Literature for peptidase C01.036: cathepsin K

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, E Expression, V Review, M Mutation, I Inhibitor, L Localization, U Therapeutic. To select only the references relevant to a single topic, click the link above. See explanation.)

2026

Kuo,A., Tender,G.S., Chow,W.D., Riley,N.M., Wen,K.C., Park,S., Paek,J.H., Roberts,D.S., Peltan,E.L., Paszek,M.J. and Bertozzi,C.R. The protease Cathepsin K can debulk the cancer glycocalyx J Biol Chem (2026) , 111206-111206. PubMed Europe PubMed DOI
Soundararajan,A., Jayasankar,K., Doud,E.H., Pasteurin,R.P., Surma,M. and Pattabiraman,P.P. Loss of Cathepsin K Impairs Collagen Biogenesis and Enhances Actin Polymerization in Trabecular Meshwork Invest Ophthalmol Vis Sci (2026) 67, 63-63. PubMed Europe PubMed DOI PMC EPMC K

2025

Brizuela,L., Buchet,R., Bougault,C. and Mebarek,S. Cathepsin K Inhibitors as Potential Drugs for the Treatment of Osteoarthritis Int J Mol Sci (2025) 26 PubMed Europe PubMed DOI PMC EPMC V
Dey,G., Yakobovich,E., Loboda,J., Sinai-Turyansky,R., Abramovitch-Dahan,C., Merquiol,E., Sridharan,N., Itzhak,G., Turk,B., Wald,O., Turk,D., Yona,S., Levaot,N. and Blum,G. Development and Application of Small Molecule-Peptide Conjugates as Cathepsin K-Specific Covalent Irreversible Inhibitors in Human Osteoclast and Lung Cancer JACS Au (2025) 5, 1104-1120. PubMed Europe PubMed DOI PMC EPMC
Gawor,J., Gawor,D.Z., Druet,I., Salindre,J., Gajosz,A., Kowalczyk,P., Dam,N., Tierny,D., Dubruque,M. and Hanf,R. Cathepsin K inhibition by VBX1000 alleviates canine periodontitis Front Vet Sci (2025) 12, 1656782-1656782. PubMed Europe PubMed DOI PMC EPMC I
Guan,X., Cheng,S., Yin,Y. and Du,S. Small-molecule Cathepsin K inhibitors: a medicinal chemistry perspective Future Med Chem (2025) 17, 1757-1770. PubMed Europe PubMed DOI
Lee,J., Jung,G.N., Jung,K.J., Kim,J.W., Ma,M.J., Lee,Y., Yu,J.H., Min,S.H. and Lee,J.H. Pyrrolopyrimidines: A promising scaffold for the development of novel cathepsin K inhibitors Eur J Med Chem (2025) 302, 118323-118323. PubMed Europe PubMed DOI I
Lin,S., Wang,T. and Zuo,C. Cathepsin K (CTSK) in Inflammatory and Immune-Mediated Diseases Immunol Invest (2025) , 1-23. PubMed Europe PubMed DOI
Lin,X., Chen,Y., Zhong,B. and Yu,H. Cathepsin K and glycosaminoglycans differentially regulate matrix metalloproteinase activity in dentin under various pH conditions Int J Biol Macromol (2025) 327, 147486-147486. PubMed Europe PubMed DOI L
Liu,H., Wang,P., Li,J., Zhao,J., Mu,Y. and Gu,W. Role of Cathepsin K in bone invasion of pituitary adenomas: A dual mechanism involving cell proliferation and osteoclastogenesis Cancer Lett (2025) 611, 217443-217443. PubMed Europe PubMed DOI
Ma,L., Lu,B., Si,Y., Dai,L., Tan,M., Liu,W., Sun,D., Shu,J., Chen,C., Xiang,Q., Jiang,D., Wei,X. and Wang,W.E. Cathepsin K as a key regulator of myocardial fibrosis in dilated cardiomyopathy and a promising therapeutic target J Biol Chem (2025) 301, 110421-110421. PubMed Europe PubMed DOI PMC EPMC K
Panwar,P., Olesen,J.B., Delaisse,J.M., Soe,K. and Bromme,D. Cathepsin K inhibitors promote osteoclast-osteoblast communication and engagement of osteogenesis JBMR Plus (2025) 9, ziaf079-ziaf079. PubMed Europe PubMed DOI PMC EPMC
Soundararajan,A., Jaysankar,K., Doud,E., Pasteurin,R.P., Surma,M. and Pattabiraman,P.P. Loss of Cathepsin K impairs collagen biogenesis and enhances actin polymerization in trabecular meshwork bioRxiv (2025) PubMed Europe PubMed DOI PMC EPMC K
Suzuki,T., Loyde,E., Chen,S., Etzrodt,V., Idowu,T.O., Clark,A.J., Saade,M.C., Flores,B.M., Lu,S., Birrane,G., Vemireddy,V., Seeliger,B., David,S. and Parikh,S.M. Cathepsin K cleavage of Angiopoietin-2 creates detrimental Tie2 antagonist fragments in sepsis J Clin Invest (2025) PubMed Europe PubMed DOI
Wang,Y., Cui,Y., Liu,X., Liang,S., Zhong,L. and Guo,R. Cathepsin K inhibition promotes efficient differentiation of human embryonic stem cells to mature cardiomyocytes by mediating glucolipid metabolism and cellular energy homeostasis Stem Cell Res Ther (2025) 16, 118-118. PubMed Europe PubMed DOI PMC EPMC

2024

Ilyas,S., Lee,J., Hwang,Y., Choi,Y. and Lee,D. Deciphering Cathepsin K inhibitors: a combined QSAR, docking and MD simulation based machine learning approaches for drug design SAR QSAR Environ Res (2024) 35, 771-793. PubMed Europe PubMed DOI
Janin,Y.L. On the origins of SARS-CoV-2 main protease inhibitors RSC Med Chem (2024) 15, 81-118. PubMed Europe PubMed DOI PMC EPMC V I
Jiang,N.W., Chen,Y.Y., Lin,X.J. and Yu,H. Impact of cathepsin K-induced proteoglycans degradation on dentin collagen Arch Oral Biol (2024) 169, 106091-106091. PubMed Europe PubMed DOI
Jin,X., Yue,X., Huang,Z., Meng,X., Xu,S., Wu,Y., Wan,Y., Inoue,A., Narisawa,M., Hu,L., Shi,G.P., Umegaki,H., Murohara,T., Lei,Y., Kuzuya,M. and Cheng,X.W. Cathepsin K deficiency prevented stress-related thrombosis in a mouse FeCl(3) model Cell Mol Life Sci (2024) 81, 205-205. PubMed Europe PubMed DOI PMC EPMC
Liu,R., Jiao,Y.R., Huang,M., Zou,N.Y., He,C., Huang,M., Chen,K.X., He,W.Z., Liu,L., Sun,Y.C., Xia,Z.Y., Quarles,L.D., Yang,H.L., Wang,W.S., Xiao,Z.S., Luo,X.H. and Li,C.J. Mechanosensitive protein polycystin-1 promotes periosteal stem/progenitor cells osteochondral differentiation in fracture healing Theranostics (2024) 14, 2544-2559. PubMed Europe PubMed DOI PMC EPMC
Matouskova,Z., Orsaghova,K., Srb,P., Pytelkova,J., Kukacka,Z., Busa,M., Hajdusek,O., Sima,R., Fabry,M., Novak,P., Horn,M., Kopacek,P. and Mares,M. An Unusual Two-Domain Thyropin from Tick Saliva: NMR Solution Structure and Highly Selective Inhibition of Cysteine Cathepsins Modulated by Glycosaminoglycans Int J Mol Sci (2024) 25 PubMed Europe PubMed DOI PMC EPMC
Moon,D.O. Review of Cathepsin K Inhibitor Development and the Potential Role of Phytochemicals Molecules (2024) 30 PubMed Europe PubMed DOI PMC EPMC V
Wang,Y., Guan,T., Xiong,H., Hu,W., Zhu,X., Ma,Y. and Zhang,Z. Synthesis and Biological Evaluation of Novel Piperidine-3-Carboxamide Derivatives as Anti-Osteoporosis Agents Targeting Cathepsin K Molecules (2024) 29 PubMed Europe PubMed DOI PMC EPMC I
Zhalsanova,I.Z., Fonova,E.A., Valiakhmetov,N.R., Kolesnikov,N.A., Gosudarkina,S.N., Agafonova,A.A., Ravzhaeva,E.G., Seitova,G.N., Stepanov,V.A. and Skryabin,N.A. Case Report: A Novel Homozygous Variant of the CTSK Gene in Rare Pycnodysostosis Int J Mol Sci (2024) 25 PubMed Europe PubMed DOI PMC EPMC
Zhang,M., Yue,X., Xu,S., Piao,J., Zhao,L., Shu,S., Kuzuya,M., Li,P., Hong,L., Kim,W., Liu,B. and Cheng,X.W. Dipeptidyl peptidase-4 disturbs adipocyte differentiation via the negative regulation of the glucagon-like peptide-1/adiponectin-cathepsin K axis in mice under chronic stress conditions FASEB J (2024) 38, e23684-e23684. PubMed Europe PubMed DOI
Zhou,H., Zhang,Y.F., Zhang,Q.Q., Liu,F., Zhang,J.Y. and Chen,Y. Cathepsin K inhibition alleviates periodontal bone resorption by promoting type H vessel formation through PDGF-BB/PDGFR-beta axis Oral Dis (2024) 30, 5335-5348. PubMed Europe PubMed DOI

2023

Chai,W., Hao,W., Liu,J., Han,Z., Chang,S., Cheng,L., Sun,M., Yan,G., Liu,Z., Liu,Y., Zhang,G., Xing,L., Chen,H. and Liu,P. Visualizing Cathepsin K-Cre Expression at the Single-Cell Level with GFP Reporters JBMR Plus (2023) 7, e10706-e10706. PubMed Europe PubMed DOI PMC EPMC
Endres,E., Yuan Chen,N. and Sotriffer,C. MD-Based Assessment of Covalent Inhibitors in Noncovalent Association Complexes: Learning from Cathepsin K as a Test Case J Chem Inf Model (2023) 63, 3186-3197. PubMed Europe PubMed DOI
Fabrik,I., Bilkei-Gorzo,O., Oberg,M., Fabrikova,D., Fuchs,J., Sihlbom,C., Goransson,M. and Hartlova,A. Lung macrophages utilize unique cathepsin K-dependent phagosomal machinery to degrade intracellular collagen Life Sci Alliance (2023) 6 PubMed Europe PubMed DOI PMC EPMC
Houchen,C.J., Castro,B., Hahn Leat,P., Mohammad,N., Hall-Glenn,F. and Bumann,E.E. Treatment with an inhibitor of matrix metalloproteinase 9 or cathepsin K lengthens embryonic lower jaw bone Orthod Craniofac Res (2023) PubMed Europe PubMed DOI
Kawai,R., Sugisaki,R., Miyamoto,Y., Yano,F., Sasa,K., Minami,E., Maki,K. and Kamijo,R. Cathepsin K degrades osteoprotegerin to promote osteoclastogenesis in vitro In Vitro Cell Dev Biol Anim (2023) 59, 10-18. PubMed Europe PubMed DOI
Khoshdel,A., Forootan,M., Afsharinasab,M., Rezaian,M. and Abbasifard,M. Assessment of the circulatory concentrations of cathepsin D, cathepsin K, and alpha-1 antitrypsin in patients with knee osteoarthritis Ir J Med Sci (2023) 192, 1191-1196. PubMed Europe PubMed DOI
Seo,S.U., Woo,S.M. and Kwon,T.K. Cathepsin K inhibition induces Raptor destabilization and mitochondrial dysfunction via Syk/SHP2/Src/OTUB1 axis-mediated signaling Cell Death Dis (2023) 14, 366-366. PubMed Europe PubMed DOI PMC EPMC K
Song,Z., Miao,J., Miao,M., Cheng,B., Li,S., Liu,Y., Miao,Q., Li,Q. and Gao,M. Cathepsin K-Activated Probe for Fluoro-Photoacoustic Imaging of Early Osteolytic Metastasis Adv Sci (Weinh) (2023) 10, e2300217-e2300217. PubMed Europe PubMed DOI PMC EPMC
Tusar,L., Loboda,J., Impens,F., Sosnowski,P., Van Quickelberghe,E., Vidmar,R., Demol,H., Sedeyn,K., Saelens,X., Vizovisek,M., Mihelic,M., Fonovic,M., Horvat,J., Kosec,G., Turk,B., Gevaert,K. and Turk,D. Proteomic data and structure analysis combined reveal interplay of structural rigidity and flexibility on selectivity of cysteine cathepsins Commun Biol (2023) 6, 450-450. PubMed Europe PubMed DOI PMC EPMC
Venugopalan,V., Rehders,M., Weber,J., Rodermund,L., Al-Hashimi,A., Bargmann,T., Golchert,J., Reinecke,V., Homuth,G., Volker,U., Verrey,F., Kirstein,J., Heuer,H., Schweizer,U., Braun,D., Wirth,E.K. and Brix,K. Lack of L-type amino acid transporter 2 in murine thyroid tissue induces autophagy J Mol Endocrinol (2023) 70 PubMed Europe PubMed DOI

2022

Gai,D., Chen,J.R., Stewart,J.P., Nookaew,I., Habelhah,H., Ashby,C., Sun,F., Cheng,Y., Li,C., Xu,H., Peng,B., Garg,T.K., Schinke,C., Thanendrarajan,S., Zangari,M., Chen,F., Barlogie,B., van Rhee,F., Tricot,G., Shaughnessy,J.D., Jr. and Zhan,F. CST6 suppresses osteolytic bone disease in multiple myeloma by blocking osteoclast differentiation J Clin Invest (2022) 132 PubMed Europe PubMed DOI PMC EPMC
Kondo,S., Tohgasaki,T., Shiga,S., Nishizawa,S., Ishiwatari,S., Ishikawa,S., Takeda,A. and Sakurai,T. Elastin microfibril interface-located protein 1 and its catabolic enzyme, cathepsin K, regulate the age-related structure of elastic fibers in the skin J Cosmet Dermatol (2022) 21, 4796-4804. PubMed Europe PubMed DOI
Meng,X., Huang,Z., Inoue,A., Wang,H., Wan,Y., Yue,X., Xu,S., Jin,X., Shi,G.P., Kuzuya,M. and Cheng,X.W. Cathepsin K activity controls cachexia-induced muscle atrophy via the modulation of IRS1 ubiquitination J Cachexia Sarcopenia Muscle (2022) 13, 1197-1209. PubMed Europe PubMed DOI
Mijanovic,O., Jakovleva,A., Brankovic,A., Zdravkova,K., Pualic,M., Belozerskaya,T.A., Nikitkina,A.I., Parodi,A. and Zamyatnin,A.A., Jr. Cathepsin K in Pathological Conditions and New Therapeutic and Diagnostic Perspectives Int J Mol Sci (2022) 23 PubMed Europe PubMed DOI PMC EPMC V
Min,H.K., Kim,S.H., Lee,J.Y., Lee,S.H. and Kim,H.R. DJ-1 controls T cell differentiation and osteoclastogenesis in rheumatoid arthritis Sci Rep (2022) 12, 12767-12767. PubMed Europe PubMed DOI PMC EPMC
Novinec,M., Bembic,P., Jankovic,M., Kisilak,M., Kljun,J. and Turel,I. Kinetic Characterization of Cerium and Gallium Ions as Inhibitors of Cysteine Cathepsins L, K, and S Int J Mol Sci (2022) 23 PubMed Europe PubMed DOI PMC EPMC
Qian,D., He,L., Zhang,Q., Li,W., Tang,D., Wu,C., Yang,F., Li,K. and Zhang,H. Cathepsin K: A Versatile Potential Biomarker and Therapeutic Target for Various Cancers Curr Oncol (2022) 29, 5963-5987. PubMed Europe PubMed DOI PMC EPMC V
Rocho,F.R., Bonatto,V., Lameiro,R.F., Lameira,J., Leitao,A. and Montanari,C.A. A patent review on cathepsin K inhibitors to treat osteoporosis (2011 - 2021) Expert Opin Ther Pat (2022) , 1-13. PubMed Europe PubMed DOI I
Seo,S.U., Woo,S.M., Lee,S.G., Kim,M.Y., Lee,H.S., Choi,Y.H., Kim,S.H., Chang,Y.C., Min,K.J. and Kwon,T.K. BAP1 phosphorylation-mediated Sp1 stabilization plays a critical role in cathepsin K inhibition-induced C-terminal p53-dependent Bax upregulation Redox Biol (2022) 53, 102336-102336. PubMed Europe PubMed DOI PMC EPMC K
Vesela,B., Killinger,M., Rihova,K., Benes,P., Svandova,E., Kratochvilova,A., Trcka,F., Kleparnik,K. and Matalova,E. Caspase-8 Deficient Osteoblastic Cells Display Alterations in Non-Apoptotic Pathways Front Cell Dev Biol (2022) 10, 794407-794407. PubMed Europe PubMed DOI PMC EPMC
Yue,X., Piao,L., Wang,H., Huang,Z., Meng,X., Sasaki,T., Inoue,A., Nakamura,K., Wan,Y., Xu,S., Shi,G.P., Kim,W., Murohara,T., Kuzuya,M. and Cheng,X.W. Cathepsin K Deficiency Prevented Kidney Damage and Dysfunction in Response to 5/6 Nephrectomy Injury in Mice With or Without Chronic Stress Hypertension (2022) 79, 1713-1723. PubMed Europe PubMed DOI PMC EPMC
Zhu,G., Chen,W., Tang,C.Y., McVicar,A., Edwards,D., Wang,J., McConnell,M., Yang,S., Li,Y., Chang,Z. and Li,Y.P. Knockout and Double Knockout of Cathepsin K and Mmp9 reveals a novel function of Cathepsin K as a regulator of osteoclast gene expression and bone homeostasis Int J Biol Sci (2022) 18, 5522-5538. PubMed Europe PubMed DOI PMC EPMC
Zou,N., Liu,R. and Li,C. Cathepsin K(+) Non-Osteoclast Cells in the Skeletal System: Function, Models, Identity, and Therapeutic Implications Front Cell Dev Biol (2022) 10, 818462-818462. PubMed Europe PubMed DOI PMC EPMC V

2021

Bollavaram,K., Leeman,T.H., Lee,M.W., Kulkarni,A., Upshaw,S.G., Yang,J., Song,H. and Platt,M.O. Multiple sites on SARS-CoV-2 spike protein are susceptible to proteolysis by cathepsins B, K, L, S, and V Protein Sci (2021) PubMed Europe PubMed DOI
Bourgi,R., Daood,U., Bijle,M.N., Fawzy,A., Ghaleb,M. and Hardan,L. Reinforced Universal Adhesive by Ribose Crosslinker: A Novel Strategy in Adhesive Dentistry Polymers (Basel) (2021) 13 PubMed Europe PubMed DOI PMC EPMC
Calio,A., Brunelli,M., Gobbo,S., Argani,P., Munari,E., Netto,G. and Martignoni,G. Cathepsin K: A Novel Diagnostic and Predictive Biomarker for Renal Tumors Cancers (Basel) (2021) 13 PubMed Europe PubMed DOI PMC EPMC V
Gontijo,T.B., Lima,P.S., Icimoto,M.Y., Neves,R.L., de Alvarenga,E.C., Carmona,A.K., de Castro,A.A., Ramalho,T.C., da Silva Junior,E.N. and de Freitas,R.P. Cathepsin K inhibitors based on 2-amino-1,3,4-oxadiazole derivatives Bioorg Chem (2021) 109, 104662-104662. PubMed Europe PubMed DOI I
Gorican,T., Ciber,L., Petek,N., Svete,J. and Novinec,M. Synthesis and kinetic characterization of hyperbolic inhibitors of human cathepsins K and S based on a succinimide scaffold Bioorg Chem (2021) 115, 105213-105213. PubMed Europe PubMed DOI
Hausinger,R., Hackl,M., Jardon Alvarez,A., Kehr,M., Romero Marquez,S., Hettler,F., Kehr,C., Grziwok,S., Schreck,C., Peschel,C., Istvanffy,R. and Oostendorp,R.A.J. Cathepsin K maintains the compartment of bone marrow T lymphocytes in vivo Immun Inflamm Dis (2021) PubMed Europe PubMed DOI
Heo,S.C., Kim,Y.N., Choi,Y., Joo,J.Y., Hwang,J.J., Bae,M.K. and Kim,H.J. Elevated Expression of Cathepsin K in Periodontal Ligament Fibroblast by Inflammatory Cytokines Accelerates Osteoclastogenesis via Paracrine Mechanism in Periodontal Disease Int J Mol Sci (2021) 22 PubMed Europe PubMed DOI PMC EPMC
Nakamura,M., Aoyama,N., Yamaguchi,S. and Sasano,Y. Expression of tartrate-resistant acid phosphatase and cathepsin K during osteoclast differentiation in developing mouse mandibles Biomed Res (2021) 42, 13-21. PubMed Europe PubMed DOI
Pomeislova,A., Otmar,M., Rubesova,P., Benysek,J., Matousova,M., Mertlikova-Kaiserova,H., Pohl,R., Postova Slavetinska,L., Pomeisl,K. and Krecmerova,M. 1,2,4-Thiadiazole acyclic nucleoside phosphonates as inhibitors of cysteine dependent enzymes cathepsin K and GSK-3beta Bioorg Med Chem (2021) 32, 115998-115998. PubMed Europe PubMed DOI I
Soundararajan,A., Ghag,S.A., Vuda,S.S., Wang,T. and Pattabiraman,P.P. Cathepsin K Regulates Intraocular Pressure by Modulating Extracellular Matrix Remodeling and Actin-Bundling in the Trabecular Meshwork Outflow Pathway Cells (2021) 10 PubMed Europe PubMed DOI PMC EPMC I
Tsegaye,S., Mehdi,M., Labisso,W.L. and Melka,D.S. Cysteine Cathepsins and Matrix Metalloproteases Among Breast Cancer Patients Breast Cancer (Dove Med Press) (2021) 13, 271-283. PubMed Europe PubMed DOI PMC EPMC L
Vashum,Y., Premsingh,R., Kottaiswamy,A., Soma,M., Padmanaban,A., Kalaiselvan,P. and Samuel,S. Inhibitory effect of cathepsin K inhibitor (ODN-MK-0822) on invasion, migration and adhesion of human breast cancer cells in vitro Mol Biol Rep (2021) 48, 105-116. PubMed Europe PubMed DOI I
Vashum,Y., Kottaiswamy,A., Bupesh,G., Singh,R.P., Kalaiselvan,P., Thiagarajan,K. and Samuel,S. Inhibitory Effects of Cathepsin K Inhibitor (ODN-MK-0822) on the Paracrine Pro-Osteoclast Factors of Breast Cancer Cells Curr Mol Pharmacol (2021) PubMed Europe PubMed DOI I
Venugopalan,V., Al-Hashimi,A., Weber,J., Rehders,M., Qatato,M., Wirth,E.K., Schweizer,U., Heuer,H., Verrey,F. and Brix,K. The Amino Acid Transporter Mct10/Tat1 Is Important to Maintain the TSH Receptor at Its Canonical Basolateral Localization and Assures Regular Turnover of Thyroid Follicle Cells in Male Mice Int J Mol Sci (2021) 22 PubMed Europe PubMed DOI PMC EPMC

2020

Bennacef,I., Rubins,D., Riffel,K., Williams,M., Posavec,D.J., Holahan,M.A., Purcell,M.L., Haley,H.D., Wolf,M., Stachel,S.J., Lubbers,L.S., Wesolowski,G.A., Duong,L.T., Hamill,T.G., Evelhoch,J.L. and Hostetler,E.D. Preclinical evaluation of [(11) C]L-235 as a radioligand for Positron Emission Tomography cathepsin K imaging in bone J Labelled Comp Radiopharm (2020) PubMed Europe PubMed DOI I
Bolignano,D., Greco,M., Arcidiacono,V., Tripolino,O., Vita,C., Provenzano,M., Donato,C., Chiarella,S., Fuiano,G., De Sarro,G., Russo,E., Andreucci,M., Foti,D.P. and Coppolino,G. Increased circulating Cathepsin-K levels reflect PTH control in chronic hemodialysis patients J Nephrol (2020) PubMed Europe PubMed DOI
Bolignano,D., Greco,M., Arcidiacono,V., Tripolino,O., Vita,C., Provenzano,M., Donato,C., Chiarella,S., Fuiano,G., De Sarro,G., Russo,E., Andreucci,M., Foti,D.P. and Coppolino,G. Cathepsin-K is a potential cardiovascular risk biomarker in prevalent hemodialysis patients Int Urol Nephrol (2020) PubMed Europe PubMed DOI
Borggaard,X.G., Pirapaharan,D.C., Delaisse,J.M. and Soe,K. Osteoclasts' Ability to Generate Trenches Rather Than Pits Depends on High Levels of Active Cathepsin K and Efficient Clearance of Resorption Products Int J Mol Sci (2020) 21 PubMed Europe PubMed DOI PMC EPMC
Cianni,L., Rocho,F.D.R., Rosini,F., Bonatto,V., Ribeiro,J.F.R., Lameira,J., Leitao,A., Shamim,A. and Montanari,C.A. Optimization strategy of single-digit nanomolar cross-class inhibitors of mammalian and protozoa cysteine proteases Bioorg Chem (2020) 101, 104039-104039. PubMed Europe PubMed DOI I
Conaghan,P.G., Bowes,M.A., Kingsbury,S.R., Brett,A., Guillard,G., Rizoska,B., Sjogren,N., Graham,P., Jansson,A., Wadell,C., Bethell,R. and Ohd,J. Disease-modifying effects of a novel cathepsin K inhibitor in osteoarthritis: a randomized, placebo-controlled study Ann Intern Med (2020) 172, 86-95. PubMed Europe PubMed DOI I
Diaz-Espinosa,A.M., Link,P.A., Sicard,D., Jorba,I., Tschumperlin,D.J. and Haak,A.J. Dopamine D1 receptor stimulates cathepsin K-dependent degradation and resorption of collagen I in lung fibroblasts J Cell Sci (2020) PubMed Europe PubMed DOI
Feng,H., Xing,W., Han,Y., Sun,J., Kong,M., Gao,B., Yang,Y., Yin,Z., Chen,X., Zhao,Y., Bi,Q. and Zou,W. Tendon-derived cathepsin K-expressing progenitor cells activate Hedgehog signaling to drive heterotopic ossification J Clin Invest (2020) PubMed Europe PubMed DOI
He,S.W., Du,X., Wang,G.H., Wang,J.J., Xie,B., Gu,Q.Q., Zhang,M. and Gu,H.J. Identification and characterization of a cathepsin K homologue that interacts with pathogen bacteria in black rockfish, Sebastes schlegelii Fish Shellfish Immunol (2020) 98, 499-507. PubMed Europe PubMed DOI
Jastaniah,A., Gaisina,I.N., Knopp,R.C. and Thatcher,G.R.J. Synthesis of alpha-Ketoamide-Based Stereoselective Calpain-1 Inhibitors as Neuroprotective Agents ChemMedChem (2020) PubMed Europe PubMed DOI I
Kensara,A., Hefni,E., Williams,M.A., Saito,H., Mongodin,E. and Masri,R. Microbiological Profile and Human Immune Response Associated with Peri-Implantitis: A Systematic Review J Prosthodont (2020) PubMed Europe PubMed DOI V
Lecaille,F., Chazeirat,T., Bojarski,K.K., Renault,J., Saidi,A., Prasad,V.G.N.V., Samsonov,S. and Lalmanach,G. Rat cathepsin K: enzymatic specificity and regulation of its collagenolytic activity Biochim Biophys Acta Proteins Proteom (2020) 1868, 140318-140318. PubMed Europe PubMed DOI
Meng,X., Piao,L., Wang,H., Inoue,A., Huang,Z., Jiang,H., Nakamura,K., Sasaki,T., Li,X., Xu,W., Yu,C., Hu,L., Wu,H., Murohara,T., Shi,G.P., Kuzuya,M. and Cheng,X.W. Deficiency of cysteinyl cathepsin K suppresses the development of experimental intimal hyperplasia in response to chronic stress J Hypertens (2020) PubMed Europe PubMed DOI
Oso,B.J., Adeoye,A.O. and Olaoye,I.F. Pharmacoinformatics and hypothetical studies on allicin, curcumin, and gingerol as potential candidates against COVID-19-associated proteases J Biomol Struct Dyn (2020) , 1-12. PubMed Europe PubMed DOI I
Pritsch,I.C., Tikhonova,I.G., Jewhurst,H.L., Drysdale,O., Cwiklinski,K., Molento,M.B., Dalton,J.P. and Verissimo,C.M. Regulation of the Fasciola hepatica newly excysted juvenile cathepsin L3 (FhCL3) by its propeptide: a proposed 'clamp-like' mechanism of binding and inhibition BMC Mol Cell Biol (2020) 21, 90-90. PubMed Europe PubMed DOI PMC EPMC
Reithmeier,A., Norgard,M., Ek-Rylander,B., Nareoja,T. and Andersson,G. Cathepsin K regulates localization and secretion of tartrate-resistant acid phosphatase (TRAP) in TRAP-overexpressing MDA-MB-231 breast cancer cells BMC Mol Cell Biol (2020) 21, 15-15. PubMed Europe PubMed DOI PMC EPMC I
Rocha,G.V., Bastos,L.S. and Costa,M.G.S. Identification of Potential Allosteric Binding Sites in Cathepsin K Based on Intramolecular Communication Proteins (2020) PubMed Europe PubMed DOI
Seo,S.U., Woo,S.M., Kim,M.W., Lee,H.S., Kim,S.H., Kang,S.C., Lee,E.W., Min,K.J. and Kwon,T.K. Cathepsin K inhibition-induced mitochondrial ROS enhances sensitivity of cancer cells to anti-cancer drugs through USP27x-mediated Bim protein stabilization Redox Biol (2020) 30, 101422-101422. PubMed Europe PubMed DOI PMC EPMC I
Silva,T.L., Dos Santos,D.A., de Jesus,H.C.R., Bromme,D., Fernandes,J.B., Paixao,M.W., Correa,A.G. and Vieira,P.C. Green asymmetric synthesis of epoxypeptidomimetics and evaluation as human cathepsin K inhibitors Bioorg Med Chem (2020) 28, 115597-115597. PubMed Europe PubMed DOI I
Smith,D., Cwiklinski,K., Jewhurst,H., Tikhonova,I.G. and Dalton,J.P. An atypical and functionally diverse family of Kunitz-type cysteine/serine proteinase inhibitors secreted by the helminth parasite Fasciola hepatica Sci Rep (2020) 10, 20657-20657. PubMed Europe PubMed DOI PMC EPMC
Yue,X., Jiang,H., Xu,Y., Xia,M. and Cheng,X.W. Cathepsin K Deficiency Impaired Ischemia-Induced Neovascularization in Aged Mice Stem Cells Int (2020) 2020, 6938620-6938620. PubMed Europe PubMed DOI PMC EPMC K
Zajic,S., Stoch,S.A., McCrea,J.B., Witter,R., Fayad,G.N., Martinho,M. and Stone,J.A. A phase 1 pooled PK/PD analysis of bone resorption biomarkers for odanacatib, a Cathepsin K inhibitor J Pharmacokinet Pharmacodyn (2020) 47, 473-484. PubMed Europe PubMed DOI I

2019

Bafail,A., Azizalrahman,M., Vilde,T., Kishen,A. and Prakki,A. Alternative model for cathepsin K activation in human dentin Dent Mater (2019) 35, 1630-1636. PubMed Europe PubMed DOI
Law,S., Du,X., Panwar,P., Honson,N.S., Pfeifer,T., Roberge,M. and Bromme,D. Identification of substrate-specific inhibitors of cathepsin K through high-throughput screening Biochem J (2019) 476, 499-512. PubMed Europe PubMed DOI I
Lotinun,S., Ishihara,Y., Nagano,K., Kiviranta,R., Carpentier,V.T., Neff,L., Parkman,V., Ide,N., Hu,D., Dann,P., Brooks,D., Bouxsein,M.L., Wysolmerski,J., Gori,F. and Baron,R. Cathepsin K-deficient osteocytes prevent lactation-induced bone loss and parathyroid hormone suppression J Clin Invest (2019) 129, 3058-3071. PubMed Europe PubMed DOI K
Ma,B., Wesolowski,G., Luo,B., Lifsted,T., Wessner,K., Adamson,G., Glantschnig,H. and Lubbers,L.S. Suppression of cathepsin K biomarker in synovial fluid as a free-drug-driven process J Circ Biomark (2019) 8, 1849454418821819-1849454418821819. PubMed Europe PubMed DOI PMC EPMC I
Mons,E., Jansen,I.D.C., Loboda,J., van Doodewaerd,B.R., Hermans,J., Verdoes,M., van Boeckel,C.A.A., van Veelen,P.A., Turk,B., Turk,D. and Ovaa,H. The alkyne moiety as a latent electrophile in irreversible covalent small molecule inhibitors of cathepsin K J Am Chem Soc (2019) 141, 3507-3514. PubMed Europe PubMed DOI I
Parks,A.N., Nahata,J., Edouard,N.E., Temenoff,J.S. and Platt,M.O. Sequential, but not concurrent, incubation of cathepsin K and L with type I collagen results in extended proteolysis Sci Rep (2019) 9, 5399-5399. PubMed Europe PubMed DOI PMC EPMC
Petek,N., Stefane,B., Novinec,M. and Svete,J. Synthesis and biological evaluation of 7-(aminoalkyl)pyrazolo[1,5-a]pyrimidine derivatives as cathepsin K inhibitors Bioorg Chem (2019) 84, 226-238. PubMed Europe PubMed DOI I
Pirapaharan,D.C., Soe,K., Panwar,P., Madsen,J.S., Bergmann,M.L., Overgaard,M., Bromme,D. and Delaisse,J.M. A mild inhibition of cathepsin K paradoxically stimulates the resorptive activity of osteoclasts in culture Calcif Tissue Int (2019) 104, 92-101. PubMed Europe PubMed DOI I
Ricci,C., De Leo,A., Dika,E., Lambertini,M., Veronesi,G. and Corti,B. Could cathepsin-k be a driver of the myofibroblastic differentiation observed in dermatofibroma, atypical fibroxanthoma and pleomorphic dermal sarcoma? Acta Histochem (2019) , 151498-151498. PubMed Europe PubMed DOI
Tian,M., Cao,M., Zhang,L., Fu,Q., Yang,N., Tan,F., Song,L., Su,B. and Li,C. Characterization and initial functional analysis of cathepsin K in turbot (Scophthalmus maximus L.) Fish Shellfish Immunol (2019) 93, 153-160. PubMed Europe PubMed DOI
Visetvichaporn,V., Kim,K.H., Jung,K., Cho,Y.S. and Kim,D.D. Formulation of self-microemulsifying drug delivery system (SMEDDS) by D-optimal mixture design to enhance the oral bioavailability of a new cathepsin K inhibitor (HL235) Int J Pharm (2019) , 118772-118772. PubMed Europe PubMed DOI I
Yuan,X.Y., Ren,Z., Wu,Y., Bougault,C., Brizuela,L., Magne,D., Buchet,R. and Mebarek,S. Design, synthesis and biological evaluation of inhibitors of cathepsin K on dedifferentiated chondrocytes Bioorg Med Chem (2019) 27, 1034-1042. PubMed Europe PubMed DOI I

2018

Colon-Bernal,I.D., Duong,L.T., Pennypacker,B., Henderson,J., Kozloff,K.M. and Banaszak Holl,M.M. Cathepsin K inhibition preserves compressive load in lumbar vertebrae of osteoporotic monkeys Bone Rep (2018) 9, 159-164. PubMed Europe PubMed DOI PMC EPMC I
Douglas,S.A., Lamothe,S.E., Singleton,T.S., Averett,R.D. and Platt,M.O. Human cathepsins K, L, and S: related proteases, but unique fibrinolytic activity Biochim Biophys Acta (2018) 1862, 1925-1932. PubMed Europe PubMed DOI
Guo,R., Hua,Y., Ren,J., Bornfeldt,K.E. and Nair,S. Cardiomyocyte-specific disruption of cathepsin K protects against doxorubicin-induced cardiotoxicity Cell Death Dis (2018) 9, 692-692. PubMed Europe PubMed DOI PMC EPMC K
Lindstrom,E., Rizoska,B., Tunblad,K., Edenius,C., Bendele,A.M., Maul,D., Larson,M., Shah,N., Yoder Otto,V., Jerome,C. and Grabowska,U. The selective cathepsin K inhibitor MIV-711 attenuates joint pathology in experimental animal models of osteoarthritis J Transl Med (2018) 16, 56-56. PubMed Europe PubMed DOI PMC EPMC I
Lu,J., Wang,M., Wang,Z., Fu,Z., Lu,A. and Zhang,G. Advances in the discovery of cathepsin K inhibitors on bone resorption J Enzyme Inhib Med Chem (2018) 33, 890-904. PubMed Europe PubMed DOI V I
Ogasawara,S., Cheng,X.W., Inoue,A., Hu,L., Piao,L., Yu,C., Goto,H., Xu,W., Zhao,G., Lei,Y., Yang,G., Kimura,K., Umegaki,H., Shi,G.P. and Kuzuya,M. Cathepsin K activity controls cardiotoxin-induced skeletal muscle repair in mice J Cachexia Sarcopenia Muscle (2018) 9, 160-175. PubMed Europe PubMed DOI K
Roy,S., Das Chakraborty,S. and Biswas,S. Not all pycnodysostosis-related mutants of human cathepsin K are inactive - crystal structure and biochemical studies of an active mutant I249T FEBS J (2018) 285, 4265-4280. PubMed Europe PubMed DOI M S
Walia,B., Lingenheld,E., Duong,L., Sanjay,A. and Drissi,H. A novel role for cathepsin K in periosteal osteoclast precursors during fracture repair Ann N Y Acad Sci (2018) 1415, 57-68. PubMed Europe PubMed DOI K
Whitty,C., Wardale,R.J. and Henson,F.M.D. The regulation of sclerostin by cathepsin K in periodontal ligament cells Biochem Biophys Res Commun (2018) 503, 550-555. PubMed Europe PubMed DOI

2017

Bonnet,N., Brun,J., Rousseau,J.C., Duong,L.T. and Ferrari,S.L. Cathepsin K controls cortical bone formation by degrading periostin J Bone Miner Res (2017) 32, 1432-1441. PubMed Europe PubMed DOI
Drake,M.T., Clarke,B.L., Oursler,M.J. and Khosla,S. Cathepsin K inhibitors for osteoporosis: biology, potential clinical utility, and lessons learned Endocr Rev (2017) 38, 325-350. PubMed Europe PubMed DOI I
Galibert,M., Wartenberg,M., Lecaille,F., Saidi,A., Mavel,S., Joulin-Giet,A., Korkmaz,B., Bromme,D., Aucagne,V., Delmas,A.F. and Lalmanach,G. Substrate-derived triazolo- and azapeptides as inhibitors of cathepsins K and S Eur J Med Chem (2017) 144, 201-210. PubMed Europe PubMed DOI I
Garnero,P., Bonnet,N. and Ferrari,S.L. Development of a new immunoassay for human cathepsin K-generated periostin fragments as a serum biomarker for cortical bone Calcif Tissue Int (2017) 101, 501-509. PubMed Europe PubMed DOI
Guo,R., Hua,Y., Rogers,O., Brown,T.E., Ren,J. and Nair,S. Cathepsin K knockout protects against cardiac dysfunction in diabetic mice Sci Rep (2017) 7, 8703-8703. PubMed Europe PubMed DOI PMC EPMC K
Hira,V.V., Verbovsek,U., Breznik,B., Srdic,M., Novinec,M., Kakar,H., Wormer,J., der Swaan,B.V., Lenarcic,B., Juliano,L., Mehta,S., Van Noorden,C.J. and Lah,T.T. Cathepsin K cleavage of SDF-1alpha inhibits its chemotactic activity towards glioblastoma stem-like cells Biochim Biophys Acta (2017) 1864, 594-603. PubMed Europe PubMed DOI P
Jennewine,B., Fox,J. and Ramamurthi,A. Cathepsin K-targeted sub-micron particles for regenerative repair of vascular elastic matrix Acta Biomater (2017) 52, 60-73. PubMed Europe PubMed DOI
Kruglyak,N., Williams,D.E., Chen,H., Law,S., Kaleta,J., Villanueva,I., Davies,J.E., Andersen,R.J. and Bromme,D. Leupeptazin, a highly modified tripeptide isolated from cultures of a Streptomyces sp. inhibits cathepsin K Bioorg Med Chem Lett (2017) 27, 1397-1400. PubMed Europe PubMed DOI I
Law,S., Andrault,P.M., Aguda,A.H., Nguyen,N.T., Kruglyak,N., Brayer,G.D. and Bromme,D. Identification of mouse cathepsin K structural elements that regulate the potency of odanacatib Biochem J (2017) 474, 851-864. PubMed Europe PubMed DOI S I
Law,S., Panwar,P., Li,J., Aguda,A.H., Jamroz,A., Guido,R.V.C. and Bromme,D. A composite docking approach for the identification and characterization of ectosteric inhibitors of cathepsin K PLoS ONE (2017) 12, e0186869-e0186869. PubMed Europe PubMed DOI PMC EPMC I
Ma,B., Luo,B., Euler,D.H., Cusick,T.E., Wesolowski,G., Glantschnig,H., Duong,L.T., Ou,Y., Carroll,S.S. and Lubbers,L.S. Applicability of in vitro-in vivo translation of cathepsin K inhibition from animal species to human with the use of free-drug hypothesis Naunyn Schmiedebergs Arch Pharmacol (2017) 390, 435-441. PubMed Europe PubMed DOI I
Munari,E., Cima,L., Massari,F., Bertoldo,F., Porcaro,A.B., Calio,A., Riva,G., Ciocchetta,E., Ciccarese,C., Modena,A., Iacovelli,R., Sava,T., Eccher,A., Ghimenton,C., Tortora,G., Artibani,W., Novella,G., Bogina,G., Zamboni,G., Sanguedolce,F., D'Amuri,A., Martignoni,G. and Brunelli,M. Cathepsin K expression in castration-resistant prostate carcinoma: a therapeutical target for patients at risk for bone metastases Int J Biol Markers (2017) 32, e243-e247. PubMed Europe PubMed DOI T
Noe,B., Poole,A.R., Mort,J.S., Richard,H., Beauchamp,G. and Laverty,S. C2K77 ELISA detects cleavage of type II collagen by cathepsin K in equine articular cartilage Osteoarthritis Cartilage (2017) 25, 2119-2126. PubMed Europe PubMed DOI
Novinec,M. Computational investigation of conformational variability and allostery in cathepsin K and other related peptidases PLoS ONE (2017) 12, e0182387-e0182387. PubMed Europe PubMed DOI PMC EPMC
Panwar,P., Xue,L., Soe,K., Srivastava,K., Law,S., Delaisse,J.M. and Bromme,D. An ectosteric inhibitor of cathepsin K inhibits bone resorption in ovariectomized mice J Bone Miner Res (2017) 32, 2415-2430. PubMed Europe PubMed DOI I
Song,H.K., Sohn,Y.B., Choi,Y.J., Chung,Y.S. and Jang,J.H. A case report of pycnodysostosis with atypical femur fracture diagnosed by next-generation sequencing of candidate genes Medicine (Baltimore) (2017) 96, e6367-e6367. PubMed Europe PubMed DOI M
Tatara,Y., Suto,S. and Itoh,K. Novel roles of glycosaminoglycans in the degradation of type I collagen by cathepsin K Glycobiology (2017) 27, 1089-1098. PubMed Europe PubMed DOI
Yamashita,K., Iwatake,M., Okamoto,K., Yamada,S.I., Umeda,M. and Tsukuba,T. Cathepsin K modulates invasion, migration, and adhesion of oral squamous cell carcinomas in vitro Oral Dis (2017) 23, 518-525. PubMed Europe PubMed DOI I
Zhou,Y., Chen,H., Liu,L., Yu,X., Sukhova,G.K., Yang,M., Kyttaris,V.C., Stillman,I.E., Gelb,B., Libby,P., Tsokos,G.C. and Shi,G.P. Cathepsin K deficiency ameliorates systemic lupus erythematosus-like manifestations in Fas(lpr) mice J Immunol (2017) 198, 1846-1854. PubMed Europe PubMed DOI K

2016

Andrade,S.S., Gouvea,I.E., Silva,M.C., Castro,E.D., de Paula,C.A., Okamoto,D., Oliveira,L., Peres,G.B., Ottaiano,T., Facina,G., Nazario,A.C., Campos,A.H., Paredes-Gamero,E.J., Juliano,M., da Silva,I.D., Oliva,M.L. and Girao,M.J. Cathepsin K induces platelet dysfunction and affects cell signaling in breast cancer - molecularly distinct behavior of cathepsin K in breast cancer BMC Cancer (2016) 16, 173-173. PubMed Europe PubMed DOI PMC EPMC
Bromme,D., Panwar,P. and Turan,S. Cathepsin K osteoporosis trials, pycnodysostosis and mouse deficiency models: commonalities and differences Expert Opin Drug Discov (2016) 11, 457-472. PubMed Europe PubMed DOI I
Chen,W., Gao,B., Hao,L., Zhu,G., Jules,J., MacDougall,M.J., Wang,J., Han,X., Zhou,X. and Li,Y.P. The silencing of cathepsin K used in gene therapy for periodontal disease reveals the role of cathepsin K in chronic infection and inflammation J Periodontal Res (2016) 51, 647-660. PubMed Europe PubMed DOI K T
Duong,l.T., Leung,A.T. and Langdahl,B. Cathepsin K inhibition: a new mechanism for the treatment of osteoporosis Calcif Tissue Int (2016) 98, 381-397. PubMed Europe PubMed DOI I
Herroon,M.K., Sharma,R., Rajagurubandara,E., Turro,C., Kodanko,J.J. and Podgorski,I. Photoactivated inhibition of cathepsin K in a 3D tumor model Biol Chem (2016) 397, 571-582. PubMed Europe PubMed DOI I
Ihmaid,S.K., Ahmed,H.E., Zayed,M.F. and Abadleh,M.M. Self organizing map-based classification of cathepsin K and S inhibitors with different selectivity profiles using different structural molecular fingerprints: design and application for discovery of novel hits Molecules (2016) 21, 175-175. PubMed Europe PubMed DOI I
Izumi,Y., Hayashi,M., Morimoto,R., Cheng,X.W., Wu,H., Ishii,H., Yasuda,Y., Yoshikawa,D., Izawa,H., Matsuo,S., Oiso,Y. and Murohara,T. Impact of circulating cathepsin K on the coronary calcification and the clinical outcome in chronic kidney disease patients Heart Vessels (2016) 31, 6-14. PubMed Europe PubMed DOI
Jiang,Y.-T., Ma,Z.-G., Jiao,J.-B., Guo,Z., Qian,L.-G., Chen,T.-P., Li,Q.-G., Wang,Y.-F. and Xue,J.-W. Cathepsin K inhibitor, icariin, increases the healing potential and biomechanical properties of femoral neck in a mice fractured model Int J Clin Exp Med (2016) 9, 15788-15795. I
Mort,J.S., Beaudry,F., Theroux,K., Emmott,A.A., Richard,H., Fisher,W.D., Lee,E.R., Poole,A.R. and Laverty,S. Early cathepsin K degradation of type II collagen in vitro and in vivo in articular cartilage Osteoarthritis Cartilage (2016) 24, 1461-1469. PubMed Europe PubMed DOI
Mukherjee,K. and Chattopadhyay,N. Pharmacological inhibition of cathepsin K: a promising novel approach for postmenopausal osteoporosis therapy Biochem Pharmacol (2016) 117, 10-19. PubMed Europe PubMed DOI I
Nishiyama,K. Decision tree for the binding of dipeptides to the thermally fluctuating surface of cathepsin K Chem Phys Lett (2016) 647, 42-45. DOI
Novinec,M., Rebernik,M. and Lenarcic,B. An allosteric site enables fine-tuning of cathepsin K by diverse effectors FEBS Lett (2016) 590, 4507-4518. PubMed Europe PubMed DOI
Ochi,Y., Yamada,H., Mori,H., Kawada,N., Tanaka,M., Imagawa,A., Ohmoto,K. and Kawabata,K. Combination therapy with ONO-KK1-300-01, a cathepsin K inhibitor, and parathyroid hormone results in additive beneficial effect on bone mineral density in ovariectomized rats J Bone Miner Metab (2016) 34, 33-40. PubMed Europe PubMed DOI I
Panwar,P., Soe,K., Guido,R.V., Bueno,R.V., Delaisse,J.M. and Bromme,D. A novel approach to inhibit bone resorption: exosite inhibitors against cathepsin K Br J Pharmacol (2016) 173, 396-410. PubMed Europe PubMed DOI I
Plebanek,E., Chevrier,F., Roy,V., Garenne,T., Lecaille,F., Warszycki,D., Bojarski,A.J., Lalmanach,G. and Agrofoglio,L.A. Straightforward synthesis of 2,4,6-trisubstituted 1,3,5-triazine compounds targeting cysteine cathepsins K and S Eur J Med Chem (2016) 121, 12-20. PubMed Europe PubMed DOI I
Qiu,Z.C., Dong,X.L., Dai,Y., Xiao,G.K., Wang,X.L., Wong,K.C., Wong,M.S. and Yao,X.S. Discovery of a new class of cathepsin K inhibitors in Rhizoma drynariae as potential candidates for the treatment of osteoporosis Int J Mol Sci (2016) 17 PubMed Europe PubMed DOI I
Tanaka,M., Yamada,H., Nishikawa,S., Mori,H., Ochi,Y., Horai,N., Li,M. and Amizuka,N. Joint degradation in a monkey model of collagen-induced arthritis: role of cathepsin K based on biochemical markers and histological evaluation Int J Rheumatol (2016) 2016, 8938916-8938916. PubMed Europe PubMed DOI PMC EPMC
Wang,Y., Li,R., Zheng,Z., Yi,H. and Li,Z. Identification of novel cathepsin K inhibitors using ligand-based virtual screening and structure-based docking RSC Adv (2016) 6, 82961-82968. DOI I

2015

Abdel-Magid,A.F. Inhibition of cathepsin K: a novel and promising treatment for osteoporosis ACS Med Chem Lett (2015) 6, 628-629. PubMed Europe PubMed DOI PMC EPMC I
Andrault,P.M., Samsonov,S.A., Weber,G., Coquet,L., Nazmi,K., Bolscher,J.G., Lalmanach,A.C., Jouenne,T., Bromme,D., Pisabarro,M.T., Lalmanach,G. and Lecaille,F. Antimicrobial peptide LL-37 is both a substrate of cathepsins S and K and a selective inhibitor of cathepsin L Biochemistry (2015) 54, 2785-2798. PubMed Europe PubMed DOI
Borisek,J., Vizovisek,M., Sosnowski,P., Turk,B., Turk,D., Mohar,B. and Novic,M. Development of N-(functionalized benzoyl)-homocycloleucyl-glycinonitriles as potent cathepsin K inhibitors J Med Chem (2015) 58, 6928-6937. PubMed Europe PubMed DOI I
Christensen,J. and Shastri,V.P. Matrix-metalloproteinase-9 is cleaved and activated by cathepsin K BMC Res Notes (2015) 8, 322-322. PubMed Europe PubMed DOI PMC EPMC
Fujii,T., Ishikawa,M., Kubo,A. and Tanaka,Y. Effect of SI-591, a new class of cathepsin K inhibitor with peptidomimetic structure, on bone metabolism in vitro and in vivo Bone (2015) 81, 427-434. PubMed Europe PubMed DOI I
Gamsjager,M. and Resch,H. [Cathepsin K antagonists: preclinical and clinical data] Wien Med Wochenschr (2015) 165, 65-70. PubMed Europe PubMed DOI I
Gruber,R. Molecular and cellular basis of bone resorption Wien Med Wochenschr (2015) 165, 48-53. PubMed Europe PubMed DOI I
Hao,L., Zhu,G., Lu,Y., Wang,M., Jules,J., Zhou,X. and Chen,W. Deficiency of cathepsin K prevents inflammation and bone erosion in rheumatoid arthritis and periodontitis and reveals its shared osteoimmune role FEBS Lett (2015) 589, 1331-1339. PubMed Europe PubMed DOI K
Hua,Y., Robinson,T.J., Cao,Y., Shi,G.P., Ren,J. and Nair,S. Cathepsin K knockout alleviates aging-induced cardiac dysfunction Aging Cell (2015) 14, 345-351. PubMed Europe PubMed DOI K
Huang,X., Qi,X., Li,M., Wang,O., Jiang,Y., Xing,X., Hu,Y.Y. and Xia,W. A mutation in CTSK gene in an autosomal recessive pycnodysostosis family of Chinese origin Calcif Tissue Int (2015) 96, 373-378. PubMed Europe PubMed DOI M
Knaapi,J., Kiviranta,R., Laine,J., Kaapa,P. and Lukkarinen,H. Cathepsin K overexpression modifies lung development in newborn mice Pediatr Pulmonol (2015) 50, 164-172. PubMed Europe PubMed DOI
Kyostio-Moore,S., Piraino,S., Berthelette,P., Moran,N., Serriello,J., Bendele,A., Sookdeo,C., Nambiar,B., Ewing,P., Armentano,D. and Matthews,G.L. Overexpression of cystatin C in synovium does not reduce synovitis or cartilage degradation in established osteoarthritis Arthritis Res Ther (2015) 17, 5-5. PubMed Europe PubMed DOI
Pietschmann,P. Cathepsin K inhibitors: emerging treatment options for osteoporosis Wien Med Wochenschr (2015) 165, 47-47. PubMed Europe PubMed DOI I
Ren,Z.Y., Machuca-Gayet,I., Domenget,C., Buchet,R., Wu,Y., Jurdic,P. and Mebarek,S. Azanitrile cathepsin K inhibitors: effects on cell toxicity, osteoblast-induced mineralization and osteoclast-mediated bone resorption PLoS ONE (2015) 10, e0132513-e0132513. PubMed Europe PubMed DOI PMC EPMC
Sharma,V., Panwar,P., O'Donoghue,A.J., Cui,H., Guido,R.V., Craik,C.S. and Bromme,D. Structural requirements for the collagenase and elastase activity of cathepsin K and its selective inhibition by an exosite inhibitor Biochem J (2015) 465, 163-173. PubMed Europe PubMed DOI
Suzuki,N., Takimoto,K. and Kawashima,N. Cathepsin K inhibitor regulates inflammation and bone destruction in experimentally induced rat periapical lesions J Endod (2015) 41, 1474-1479. PubMed Europe PubMed DOI I
Verbovsek,U., Van Noorden,C.J. and Lah,T.T. Complexity of cancer protease biology: cathepsin K expression and function in cancer progression Semin Cancer Biol (2015) 35, 71-84. PubMed Europe PubMed DOI
Vizovisek,M., Vidmar,R., Van Quickelberghe,E., Impens,F., Andjelkovic,U., Sobotic,B., Stoka,V., Gevaert,K., Turk,B. and Fonovic,M. Fast profiling of protease specificity reveals similar substrate specificities for cathepsins K, L and S Proteomics (2015) 15, 2479-2490. PubMed Europe PubMed DOI P
Xue,Y., Wang,L., Xia,D., Li,Q., Gao,S., Dong,M., Cai,T., Shi,S., He,L., Hu,K., Mao,T. and Duan,X. Dental abnormalities caused by novel compound heterozygous CTSK mutations J Dent Res (2015) 94, 674-681. PubMed Europe PubMed DOI M
Yuan,X., Liu,Y., Hua,X., Deng,X., Sun,P., Yu,C., Chen,L., Yu,S., Liu,S. and Pang,H. Myricetin ameliorates the symptoms of collagen-induced arthritis in mice by inhibiting cathepsin K activity Immunopharmacol Immunotoxicol (2015) 37, 513-519. PubMed Europe PubMed DOI I

2014

Aguda,A.H., Panwar,P., Du,X., Nguyen,N.T., Brayer,G.D. and Bromme,D. Structural basis of collagen fiber degradation by cathepsin K Proc Natl Acad Sci U S A (2014) 111, 17474-17479. PubMed Europe PubMed DOI
Arman,A., Bereket,A., Coker,A., Kiper,P.O., Guran,T., Ozkan,B., Atay,Z., Akcay,T., Halilo Lu,B., Boduro Lu,K., Alanay,Y. and Turan,S. Cathepsin K analysis in a pycnodysostosis cohort: demographic, genotypic and phenotypic features Orphanet J Rare Dis (2014) 9, 60-60. PubMed Europe PubMed DOI M
Borisek,J., Drgan,V., Minovski,N. and Novic,M. Mechanistic interpretation of artificial neural network-based QSAR model for prediction of cathepsin K inhibition potency J Chemometr (2014) 28, 272-281. DOI I
Hu,L., Cheng,X.W., Song,H., Inoue,A., Jiang,H., Li,X., Shi,G.P., Kozawa,E., Okumura,K. and Kuzuya,M. Cathepsin K activity controls injury-related vascular repair in mice Hypertension (2014) 63, 607-615. PubMed Europe PubMed DOI K
Hussein,H., Ishihara,A., Menendez,M. and Bertone,A. Pharmacokinetics and bone resorption evaluation of a novel cathepsin K inhibitor (VEL-0230) in healthy adult horses J Vet Pharmacol Ther (2014) 37, 556-564. PubMed Europe PubMed DOI I
Jacome-Galarza,C., Soung,d.Y., Adapala,N.S., Pickarski,M., Sanjay,A., Duong,l.T., Lorenzo,J.A. and Drissi,H. Altered hematopoietic stem cell and osteoclast precursor frequency in cathepsin K null mice J Cell Biochem (2014) 115, 1449-1457. PubMed Europe PubMed DOI K
Lemaire,P.A., Huang,L., Zhuo,Y., Lu,J., Bahnck,C., Stachel,S.J., Carroll,S.S. and Duong,l.T. Chondroitin sulfate promotes activation of cathepsin K J Biol Chem (2014) 289, 21562-21572. PubMed Europe PubMed DOI
Lustigman,S., Melnikow,E., Anand,S.B., Contreras,A., Nandi,V., Liu,J., Bell,A., Unnasch,T.R., Rogers,M.B. and Ghedin,E. Potential involvement of Brugia malayi cysteine proteases in the maintenance of the endosymbiotic relationship with Wolbachia Int J Parasitol Drugs Drug Resist (2014) 4, 267-277. PubMed Europe PubMed DOI PMC EPMC
Muller,S., Faulhaber,A., Sieber,C., Pfeifer,D., Hochberg,T., Gansz,M., Deshmukh,S.D., Dauth,S., Brix,K., Saftig,P., Peters,C., Henneke,P. and Reinheckel,T. The endolysosomal cysteine cathepsins L and K are involved in macrophage-mediated clearance of Staphylococcus aureus and the concomitant cytokine induction FASEB J (2014) 28, 162-175. PubMed Europe PubMed DOI
Novinec,M., Korenc,M., Caflisch,A., Ranganathan,R., Lenarcic,B. and Baici,A. A novel allosteric mechanism in the cysteine peptidase cathepsin K discovered by computational methods Nat Commun (2014) 5, 3287-3287. PubMed Europe PubMed DOI S I
Novinec,M., Lenarcic,B. and Baici,A. Probing the activity modification space of the cysteine peptidase cathepsin K with novel allosteric modifiers PLoS ONE (2014) 9, e106642-e106642. PubMed Europe PubMed DOI PMC EPMC
Pennypacker,B.L., Chen,C.M., Zheng,H., Shih,M.S., Belfast,M., Samadfam,R. and Duong,l.T. Inhibition of cathepsin K increases modeling-based bone formation, and improves cortical dimension and strength in adult ovariectomized monkeys J Bone Miner Res (2014) 29, 1847-1858. PubMed Europe PubMed DOI I
Respondek,T., Sharma,R., Herroon,M.K., Garner,R.N., Knoll,J.D., Cueny,E., Turro,C., Podgorski,I. and Kodanko,J.J. Inhibition of cathepsin activity in a cell-based assay by a light-activated ruthenium compound ChemMedChem (2014) 9, 1306-1315. PubMed Europe PubMed DOI I
Rodnick,M.E., Shao,X., Kozloff,K.M., Scott,P.J. and Kilbourn,M.R. Carbon-11 labeled cathepsin K inhibitors: syntheses and preliminary in vivo evaluation Nucl Med Biol (2014) 41, 384-389. PubMed Europe PubMed DOI I
Xu,Q., Hou,W., Zheng,Y., Liu,C., Gong,Z., Lu,C., Lai,W. and Maibach,H.I. Ultraviolet A-induced cathepsin K expression is mediated via MAPK/AP-1 pathway in human dermal fibroblasts PLoS ONE (2014) 9, e102732-e102732. PubMed Europe PubMed DOI PMC EPMC
Zhuo,Y., Gauthier,J.Y., Black,W.C., Percival,M.D. and Duong,L.T. Inhibition of bone resorption by the cathepsin K inhibitor odanacatib is fully reversible Bone (2014) 67, 269-280. PubMed Europe PubMed DOI I

2013

Activating cathepsin K in osteoclasts stimulates bone formation through S1P Bonekey Rep (2013) 2, 362-362. PubMed Europe PubMed DOI PMC EPMC K
Cheng,X.W., Kikuchi,R., Ishii,H., Yoshikawa,D., Hu,L., Takahashi,R., Shibata,R., Ikeda,N., Kuzuya,M., Okumura,K. and Murohara,T. Circulating cathepsin K as a potential novel biomarker of coronary artery disease Atherosclerosis (2013) 228, 211-216. PubMed Europe PubMed DOI
Feth,M.P., Heyse,W., Baumgartner,B., Nagel,N., Tappertzhofen,C., Olpp,T., Jurascheck,J., Ulrich,J., Helmdach,L. and Petzoldt,C. From laboratory to pilot plant: the solid-state process development of a highly potent cathepsin S/K inhibitor Eur J Pharm Biopharm (2013) 83, 436-448. PubMed Europe PubMed DOI I
Gao,B., Chen,W., Hao,L., Zhu,G., Feng,S., Ci,H., Zhou,X., Stashenko,P. and Li,Y.P. Inhibiting periapical lesions through AAV-RNAi silencing of cathepsin K J Dent Res (2013) 92, 180-186. PubMed Europe PubMed DOI K
Helali,A.M., Iti,F.M. and Mohamed,I.N. Cathepsin K inhibitors: a novel target but promising approach in the treatment of osteoporosis Curr Drug Targets (2013) 14, 1591-1600. PubMed Europe PubMed DOI V I
Herroon,M.K., Rajagurubandara,E., Rudy,D.L., Chalasani,A., Hardaway,A.L. and Podgorski,I. Macrophage cathepsin K promotes prostate tumor progression in bone Oncogene (2013) 32, 1580-1593. PubMed Europe PubMed DOI K
Hua,Y., Zhang,Y., Dolence,J., Shi,G.P., Ren,J. and Nair,S. Cathepsin K knockout mitigates high-fat diet-induced cardiac hypertrophy and contractile dysfunction Diabetes (2013) 62, 498-509. PubMed Europe PubMed DOI K
Hua,Y., Xu,X., Shi,G.P., Chicco,A.J., Ren,J. and Nair,S. Cathepsin K knockout alleviates pressure overload-induced cardiac hypertrophy Hypertension (2013) 61, 1184-1192. PubMed Europe PubMed DOI K
Lotinun,S., Kiviranta,R., Matsubara,T., Alzate,J.A., Neff,L., Luth,A., Koskivirta,I., Kleuser,B., Vacher,J., Vuorio,E., Horne,W.C. and Baron,R. Osteoclast-specific cathepsin K deletion stimulates S1P-dependent bone formation J Clin Invest (2013) 123, 666-681. PubMed Europe PubMed DOI K
Miller,R.E., Lu,Y., Tortorella,M.D. and Malfait,A.M. Genetically engineered mouse models reveal the importance of proteases as osteoarthritis drug targets Curr Rheumatol Rep (2013) 15, 350-350. PubMed Europe PubMed DOI K
Nallaseth,F.S., Lecaille,F., Li,Z. and Bromme,D. The role of basic amino acid surface clusters on the collagenase activity of cathepsin K Biochemistry (2013) 52, 7742-7752. PubMed Europe PubMed DOI
Novinec,M. and Lenarcic,B. Cathepsin K: a unique collagenolytic cysteine peptidase Biol Chem (2013) 394, 1163-1179. PubMed Europe PubMed DOI V
Panwar,P., Du,X., Sharma,V., Lamour,G., Castro,M., Li,H. and Bromme,D. Effects of cysteine proteases on the structural and mechanical properties of collagen fibers J Biol Chem (2013) 288, 5940-5950. PubMed Europe PubMed DOI
Park,J.K., Rosen,A., Saffitz,J.E., Asimaki,A., Litovsky,S.H., Mackey-Bojack,S.M. and Halushka,M.K. Expression of cathepsin K and tartrate-resistant acid phosphatase is not confined to osteoclasts but is a general feature of multinucleated giant cells: systematic analysis Rheumatology (Oxford) (2013) 52, 1529-1533. PubMed Europe PubMed DOI
Ren,X.F., Li,H.W., Fang,X., Wu,Y., Wang,L. and Zou,S. Highly selective azadipeptide nitrile inhibitors for cathepsin K: design, synthesis and activity assays Org Biomol Chem (2013) 11, 1143-1148. PubMed Europe PubMed DOI I
Sina,C., Lipinski,S., Gavrilova,O., Aden,K., Rehman,A., Till,A., Rittger,A., Podschun,R., Meyer-Hoffert,U., Haesler,R., Midtling,E., Putsep,K., McGuckin,M.A., Schreiber,S., Saftig,P. and Rosenstiel,P. Extracellular cathepsin K exerts antimicrobial activity and is protective against chronic intestinal inflammation in mice Gut (2013) 62, 520-530. PubMed Europe PubMed DOI
Stoch,S.A., Zajic,S., Stone,J.A., Miller,D.L., van Bortel,L., Lasseter,K.C., Pramanik,B., Cilissen,C., Liu,Q., Liu,L., Scott,B.B., Panebianco,D., Ding,Y., Gottesdiener,K. and Wagner,J.A. Odanacatib, a selective cathepsin K inhibitor to treat osteoporosis: safety, tolerability, pharmacokinetics and pharmacodynamics - results from single oral dose studies in healthy volunteers Br J Clin Pharmacol (2013) 75, 1240-1254. PubMed Europe PubMed DOI I
Sun,P., Liu,Y., Deng,X., Yu,C., Dai,N., Yuan,X., Chen,L., Yu,S., Si,W., Wang,X., Wu,D., Liu,S. and Pang,H. An inhibitor of cathepsin K, icariin suppresses cartilage and bone degradation in mice of collagen-induced arthritis Phytomedicine (2013) 20, 975-979. PubMed Europe PubMed DOI I
Sun,S., Karsdal,M.A., Bay-Jensen,A.C., Sorensen,M.G., Zheng,Q., Dziegiel,M.H., Maksymowych,W.P. and Henriksen,K. The development and characterization of an ELISA specifically detecting the active form of cathepsin K Clin Biochem (2013) 46, 1601-1606. PubMed Europe PubMed DOI
Utokpat,P., Panmontha,W., Tongkobpetch,S., Suphapeetiporn,K. and Shotelersuk,V. Novel CTSK mutation resulting in an entire exon 2 skipping in a Thai girl with pycnodysostosis Pediatr Int (2013) 55, 651-655. PubMed Europe PubMed DOI M
Yu,Y.Y., Sun,W., Dong,L., Liu,H.D., Jiang,D., Xiao,J.H., Yang,X.H. and Li,S. Design, synthesis, and screen of cathepsin K inhibitors Chin Chem Lett (2013) 24, 715-718. DOI I
Yuan,X.Y., Fu,D.Y., Ren,X.F., Fang,X., Wang,L., Zou,S. and Wu,Y. Highly selective aza-nitrile inhibitors for cathepsin K, structural optimization and molecular modeling Org Biomol Chem (2013) 11, 5847-5852. PubMed Europe PubMed DOI S I
Zheng,H., Zhang,Z., He,J.W., Fu,W.Z. and Zhang,Z.L. A novel mutation (R122Q) in the cathepsin K gene in a Chinese child with pyknodysostosis Gene (2013) 521, 176-179. PubMed Europe PubMed DOI M

2012

Arampatzidou,M., Schutte,A., Hansson,G.C., Saftig,P. and Brix,K. Effects of cathepsin K deficiency on intercellular junction proteins, luminal mucus layers, and extracellular matrix constituents in the mouse colon Biol Chem (2012) 393, 1391-1403. PubMed Europe PubMed DOI K
Barry,Z.T. and Platt,M.O. Cathepsin S cannibalism of cathepsin K as a mechanism to reduce type I collagen degradation J Biol Chem (2012) 287, 27723-27730. PubMed Europe PubMed DOI
Boonen,S., Rosenberg,E., Claessens,F., Vanderschueren,D. and Papapoulos,S. Inhibition of cathepsin K for treatment of osteoporosis Curr Osteoporos Rep (2012) 10, 73-79. PubMed Europe PubMed DOI I
Borel,O., Gineyts,E., Bertholon,C. and Garnero,P. Cathepsin K preferentially solubilizes matured bone matrix Calcif Tissue Int (2012) 91, 32-39. PubMed Europe PubMed DOI
Bromme,D. Cathepsin K [ISSN:978-0-12-407743-0] (2012) 3, 1801-1807. DOI
Crawford,J.J., Kenny,P.W., Bowyer,J., Cook,C.R., Finlayson,J.E., Heyes,C., Highton,A.J., Hudson,J.A., Jestel,A., Krapp,S., Martin,S., Macfaul,P.A., McDermott,B.P., McGuire,T.M., Morley,A.D., Morris,J.J., Page,K.M., Ribeiro,L.R., Sawney,H., Steinbacher,S., Smith,C. and Dossetter,A.G. Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors J Med Chem (2012) 55, 8827-8837. PubMed Europe PubMed DOI I
Dauth,S., Schmidt,M.M., Rehders,M., Dietz,F., Kelm,S., Dringen,R. and Brix,K. Characterisation and metabolism of astroglia-rich primary cultures from cathepsin K-deficient mice Biol Chem (2012) 393, 959-970. PubMed Europe PubMed DOI K
Dossetter,A.G., Beeley,H., Bowyer,J., Cook,C.R., Crawford,J.J., Finlayson,J.E., Heron,N.M., Heyes,C., Highton,A.J., Hudson,J.A., Jestel,A., Kenny,P.W., Krapp,S., Martin,S., Macfaul,P.A., McGuire,T.M., Gutierrez,P.M., Morley,A.D., Morris,J.J., Page,K.M., Ribeiro,L.R., Sawney,H., Steinbacher,S., Smith,C. and Vickers,M. (1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): A potent and highly selective Cathepsin K inhibitor for the treatment of osteoarthritis J Med Chem (2012) 55, 6363-6374. PubMed Europe PubMed DOI I
Dossetter,A.G., Bowyer,J., Cook,C.R., Crawford,J.J., Finlayson,J.E., Heron,N.M., Heyes,C., Highton,A.J., Hudson,J.A., Jestel,A., Krapp,S., Macfaul,P.A., McGuire,T.M., Morley,A.D., Morris,J.J., Page,K.M., Ribeiro,L.R., Sawney,H., Steinbacher,S. and Smith,C. Isosteric replacements for benzothiazoles and optimisation to potent cathepsin K inhibitors free from hERG channel inhibition Bioorg Med Chem Lett (2012) 22, 5563-5568. PubMed Europe PubMed DOI I
Hayami,T., Zhuo,Y., Wesolowski,G.A., Pickarski,M. and Duong,L.T. Inhibition of cathepsin K reduces cartilage degeneration in the anterior cruciate ligament transection rabbit and murine models of osteoarthritis Bone (2012) 50, 1250-1259. PubMed Europe PubMed DOI I
Jerome,C., Missbach,M. and Gamse,R. Balicatib, a cathepsin K inhibitor, stimulates periosteal bone formation in monkeys Osteoporos Int (2012) 23, 339-349. PubMed Europe PubMed DOI I
Kozawa,E., Nishida,Y., Cheng,X.W., Urakawa,H., Arai,E., Futamura,N., Shi,G.P., Kuzuya,M., Hu,L., Sasaki,T. and Ishiguro,N. Osteoarthritic change is delayed in a Ctsk-knockout mouse model of osteoarthritis Arthritis Rheum (2012) 64, 454-464. PubMed Europe PubMed DOI K
Petrey,A.C., Flanagan-Steet,H., Johnson,S., Fan,X., De la Rosa,M., Haskins,M.E., Nairn,A.V., Moremen,K.W. and Steet,R. Excessive activity of cathepsin K is associated with cartilage defects in a zebrafish model of mucolipidosis II Dis Model Mech (2012) 5, 177-190. PubMed Europe PubMed DOI
Roy,S., Dattagupta,J.K. and Biswas,S. Expression of recombinant human cathepsin K is enhanced by codon optimization Process Biochem (2012) 47, 1944-1947. DOI E
Schmit,J.M., Pondenis,H.C., Barger,A.M., Borst,L.B., Garrett,L.D., Wypij,J.M., Neumann,Z.L. and Fan,T.M. Cathepsin K expression and activity in canine osteosarcoma J Vet Intern Med (2012) 26, 126-134. PubMed Europe PubMed DOI
Winkeler,C.L., Kladney,R.D., Maggi,L.B., Jr. and Weber,J.D. Cathepsin K-cre causes unexpected germline deletion of genes in mice PLoS ONE (2012) 7, e42005-e42005. PubMed Europe PubMed DOI PMC EPMC K
Zhang,Y., Li,J., Zhu,J., Zhou,G., Zhang,W.J., Cao,Y. and Liu,W. Enhanced cartilage formation by inhibiting cathepsin K expression in chondrocytes expanded invitro Biomaterials (2012) 33, 7394-7404. PubMed Europe PubMed DOI K

2011

Arbuckle,W., Baugh,M., Belshaw,S., Bennett,D.J., Bruin,J., Cai,J., Cameron,K.S., Claxton,C., Dempster,M., Everett,K., Fradera,X., Hamilton,W., Jones,P.S., Kinghorn,E., Long,C., Martin,I., Robinson,J. and Westwood,P. 1H-Imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors: separation of desired cellular activity from undesired tissue accumulation through optimization of basic nitrogen pka Bioorg Med Chem Lett (2011) 21, 932-935. PubMed Europe PubMed DOI I
Bauer,D.C. Discontinuation of odanacatib and other osteoporosis treatments: here today and gone tomorrow? J Bone Miner Res (2011) 26, 239-241. PubMed Europe PubMed DOI I
Cherney,M.M., Lecaille,F., Kienitz,M., Nallaseth,F.S., Li,Z., James,M.N. and Bromme,D. Structure-activity analysis of cathepsin K/chondroitin 4-sulfate interactions J Biol Chem (2011) 286, 8988-8998. PubMed Europe PubMed DOI
Costa,A.G., Cusano,N.E., Silva,B.C., Cremers,S. and Bilezikian,J.P. Cathepsin K: its skeletal actions and role as a therapeutic target in osteoporosis Nat Rev Rheumatol (2011) 7, 447-456. PubMed Europe PubMed DOI V I
Dauth,S., Sirbulescu,R.F., Jordans,S., Rehders,M., Avena,L., Oswald,J., Lerchl,A., Saftig,P. and Brix,K. Cathepsin K deficiency in mice induces structural and metabolic changes in the central nervous system that are associated with learning and memory deficits BMC Neurosci (2011) 12, 74-74. PubMed Europe PubMed DOI K
Eisman,J.A., Bone,H.G., Hosking,D.J., McClung,M.R., Reid,I.R., Rizzoli,R., Resch,H., Verbruggen,N., Hustad,C.M., Dasilva,C., Petrovic,R., Santora,A.C., Ince,B.A. and Lombardi,A. Odanacatib in the treatment of postmenopausal women with low bone mineral density: three-year continued therapy and resolution of effect J Bone Miner Res (2011) 26, 242-251. PubMed Europe PubMed DOI I
Frizler,M., Lohr,F., Furtmann,N., Klas,J. and Gutschow,M. Structural optimization of azadipeptide nitriles strongly increases association rates and allows the development of selective cathepsin inhibitors J Med Chem (2011) 54, 396-400. PubMed Europe PubMed DOI I
Gruber,H.E., Ingram,J.A., Hoelscher,G.L., Zinchenko,N., Norton,H.J. and Hanley,E.N., Jr. Constitutive expression of cathepsin K in the human intervertebral disc: new insight into disc extracellular matrix remodeling via cathepsin K and receptor activator of nuclear factor-kappaB ligand Arthritis Res Ther (2011) 13, R140-R140. PubMed Europe PubMed DOI
Hsu,C.W., Olabisi,R.M., Olmsted-Davis,E.A., Davis,A.R. and West,J.L. Cathepsin K-sensitive poly(ethylene glycol) hydrogels for degradation in response to bone resorption J Biomed Mater Res A (2011) 98, 53-62. PubMed Europe PubMed DOI
Isabel,E., Mellon,C., Boyd,M.J., Chauret,N., Deschenes,D., Desmarais,S., Falgueyret,J.P., Gauthier,J.Y., Khougaz,K., Lau,C.K., Leger,S., Levorse,D.A., Li,C.S., Masse,F., David Percival,M., Roy,B., Scheigetz,J., Therien,M., Truong,V.L., Wesolowski,G., Young,R.N., Zamboni,R. and Cameron Black,W. Difluoroethylamines as an amide isostere in inhibitors of cathepsin K Bioorg Med Chem Lett (2011) 21, 920-923. PubMed Europe PubMed DOI I
Knaapi,J., Lukkarinen,H., Kiviranta,R., Vuorio,E. and Kaapa,P. Cathepsin K deficiency aggravates lung injury in hyperoxia-exposed newborn mice Exp Lung Res (2011) 37, 408-418. PubMed Europe PubMed DOI K
Leah,E. Cathepsin K inhibition halts bone destruction, while remodeling merry-go-round runs merrily on Nat Rev Rheumatol (2011) 7, 191-191. I
Manako,J. [New approach for osteoporosis treatment: cathepsin K inhibitor, ONO-5334] Clin Calcium (2011) 21, 64-69. PubMed Europe PubMed DOI I
Pennypacker,B.L., Duong,l.T., Cusick,T.E., Masarachia,P.J., Gentile,M.A., Gauthier,J.Y., Black,W.C., Scott,B.B., Samadfam,R., Smith,S.Y. and Kimmel,D.B. Cathepsin K inhibitors prevent bone loss in estrogen-deficient rabbits J Bone Miner Res (2011) 26, 252-262. PubMed Europe PubMed DOI I
Shahlaei,M., Fassihi,A., Saghaie,L., Arkan,E. and Pourhossein,A. A modeling study of aldehyde inhibitors of human cathepsin K using partial least squares method Res Pharm Sci (2011) 6, 71-80. PubMed Europe PubMed I
Toral-Lopez,J., Gonzalez-Huerta,L.M., Sosa,B., Orozco,S., Gonzalez,H.P. and Cuevas-Covarrubias,S.A. Familial pycnodysostosis: identification of a novel mutation in the CTSK gene (cathepsin K) J Investig Med (2011) 59, 277-280. PubMed Europe PubMed DOI M
Wijkmans,J. and Gossen,J. Inhibitors of cathepsin K: a patent review (2004 - 2010) Expert Opin Ther Pat (2011) 21, 1611-1629. PubMed Europe PubMed DOI I
Xie,L., Moroi,Y., Hayashida,S., Tsuji,G., Takeuchi,S., Shan,B., Nakahara,T., Uchi,H., Takahara,M. and Furue,M. Cathepsin K-upregulation in fibroblasts promotes matrigel invasive ability of squamous cell carcinoma cells via tumor-derived IL-1alpha J Dermatol Sci (2011) 61, 45-50. PubMed Europe PubMed DOI
Xue,Y., Cai,T., Shi,S., Wang,W., Zhang,Y., Mao,T. and Duan,X. Clinical and animal research findings in pycnodysostosis and gene mutations of cathepsin K from 1996 to 2011 Orphanet J Rare Dis (2011) 6, 20-20. PubMed Europe PubMed DOI M V
Zhang,D., Leung,N., Weber,E., Saftig,P. and Bromme,D. The effect of cathepsin K deficiency on airway development and TGF-beta1 degradation Respir Res (2011) 12, 72-72. PubMed Europe PubMed DOI K
Zhu,Y., Cameron,B.R., Mosi,R., Anastassov,V., Cox,J., Qin,L., Santucci,Z., Metz,M., Skerlj,R.T. and Fricker,S.P. Inhibition of the cathepsin cysteine proteases B and K by square-planar cycloaurated gold(III) compounds and investigation of their anti-cancer activity J Inorg Biochem (2011) 105, 754-762. PubMed Europe PubMed DOI I

2010

Bai,L., Beckers,L., Wijnands,E., Lutgens,S.P., Herias,M.V., Saftig,P., Daemen,M.J., Cleutjens,K., Lutgens,E., Biessen,E.A. and Heeneman,S. Cathepsin K gene disruption does not affect murine aneurysm formation Atherosclerosis (2010) 209, 96-103. PubMed Europe PubMed DOI K
Barascuk,N., Skjot-Arkil,H., Register,T.C., Larsen,L., Byrjalsen,I., Christiansen,C. and Karsdal,M.A. Human macrophage foam cells degrade atherosclerotic plaques through cathepsin K mediated processes BMC Cardiovasc Disord (2010) 10, 19-19. PubMed Europe PubMed DOI
Black,W.C. Peptidomimetic inhibitors of cathepsin K Curr Top Med Chem (2010) 10, 745-751. PubMed Europe PubMed DOI I
Fontanesi,L., Scotti,E., Buttazzoni,L., Dall'Olio,S., Davoli,R. and Russo,V. A single nucleotide polymorphism in the porcine cathepsin K (CTSK) gene is associated with back fat thickness and production traits in Italian Duroc pigs Mol Biol Rep (2010) 37, 491-495. PubMed Europe PubMed DOI M
Frizler,M., Stirnberg,M., Sisay,M.T. and Gutschow,M. Development of nitrile-based peptidic inhibitors of cysteine cathepsins Curr Top Med Chem (2010) 10, 294-322. PubMed Europe PubMed DOI T I
Fuller,K., Lindstrom,E., Edlund,M., Henderson,I., Grabowska,U., Szewczyk,K.A., Moss,R., Samuelsson,B. and Chambers,T.J. The resorptive apparatus of osteoclasts supports lysosomotropism and increases potency of basic versus non-basic inhibitors of cathepsin K Bone (2010) 46, 1400-1407. PubMed Europe PubMed DOI I
Khan,B., Ahmed,Z. and Ahmad,W. A novel missense mutation in cathepsin K (CTSK) gene in a consanguineous Pakistani family with pycnodysostosis J Investig Med (2010) 58, 720-724. PubMed Europe PubMed DOI M
Kometani,M., Nonomura,K., Tomoo,T. and Niwa,S. Hurdles in the drug discovery of cathepsin K inhibitors Curr Top Med Chem (2010) 10, 733-744. PubMed Europe PubMed DOI V I
Li,W.A., Barry,Z.T., Cohen,J.D., Wilder,C.L., Deeds,R.J., Keegan,P.M. and Platt,M.O. Detection of femtomole quantities of mature cathepsin K with zymography Anal Biochem (2010) 401, 91-98. PubMed Europe PubMed DOI
Lorenz,J.C., Busacca,C.A., Feng,X., Grinberg,N., Haddad,N., Johnson,J., Kapadia,S., Lee,H., Saha,A., Sarvestani,M., Spinelli,E.M., Varsolona,R., Wei,X., Zeng,X. and Senanayake,C.H. Large-scale asymmetric synthesis of a cathepsin S inhibitor J Org Chem (2010) 75, 1155-1161. PubMed Europe PubMed DOI I
McDougall,J.J., Schuelert,N. and Bowyer,J. Cathepsin K inhibition reduces CTXII levels and joint pain in the guinea pig model of spontaneous osteoarthritis Osteoarthritis Cartilage (2010) 18, 1355-1357. PubMed Europe PubMed DOI I
Novinec,M., Kovacic,L., Lenarcic,B. and Baici,A. Conformational flexibility and allosteric regulation of cathepsin K Biochem J (2010) 429, 379-389. PubMed Europe PubMed DOI
Pan,X., Tan,N., Zeng,G., Huang,H. and Yan,H. 3D QSAR studies on ketoamides of human cathepsin K inhibitors based on two different alignment methods Eur J Med Chem (2010) 45, 667-681. PubMed Europe PubMed DOI I
Rankovic,Z., Cai,J., Kerr,J., Fradera,X., Robinson,J., Mistry,A., Hamilton,E., McGarry,G., Andrews,F., Caulfield,W., Cumming,I., Dempster,M., Waller,J., Scullion,P., Martin,I., Mitchell,A., Long,C., Baugh,M., Westwood,P., Kinghorn,E., Bruin,J., Hamilton,W., Uitdehaag,J., van Zeeland,M., Potin,D., Saniere,L., Fouquet,A., Chevallier,F., Deronzier,H., Dorleans,C. and Nicolai,E. Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors Bioorg Med Chem Lett (2010) 20, 1524-1527. PubMed Europe PubMed DOI I
Rankovic,Z., Cai,J., Fradera,X., Dempster,M., Mistry,A., Mitchell,A., Long,C., Hamilton,E., King,A., Boucharens,S., Jamieson,C., Gillespie,J., Cumming,I., Uitdehaag,J. and van Zeeland,M. Dioxo-triazines as a novel series of cathepsin K inhibitors Bioorg Med Chem Lett (2010) 20, 1488-1490. PubMed Europe PubMed DOI I
Rankovic,Z., Cai,J., Kerr,J., Fradera,X., Robinson,J., Mistry,A., Finlay,W., McGarry,G., Andrews,F., Caulfield,W., Cumming,I., Dempster,M., Waller,J., Arbuckle,W., Anderson,M., Martin,I., Mitchell,A., Long,C., Baugh,M., Westwood,P., Kinghorn,E., Jones,P., Uitdehaag,J.C., van Zeeland,M., Potin,D., Saniere,L., Fouquet,A., Chevallier,F., Deronzier,H., Dorleans,C. and Nicolai,E. Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: improving selectivity over hERG Bioorg Med Chem Lett (2010) 20, 6237-6241. PubMed Europe PubMed DOI I
Sanchez,J.F., Chiang,Y.M., Szewczyk,E., Davidson,A.D., Ahuja,M., Elizabeth Oakley,C., Woo Bok,J., Keller,N., Oakley,B.R. and Wang,C.C. Molecular genetic analysis of the orsellinic acid/F9775 gene cluster of Aspergillus nidulans Mol Biosyst (2010) 6, 587-593. PubMed Europe PubMed DOI PMC EPMC I
Teno,N. and Masuya,K. Orally bioavailable cathepsin K inhibitors with pyrrolopyrimidine scaffold Curr Top Med Chem (2010) 10, 752-766. PubMed Europe PubMed DOI V I
Wilson,S. and Bromme,D. Potential role of cathepsin K in the pathophysiology of mucopolysaccharidoses J Pediatr Rehabil Med (2010) 3, 139-146. PubMed Europe PubMed DOI
Yan,X., Takahara,M., Xie,L., Tu,Y. and Furue,M. Cathepsin K expression: a useful marker for the differential diagnosis of dermatofibroma and dermatofibrosarcoma protuberans Histopathology (2010) 57, 486-488. PubMed Europe PubMed DOI

2009

Aydin,H.M. and Piskin,E. Cathepsin K/TRAP: can they be used to induce osteogenesis? Med Hypotheses (2009) 72, 464-465. PubMed Europe PubMed DOI U
Bethel,P.A., Gerhardt,S., Jones,E.V., Kenny,P.W., Karoutchi,G.I., Morley,A.D., Oldham,K., Rankine,N., Augustin,M., Krapp,S., Simader,H. and Steinbacher,S. Design of selective cathepsin inhibitors Bioorg Med Chem Lett (2009) 19, 4622-4625. PubMed Europe PubMed DOI I
Boyd,M.J., Crane,S.N., Robichaud,J., Scheigetz,J., Black,W.C., Chauret,N., Wang,Q., Masse,F. and Oballa,R.M. Investigation of ketone warheads as alternatives to the nitrile for preparation of potent and selective cathepsin K inhibitors Bioorg Med Chem Lett (2009) 19, 675-679. PubMed Europe PubMed DOI I
Bromme,D. and Lecaille,F. Cathepsin K inhibitors for osteoporosis and potential off-target effects Expert Opin Investig Drugs (2009) 18, 585-600. PubMed Europe PubMed DOI I
Codriansky,K.A., Quintanilla-Dieck,M.J., Gan,S., Keady,M., Bhawan,J. and Runger,T.M. Intracellular degradation of elastin by cathepsin K in skin fibroblasts - a possible role in photoaging Photochem Photobiol (2009) 85, 1356-1363. PubMed Europe PubMed DOI
Connor,J.R., LePage,C., Swift,B.A., Yamashita,D., Bendele,A.M., Maul,D. and Kumar,S. Protective effects of a cathepsin K inhibitor, SB-553484, in the canine partial medial meniscectomy model of osteoarthritis Osteoarthritis Cartilage (2009) 17, 1236-1243. PubMed Europe PubMed DOI I
Desmarais,S., Masse,F. and Percival,M.D. Pharmacological inhibitors to identify roles of cathepsin K in cell-based studies: a comparison of available tools Biol Chem (2009) 390, 941-948. PubMed Europe PubMed DOI I
Guo,J., Bot,I., de Nooijer,R., Hoffman,S.J., Stroup,G.B., Biessen,E.A., Benson,G.M., Groot,P.H., Van Eck,M. and van Berkel,T.J. Leucocyte cathepsin K affects atherosclerotic lesion composition and bone mineral density in low-density lipoprotein receptor deficient mice Cardiovasc Res (2009) 81, 278-285. PubMed Europe PubMed DOI
Han,J., Luo,T., Gu,Y., Li,G., Jia,W. and Luo,M. Cathepsin K regulates adipocyte differentiation: possible involvement of type I collagen degradation Endocr J (2009) 56, 55-63. PubMed Europe PubMed DOI
Je,J.E., Ahn,S.J., Kim,N.Y., Seo,J.S., Kim,M.S., Park,N.G., Kim,J.K., Chung,J.K. and Lee,H.H. Molecular cloning, expression analysis and enzymatic characterization of cathepsin K from olive flounder (Paralichthys olivaceus) Comp Biochem Physiol A Mol Integr Physiol (2009) 154, 474-485. PubMed Europe PubMed DOI
Jordans,S., Jenko-Kokalj,S., Kuhl,N.M., Tedelind,S., Sendt,W., Bromme,D., Turk,D. and Brix,K. Monitoring compartment-specific substrate cleavage by cathepsins B, K, L, and S at physiological pH and redox conditions BMC Biochem (2009) 10, 23-23. PubMed Europe PubMed DOI PMC EPMC
Lendeckel,U., Kahne,T., Ten Have,S., Bukowska,A., Wolke,C., Bogerts,B., Keilhoff,G. and Bernstein,H.G. Cathepsin K generates enkephalin from beta-endorphin: a new mechanism with possible relevance for schizophrenia Neurochem Int (2009) 54, 410-417. PubMed Europe PubMed DOI
Li,H.W., Liu,X.C., Yang,J.G., Jiang,K., Fang,X.X. and Wu,Y.Q. Synthesis, characterization and enzyme activity assays of peptides nitriles as inhibitors of cathepsin K Gaodeng Xuexiao Huaxue Xuebao/Chemical Journal of Chinese Universities (2009) 30, 716-719. I
Li,H.Y., Ma,H.W., Wang,H.Q. and Ma,W.H. Molecular analysis of a novel cathepsin K gene mutation in a Chinese child with pycnodysostosis J Int Med Res (2009) 37, 264-269. PubMed Europe PubMed M
Morko,J., Kiviranta,R., Mulari,M.T., Ivaska,K.K., Vaananen,H.K., Vuorio,E. and Laitala-Leinonen,T. Overexpression of cathepsin K accelerates the resorption cycle and osteoblast differentiation in vitro Bone (2009) 44, 717-728. PubMed Europe PubMed DOI
Morley,A.D., Kenny,P.W., Burton,B., Heald,R.A., Macfaul,P.A., Mullett,J., Page,K., Porres,S.S., Ribeiro,L.R., Smith,P., Ward,S. and Wilkinson,T.J. 5-Aminopyrimidin-2-ylnitriles as cathepsin K inhibitors Bioorg Med Chem Lett (2009) 19, 1658-1661. PubMed Europe PubMed DOI I
Pennypacker,B., Shea,M., Liu,Q., Masarachia,P., Saftig,P., Rodan,S., Rodan,G. and Kimmel,D. Bone density, strength, and formation in adult cathepsin K (-/-) mice Bone (2009) 44, 199-207. PubMed Europe PubMed DOI K
Podgorski,I., Linebaugh,B.E., Koblinski,J.E., Rudy,D.L., Herroon,M.K., Olive,M.B. and Sloane,B.F. Bone marrow-derived cathepsin K cleaves SPARC in bone metastasis Am J Pathol (2009) 175, 1255-1269. PubMed Europe PubMed DOI PMC EPMC
Podgorski,I. Future of anticathepsin K drugs: dual therapy for skeletal disease and atherosclerosis? Future Med Chem (2009) 1, 21-34. PubMed Europe PubMed DOI PMC EPMC I
Quintanilla-Dieck,M.J., Codriansky,K., Keady,M., Bhawan,J. and Runger,T.M. Expression and regulation of cathepsin K in skin fibroblasts Exp Dermatol (2009) 18, 596-602. PubMed Europe PubMed DOI
Schilling,K., Korner,A., Sehmisch,S., Kreusch,A., Kleint,R., Benedix,Y., Schlabrakowski,A. and Wiederanders,B. Selectivity of propeptide-enzyme interaction in cathepsin L-like cysteine proteases Biol Chem (2009) 390, 167-174. PubMed Europe PubMed DOI
Schroeckh,V., Scherlach,K., Nutzmann,H.W., Shelest,E., Schmidt-Heck,W., Schuemann,J., Martin,K., Hertweck,C. and Brakhage,A.A. Intimate bacterial-fungal interaction triggers biosynthesis of archetypal polyketides in Aspergillus nidulans Proc Natl Acad Sci U S A (2009) 106, 14558-14563. PubMed Europe PubMed DOI PMC EPMC I
Stoch,S.A., Zajic,S., Stone,J., Miller,D.L., Van Dyck,K., Gutierrez,M.J., De Decker,M., Liu,L., Liu,Q., Scott,B.B., Panebianco,D., Jin,B., Duong,L.T., Gottesdiener,K. and Wagner,J.A. Effect of the cathepsin K inhibitor odanacatib on bone resorption biomarkers in healthy postmenopausal women: two double-blind, randomized, placebo-controlled phase I studies Clin Pharmacol Ther (2009) 86, 175-182. PubMed Europe PubMed DOI I
Stroup,G.B., Kumar,S. and Jerome,C.P. Treatment with a potent cathepsin K inhibitor preserves cortical and trabecular bone mass in ovariectomized monkeys Calcif Tissue Int (2009) 85, 344-355. PubMed Europe PubMed DOI I
Svelander,L., Erlandsson-Harris,H., Astner,L., Grabowska,U., Klareskog,L., Lindstrom,E. and Hewitt,E. Inhibition of cathepsin K reduces bone erosion, cartilage degradation and inflammation evoked by collagen-induced arthritis in mice Eur J Pharmacol (2009) 613, 155-162. PubMed Europe PubMed DOI I
Wang,H., Matsuhashi,H., Doan,B.D., Goodman,S.N., Ouyang,X. and Clark,W.M., Jr. Large-scale synthesis of SB-462795, a cathepsin K inhibitor: the RCM-based approaches Tetrahedron (2009) 65, 6291-6303. DOI I
Wilson,S., Hashamiyan,S., Clarke,L., Saftig,P., Mort,J., Dejica,V.M. and Bromme,D. Glycosaminoglycan-mediated loss of cathepsin K collagenolytic activity in MPS I contributes to osteoclast and growth plate abnormalities Am J Pathol (2009) 175, 2053-2062. PubMed Europe PubMed DOI PMC EPMC
Zhao,Q., Jia,Y. and Xiao,Y. Cathepsin K: a therapeutic target for bone diseases Biochem Biophys Res Commun (2009) 380, 721-723. PubMed Europe PubMed DOI V

2008

Asagiri,M., Hirai,T., Kunigami,T., Kamano,S., Gober,H.J., Okamoto,K., Nishikawa,K., Latz,E., Golenbock,D.T., Aoki,K., Ohya,K., Imai,Y., Morishita,Y., Miyazono,K., Kato,S., Saftig,P. and Takayanagi,H. Cathepsin K-dependent toll-like receptor 9 signaling revealed in experimental arthritis Science (2008) 319, 624-627. PubMed Europe PubMed DOI T
Bell,E. Innate immunity: new role for cathepsin K Nat Rev Immunol (2008) 8, 166-167. DOI
Dejica,V.M., Mort,J.S., Laverty,S., Percival,M.D., Antoniou,J., Zukor,D.J. and Poole,A.R. Cleavage of type II collagen by cathepsin K in human osteoarthritic cartilage Am J Pathol (2008) 173, 161-169. PubMed Europe PubMed DOI PMC EPMC
Desmarais,S., Black,W.C., Oballa,R., Lamontagne,S., Riendeau,D., Tawa,P., Duong,l.T., Pickarski,M. and Percival,M.D. Effect of cathepsin K inhibitor basicity on in vivo off-target activities Mol Pharmacol (2008) 73, 147-156. PubMed Europe PubMed DOI I
Fuller,K., Lawrence,K.M., Ross,J.L., Grabowska,U.B., Shiroo,M., Samuelsson,B. and Chambers,T.J. Cathepsin K inhibitors prevent matrix-derived growth factor degradation by human osteoclasts Bone (2008) 42, 200-211. PubMed Europe PubMed DOI I
Gauthier,J.Y., Chauret,N., Cromlish,W., Desmarais,S., Duong,l.T., Falgueyret,J.P., Kimmel,D.B., Lamontagne,S., Leger,S., LeRiche,T., Li,C.S., Masse,F., McKay,D.J., Nicoll-Griffith,D.A., Oballa,R.M., Palmer,J.T., Percival,M.D., Riendeau,D., Robichaud,J., Rodan,G.A., Rodan,S.B., Seto,C., Therien,M., Truong,V.L., Venuti,M.C., Wesolowski,G., Young,R.N., Zamboni,R. and Black,W.C. The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K Bioorg Med Chem Lett (2008) 18, 923-928. PubMed Europe PubMed DOI I
Godat,E., Herve-Grvepinet,V., Veillard,F., Lecaille,F., Belghazi,M., Bromme,D. and Lalmanach,G. Regulation of cathepsin K activity by hydrogen peroxide Biol Chem (2008) 389, 1123-1126. PubMed Europe PubMed DOI I
Husmann,K., Muff,R., Bolander,M.E., Sarkar,G., Born,W. and Fuchs,B. Cathepsins and osteosarcoma: expression analysis identifies cathepsin K as an indicator of metastasis Mol Carcinog (2008) 47, 66-73. PubMed Europe PubMed DOI
Kim,S.H., Jhon,D.J., Song,J.H., No,J.S. and Kang,N.S. Effect of novel N-cyano-tetrahydro-pyridazine compounds, a class of cathepsin K inhibitors, on the bone resorptive activity of mature osteoclasts Bioorg Med Chem Lett (2008) 18, 3988-3991. PubMed Europe PubMed DOI I
Krieg,A.M. and Lipford,G.B. Immunology. The toll of cathepsin K deficiency Science (2008) 319, 576-577. PubMed Europe PubMed DOI
Lecaille,F., Bromme,D. and Lalmanach,G. Biochemical properties and regulation of cathepsin K activity Biochimie (2008) 90, 208-226. PubMed Europe PubMed DOI V T
Li,Z., Kienetz,M., Cherney,M.M., James,M.N. and Bromme,D. The crystal and molecular structures of a cathepsin K:chondroitin sulfate complex J Mol Biol (2008) 383, 78-91. PubMed Europe PubMed DOI S
Prezelj,J., Ostanek,B., Logar,D.B., Marc,J., Hawa,G. and Kocjan,T. Cathepsin K predicts femoral neck bone mineral density change in nonosteoporotic peri- and early postmenopausal women Menopause (2008) 15, 369-373. PubMed Europe PubMed DOI
Quintanilla-Dieck,M.J., Codriansky,K., Keady,M., Bhawan,J. and Runger,T.M. Cathepsin K in melanoma invasion J Invest Dermatol (2008) 128, 2281-2288. PubMed Europe PubMed DOI
Ravikumar,M., Pavan,S., Bairy,S., Pramod,A.B., Sumakanth,M., Kishore,M. and Sumithra,T. Virtual screening of cathepsin K inhibitors using docking and pharmacophore models Chem Biol Drug Des (2008) 72, 79-90. PubMed Europe PubMed DOI I
Robichaud,J., Black,W.C., Therien,M., Paquet,J., Oballa,R.M., Bayly,C.I., McKay,D.J., Wang,Q., Isabel,E., Leger,S., Mellon,C., Kimmel,D.B., Wesolowski,G., Percival,M.D., Masse,F., Desmarais,S., Falgueyret,J.P. and Crane,S.N. Identification of a nonbasic, nitrile-containing cathepsin K inhibitor (MK-1256) that is efficacious in a monkey model of osteoporosis J Med Chem (2008) 51, 6410-6420. PubMed Europe PubMed DOI I
Samokhin,A.O., Wong,A., Saftig,P. and Bromme,D. Role of cathepsin K in structural changes in brachiocephalic artery during progression of atherosclerosis in apoE-deficient mice Atherosclerosis (2008) 200, 58-68. PubMed Europe PubMed DOI K
Schurigt,U., Hummel,K.M., Petrow,P.K., Gajda,M., Stockigt,R., Middel,P., Zwerina,J., Janik,T., Bernhardt,R., Schuler,S., Scharnweber,D., Beckmann,F., Saftig,P., Kollias,G., Schett,G., Wiederanders,B. and Brauer,R. Cathepsin K deficiency partially inhibits, but does not prevent, bone destruction in human tumor necrosis factor-transgenic mice Arthritis Rheum (2008) 58, 422-434. PubMed Europe PubMed DOI K
Simpson,S.J. T cell role for cathepsin K Sci Signal (2008) 1, ec49-ec49. DOI
Srivastava,M., Steinwede,K., Kiviranta,R., Morko,J., Hoymann,H.G., Langer,F., Buhling,F., Welte,T. and Maus,U.A. Overexpression of cathepsin K in mice decreases collagen deposition and lung resistance in response to bleomycin-induced pulmonary fibrosis Respir Res (2008) 9, 54-54. PubMed Europe PubMed DOI PMC EPMC U
Stoch,S.A. and Wagner,J.A. Cathepsin K inhibitors: a novel target for osteoporosis therapy Clin Pharmacol Ther (2008) 83, 172-176. PubMed Europe PubMed DOI V
Tada,S., Tsutsumi,K., Ishihara,H., Suzuki,K., Gohda,K. and Teno,N. Species differences between human and rat in the substrate specificity of cathepsin K J Biochem (2008) 144, 499-506. PubMed Europe PubMed DOI P
Teno,N., Irie,O., Miyake,T., Gohda,K., Horiuchi,M., Tada,S., Nonomura,K., Kometani,M., Iwasaki,G. and Betschart,C. New chemotypes for cathepsin K inhibitors Bioorg Med Chem Lett (2008) 18, 2599-2603. PubMed Europe PubMed DOI I
Teno,N., Masuya,K., Ehara,T., Kosaka,T., Miyake,T., Irie,O., Hitomi,Y., Matsuura,N., Umemura,I., Iwasaki,G., Fukaya,H., Toriyama,K., Uchiyama,N., Nonomura,K., Sugiyama,I. and Kometani,M. Effect of cathepsin K inhibitors on bone resorption J Med Chem (2008) 51, 5459-5462. PubMed Europe PubMed DOI I
Yang,M., Sun,J., Zhang,T., Liu,J., Zhang,J., Shi,M.A., Darakhshan,F., Guerre-Millo,M., Clement,K., Gelb,B.D., Dolgnov,G. and Shi,G.P. Deficiency and inhibition of cathepsin K reduce body weight gain and increase glucose metabolism in mice Arterioscler Thromb Vasc Biol (2008) 28, 2202-2208. PubMed Europe PubMed DOI PMC EPMC

2007

Altmann,E., Aichholz,R., Betschart,C., Buhl,T., Green,J., Irie,O., Teno,N., Lattmann,R., Tintelnot-Blomley,M. and Missbach,M. 2-Cyano-pyrimidines: a new chemotype for inhibitors of the cysteine protease cathepsin K J Med Chem (2007) 50, 591-594. PubMed Europe PubMed DOI I
[YEAR:1-1-2007]Barrett,D.G., Catalano,J.G., Deaton,D.N., Long,S.T., McFadyen,R.B., Miller,A.B., Miller,L.R., Samano,V., Tavares,F.X., Wells-Knecht,K.J., Wright,L.L. and Zhou,H.Q. Acyclic, orally bioavailable ketone-based cathepsin K inhibitors Bioorg Med Chem Lett (1-1-2007) 17, 22-27. PubMed Europe PubMed DOI I
Cameron Black,W. and David Percival,M. Chapter 8 Cathepsin K Inhibitors Annu Rep Med Chem (2007) 42, 111-127. DOI V
Chen,W., Yang,S., Abe,Y., Li,M., Wang,Y., Shao,J., Li,E. and Li,Y.P. Novel pycnodysostosis mouse model uncovers cathepsin K function as a potential regulator of osteoclast apoptosis and senescence Hum Mol Genet (2007) 16, 410-423. PubMed Europe PubMed DOI T
Funicello,M., Novelli,M., Ragni,M., Vottari,T., Cocuzza,C., Soriano-Lopez,J., Chiellini,C., Boschi,F., Marzola,P., Masiello,P., Saftig,P., Santini,F., St-Jacques,R., Desmarais,S., Morin,N., Mancini,J., Percival,M.D., Pinchera,A. and Maffei,M. Cathepsin K null mice show reduced adiposity during the rapid accumulation of fat stores PLoS ONE (2007) 2, e683-e683. PubMed Europe PubMed DOI PMC EPMC K
Jaffer,F.A., Kim,D.E., Quinti,L., Tung,C.H., Aikawa,E., Pande,A.N., Kohler,R.H., Shi,G.P., Libby,P. and Weissleder,R. Optical visualization of cathepsin K activity in atherosclerosis with a novel, protease-activatable fluorescence sensor Circulation (2007) 115, 2292-2298. PubMed Europe PubMed DOI L
Kumar,S., Dare,L., Vasko-Moser,J.A., James,I.E., Blake,S.M., Rickard,D.J., Hwang,S.M., Tomaszek,T., Yamashita,D.S., Marquis,R.W., Oh,H., Jeong,J.U., Veber,D.F., Gowen,M., Lark,M.W. and Stroup,G. A highly potent inhibitor of cathepsin K (relacatib) reduces biomarkers of bone resorption both in vitro and in an acute model of elevated bone turnover in vivo in monkeys Bone (2007) 40, 122-131. PubMed Europe PubMed DOI I
Le Gall,C., Bellahcene,A., Bonnelye,E., Gasser,J.A., Castronovo,V., Green,J., Zimmermann,J. and Clezardin,P. A cathepsin K inhibitor reduces breast cancer induced osteolysis and skeletal tumor burden Cancer Res (2007) 67, 9894-9902. PubMed Europe PubMed DOI I
Lecaille,F., Vandier,C., Godat,E., Herve-Grepinet,V., Bromme,D. and Lalmanach,G. Modulation of hypotensive effects of kinins by cathepsin K Arch Biochem Biophys (2007) 459, 129-136. PubMed Europe PubMed DOI
Leger,S., Bayly,C.I., Black,W.C., Desmarais,S., Falgueyret,J.P., Masse,F., Percival,M.D. and Truchon,J.F. Primary amides as selective inhibitors of cathepsin K Bioorg Med Chem Lett (2007) 17, 4328-4332. PubMed Europe PubMed DOI I
Ma,S., Devi-Kesavan,L.S. and Gao,J. Molecular dynamics simulations of the catalytic pathway of a cysteine protease: a combined QM/MM study of human cathepsin K J Am Chem Soc (2007) 129, 13633-13645. PubMed Europe PubMed DOI PMC EPMC
Pang,M., Martinez,A.F., Fernandez,I., Balkan,W. and Troen,B.R. AP-1 stimulates the cathepsin K promoter in RAW 264.7 cells Gene (2007) 403, 151-158. PubMed Europe PubMed DOI
Podgorski,I., Linebaugh,B.E. and Sloane,B.F. Cathepsin K in the bone microenvironment: link between obesity and prostate cancer? Biochem Soc Trans (2007) 35, 701-703. PubMed Europe PubMed DOI
Robichaud,J., Bayly,C.I., Black,W.C., Desmarais,S., Leger,S., Masse,F., McKay,D.J., Oballa,R.M., Paquet,J., Percival,M.D., Truchon,J.F., Wesolowski,G. and Crane,S.N. beta-Substituted cyclohexanecarboxamide cathepsin K inhibitors: modification of the 1,2-disubstituted aromatic core Bioorg Med Chem Lett (2007) 17, 3146-3151. PubMed Europe PubMed DOI I
Ruettger,A. and Wiederanders,B. Microplate assay for cathepsin detection in viable cells using derivatives of 4-methoxy-beta-naphthylamide Curr Protoc Protein Sci (2007) Unit 21.21, Unit 21.21- PubMed Europe PubMed DOI A
Runger,T.M., Quintanilla-Dieck,M.J. and Bhawan,J. Role of cathepsin K in the turnover of the dermal extracellular matrix during scar formation J Invest Dermatol (2007) 127, 293-297. PubMed Europe PubMed DOI
Salminen-Mankonen,H.J., Morko,J. and Vuorio,E. Role of cathepsin K in normal joints and in the development of arthritis Curr Drug Targets (2007) 8, 315-323. PubMed Europe PubMed DOI T
Schilling,A.F., Mulhausen,C., Lehmann,W., Santer,R., Schinke,T., Rueger,J.M. and Amling,M. High bone mineral density in pycnodysostotic patients with a novel mutation in the propeptide of cathepsin K Osteoporos Int (2007) 18, 659-669. PubMed Europe PubMed DOI M
Selent,J., Kaleta,J., Li,Z., Lalmanach,G. and Bromme,D. Selective inhibition of the collagenase activity of cathepsin K J Biol Chem (2007) 282, 16492-16501. PubMed Europe PubMed DOI I
Taillier,C., Hameury,T., Bellosta,V. and Cossy,J. Synthesis of 3-oxooxa- and 3-oxoazacycloalk-4-enes by ring-closing metathesis. Application to the synthesis of an inhibitor of cathepsin K Tetrahedron (2007) 63, 4472-4490. DOI I
Teno,N., Miyake,T., Ehara,T., Irie,O., Sakaki,J., Ohmori,O., Gunji,H., Matsuura,N., Masuya,K., Hitomi,Y., Nonomura,K., Horiuchi,M., Gohda,K., Iwasaki,A., Umemura,I., Tada,S., Kometani,M., Iwasaki,G., Cowan-Jacob,S.W., Missbach,M., Lattmann,R. and Betschart,C. Novel scaffold for cathepsin K inhibitors Bioorg Med Chem Lett (2007) 17, 6096-6100. PubMed Europe PubMed DOI I
Xiang,A., Kanematsu,M., Kumar,S., Yamashita,D., Kaise,T., Kikkawa,H., Asano,S. and Kinoshita,M. Changes in micro-CT 3D bone parameters reflect effects of a potent cathepsin K inhibitor (SB-553484) on bone resorption and cortical bone formation in ovariectomized mice Bone (2007) 40, 1231-1237. PubMed Europe PubMed DOI I

2006

[YEAR:13-11-2006]Adkison,K.K., Barrett,D.G., Deaton,D.N., Gampe,R.T., Hassell,A.M., Long,S.T., McFadyen,R.B., Miller,A.B., Miller,L.R., Payne,J.A., Shewchuk,L.M., Wells-Knecht,K.J., Willard,D.H., Jr. and Wright,L.L. Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors? Bioorg Med Chem Lett (13-11-2006) 16, 978-983. PubMed Europe PubMed DOI I
[YEAR:22-6-2006]Avnet,S., Lamolinara,A., Zini,N., Solimando,L., Quacquaruccio,G., Granchi,D., Maraldi,N.M., Giunti,A. and Baldini,N. Effects of antisense mediated inhibition of cathepsin K on human osteoclasts obtained from peripheral blood J Orthop Res (22-6-2006) 24, 1699-1708. PubMed Europe PubMed DOI
Baird,I.R., Mosi,R., Olsen,M., Cameron,B.R., Fricker,S.P. and Skerlj,R.T. '3 + 1' mixed-ligand oxorhenium(V) complexes and their inhibition of the cysteine proteases cathepsin B and cathepsin K Inorganica Chimica Acta (2006) 359, 2736-2750. I
[YEAR:20-12-2006]Barrett,D.G., Catalano,J.G., Deaton,D.N., Hassell,A.M., Long,S.T., Miller,A.B., Miller,L.R., Ray,J.A., Samano,V., Shewchuk,L.M., Wells-Knecht,K.J., Willard,D.H., Jr. and Wright,L.L. Novel, potent P2-P3 pyrrolidine derivatives of ketoamide-based cathepsin K inhibitors Bioorg Med Chem Lett (20-12-2006) 16, 1735-1739. PubMed Europe PubMed DOI I
[YEAR:6-3-2006]Choe,Y., Leonetti,F., Greenbaum,D.C., Lecaille,F., Bogyo,M., Bromme,D., Ellman,J.A. and Craik,C.S. Substrate profiling of cysteine proteases using a combinatorial peptide library identifies functionally unique specificities J Biol Chem (6-3-2006) 281, 12824-12832. PubMed Europe PubMed DOI P
[YEAR:9-2-2006]Crane,S.N., Black,W.C., Palmer,J.T., Davis,D.E., Setti,E., Robichaud,J., Paquet,J., Oballa,R.M., Bayly,C.I., McKay,D.J., Somoza,J.R., Chauret,N., Seto,C., Scheigetz,J., Wesolowski,G., Masse,F., Desmarais,S. and Ouellet,M. beta-Substituted cyclohexanecarboxamide: a nonpeptidic framework for the design of potent inhibitors of cathepsin K J Med Chem (9-2-2006) 49, 1066-1079. PubMed Europe PubMed DOI I
[YEAR:12-5-2006]Kim,M.K., Kim,H.D., Park,J.H., Lim,J.I., Yang,J.S., Kwak,W.Y., Sung,S.Y., Kim,H.J., Kim,S.H., Lee,C.H., Shim,J.Y., Bae,M.H., Shin,Y.A., Huh,Y., Han,T.D., Chong,W., Choi,H., Ahn,B.N., Yang,S.O. and Son,M.H. An orally active cathepsin K inhibitor, furan-2-carboxylic acid, 1-{1-[4-fluoro-2-(2-oxo-pyrrolidin-1-yl)-phenyl]-3-oxo-piperidin-4-ylcarb amoyl}-cyclohexyl)-amide (OST-4077), inhibits osteoclast activity in vitro and bone loss in ovariectomized rats J Pharmacol Exp Ther (12-5-2006) 318, 555-562. PubMed Europe PubMed DOI I
Kim,T.S. and Tasker,A.S. Non-covalent cathepsin K inhibitors for the treatment of osteoporosis Curr Top Med Chem (2006) 6, 355-360. PubMed Europe PubMed DOI I
[YEAR:15-4-2006]Lange,A.W. and Yutzey,K.E. NFATc1 expression in the developing heart valves is responsive to the RANKL pathway and is required for endocardial expression of cathepsin K Dev Biol (15-4-2006) 292, 407-417. PubMed Europe PubMed DOI
[YEAR:12-1-2006]Li,C.S., Deschenes,D., Desmarais,S., Falgueyret,J.P., Gauthier,J.Y., Kimmel,D.B., Leger,S., Masse,F., McGrath,M.E., McKay,D.J., Percival,M.D., Riendeau,D., Rodan,S.B., Therien,M., Truong,V.L., Wesolowski,G., Zamboni,R. and Black,W.C. Identification of a potent and selective non-basic cathepsin K inhibitor Bioorg Med Chem Lett (12-1-2006) 16, 1985-1989. PubMed Europe PubMed DOI I
Li,C.Y., Jepsen,K.J., Majeska,R.J., Zhang,J., Ni,R., Gelb,B.D. and Schaffler,M.B. Mice lacking cathepsin K maintain bone remodeling but develop bone fragility despite high bone mass J Bone Miner Res (2006) 21, 865-875. PubMed Europe PubMed DOI K
Linke,M., Gordon,R.E., Brillard,M., Lecaille,F., Lalmanach,G. and Bromme,D. Degradation of apolipoprotein B-100 by lysosomal cysteine cathepsins Biol Chem (2006) 387, 1295-1303. PubMed Europe PubMed DOI P
[YEAR:19-12-2006]Lutgens,E., Lutgens,S.P., Faber,B.C., Heeneman,S., Gijbels,M.M., de Winther,M.P., Frederik,P., van der Made,I., Daugherty,A., Sijbers,A.M., Fisher,A., Long,C.J., Saftig,P., Black,D., Daemen,M.J. and Cleutjens,K.B. Disruption of the cathepsin K gene reduces atherosclerosis progression and induces plaque fibrosis but accelerates macrophage foam cell formation Circulation (19-12-2006) 113, 98-107. PubMed Europe PubMed DOI K
[YEAR:14-9-2006]Lutgens,S.P., Kisters,N., Lutgens,E., van Haaften,R.I., Evelo,C.T., de Winther,M.P., Saftig,P., Daemen,M.J., Heeneman,S. and Cleutjens,K.B. Gene profiling of cathepsin K deficiency in atherogenesis: profibrotic but lipogenic J Pathol (14-9-2006) 210, 334-343. PubMed Europe PubMed DOI K
[YEAR:3-12-2006]Mandelin,J., Hukkanen,M., Li,T.F., Korhonen,M., Liljestrom,M., Sillat,T., Hanemaaijer,R., Salo,J., Santavirta,S. and Konttinen,Y.T. Human osteoblasts produce cathepsin K Bone (3-12-2006) 38, 769-777. PubMed Europe PubMed DOI
McIntyre,J.A., Serradell,N. and Bolos,J. Relacatib: prevention and treatment of bone metastases treatment of osteoarthritis treatment of osteoporosis cathepsin K inhibitor Drugs Future (2006) 31, 406-411. DOI I
Meier,C., Meinhardt,U., Greenfield,J.R., De Winter,J., Nguyen,T.V., Dunstan,C.R. and Seibel,M.J. Serum cathepsin K concentrations reflect osteoclastic activity in women with postmenopausal osteoporosis and patients with Paget's disease Clin Lab (2006) 52, 1-10. PubMed Europe PubMed
[YEAR:17-3-2006]Palmer,J.T., Hirschbein,B.L., Cheung,H., McCarter,J., Janc,J.W., Yu,Z.W. and Wesolowski,G. Keto-1,3,4-oxadiazoles as cathepsin K inhibitors Bioorg Med Chem Lett (17-3-2006) 16, 2909-2914. PubMed Europe PubMed DOI I
Pan,H., Kopeckova,P., Wang,D., Yang,J., Miller,S. and Kopecek,J. Water-soluble HPMA copolymer - prostaglandin E1 conjugates containing a cathepsin K sensitive spacer J Drug Target (2006) 14, 425-435. PubMed Europe PubMed DOI
[YEAR:21-12-2006]Pan,X., Tan,N., Zeng,G., Han,H. and Huang,H. 3D-QSAR and docking studies of aldehyde inhibitors of human cathepsin K Bioorg Med Chem (21-12-2006) 14, 2771-2778. PubMed Europe PubMed DOI I
[YEAR:26-5-2006]Roy,A., Gosselin,F., O'Shea,P.D. and Chen,C.Y. Diastereoselective arylithium addition to an alpha-trifluoromethyl imine. Practical synthesis of a potent cathepsin K inhibitor J Org Chem (26-5-2006) 71, 4320-4323. PubMed Europe PubMed DOI I
Ruttger,A., Mollenhauer,J., Loser,R., Gutschow,M. and Wiederanders,B. Microplate assay for quantitative determination of cathepsin activities in viable cells using derivatives of 4-methoxy-beta-naphthylamide Biotechniques (2006) 41, 469-473. PubMed Europe PubMed DOI A
[YEAR:1-6-2006]Setti,E.L., Venkatraman,S., Palmer,J.T., Xie,X., Cheung,H., Yu,W., Wesolowski,G. and Robichaud,J. Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K Bioorg Med Chem Lett (1-6-2006) 16, 4296-4299. PubMed Europe PubMed DOI I
[YEAR:24-12-2006]Shinozuka,T., Shimada,K., Matsui,S., Yamane,T., Ama,M., Fukuda,T., Taki,M. and Naito,S. 4-Aminophenoxyacetic acids as a novel class of reversible cathepsin K inhibitors Bioorg Med Chem Lett (24-12-2006) 16, 1502-1505. PubMed Europe PubMed DOI I
[YEAR:6-7-2006]Shinozuka,T., Shimada,K., Matsui,S., Yamane,T., Ama,M., Fukuda,T., Taki,M., Takeda,Y., Otsuka,E., Yamato,M. and Naito,S. Arylamine based cathepsin K inhibitors: Investigating P3 heterocyclic substituents Bioorg Med Chem (6-7-2006) 14, 6807-6819. PubMed Europe PubMed DOI I
[YEAR:12-7-2006]Shinozuka,T., Shimada,K., Matsui,S., Yamane,T., Ama,M., Fukuda,T., Taki,M., Takeda,Y., Otsuka,E., Yamato,M., Mochizuki,S., Ohhata,K. and Naito,S. Potent and selective cathepsin K inhibitors Bioorg Med Chem (12-7-2006) 14, 6789-6806. PubMed Europe PubMed DOI I
Taillier,C., Hameury,T., Bellosta,V. and Cossy,J. Synthesis of 3-oxoazacyclohept-4-enes by ring-closing metathesis. Application to the synthesis of an inhibitor of cathepsin K Heterocycles (2006) 67, 549-+.
Troen,B.R. The regulation of cathepsin K gene expression Ann N Y Acad Sci (2006) 1068, 165-172. PubMed Europe PubMed DOI
[YEAR:28-9-2006]Urbina,H.D., Debaene,F., Jost,B., Bole-Feysot,C., Mason,D.E., Kuzmic,P., Harris,J.L. and Winssinger,N. Self-assembled small-molecule microarrays for protease screening and profiling Chembiochem (28-9-2006) 7, 1790-1797. PubMed Europe PubMed DOI I
[YEAR:15-8-2006]Xiao,Y., Junfeng,H., Tianhong,L., Lu,W., Shulin,C., Yu,Z., Xiaohua,L., Weixia,J., Sheng,Z., Yanyun,G., Guo,L. and Min,L. Cathepsin K in adipocyte differentiation and its potential role in the pathogenesis of obesity J Clin Endocrinol Metab (15-8-2006) 91, 4520-4527. PubMed Europe PubMed DOI
[YEAR:9-3-2006]Yamashita,D.S., Marquis,R.W., Xie,R., Nidamarthy,S.D., Oh,H.J., Jeong,J.U., Erhard,K.F., Ward,K.W., Roethke,T.J., Smith,B.R., Cheng,H.Y., Geng,X., Lin,F., Offen,P.H., Wang,B., Nevins,N., Head,M.S., Haltiwanger,R.C., Narducci Sarjeant,A.A., Liable-Sands,L.M., Zhao,B., Smith,W.W., Janson,C.A., Gao,E., Tomaszek,T., McQueney,M., James,I.E., Gress,C.J., Zembryki,D.L., Lark,M.W. and Veber,D.F. Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors J Med Chem (9-3-2006) 49, 1597-1612. PubMed Europe PubMed DOI I
[YEAR:5-7-2006]Zeng,G.Z., Pan,X.L., Tan,N.H., Xiong,J. and Zhang,Y.M. Natural biflavones as novel inhibitors of cathepsin B and K Eur J Med Chem (5-7-2006) 41, 1247-1252. PubMed Europe PubMed DOI I

2005

[YEAR:2-5-2005]Barrett,D.G., Catalano,J.G., Deaton,D.N., Long,S.T., McFadyen,R.B., Miller,A.B., Miller,L.R., Wells-Knecht,K.J. and Wright,L.L. A structural screening approach to ketoamide-based inhibitors of cathepsin K Bioorg Med Chem Lett (2-5-2005) 15, 2209-2213. PubMed Europe PubMed DOI I
[YEAR:15-6-2005]Barrett,D.G., Deaton,D.N., Hassell,A.M., McFadyen,R.B., Miller,A.B., Miller,L.R., Payne,J.A., Shewchuk,L.M., Willard,D.H., Jr. and Wright,L.L. Acyclic cyanamide-based inhibitors of cathepsin K Bioorg Med Chem Lett (15-6-2005) 15, 3039-3043. PubMed Europe PubMed DOI I
Barrett,D.G., Boncek,V.M., Catalano,J.G., Deaton,D.N., Hassell,A.M., Jurgensen,C.H., Long,S.T., McFadyen,R.B., Miller,A.B., Miller,L.R., Payne,J.A., Ray,J.A., Samano,V., Shewchuk,L.M., Tavares,F.X., Wells-Knecht,K.J., Willard,D.H., Jr., Wright,L.L. and Zhou,H.Q. P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K Bioorg Med Chem Lett (2005) 15, 3540-3546. PubMed Europe PubMed DOI I
[YEAR:1-11-2005]Black,W.C., Bayly,C.I., Davis,D.E., Desmarais,S., Falgueyret,J.P., Leger,S., Li,C.S., Masse,F., McKay,D.J., Palmer,J.T., Percival,M.D., Robichaud,J., Tsou,N. and Zamboni,R. Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K Bioorg Med Chem Lett (1-11-2005) 15, 4741-4744. PubMed Europe PubMed DOI I
Cai,J.Q., Jamieson,C., Moir,J. and Rankovic,Z. Cathepsin K inhibitors, 2000-2004 Expert Opin Ther Pat (2005) 15, 33-48. V
[YEAR:1-4-2005]Deaton,D.N., Hassell,A.M., McFadyen,R.B., Miller,A.B., Miller,L.R., Shewchuk,L.M., Tavares,F.X., Willard,D.H., Jr. and Wright,L.L. Novel and potent cyclic cyanamide-based cathepsin K inhibitors Bioorg Med Chem Lett (1-4-2005) 15, 1815-1819. PubMed Europe PubMed DOI S I
Deaton,D.N. and Tavares,F.X. Design of cathepsin K inhibitors for osteoporosis Curr Top Med Chem (2005) 5, 1639-1675. PubMed Europe PubMed DOI V I
[YEAR:1-12-2005]Falgueyret,J.P., Desmarais,S., Oballa,R., Black,W.C., Cromlish,W., Khougaz,K., Lamontagne,S., Masse,F., Riendeau,D., Toulmond,S. and Percival,M.D. Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity J Med Chem (1-12-2005) 48, 7535-7543. PubMed Europe PubMed DOI I
Grabowskal,U., Chambers,T.J. and Shiroo,M. Recent developments in cathepsin K inhibitor design Curr Opin Drug Discov Devel (2005) 8, 619-630. PubMed Europe PubMed V
Holzer,G., Noske,H., Lang,T., Holzer,L. and Willinger,U. Soluble cathepsin K: a novel marker for the prediction of nontraumatic fractures? J Lab Clin Med (2005) 146, 13-17. PubMed Europe PubMed DOI
[YEAR:31-5-2005]Kerschan-Schindl,K., Hawa,G., Kudlacek,S., Woloszczuk,W. and Pietschmann,P. Serum levels of cathepsin K decrease with age in both women and men Exp Gerontol (31-5-2005) 40, 532-535. PubMed Europe PubMed DOI
Kiviranta,R., Morko,J., Alatalo,S.L., NicAmhlaoibh,R., Risteli,J., Laitala-Leinonen,T. and Vuorio,E. Impaired bone resorption in cathepsin K-deficient mice is partially compensated for by enhanced osteoclastogenesis and increased expression of other proteases via an increased RANKL/OPG ratio Bone (2005) 36, 159-172. PubMed Europe PubMed DOI
[YEAR:1-6-2005]Ljusberg,J., Wang,Y., Lang,P., Norgard,M., Dodds,R., Hultenby,K., Ek-Rylander,B. and Andersson,G. Proteolytic excision of a repressive loop domain in tartrate-resistant acid phosphatase by cathepsin K in osteoclasts J Biol Chem (1-6-2005) 280, 28370-28381. PubMed Europe PubMed DOI
Morko,J., Kiviranta,R., Hurme,S., Rantakokko,J. and Vuorio,E. Differential turnover of cortical and trabecular bone in transgenic mice overexpressing cathepsin K Bone (2005) 36, 854-865. PubMed Europe PubMed DOI
Morko,J., Kiviranta,R., Joronen,K., Saamanen,A.M., Vuorio,E. and Salminen-Mankonen,H. Spontaneous development of synovitis and cartilage degeneration in transgenic mice overexpressing cathepsin K Arthritis Rheum (2005) 52, 3713-3717. PubMed Europe PubMed DOI K
[YEAR:1-12-2005]Palmer,J.T., Bryant,C., Wang,D.X., Davis,D.E., Setti,E.L., Rydzewski,R.M., Venkatraman,S., Tian,Z.Q., Burrill,L.C., Mendonca,R.V., Springman,E., McCarter,J., Chung,T., Cheung,H., Janc,J.W., McGrath,M., Somoza,J.R., Enriquez,P., Yu,Z.W., Strickley,R.M., Liu,L., Venuti,M.C., Percival,M.D., Falgueyret,J.P., Prasit,P., Oballa,R., Riendeau,D., Young,R.N., Wesolowski,G., Rodan,S.B., Johnson,C., Kimmel,D.B. and Rodan,G. Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K J Med Chem (1-12-2005) 48, 7520-7534. PubMed Europe PubMed DOI S I
[YEAR:7-9-2005]Selinger,C.I., Day,C.J. and Morrison,N.A. Optimized transfection of diced siRNA into mature primary human osteoclasts: inhibition of cathepsin K mediated bone resorption by siRNA J Cell Biochem (7-9-2005) 96, 996-1002. PubMed Europe PubMed DOI
[YEAR:1-3-2005]Setti,E.L., Davis,D., Janc,J.W., Jeffery,D.A., Cheung,H. and Yu,W. 3,4-Disubstituted azetidinones as selective inhibitors of the cysteine protease cathepsin K. Exploring P3 elements for potency and selectivity Bioorg Med Chem Lett (1-3-2005) 15, 1529-1534. PubMed Europe PubMed DOI I
Skoumal,M., Haberhauer,G., Kolarz,G., Hawa,G., Woloszczuk,W. and Klingler,A. Serum cathepsin K levels of patients with longstanding rheumatoid arthritis: correlation with radiological destruction Arthritis Res Ther (2005) 7, R65-R70. PubMed Europe PubMed DOI PMC EPMC
[YEAR:18-4-2005]Trout,R.E.L. and Marquis,R.W. Asymmetric synthesis of a potent azepanone-based inhibitor of the cysteine protease cathepsin K Tetrahedron Lett (18-4-2005) 46, 2799-2801. I
[YEAR:1-3-2005]Wang,Y., Benn,A., Flinn,N., Monk,T., Ramjee,M., Watts,J. and Quibell,M. cis-6-Oxo-hexahydro-2-oxa-1,4-diazapentalene and cis-6-oxo-hexahydropyrrolo[3,2-c]pyrazole based scaffolds: design rationale, synthesis and cysteinyl proteinase inhibition Bioorg Med Chem Lett (1-3-2005) 15, 1327-1331. PubMed Europe PubMed DOI I
Wieczerzak,E., Jankowska,E., Rodziewicz-Motowidlo,S., Gieldon,A., Lagiewka,J., Grzonka,Z., Abrahamson,M., Grubb,A. and Bromme,D. Novel azapeptide inhibitors of cathepsins B and K. Structural background to increased specificity for cathepsin B J Pept Res (2005) 66 Suppl 1, 1-11. PubMed Europe PubMed DOI I
Yasuda,Y., Kaleta,J. and Bromme,D. The role of cathepsins in osteoporosis and arthritis: rationale for the design of new therapeutics Adv Drug Deliv Rev (2005) 57, 973-993. PubMed Europe PubMed DOI T I

2004

[YEAR:18-11-2004]Altmann,E., Cowan-Jacob,S.W. and Missbach,M. Novel purine nitrile derived inhibitors of the cysteine protease cathepsin K J Med Chem (18-11-2004) 47, 5833-5836. PubMed Europe PubMed DOI S I
[YEAR:29-10-2004]Anway,M.D., Wright,W.W., Zirkin,B.R., Korah,N., Mort,J.S. and Hermo,L. Expression and localization of cathepsin K in adult rat Sertoli cells Biol Reprod (29-10-2004) 70, 562-569. PubMed Europe PubMed DOI
[YEAR:17-5-2004]Barrett,D.G., Catalano,J.G., Deaton,D.N., Long,S.T., Miller,L.R., Tavares,F.X., Wells-Knecht,K.J., Wright,L.L. and Zhou,H.Q. Orally bioavailable small molecule ketoamide-based inhibitors of cathepsin K Bioorg Med Chem Lett (17-5-2004) 14, 2543-2546. PubMed Europe PubMed DOI I
[YEAR:4-10-2004]Barrett,D.G., Catalano,J.G., Deaton,D.N., Hassell,A.M., Long,S.T., Miller,A.B., Miller,L.R., Shewchuk,L.M., Wells-Knecht,K.J., Willard,D.H., Jr. and Wright,L.L. Potent and selective P2-P3 ketoamide inhibitors of cathepsin K with good pharmacokinetic properties via favorable P1', P1, and/or P3 substitutions Bioorg Med Chem Lett (4-10-2004) 14, 4897-4902. PubMed Europe PubMed DOI I
[YEAR:5-7-2004]Boros,E.E., Deaton,D.N., Hassell,A.M., McFadyen,R.B., Miller,A.B., Miller,L.R., Paulick,M.G., Shewchuk,L.M., Thompson,J.B., Willard,D.H., Jr. and Wright,L.L. Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors Bioorg Med Chem Lett (5-7-2004) 14, 3425-3429. PubMed Europe PubMed DOI I
Bromme,D. Cathepsin K [ISSN:0-12-079610-4] (2004) 2, 1092-1097. V
Buhling,F., Rocken,C., Brasch,F., Hartig,R., Yasuda,Y., Saftig,P., Bromme,D. and Welte,T. Pivotal role of cathepsin K in lung fibrosis Am J Pathol (2004) 164, 2203-2216. PubMed Europe PubMed DOI PMC EPMC
[YEAR:9-2-2004]Catalano,J.G., Deaton,D.N., Long,S.T., McFadyen,R.B., Miller,L.R., Payne,J.A., Wells-Knecht,K.J. and Wright,L.L. Design of small molecule ketoamide-based inhibitors of cathepsin K Bioorg Med Chem Lett (9-2-2004) 14, 719-722. PubMed Europe PubMed DOI I
[YEAR:5-1-2004]Catalano,J.G., Deaton,D.N., Furfine,E.S., Hassell,A.M., McFadyen,R.B., Miller,A.B., Miller,L.R., Shewchuk,L.M., Willard,D.H., Jr. and Wright,L.L. Exploration of the P1 SAR of aldehyde cathepsin K inhibitors Bioorg Med Chem Lett (5-1-2004) 14, 275-278. PubMed Europe PubMed DOI I
Deaton,D.N. and Kumar,S. 6. Cathepsin K inhibitors: their potential as anti-osteoporosis agents Prog Med Chem (2004) 42, 245-375. PubMed Europe PubMed DOI
Fratzl-Zelman,N., Valenta,A., Roschger,P., Nader,A., Gelb,B.D., Fratzl,P. and Klaushofer,K. Decreased bone turnover and deterioration of bone structure in two cases of pycnodysostosis J Clin Endocrinol Metab (2004) 89, 1538-1547. PubMed Europe PubMed DOI M
[YEAR:20-7-2004]Godat,E., Lecaille,F., Desmazes,C., Duchene,S., Weidauer,E., Saftig,P., Bromme,D., Vandier,C. and Lalmanach,G. Cathepsin K: a cysteine protease with unique kinin-degrading properties Biochem J (20-7-2004) 383, 501-506. PubMed Europe PubMed DOI PMC EPMC
[YEAR:5-1-2004]Kim,T.S., Hague,A.B., Lee,T.I., Lian,B., Tegley,C.M., Wang,X., Burgess,T.L., Qian,Y.X., Ross,S., Tagari,P., Lin,C.H., Mayeda,C., Dao,J., Jordan,S., Mohr,C., Cheetham,J., Viswanadhan,V. and Tasker,A.S. (4-Piperidinylphenyl)aminoethyl amides as a novel class of non-covalent cathepsin K inhibitors Bioorg Med Chem Lett (5-1-2004) 14, 87-90. PubMed Europe PubMed DOI I
Lindeman,J.H., Hanemaaijer,R., Mulder,A., Dijkstra,P.D., Szuhai,K., Bromme,D., Verheijen,J.H. and Hogendoorn,P.C. Cathepsin K is the principal protease in giant cell tumor of bone Am J Pathol (2004) 165, 593-600. PubMed Europe PubMed DOI PMC EPMC
[YEAR:12-1-2004]Marquis,R.W., Ward,K.W., Roethke,T., Smith,B.R., Ru,Y., Yamashita,D.S., Tomaszek,T.A., Gorycki,P.D., Cheng,H.Y., James,I.E., Stroup,G.B., Lark,M.W., Gowen,M. and Veber,D.F. An azepanone-based inhibitor of human cathepsin K with improved oral bioavailability in the rat and the monkey Mol Pharm (12-1-2004) 1, 97-100. PubMed Europe PubMed I
Marquis,R.W. Inhibition of the cysteine protease cathepsin K (EC 3.4.22.38) Annu Rep Med Chem (2004) 39, 79-98. DOI V I
Morko,J.P., Soderstrom,M., Saamanen,A.M., Salminen,H.J. and Vuorio,E.I. Up regulation of cathepsin K expression in articular chondrocytes in a transgenic mouse model for osteoarthritis Ann Rheum Dis (2004) 63, 649-655. PubMed Europe PubMed DOI PMC EPMC
[YEAR:1-11-2004]Quibell,M., Benn,A., Flinn,N., Monk,T., Ramjee,M., Wang,Y. and Watts,J. Bicyclic peptidomimetic tetrahydrofuro[3,2-b]pyrrol-3-one and hexahydrofuro[3,2-b]pyridine-3-one based scaffolds: synthesis and cysteinyl proteinase inhibition Bioorg Med Chem (1-11-2004) 12, 5689-5710. PubMed Europe PubMed DOI I
[YEAR:16-8-2004]Robichaud,J., Bayly,C., Oballa,R., Prasit,P., Mellon,C., Falgueyret,J.P., Percival,M.D., Wesolowski,G. and Rodan,S.B. Rational design of potent and selective NH-linked aryl/heteroaryl cathepsin K inhibitors Bioorg Med Chem Lett (16-8-2004) 14, 4291-4295. PubMed Europe PubMed DOI I
[YEAR:29-1-2004]Tavares,F.X., Boncek,V., Deaton,D.N., Hassell,A.M., Long,S.T., Miller,A.B., Payne,A.A., Miller,L.R., Shewchuk,L.M., Wells-Knecht,K., Willard,D.H., Jr., Wright,L.L. and Zhou,H.Q. Design of potent, selective, and orally bioavailable inhibitors of cysteine protease cathepsin K J Med Chem (29-1-2004) 47, 588-599. PubMed Europe PubMed DOI I
[YEAR:7-10-2004]Tavares,F.X., Deaton,D.N., Miller,A.B., Miller,L.R., Wright,L.L. and Zhou,H.Q. Potent and selective ketoamide-based inhibitors of cysteine protease, cathepsin K J Med Chem (7-10-2004) 47, 5049-5056. PubMed Europe PubMed DOI I
[YEAR:7-10-2004]Tavares,F.X., Deaton,D.N., Miller,L.R. and Wright,L.L. Ketoamide-based inhibitors of cysteine protease, cathepsin K: P3 modifications J Med Chem (7-10-2004) 47, 5057-5068. PubMed Europe PubMed DOI I
Troen,B.R. The role of cathepsin K in normal bone resorption Drug News Perspect (2004) 17, 19-28. PubMed Europe PubMed DOI
[YEAR:11-6-2004]Wang,D., Li,W., Pechar,M., Kopeckova,P., Bromme,D. and Kopecek,J. Cathepsin K inhibitor-polymer conjugates: potential drugs for the treatment of osteoporosis and rheumatoid arthritis Int J Pharm (11-6-2004) 277, 73-79. PubMed Europe PubMed DOI I
Yamashita,D.S., Xie,R., Lin,H., Wang,B., Shi,S.D., Quinn,C.J., Hemling,M.E., Hissong,C., Tomaszek,T.A. and Veber,D.F. Benzodioxocin-3-ones and N-acyl-3-amino-3-buten-2-ones: novel classes of cathepsin K cysteine protease inhibitors J Pept Res (2004) 63, 265-269. PubMed Europe PubMed DOI I

2003

[YEAR:16-6-2003]Altmann,E., Green,J. and Tintelnot-Blomley,M. Arylaminoethyl amides as inhibitors of the cysteine protease cathepsin K - investigating P1' substituents Bioorg Med Chem Lett (16-6-2003) 13, 1997-2001. PubMed Europe PubMed DOI I
[YEAR:1-8-2003]Alves,M.F., Puzer,L., Cotrin,S.S., Juliano,M.A., Juliano,L., Bromme,D. and Carmona,A.K. S3 to S3' subsite specificity of recombinant human cathepsin K and development of selective internally quenched fluorescent substrates Biochem J (1-8-2003) 373, 981-986. PubMed Europe PubMed DOI PMC EPMC
Chiellini,C., Costa,M., Novelli,S.E., Amri,E.Z., Benzi,L., Bertacca,A., Cohen,P., Del Prato,S., Friedman,J.M. and Maffei,M. Identification of cathepsin K as a novel marker of adiposity in white adipose tissue J Cell Physiol (2003) 195, 309-321. PubMed Europe PubMed DOI
Desmazes,C., Galineau,L., Gauthier,F., Bromme,D. and Lalmanach,G. Kininogen-derived peptides for investigating the putative vasoactive properties of human cathepsins K and L Eur J Biochem (2003) 270, 171-178. PubMed Europe PubMed DOI
Everts,V., Hou,W.S., Rialland,X., Tigchelaar,W., Saftig,P., Bromme,D., Gelb,B.D. and Beertsen,W. Cathepsin K deficiency in pycnodysostosis results in accumulation of non-digested phagocytosed collagen in fibroblasts Calcif Tissue Int (2003) 73, 380-386. PubMed Europe PubMed DOI M
Hou,W.S., Li,Z., Buttner,F.H., Bartnik,E. and Bromme,D. Cleavage site specificity of cathepsin K toward cartilage proteoglycans and protease complex formation Biol Chem (2003) 384, 891-897. PubMed Europe PubMed DOI
[YEAR:15-10-2003]Lecaille,F., Weidauer,E., Juliano,M.A., Bromme,D. and Lalmanach,G. Probing cathepsin K activity with a selective substrate spanning its active site Biochem J (15-10-2003) 375, 307-312. PubMed Europe PubMed DOI PMC EPMC
[YEAR:30-12-2003]McGrath,M.E., Sprengeler,P.A., Hill,C.M., Martichonok,V., Cheung,H., Somoza,J.R., Palmer,J.T. and Janc,J.W. Peptide ketobenzoxazole inhibitors bound to cathepsin K Biochemistry (30-12-2003) 42, 15018-15028. PubMed Europe PubMed DOI S I
Okaji,M., Sakai,H., Sakai,E., Shibata,M., Hashimoto,F., Kobayashi,Y., Yoshida,N., Okamoto,K., Yamamoto,K. and Kato,Y. The regulation of bone resorption in tooth formation and eruption processes in mouse alveolar crest devoid of cathepsin K Jpn J Pharmacol (2003) 91, 285-294.
[YEAR:14-8-2003]Robichaud,J., Oballa,R., Prasit,P., Falgueyret,J.P., Percival,M.D., Wesolowski,G., Rodan,S.B., Kimmel,D., Johnson,C., Bryant,C., Venkatraman,S., Setti,E., Mendonca,R. and Palmer,J.T. A novel class of nonpeptidic biaryl inhibitors of human cathepsin K J Med Chem (14-8-2003) 46, 3709-3727. PubMed Europe PubMed DOI I
[YEAR:16-6-2003]Setti,E.L., Davis,D., Chung,T. and McCarter,J. 3,4-Disubstituted azetidinones as selective inhibitors of the cysteine protease cathepsin K. Exploring P2 elements for selectivity Bioorg Med Chem Lett (16-6-2003) 13, 2051-2053. PubMed Europe PubMed DOI I

2002

[YEAR:6-6-2002]Altmann,E., Renaud,J., Green,J., Farley,D., Cutting,B. and Jahnke,W. Arylaminoethyl amides as novel non-covalent cathepsin K inhibitors J Med Chem (6-6-2002) 45, 2352-2354. PubMed Europe PubMed DOI I
Gray,A.W., Davies,M.E. and Jeffcott,L.B. Localisation and activity of cathepsins K and B in equine osteoclasts Res Vet Sci (2002) 72, 95-103. PubMed Europe PubMed DOI
Hou,W.S., Li,W., Keyszer,G., Weber,E., Levy,R., Klein,M.J., Gravallese,E.M., Goldring,S.R. and Bromme,D. Comparison of cathepsins K and S expression within the rheumatoid and osteoarthritic synovium Arthritis Rheum (2002) 46, 663-674. PubMed Europe PubMed DOI
Hwang,H.S. and Chung,H.S. Preparation of active recombinant cathepsin K expressed in bacteria as inclusion body Protein Expr Purif (2002) 25, 541-546. PubMed Europe PubMed DOI E
Konttinen,Y.T., Mandelin,J., Li,T.F., Salo,J., Lassus,J., Liljestrom,M., Hukkanen,M., Takagi,M., Virtanen,I. and Santavirta,S. Acidic cysteine endoproteinase cathepsin K in the degeneration of the superficial articular hyaline cartilage in osteoarthritis Arthritis Rheum (2002) 46, 953-960. PubMed Europe PubMed DOI
Lark,M.W., Stroup,G.B., James,I.E., Dodds,R.A., Hwang,S.M., Blake,S.M., Lechowska,B.A., Hoffman,S.J., Smith,B.R., Kapadia,R., Liang,X., Erhard,K., Ru,Y., Dong,X., Marquis,R.W., Veber,D. and Gowen,M. A potent small molecule, nonpeptide inhibitor of cathepsin K (SB 331750) prevents bone matrix resorption in the ovariectomized rat Bone (2002) 30, 746-753. PubMed Europe PubMed DOI I
[YEAR:2-7-2002]Lecaille,F., Choe,Y., Brandt,W., Li,Z., Craik,C.S. and Bromme,D. Selective inhibition of the collagenolytic activity of human cathepsin K by altering its S2 subsite specificity Biochemistry (2-7-2002) 41, 8447-8454. PubMed Europe PubMed DOI
[YEAR:9-8-2002]Li,Z., Hou,W.S., Escalante-Torres,C.R., Gelb,B.D. and Bromme,D. Collagenase activity of cathepsin K depends on complex formation with chondroitin sulfate J Biol Chem (9-8-2002) 277, 28669-28676. PubMed Europe PubMed DOI
[YEAR:16-7-2002]Wang,D., Pechar,M., Li,W., Kopeckova,P., Bromme,D. and Kopecek,J. Inhibition of cathepsin K with lysosomotropic macromolecular inhibitors Biochemistry (16-7-2002) 41, 8849-8859. PubMed Europe PubMed DOI I

2001

Buhling,F., Reisenauer,A., Gerber,A., Kruger,S., Weber,E., Bromme,D., Roessner,A., Ansorge,S., Welte,T. and Rocken,C. Cathepsin K - a marker of macrophage differentiation? J Pathol (2001) 195, 375-382. PubMed Europe PubMed DOI
[YEAR:13-7-2001]Corisdeo,S., Gyda,M., Zaidi,M., Moonga,B.S. and Troen,B.R. New insights into the regulation of cathepsin K gene expression by osteoprotegerin ligand Biochem Biophys Res Commun (13-7-2001) 285, 335-339. PubMed Europe PubMed DOI
Dodds,R.A., James,I.E., Rieman,D., Ahern,R., Hwang,S.M., Connor,J.R., Thompson,S.D., Veber,D.F., Drake,F.H., Holmes,S., Lark,M.W. and Gowen,M. Human osteoclast cathepsin K is processed intracellularly prior to attachment and bone resorption J Bone Miner Res (2001) 16, 478-486. PubMed Europe PubMed DOI
Hansen,T., Otto,M., Gaumann,A., Eckardt,A., Petrow,P.K., Delank,K.S., Kirkpatrick,C.J. and Kriegsmann,J. Cathepsin K in aseptic hip prosthesis loosening: Expression in osteoclasts without polyethylene wear particles J Rheumatol (2001) 28, 1615-1619. PubMed Europe PubMed
Hou,W.S., Li,Z.Q., Gordon,R.E., Chan,K., Klein,M.J., Levy,R., Keysser,M., Keyszer,G. and Bromme,D. Cathepsin K is a critical protease in synovial fibroblast-mediated collagen degradation Am J Pathol (2001) 159, 2167-2177. PubMed Europe PubMed DOI PMC EPMC
[YEAR:13-4-2001]James,I.E., Marquis,R.W., Blake,S.M., Hwang,S.M., Gress,C.J., Ru,Y., Zembryki,D., Yamashita,D.S., McQueney,M.S., Tomaszek,T.A., Oh,H.J., Gowen,M., Veber,D.F. and Lark,M.W. Potent and selective cathepsin L inhibitors do not inhibit human osteoclast resorption in vitro J Biol Chem (13-4-2001) 276, 11507-11511. PubMed Europe PubMed DOI I
Kamolmatyakul,S., Chen,W. and Li,Y.P. Interferon-gamma down-regulates gene expression of cathepsin K in osteoclasts and inhibits osteoclast formation J Dent Res (2001) 80, 351-355. PubMed Europe PubMed
Kiviranta,R., Morko,J., Uusitalo,H., Aro,H.T., Vuorio,E. and Rantakokko,J. Accelerated turnover of metaphyseal trabecular bone in mice overexpressing cathepsin K J Bone Miner Res (2001) 16, 1444-1452. PubMed Europe PubMed DOI
[YEAR:26-4-2001]Marquis,R.W., Ru,Y., LoCastro,S.M., Zeng,J., Yamashita,D.S., Oh,H.J., Erhard,K.F., Davis,L.D., Tomaszek,T.A., Tew,D., Salyers,K., Proksch,J., Ward,K., Smith,B., Levy,M., Cummings,M.D., Haltiwanger,R.C., Trescher,G., Wang,B., Hemling,M.E., Quinn,C.J., Cheng,H.Y., Lin,F., Smith,W.W., Janson,C.A., Zhao,B., McQueney,M.S., D'Alessio,K., Lee,C.P., Marzulli,A., Dodds,R.A., Blake,S., Hwang,S.M., James,I.E., Gress,C.J., Bradley,B.R., Lark,M.W., Gowen,M. and Veber,D.F. Azepanone-based inhibitors of human and rat cathepsin K J Med Chem (26-4-2001) 44, 1380-1395. PubMed Europe PubMed DOI I
[YEAR:1-3-2001]Marquis,R.W., Ru,Y., Zeng,J., Trout,R.E., LoCastro,S.M., Gribble,A.D., Witherington,J., Fenwick,A.E., Garnier,B., Tomaszek,T., Tew,D., Hemling,M.E., Quinn,C.J., Smith,W.W., Zhao,B., McQueney,M.S., Janson,C.A., D'Alessio,K. and Veber,D.F. Cyclic ketone inhibitors of the cysteine protease cathepsin K J Med Chem (1-3-2001) 44, 725-736. PubMed Europe PubMed DOI I
[YEAR:8-5-2001]Motyckova,G., Weilbaecher,K.N., Horstmann,M., Rieman,D.J., Fisher,D.Z. and Fisher,D.E. Linking osteopetrosis and pycnodysostosis: regulation of cathepsin K expression by the microphthalmia transcription factor family Proc Natl Acad Sci U S A (8-5-2001) 98, 5798-5803. PubMed Europe PubMed DOI PMC EPMC
Rocken,C., Stix,B., Bromme,D., Ansorge,S., Roessner,A. and Buhling,F. A putative role for cathepsin K in degradation of AA and AL amyloidosis Am J Pathol (2001) 158, 1029-1038. PubMed Europe PubMed DOI PMC EPMC
[YEAR:1-6-2001]Sahara,T. and Sasaki,T. Effects of brefeldin-A: potent inhibitor of intracellular protein transport on ultrastructure and resorptive function of cultured osteoclasts Anat Rec (1-6-2001) 263, 127-138. PubMed Europe PubMed DOI
Stroup,G.B., Lark,M.W., Veber,D.F., Bhattacharyya,A., Blake,S., Dare,L.C., Erhard,K.F., Hoffman,S.J., James,I.E., Marquis,R.W., Ru,Y., Vasko-Moser,J.A., Smith,B.R., Tomaszek,T. and Gowen,M. Potent and selective inhibition of human cathepsin K leads to inhibition of bone resorption in vivo in a nonhuman primate J Bone Miner Res (2001) 16, 1739-1746. PubMed Europe PubMed DOI

2000

[YEAR:5-10-2000]Billington,C.J., Mason,P., Magny,M.C. and Mort,J.S. The slow-binding inhibition of cathepsin K by its propeptide Biochem Biophys Res Commun (5-10-2000) 276, 924-929. PubMed Europe PubMed DOI
[YEAR:15-9-2000]Claveau,D., Riendeau,D. and Mancini,J.A. Expression, maturation, and rhodamine-based fluorescence assay of human cathepsin K expressed in CHO cells Biochem Pharmacol (15-9-2000) 60, 759-769. PubMed Europe PubMed DOI A
Fujita,Y., Nakata,K., Yasui,N., Matsui,Y., Kataoka,E., Hiroshima,K., Shiba,R.I. and Ochi,T. Novel mutations of the cathepsin K gene in patients with pycnodysostosis and their characterization J Clin Endocrinol Metab (2000) 85, 425-431. PubMed Europe PubMed DOI K M
Guay,J., Falgueyret,J.P., Ducret,A., Percival,M.D. and Mancini,J.A. Potency and selectivity of inhibition of cathepsin K, L and S by their respective propeptides Eur J Biochem (2000) 267, 6311-6318. PubMed Europe PubMed DOI
Haagerup,A., Hertz,J.M., Christensen,M.F., Binderup,H. and Kruse,T.A. Cathepsin K gene mutations and 1q21 haplotypes in patients with pycnodysostosis in an outbred population Eur J Hum Genet (2000) 8, 431-436. PubMed Europe PubMed DOI M
Haeckel,C., Krueger,S., Kuester,D., Ostertag,H., Samii,M., Buehling,F., Broemme,D., Czerniak,B. and Roessner,A. Expression of cathepsin K in chordoma Hum Pathol (2000) 31, 834-840. PubMed Europe PubMed DOI
[YEAR:15-7-2000]Krupa,J.C. and Mort,J.S. Optimization of detergents for the assay of cathepsins B, L, S, and K Anal Biochem (15-7-2000) 283, 99-103. PubMed Europe PubMed DOI A
Saftig,P., Hunziker,E., Everts,V., Jones,S., Boyde,A., Wehmeyer,O., Suter,A. and von Figura,K. Functions of cathepsin K in bone resorption. Lessons from cathepsin K deficient mice Adv Exp Med Biol (2000) 477, 293-303. PubMed Europe PubMed DOI K
Yamashita,D.S. and Dodds,R.A. Cathepsin K and the design of inhibitors of cathepsin K Curr Pharm Des (2000) 6, 1-24. PubMed Europe PubMed I

1999

D'Alessio,K.J., McQueney,M.S., Brun,K.A., Orsini,M.J. and Debouck,C.M. Expression in Escherichia coli, refolding, and purification of human procathepsin K, an osteoclast-specific protease Protein Expr Purif (1999) 15, 213-220. PubMed Europe PubMed DOI E
[YEAR:19-7-1999]Duffy,K.J., Ridgers,L.H., DesJarlais,R.L., Tomaszek,T.A., Bossard,M.J., Thompson,S.K., Keenan,R.M. and Veber,D.F. Design and synthesis of diaminopyrrolidinone inhibitors of human osteoclast cathepsin K Bioorg Med Chem Lett (19-7-1999) 9, 1907-1910. PubMed Europe PubMed DOI I
Guay,J., Riendeau,D. and Mancini,J.A. Cloning and expression of rhesus monkey cathepsin K Bone (1999) 25, 205-209. PubMed Europe PubMed DOI
Hou,W.S., Bromme,D., Zhao,Y., Mehler,E., Dushey,C., Weinstein,H., Miranda,C.S., Fraga,C., Greig,F., Carey,J., Rimoin,D.L., Desnick,R.J. and Gelb,B.D. Characterization of novel cathepsin K mutations in the pro and mature polypeptide regions causing pycnodysostosis J Clin Invest (1999) 103, 731-738. PubMed Europe PubMed DOI PMC EPMC M
[YEAR:19-1-1999]LaLonde,J.M., Zhao,B., Janson,C.A., D'Alessio,K.J., McQueney,M.S., Orsini,M.J., Debouck,C.M. and Smith,W.W. The crystal structure of human procathepsin K Biochemistry (19-1-1999) 38, 862-869. PubMed Europe PubMed DOI
Li,Y.P. and Chen,W. Characterization of mouse cathepsin K gene, the gene promoter, and the gene expression J Bone Miner Res (1999) 14, 487-499. PubMed Europe PubMed DOI
Matsumoto,K., Mizoue,K., Kitamura,K., Tse,W.C., Huber,C.P. and Ishida,T. Structural basis of inhibition of cysteine proteases by E-64 and its derivatives Biopolymers (1999) 51, 99-107. PubMed Europe PubMed DOI I
[YEAR:13-4-1999]Nagler,D.K., Tam,W., Storer,A.C., Krupa,J.C., Mort,J.S. and Menard,R. Interdependency of sequence and positional specificities for cysteine proteases of the papain family Biochemistry (13-4-1999) 38, 4868-4874. PubMed Europe PubMed DOI
Rantakokko,J., Kiviranta,R., Eerola,R., Aro,H.T. and Vuorio,E. Complete genomic structure of the mouse cathepsin K gene (Ctsk) and its localization next to the Arnt gene on mouse chromosome 3 Matrix Biol (1999) 18, 155-161. PubMed Europe PubMed DOI
Sivaraman,J., Lalumiere,M., Menard,R. and Cygler,M. Crystal structure of wild-type human procathepsin K Protein Sci (1999) 8, 283-290. PubMed Europe PubMed DOI PMC EPMC S

1998

[YEAR:1-5-1998]Kafienah,W., Bromme,D., Buttle,D.J., Croucher,L.J. and Hollander,A.P. Human cathepsin K cleaves native type I and II collagens at the N-terminal end of the triple helix Biochem J (1-5-1998) 331, 727-732. PubMed Europe PubMed PMC EPMC
[YEAR:5-11-1998]LaLonde,J.M., Zhao,B., Smith,W.W., Janson,C.A., DesJarlais,R.L., Tomaszek,T.A., Carr,T.J., Thompson,S.K., Oh,H.J., Yamashita,D.S., Veber,D.F. and Abdel-Meguid,S.S. Use of papain as a model for the structure-based design of cathepsin K inhibitors: crystal structures of two papain-inhibitor complexes demonstrate binding to S'-subsites J Med Chem (5-11-1998) 41, 4567-4576. PubMed Europe PubMed DOI S I
[YEAR:10-9-1998]Marquis,R.W., Yamashita,D.S., Ru,Y., LoCastro,S.M., Oh,H.J., Erhard,K.F., DesJarlais,R.L., Head,M.S., Smith,W.W., Zhao,B., Janson,C.A., Abdel-Meguid,S.S., Tomaszek,T.A., Levy,M.A. and Veber,D.F. Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K J Med Chem (10-9-1998) 41, 3563-3567. PubMed Europe PubMed DOI I
[YEAR:10-11-1998]Saftig,P., Hunziker,E., Wehmeyer,O., Jones,S., Boyde,A., Rommerskirch,W., Moritz,J.D., Schu,P. and von Figura,K. Impaired osteoclastic bone resorption leads to osteopetrosis in cathepsin-K-deficient mice Proc Natl Acad Sci U S A (10-11-1998) 95, 13453-13458. PubMed Europe PubMed DOI PMC EPMC K
[YEAR:1-8-1998]Sukhova,G.K., Shi,G.P., Simon,D.I., Chapman,H.A. and Libby,P. Expression of the elastolytic cathepsins S and K in human atheroma and regulation of their production in smooth muscle cells J Clin Invest (1-8-1998) 102, 576-583. PubMed Europe PubMed DOI PMC EPMC
[YEAR:8-10-1998]Thompson,S.K., Smith,W.W., Zhao,B., Halbert,S.M., Tomaszek,T.A., Tew,D.G., Levy,M.A., Janson,C.A., DAlessio,K.J., McQueney,M.S., Kurdyla,J., Jones,C.S., DesJarlais,R.L., Abdel-Meguid,S.S. and Veber,D.F. Structure-based design of cathepsin K inhibitors containing a benzyloxy-substituted benzoyl peptidomimetic J Med Chem (8-10-1998) 41, 3923-3927. PubMed Europe PubMed DOI I

1997

Gowen,M. Inhibition of cathepsin K - a novel approach to antiresorptive therapy Expert Opin Investig Drugs (1997) 6, 1199-1202. PubMed Europe PubMed DOI V
Inui,T., Ishibashi,O., Inaoka,T., Origane,Y., Kumegawa,M., Kokubo,T. and Yamamura,T. Cathepsin K antisense oligodeoxynucleotide inhibits osteoclastic bone resorption J Biol Chem (1997) 272, 8109-8112. PubMed Europe PubMed DOI K
Linnevers,C.J., McGrath,M.E., Armstrong,R., Mistry,F.R., Barnes,M.G., Klaus,J.L., Palmer,J.T., Katz,B.A. and Bromme,D. Expression of human cathepsin K in Pichia pastoris and preliminary crystallographic studies of an inhibitor complex Protein Sci (1997) 6, 919-921. PubMed Europe PubMed DOI PMC EPMC E I
McGrath,M.E., Klaus,J.L., Barnes,M.G. and Bromme,D. Crystal structure of human cathepsin K complexed with a potent inhibitor Nat Struct Biol (1997) 4, 105-109. PubMed Europe PubMed DOI S I
McQueney,M.S., Amegadzie,B.Y., D'Alessio,K., Hanning,C.R., McLaughlin,M.M., McNulty,D., Carr,S.A., Ijames,C., Kurdyla,J. and Jones,C.S. Autocatalytic activation of human cathepsin K J Biol Chem (1997) 272, 13955-13960. PubMed Europe PubMed DOI
[YEAR:15-4-1997]Rood,J.A., Van Horn,S., Drake,F.H., Gowen,M. and Debouck,C. Genomic organization and chromosome localization of the human cathepsin K gene (CTSK) Genomics (15-4-1997) 41, 169-176. PubMed Europe PubMed DOI
[YEAR:23-12-1997]Thompson,S.K., Halbert,S.M., Bossard,M.J., Tomaszek,T.A., Levy,M.A., Zhao,B.G., Smith,W.W., bdel-Meguid,S.S., Janson,C.A., D'Alessio,K.J., McQueney,M.S., Amegadzie,B.Y., Hanning,C.R., DesJarlais,R.L., Briand,J., Sarkar,S.K., Huddleston,M.J., Ijames,C.F., Carr,S.A., Garnes,K.T., Shu,A., Heys,J.R., Bradbeer,J., Zembryki,D., Lee-Rykaczewski,L., James,I.E., Lark,M.W., Drake,F.H., Gowen,M., Gleason,J.G. and Veber,D.F. Design of potent and selective human cathepsin K inhibitors that span the active site Proc Natl Acad Sci U S A (23-12-1997) 94, 14249-14254. PubMed Europe PubMed DOI PMC EPMC I
Yamashita,D.S., Smith,W.W., Zhao,B., Janson,C.A., Tomaszek,T.A., Bossard,M.J., Levy,M.A., Oh,H.J., Carr,T.J., Thompson,S.K., Ijames,C.F., Carr,S.A., McQueney,M., D'Alesso,K.J., Amegadzie,B.Y., Hanning,C.R., Abdel-Meguid,S., DeJarlais,R.L., Gleason,J.G. and Veber,D.F. Structure and design of potent and selective cathepsin K inhibitors J Am Chem Soc (1997) 119, 11351-11352. DOI I
Zhao,B., Janson,C.A., Amegadzie,B.Y., D'Alessio,K., Griffin,C., Hanning,C.R., Jones,C., Kurdyla,J., McQueney,M., Qiu,X., Smith,W.W. and Abdel-Meguid,S.S. Crystal structure of human osteoclast cathepsin K complex with E-64 Nat Struct Biol (1997) 4, 109-111. PubMed Europe PubMed DOI S

1996

Aibe,K., Yazawa,H., Abe,K., Teramura,K., Kumegawa,M., Kawashima,H. and Honda,K. Substrate specificity of recombinant osteoclast-specific cathepsin K from rabbits Biol Pharm Bull (1996) 19, 1026-1031. PubMed Europe PubMed P
Bossard,M.J., Tomaszek,T.A., Thompson,S.K., Amegadzie,B.Y., Hanning,C.R., Jones,C., Kurdyla,J.T., McNulty,D.E., Drake,F.H., Gowen,M. and Levy,M.A. Proteolytic activity of human osteoclast cathepsin K. Expression, purification, activation, and substrate identification J Biol Chem (1996) 271, 12517-12524. PubMed Europe PubMed DOI I
Bromme,D., Klaus,J.L., Okamoto,K., Rasnick,D. and Palmer,J.T. Peptidyl vinyl sulphones: a new class of potent and selective cysteine protease inhibitors: S2P2 specificity of human cathepsin O2 in comparison with cathepsins S and L Biochem J (1996) 315, 85-89. PubMed Europe PubMed PMC EPMC I
Bromme,D., Okamoto,K., Wang,B.B. and Biroc,S. Human cathepsin O2, a matrix protein-degrading cysteine protease expressed in osteoclasts. Functional expression of human cathepsin O2 in Spodoptera frugiperda and characterization of the enzyme J Biol Chem (1996) 271, 2126-2132. PubMed Europe PubMed
Gelb,B.D., Shi,G.P., Chapman,H.A. and Desnick,R.J. Pycnodysostosis, a lysosomal disease caused by cathepsin K deficiency Science (1996) 273, 1236-1238. PubMed Europe PubMed M
Johnson,M.R., Polymeropoulos,M.H., Vos,H.L., Ortiz de Luna,R.I. and Francomano,C.A. A nonsense mutation in the cathepsin K gene observed in a family with pycnodysostosis Genome Res (1996) 6, 1050-1055. PubMed Europe PubMed K M
Rantakokko,J., Aro,H.T., Savontaus,M. and Vuorio,E. Mouse cathepsin K: cDNA cloning and predominant expression of the gene in osteoclasts, and in some hypertrophying chondrocytes during mouse development FEBS Lett (1996) 393, 307-313. PubMed Europe PubMed DOI

1995

Bromme,D. and Okamoto,K. Human cathepsin O2, a novel cysteine protease highly expressed in osteoclastomas and ovary molecular cloning, sequencing and tissue distribution Biol Chem Hoppe Seyler (1995) 376, 379-384. PubMed Europe PubMed
Gelb,B.D., Edelson,J.G. and Desnick,R.J. Linkage of pycnodysostosis to chromosome 1q21 by homozygosity mapping Nat Genet (1995) 10, 235-237. PubMed Europe PubMed DOI M
Inaoka,T., Bilbe,G., Ishibashi,O., Tezuka,K., Kumegawa,M. and Kokubo,T. Molecular cloning of human cDNA for cathepsin K: novel cysteine proteinase predominantly expressed in bone Biochem Biophys Res Commun (1995) 206, 89-96. PubMed Europe PubMed DOI
Li,Y.P., Alexander,M., Wucherpfennig,A.L., Yelick,P., Chen,W. and Stashenko,P. Cloning and complete coding sequence of a novel human cathepsin expressed in giant cells of osteoclastomas J Bone Miner Res (1995) 10, 1197-1202. PubMed Europe PubMed DOI
Polymeropoulos,M.H., Ortiz de Luna,R.I., Ide,S.E., Torres,R., Rubenstein,J. and Francomano,C.A. The gene for pycnodysostosis maps to human chromosome 1cen-q21 Nat Genet (1995) 10, 238-239. PubMed Europe PubMed DOI M
Shi,G.P., Chapman,H.A., Bhairi,S.M., DeLeeuw,C., Reddy,V.Y. and Weiss,S.J. Molecular cloning of human cathepsin O, a novel endoproteinase and homologue of rabbit OC2 FEBS Lett (1995) 357, 129-134. PubMed Europe PubMed DOI

1994

[YEAR:14-1-1994]Tezuka,K., Tezuka,Y., Maejima,A., Sato,T., Nemoto,K., Kamioka,H., Hakeda,Y. and Kumegawa,M. Molecular cloning of a possible cysteine proteinase predominantly expressed in osteoclasts J Biol Chem (14-1-1994) 269, 1106-1109. PubMed Europe PubMed

1985

Everts,V., Aronson,D.C. and Beertsen,W. Phagocytosis of bone collagen by osteoclasts in two cases of pycnodysostosis Calcif Tissue Int (1985) 37, 25-31. PubMed Europe PubMed M