007) 406, 203-207. PubMed Europe PubMed DOI PMC EPMC
Mbikay,M., Mayne,J., Seidah,N.G. and Chretien,M. Of PCSK9, cholesterol homeostasis and parasitic infections: possible survival benefits of loss-of-function PCSK9 genetic polymorphisms Med Hypotheses (2007) 69, 1010-1017. PubMed Europe PubMed DOI M
McNutt,M.C., Lagace,T.A. and Horton,J.D. Catalytic activity is not required for secreted PCSK9 to reduce low density lipoprotein receptors in HepG2 cells J Biol Chem (2007) 282, 20799-20803. PubMed Europe PubMed DOI
Nassoury,N., Blasiole,D.A., Tebon Oler,A., Benjannet,S., Hamelin,J., Poupon,V., McPherson,P.S., Attie,A.D., Prat,A. and Seidah,N.G. The cellular trafficking of the secretory proprotein convertase PCSK9 and its dependence on the LDLR Traffic (2007) 8, 718-732. PubMed Europe PubMed DOI
Piper,D.E., Jackson,S., Liu,Q., Romanow,W.G., Shetterly,S., Thibault,S.T., Shan,B. and Walker,N.P. The crystal structure of PCSK9: a regulator of plasma LDL-cholesterol Structure (2007) 15, 545-552. PubMed Europe PubMed DOI S
Qian,Y.W., Schmidt,R.J., Zhang,Y., Chu,S., Lin,A., Wang,H., Wang,X., Beyer,T.P., Bensch,W.R., Li,W., Ehsani,M.E., Lu,D., Konrad,R.J., Eacho,P.I., Moller,D.E., Karathanasis,S.K. and Cao,G. Secreted PCSK9 downregulates low density lipoprotein receptor through receptor-mediated endocytosis J Lipid Res (2007) 48, 1488-1498. PubMed Europe PubMed DOI
Seidah,N.G. and Prat,A. The proprotein convertases are potential targets in the treatment of dyslipidemia J Mol Med (Berl) (2007) 85, 685-696. PubMed Europe PubMed DOI V
Wierzbicki,A.S. Proprotein convertase subtilisin/kexin type 9, its variants and regulation of low-density lipoprotein cholesterol Curr Opin Lipidol (2007) 18, 227-229. PubMed Europe PubMed DOI
Zhang,D.W., Lagace,T.A., Garuti,R., Zhao,Z., McDonald,M., Horton,J.D., Cohen,J.C. and Hobbs,H.H. Binding of proprotein convertase subtilisin/kexin type 9 to epidermal growth factor-like repeat A of low density lipoprotein receptor decreases receptor recycling and increases degradation J Biol Chem (2007) 282, 18602-18612. PubMed Europe PubMed DOI

2006

[YEAR:15-8-2006]Benjannet,S., Rhainds,D., Hamelin,J., Nassoury,N. and Seidah,N.G. The proprotein convertase (PC) PCSK9 is inactivated by furin and/or PC5/6A: functional consequences of natural mutations and post-translational modifications J Biol Chem (15-8-2006) 281, 30561-30572. PubMed Europe PubMed DOI M
Berge,K.E., Ose,L. and Leren,T.P. Missense mutations in the PCSK9 gene are associated with hypocholesterolemia and possibly increased response to statin therapy Arterioscler Thromb Vasc Biol (2006) 26, 1094-1100. PubMed Europe PubMed DOI M
[YEAR:1-11-2006]Bingham,B., Shen,R., Kotnis,S., Lo,C.F., Ozenberger,B.A., Ghosh,N., Kennedy,J.D., Jacobsen,J.S., Grenier,J.M., DiStefano,P.S., Chiang,L.W. and Wood,A. Proapoptotic effects of NARC 1 (= PCSK9), the gene encoding a novel serine proteinase Cytometry A (1-11-2006) 69, 1123-1131. PubMed Europe PubMed DOI
Kotowski,I.K., Pertsemlidis,A., Luke,A., Cooper,R.S., Vega,G.L., Cohen,J.C. and Hobbs,H.H. A spectrum of PCSK9 alleles contributes to plasma levels of low-density lipoprotein cholesterol Am J Hum Genet (2006) 78, 410-422. PubMed Europe PubMed DOI PMC EPMC M
Lambert,G., Jarnoux,A.L., Pineau,T., Pape,O., Chetiveaux,M., Laboisse,C., Krempf,M. and Costet,P. Fasting induces hyperlipidemia in mice overexpressing proprotein convertase subtilisin kexin type 9: lack of modulation of very-low-density lipoprotein hepatic output by the low-density lipoprotein receptor Endocrinology (2006) 147, 4985-4995. PubMed Europe PubMed DOI
Poirier,S., Prat,A., Marcinkiewicz,E., Paquin,J., Chitramuthu,B.P., Baranowski,D., Cadieux,B., Bennett,H.P. and Seidah,N.G. Implication of the proprotein convertase NARC-1/PCSK9 in the development of the nervous system J Neurochem (2006) 98, 838-850. PubMed Europe PubMed DOI K
Scamuffa,N., Calvo,F., Chretien,M., Seidah,N.G. and Khatib,A.M. Proprotein convertases: lessons from knockouts FASEB J (2006) 20, 1954-1963. PubMed Europe PubMed DOI K V
Seidah,N.G., Khatib,A.M. and Prat,A. The proprotein convertases and their implication in sterol and/or lipid metabolism Biol Chem (2006) 387, 871-877. PubMed Europe PubMed DOI V
Zhao,Z., Tuakli-Wosornu,Y., Lagace,T.A., Kinch,L., Grishin,N.V., Horton,J.D., Cohen,J.C. and Hobbs,H.H. Molecular characterization of loss-of-function mutations in PCSK9 and identification of a compound heterozygote Am J Hum Genet (2006) 79, 514-523. PubMed Europe PubMed DOI PMC EPMC M

2005

Allard,D., Amsellem,S., Abifadel,M., Trillard,M., Devillers,M., Luc,G., Krempf,M., Reznik,Y., Girardet,J.P., Fredenrich,A., Junien,C., Varret,M., Boileau,C., Benlian,P. and Rabes,J.P. Novel mutations of the PCSK9 gene cause variable phenotype of autosomal dominant hypercholesterolemia Hum Mutat (2005) 26, 497-497. PubMed Europe PubMed DOI M
Cohen,J., Pertsemlidis,A., Kotowski,I.K., Graham,R., Garcia,C.K. and Hobbs,H.H. Low LDL cholesterol in individuals of African descent resulting from frequent nonsense mutations in PCSK9 Nat Genet (2005) 37, 161-165. PubMed Europe PubMed DOI M
[YEAR:1-3-2005]Lalanne,F., Lambert,G., Amar,M.J., Chetiveaux,M., Zair,Y., Jarnoux,A.L., Ouguerram,K., Friburg,J., Seidah,N.G., Brewer,H.B., Jr., Krempf,M. and Costet,P. Wild-type PCSK9 inhibits LDL clearance but does not affect apoB-containing lipoprotein production in mouse and cultured cells J Lipid Res (1-3-2005) 46, 1312-1319. PubMed Europe PubMed DOI
Maxwell,K.N. and Breslow,J.L. Proprotein convertase subtilisin kexin 9: the third locus implicated in autosomal dominant hypercholesterolemia Curr Opin Lipidol (2005) 16, 167-172. PubMed Europe PubMed
[YEAR:8-2-2005]Maxwell,K.N., Fisher,E.A. and Breslow,J.L. Overexpression of PCSK9 accelerates the degradation of the LDLR in a post-endoplasmic reticulum compartment Proc Natl Acad Sci U S A (8-2-2005) 102, 2069-2074. PubMed Europe PubMed DOI PMC EPMC
Naoumova,R.P., Tosi,I., Patel,D., Neuwirth,C., Horswell,S.D., Marais,A.D., van Heyningen,C. and Soutar,A.K. Severe hypercholesterolemia in four British families with the D374Y mutation in the PCSK9 gene: long-term follow-up and treatment response Arterioscler Thromb Vasc Biol (2005) 25, 2654-2660. PubMed Europe PubMed DOI M
[YEAR:12-4-2005]Rashid,S., Curtis,D.E., Garuti,R., Anderson,N.N., Bashmakov,Y., Ho,Y.K., Hammer,R.E., Moon,Y.A. and Horton,J.D. Decreased plasma cholesterol and hypersensitivity to statins in mice lacking Pcsk9 Proc Natl Acad Sci U S A (12-4-2005) 102, 5374-5379. PubMed Europe PubMed DOI PMC EPMC K

2004

[YEAR:9-9-2004]Benjannet,S., Rhainds,D., Essalmani,R., Mayne,J., Wickham,L., Jin,W., Asselin,M.C., Hamelin,J., Varret,M., Allard,D., Trillard,M., Abifadel,M., Tebon,A., Attie,A.D., Rader,D.J., Boileau,C., Brissette,L., Chretien,M., Prat,A. and Seidah,N.G. NARC-1/PCSK9 and its natural mutants: zymogen cleavage and effects on the low density lipoprotein (LDL) receptor and LDL cholesterol J Biol Chem (9-9-2004) 279, 48865-48875. PubMed Europe PubMed DOI
Dubuc,G., Chamberland,A., Wassef,H., Davignon,J., Seidah,N.G., Bernier,L. and Prat,A. Statins upregulate PCSK9, the gene encoding the proprotein convertase neural apoptosis-regulated convertase-1 implicated in familial hypercholesterolemia Arterioscler Thromb Vasc Biol (2004) 24, 1454-1459. PubMed Europe PubMed DOI
Leren,T.P. Mutations in the PCSK9 gene in Norwegian subjects with autosomal dominant hypercholesterolemia Clin Genet (2004) 65, 419-422. PubMed Europe PubMed DOI M
[YEAR:4-5-2004]Maxwell,K.N. and Breslow,J.L. Adenoviral-mediated expression of Pcsk9 in mice results in a low-density lipoprotein receptor knockout phenotype Proc Natl Acad Sci U S A (4-5-2004) 101, 7100-7105. PubMed Europe PubMed DOI PMC EPMC
[YEAR:22-9-2004]Park,S.W., Moon,Y.A. and Horton,J.D. Post-transcriptional regulation of low density lipoprotein receptor protein by proprotein convertase subtilisin/kexin type 9a in mouse liver J Biol Chem (22-9-2004) 279, 50630-50638. PubMed Europe PubMed DOI
Timms,K.M., Wagner,S., Samuels,M.E., Forbey,K., Goldfine,H., Jammulapati,S., Skolnick,M.H., Hopkins,P.N., Hunt,S.C. and Shattuck,D.M. A mutation in PCSK9 causing autosomal-dominant hypercholesterolemia in a Utah pedigree Hum Genet (2004) 114, 349-353. PubMed Europe PubMed DOI M

2003

Abifadel,M., Varret,M., Rabes,J.P., Allard,D., Ouguerram,K., Devillers,M., Cruaud,C., Benjannet,S., Wickham,L., Erlich,D., Derre,A., Villeger,L., Farnier,M., Beucler,I., Bruckert,E., Chambaz,J., Chanu,B., Lecerf,J.M., Luc,G., Moulin,P., Weissenbach,J., Prat,A., Krempf,M., Junien,C., Seidah,N.G. and Boileau,C. Mutations in PCSK9 cause autosomal dominant hypercholesterolemia Nat Genet (2003) 34, 154-156. PubMed Europe PubMed DOI M
[YEAR:1-12-2003]Naureckiene,S., Ma,L., Sreekumar,K., Purandare,U., Lo,C.F., Huang,Y., Chiang,L.W., Grenier,J.M., Ozenberger,B.A., Jacobsen,J.S., Kennedy,J.D., DiStefano,P.S., Wood,A. and Bingham,B. Functional characterization of Narc 1, a novel proteinase related to proteinase K Arch Biochem Biophys (1-12-2003) 420, 55-67. PubMed Europe PubMed DOI
[YEAR:4-2-2003]Seidah,N.G., Benjannet,S., Wickham,L., Marcinkiewicz,J., Jasmin,S.B., Stifani,S., Basak,A., Prat,A. and Chretien,M. The secretory proprotein convertase neural apoptosis-regulated convertase 1 (NARC-1): liver regeneration and neuronal differentiation Proc Natl Acad Sci U S A (4-2-2003) 100, 928-933. PubMed Europe PubMed DOI PMC EPMC

2002

Seidah,N.G. and Prat,A. Precursor convertases in the secretory pathway, cytosol and extracellular milieu Essays Biochem (2002) 38, 79-94. PubMed Europe PubMed