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.)

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 Dev33, 101390-101390. 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 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 PubMed Europe PubMed DOI I
Martini,E.
Epigenetic silencing of PCSK9 enables durable reduction of low-density lipoprotein cholesterol
Nat Cardiovasc Res4, 347-347. 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 Gerontol201, 112701-112701. PubMed Europe PubMed DOI

2024

Agarwala,A., Asim,R. and Ballantyne,C.M.
Oral PCSK9 Inhibitors
Curr Atheroscler Rep26, 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 Trans52, 431-440. PubMed Europe PubMed DOI
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)86, 899-908. PubMed Europe PubMed DOI
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
Atherosclerosis399, 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 Pharmacol220, 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 Ther9, 13-13. PubMed Europe PubMed DOI 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
Nature627, 416-423. PubMed Europe PubMed DOI
Chackerian,B. and Remaley,A.T.
PCSK9 vaccines: a promising new strategy for the treatment of hypercholesterolemia?
J Lipid Res65, 100524-100524. PubMed Europe PubMed DOI
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
Biomedicines12, PubMed Europe PubMed DOI
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 Med53, PubMed Europe PubMed DOI 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 Pharmacol19, 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 Res100699-100699. 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 Pat1-17. PubMed Europe PubMed DOI K
Fernandez-Ruiz,I.
An epigenome editing approach induces durable silencing of Pcsk9
Nat Rev Cardiol21, 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 Chem265, 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 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
ChemMedCheme202400208-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 Pathol19, 1-9. PubMed Europe PubMed DOI V
Hoekstra,M. and Van Eck,M.
Gene Editing for the Treatment of Hypercholesterolemia
Curr Atheroscler Rep 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 Oncol41, 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 J38, 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 Pharmacol102, 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 Med11, 1431398-1431398. PubMed Europe PubMed DOI
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 Biol44, 328-333. PubMed Europe PubMed DOI
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 Dis34, 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 Lett97, 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 Chem31, 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 Dis23, 156-156. PubMed Europe PubMed DOI 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 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
Atherosclerosis401, 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 Commun723, 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 Differ15, 26-26. PubMed Europe PubMed DOI
Sabnis,R.W.
Novel PCSK9 Inhibitors for Treating Cardiovascular Diseases
ACS Med Chem Lett15, 443-444. PubMed Europe PubMed DOI
Siddiqui,Z. and Frishman,W.
New Oral PCSK9 Inhibitor: "MK-0616"
Cardiol Rev 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 Sci25, PubMed Europe PubMed DOI 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 Immun115, 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 Sin45, 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 PubMed Europe PubMed DOI K
Zendjebil,S. and Steg,P.G.
PCSK9 Monoclonal Antibodies Have Come a Long Way
Curr Atheroscler Rep26, 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 Commun742, 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 Res85, 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 Lett92, 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 Cardiol81, 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 Rev149, 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 Drugs32, 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 Rep13, 19725-19725. PubMed Europe PubMed DOI 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 Biol133, 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 Ther45, 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 Sci24, PubMed Europe PubMed DOI
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)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 Metab67, 101662-101662. PubMed Europe PubMed DOI 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 Med10, 1191303-1191303. PubMed Europe PubMed DOI
Hummelgaard,S., Vilstrup,J.P., Gustafsen,C., Glerup,S. and Weyer,K.
Targeting PCSK9 to tackle cardiovascular disease
Pharmacol Ther249, 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 Sci2023, 5932315-5932315. PubMed Europe PubMed DOI 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 Dyn1-10. 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 Res64, 100426-100426. PubMed Europe PubMed DOI 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
Circulation148, 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 Lett25, 5001-5005. PubMed Europe PubMed DOI I
Laufs,U., Bluher,M. and Isermann,B.
Third generation PCSK9-inhibitors
Eur Heart J44, 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 Bioeng7, 046103-046103. PubMed Europe PubMed DOI
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 Chem299, 104895-104895. PubMed Europe PubMed DOI 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 Biol43, 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 Med12, PubMed Europe PubMed DOI V
Newman,C.B. and Tobert,J.A.
Targeting PCSK9 With Antibodies and Gene Silencing to Reduce LDL Cholesterol
J Clin Endocrinol Metab108, 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 Biol43, 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 Chem247, 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 Cardiol18, e45-e45. PubMed Europe PubMed DOI 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 Genet55, 1831-1842. PubMed Europe PubMed DOI
Sener,Y.Z. and Tokgozoglu,L.
Pleiotropy of PCSK9: Functions in Extrahepatic Tissues
Curr Cardiol Rep25, 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 Screen26, 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 Immunol14, 1126823-1126823. PubMed Europe PubMed DOI 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 Acta547, 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 Today27, 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
Kidney3603, 1394-1410. PubMed Europe PubMed DOI
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 Immunol126, 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)11, PubMed Europe PubMed DOI V
Coppinger,C., Movahed,M.R., Azemawah,V., Peyton,L., Gregory,J. and Hashemzadeh,M.
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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 Biol27, 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
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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 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 PubMed Europe PubMed DOI V
Sabnis,R.W.
Novel Cyclic Tetramer Compounds as PCSK9 Inhibitors for Treating Metabolic Disorders
ACS Med Chem Lett11, 1671-1673. PubMed Europe PubMed DOI
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 Chem295, 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 Physiol11, 598649-598649. PubMed Europe PubMed DOI 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
ChemMedChem15, 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 Neurosurg135, 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 Rep22, 176-176. PubMed Europe PubMed DOI 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 ONE15, e0239752-e0239752. PubMed Europe PubMed DOI
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
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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 Med59, 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 Rep10, 16514-16514. 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.
Ascorbic acid enhances low-density lipoprotein receptor expression by suppressing proprotein convertase subtilisin/kexin 9 expression
J Biol Chem295, 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
EBioMedicine52, 102650-102650. PubMed Europe PubMed DOI
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
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Wu,Y.X. and Wang,Y.
[Progress on the molecular mechanisms of PCSK9-mediated degradation of low density lipoprotein receptor]
Yi Chuan42, 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 Cardiol128, 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 Res2020, 2687692-2687692. PubMed Europe PubMed DOI V
Yurtseven,E., Ural,D., Baysal,K. and Tokgozoglu,L.
An Update on the Role of PCSK9 in Atherosclerosis
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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 Dis30, 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 Neurosci11, 120-120. PubMed Europe PubMed DOI
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 J95, 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 Cardiol112, 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 ONE14, 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 Saf18, 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 Ther27, 188-199. PubMed Europe PubMed DOI
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 Chem62, 6163-6174. PubMed Europe PubMed DOI I
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 Rep9, 2343-2343. PubMed Europe PubMed DOI I
Lavecchia,A. and Cerchia,C.
Recent advances in developing PCSK9 inhibitors for lipid-lowering therapy
Future Med Chem11, 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 Cardiol34, 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
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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 Med23, 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
Atherosclerosis289, 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 Biol431, 904-907. PubMed Europe PubMed DOI
Sheridan,C.
PCSK9-gene-silencing, cholesterol-lowering drug impresses
Nat Biotechnol37, 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 Biol431, 885-903. PubMed Europe PubMed DOI
Wang,Y. and Liu,Z.P.
PCSK9 inhibitors: novel therapeutic strategies for lowering LDL-cholesterol
Mini Rev Med Chem19, 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)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
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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 Acta483, 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 Outcomes4, 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 Cardiol41, 544-550. PubMed Europe PubMed DOI
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 Exp58265-58265. PubMed Europe PubMed DOI A
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 Chem293, 1875-1886. PubMed Europe PubMed DOI P
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 Cardiol19, 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 Chem399, 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
EBioMedicine38, 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 Res192, 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 Med69, 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 Cardiol34, 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 Sci19, 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 Rep20, 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
Diseases6, 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 Virol99, 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 Lett28, 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 Ther365, 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 Med5, 199-199. PubMed Europe PubMed DOI I
Paquette,M., Hegele,R.A. and Baass,A.
PCSK9 inhibitors in familial hypercholesterolemia: what is the evidence?
J Clin Lipidol12, 1106-1108. PubMed Europe PubMed DOI
Paquette,M. and Baass,A.
A novel cause of familial hypercholesterolemia: PCSK9 gene duplication
Can J Cardiol34, 1259-1260. PubMed Europe PubMed DOI M
Pettersen,D. and Fjellstrom,O.
Small molecule modulators of PCSK9 - a literature and patent overview
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Roth,E.M. and Davidson,M.H.
PCSK9 inhibitors: mechanism of action, efficacy, and safety
Rev Cardiovasc Med19, S31-S31. PubMed Europe PubMed
Stoekenbroek,R.M., Lambert,G., Cariou,B. and Hovingh,G.K.
Inhibiting PCSK9 - biology beyond LDL control
Nat Rev Endocrinol15, 52-62. PubMed Europe PubMed DOI
Stoekenbroek,R.M. and Kastelein,J.J.P.
Proprotein convertase subtilisin/kexin type 9: from genetics to clinical trials
Curr Opin Cardiol33, 269-275. PubMed Europe PubMed DOI V
Taechalertpaisarn,J., Zhao,B., Liang,X. and Burgess,K.
Small molecule inhibitors of the PCSK9.LDLR interaction
J Am Chem Soc140, 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
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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 Cardiol119, 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 Cardiol40, 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 Cardiol9, 76-91. PubMed Europe PubMed DOI
Cirulli,E.T. and Ginsburg,G.S.
Studying genetic resilience to improve human health
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Civeira,F. and Jarauta,E.
Vaccine against PCSK9: the natural strategy from passive to active immunization for the prevention of atherosclerosis
J Thorac Dis9, 4291-4294. PubMed Europe PubMed DOI
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 Rep7, 15282-15282. PubMed Europe PubMed DOI M
Dron,J.S. and Hegele,R.A.
Complexity of mechanisms among human proprotein convertase subtilisin-kexin type 9 variants
Curr Opin Lipidol28, 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 Rep19, 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 Med376, 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 Pharmacol57, 513-523. PubMed Europe PubMed DOI
Gielen,S.
PCSK9 deficiency: a double-edged sword?
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Gouni-Berthold,I.
The efficacy of anti-PCSK9 antibodies: results from recent trials
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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
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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
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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
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Higgins,C.A. and Rees,A.
The onward march of PCSK9 inhibition
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Ito,M.K. and Santos,R.D.
PCSK9 inhibition with monoclonal antibodies: modern management of hypercholesterolemia
J Clin Pharmacol57, 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
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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
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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
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Liberale,L., Montecucco,F., Camici,G.G., Dallegri,F., Vecchie,A., Carbone,F. and Bonaventura,A.
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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.
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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)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
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2015

Alghamdi,R.H., O'Reilly,P., Lu,C., Gomes,J., Lagace,T.A. and Basak,A.
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EBioMedicine
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2010

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PCSK9-deficient mice exhibit impaired glucose tolerance and pancreatic islet abnormalities
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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
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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
Atherosclerosis208, 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
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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
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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
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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
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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
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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
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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
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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
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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
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Hedrick,J.A.
Targeting PCSK9 for the treatment of hypercholesterolemia
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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
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Kourimate,S., Chetiveaux,M., Jarnoux,A.L., Lalanne,F. and Costet,P.
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Labonte,P., Begley,S., Guevin,C., Asselin,M.C., Nassoury,N., Mayer,G., Prat,A. and Seidah,N.G.
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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
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Commentary PCSK9 variants: a new database
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Li,H., Li,H., Ziegler,N., Cui,R. and Liu,J.
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Luo,Y., Warren,L., Xia,D., Jensen,H., Sand,T., Petras,S., Qin,W., Miller,K.S. and Hawkins,J.
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McNutt,M.C., Kwon,H.J., Chen,C., Chen,J.R., Horton,J.D. and Lagace,T.A.
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Mousavi,S.A., Berge,K.E. and Leren,T.P.
The unique role of proprotein convertase subtilisin/kexin 9 in cholesterol homeostasis
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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
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Seidah,N.G.
PCSK9 as a therapeutic target of dyslipidemia
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Steinberg,D. and Witztum,J.L.
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2008

Calandra,S. and Tarugi,P.
Genetics and molecular biology: proprotein convertase subtilisin/kexin type 9 and LDL receptor - an intriguing story
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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
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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
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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
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Costet,P., Krempf,M. and Cariou,B.
PCSK9 and LDL cholesterol: unravelling the target to design the bullet
Trends Biochem Sci33, 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
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Ding,K. and Kullo,I.J.
Molecular population genetics of PCSK9: a signature of recent positive selection
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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
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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
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Grefhorst,A., McNutt,M.C., Lagace,T.A. and Horton,J.D.
Plasma PCSK9 preferentially reduces liver LDL receptors in mice
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Jonas,M.C., Costantini,C. and Puglielli,L.
PCSK9 is required for the disposal of non-acetylated intermediates of the nascent membrane protein BACE1
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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
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Kwon,H.J., Lagace,T.A., McNutt,M.C., Horton,J.D. and Deisenhofer,J.
Molecular basis for LDL receptor recognition by PCSK9
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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
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Lopez,D.
PCSK9: an enigmatic protease
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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
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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
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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
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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
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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
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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
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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
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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
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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
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Varret,M., Abifadel,M., Rabes,J.P. and Boileau,C.
Genetic heterogeneity of autosomal dominant hypercholesterolemia
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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
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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
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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
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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 Biol14, 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
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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
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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 Res48, 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
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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
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Horton,J.D., Cohen,J.C. and Hobbs,H.H.
Molecular biology of PCSK9: its role in LDL metabolism
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Lambert,G.
Unravelling the functional significance of PCSK9
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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
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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
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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 Chem282, 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
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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
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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 Res48, 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)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 Lipidol18, 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 Chem282, 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 Chem281, 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 Biol26, 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 A69, 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 Genet78, 410-422. PubMed Europe PubMed DOI 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
Endocrinology147, 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 Neurochem98, 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
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Seidah,N.G., Khatib,A.M. and Prat,A.
The proprotein convertases and their implication in sterol and/or lipid metabolism
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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 Genet79, 514-523. PubMed Europe PubMed DOI 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 Mutat26, 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 Genet37, 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 Res46, 1312-1319. PubMed Europe PubMed DOI
[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 A102, 2069-2074. 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 Lipidol16, 167-172. PubMed Europe PubMed
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 Biol25, 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 A102, 5374-5379. PubMed Europe PubMed DOI 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 Chem279, 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 Biol24, 1454-1459. PubMed Europe PubMed DOI
Leren,T.P.
Mutations in the PCSK9 gene in Norwegian subjects with autosomal dominant hypercholesterolemia
Clin Genet65, 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 A101, 7100-7105. PubMed Europe PubMed DOI
[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 Chem279, 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 Genet114, 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 Genet34, 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 Biophys420, 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 A100, 928-933. PubMed Europe PubMed DOI

2002

Seidah,N.G. and Prat,A.
Precursor convertases in the secretory pathway, cytosol and extracellular milieu
Essays Biochem38, 79-94. PubMed Europe PubMed