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.)

2025

Brizuela,L., Buchet,R., Bougault,C. and Mebarek,S.
Cathepsin K Inhibitors as Potential Drugs for the Treatment of Osteoarthritis
Int J Mol Sci26, PubMed Europe PubMed DOI 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 Au5, 1104-1120. PubMed Europe PubMed DOI
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 PubMed Europe PubMed DOI 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 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 Ther16, 118-118. PubMed Europe PubMed DOI

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 Res35, 771-793. PubMed Europe PubMed DOI
Janin,Y.L.
On the origins of SARS-CoV-2 main protease inhibitors
RSC Med Chem15, 81-118. PubMed Europe PubMed DOI V I
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 Sci81, 205-205. PubMed Europe PubMed DOI
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 Sci25, PubMed Europe PubMed DOI
Moon,D.O.
Review of Cathepsin K Inhibitor Development and the Potential Role of Phytochemicals
Molecules30, PubMed Europe PubMed DOI V
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 Sci25, 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 Dis30, 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 Plus7, e10706-e10706. PubMed Europe PubMed DOI
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 Model63, 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 Alliance6, PubMed Europe PubMed DOI
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 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 Anim59, 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 Sci192, 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 Dis14, 366-366. PubMed Europe PubMed DOI 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)10, e2300217-e2300217. PubMed Europe PubMed DOI
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 Biol6, 450-450. 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 Invest132, PubMed Europe PubMed DOI
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 Dermatol21, 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 Muscle13, 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 Sci23, PubMed Europe PubMed DOI V
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 Sci23, PubMed Europe PubMed DOI
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 Oncol29, 5963-5987. PubMed Europe PubMed DOI 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 Pat1-13. 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 Biol53, 102336-102336. PubMed Europe PubMed DOI K
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
Hypertension79, 1713-1723. PubMed Europe PubMed DOI
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 Sci18, 5522-5538. PubMed Europe PubMed DOI
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 Biol10, 818462-818462. PubMed Europe PubMed DOI 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 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)13, PubMed Europe PubMed DOI
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)13, PubMed Europe PubMed DOI 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 Chem109, 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 Chem115, 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 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 Sci22, PubMed Europe PubMed DOI
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 Res42, 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 Chem32, 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
Cells10, PubMed Europe PubMed DOI I
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 Rep48, 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 PubMed Europe PubMed DOI I

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 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 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 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 Sci21, PubMed Europe PubMed DOI
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 Chem101, 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 Med172, 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 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 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 Immunol98, 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 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 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 Proteom1868, 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 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 Dyn1-12. 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 Biol21, 90-90. PubMed Europe PubMed DOI
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 Biol21, 15-15. PubMed Europe PubMed DOI 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 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 Biol30, 101422-101422. PubMed Europe PubMed DOI 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 Chem28, 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 Rep10, 20657-20657. PubMed Europe PubMed DOI
Yue,X., Jiang,H., Xu,Y., Xia,M. and Cheng,X.W.
Cathepsin K Deficiency Impaired Ischemia-Induced Neovascularization in Aged Mice
Stem Cells Int2020, 6938620-6938620. PubMed Europe PubMed DOI 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 Pharmacodyn47, 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 Mater35, 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 J476, 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 Invest129, 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 Biomark8, 1849454418821819-1849454418821819. PubMed Europe PubMed DOI 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 Soc141, 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 Rep9, 5399-5399. PubMed Europe PubMed DOI
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 Chem84, 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 Int104, 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 Histochem151498-151498. 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 Immunol93, 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 Pharm118772-118772. 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 Chem27, 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 Rep9, 159-164. PubMed Europe PubMed DOI 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 Acta1862, 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 Dis9, 692-692. PubMed Europe PubMed DOI 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 Med16, 56-56. PubMed Europe PubMed DOI 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 Chem33, 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 Muscle9, 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 J285, 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 Sci1415, 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 Commun503, 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 Res32, 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 Rev38, 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 Chem144, 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 Int101, 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 Rep7, 8703-8703. PubMed Europe PubMed DOI 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 Acta1864, 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 Biomater52, 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 Lett27, 1397-1400. PubMed Europe PubMed DOI 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 ONE12, e0186869-e0186869. 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 J474, 851-864. PubMed Europe PubMed DOI S 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 Pharmacol390, 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 Markers32, 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 Cartilage25, 2119-2126. PubMed Europe PubMed DOI
Novinec,M.
Computational investigation of conformational variability and allostery in cathepsin K and other related peptidases
PLoS ONE12, e0182387-e0182387. PubMed Europe PubMed DOI
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 Res32, 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)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
Glycobiology27, 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 Dis23, 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 Immunol198, 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 Cancer16, 173-173. PubMed Europe PubMed DOI
Bromme,D., Panwar,P. and Turan,S.
Cathepsin K osteoporosis trials, pycnodysostosis and mouse deficiency models: commonalities and differences
Expert Opin Drug Discov11, 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 Res51, 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 Int98, 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 Chem397, 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
Molecules21, 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 Vessels31, 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 Med9, 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 Cartilage24, 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 Pharmacol117, 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 Lett647, 42-45. DOI
Novinec,M., Rebernik,M. and Lenarcic,B.
An allosteric site enables fine-tuning of cathepsin K by diverse effectors
FEBS Lett590, 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 Metab34, 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 Pharmacol173, 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 Chem121, 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 Sci17, 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 Rheumatol2016, 8938916-8938916. PubMed Europe PubMed DOI
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 Adv6, 82961-82968. DOI I

2015

Abdel-Magid,A.F.
Inhibition of cathepsin K: a novel and promising treatment for osteoporosis
ACS Med Chem Lett6, 628-629. PubMed Europe PubMed DOI 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
Biochemistry54, 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 Chem58, 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 Notes8, 322-322. PubMed Europe PubMed DOI
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
Bone81, 427-434. PubMed Europe PubMed DOI I
Gamsjager,M. and Resch,H.
[Cathepsin K antagonists: preclinical and clinical data]
Wien Med Wochenschr165, 65-70. PubMed Europe PubMed DOI I
Gruber,R.
Molecular and cellular basis of bone resorption
Wien Med Wochenschr165, 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 Lett589, 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 Cell14, 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 Int96, 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 Pulmonol50, 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 Ther17, 5-5. PubMed Europe PubMed DOI
Pietschmann,P.
Cathepsin K inhibitors: emerging treatment options for osteoporosis
Wien Med Wochenschr165, 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 ONE10, e0132513-e0132513. PubMed Europe PubMed DOI
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 J465, 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 Endod41, 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 Biol35, 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
Proteomics15, 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 Res94, 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 Immunotoxicol37, 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 A111, 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 Dis9, 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 Chemometr28, 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
Hypertension63, 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 Ther37, 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 Biochem115, 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 Chem289, 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 Resist4, 267-277. PubMed Europe PubMed DOI
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 J28, 162-175. PubMed Europe PubMed DOI
Novinec,M., Lenarcic,B. and Baici,A.
Probing the activity modification space of the cysteine peptidase cathepsin K with novel allosteric modifiers
PLoS ONE9, e106642-e106642. 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 Commun5, 3287-3287. PubMed Europe PubMed DOI S I
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 Res29, 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
ChemMedChem9, 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 Biol41, 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 ONE9, e102732-e102732. PubMed Europe PubMed DOI
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
Bone67, 269-280. PubMed Europe PubMed DOI I

2013

Activating cathepsin K in osteoclasts stimulates bone formation through S1P
Bonekey Rep2, 362-362. PubMed Europe PubMed DOI 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
Atherosclerosis228, 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 Biopharm83, 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 Res92, 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 Targets14, 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
Oncogene32, 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
Diabetes62, 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
Hypertension61, 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 Invest123, 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 Rep15, 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
Biochemistry52, 7742-7752. PubMed Europe PubMed DOI
Novinec,M. and Lenarcic,B.
Cathepsin K: a unique collagenolytic cysteine peptidase
Biol Chem394, 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 Chem288, 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)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 Chem11, 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
Gut62, 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 Pharmacol75, 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
Phytomedicine20, 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 Biochem46, 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 Int55, 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 Lett24, 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 Chem11, 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
Gene521, 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 Chem393, 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 Chem287, 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 Rep10, 73-79. PubMed Europe PubMed DOI I
Borel,O., Gineyts,E., Bertholon,C. and Garnero,P.
Cathepsin K preferentially solubilizes matured bone matrix
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Bromme,D.
Cathepsin K
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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 Chem55, 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 Chem393, 959-970. PubMed Europe PubMed DOI K
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 Lett22, 5563-5568. PubMed Europe PubMed DOI I
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 Chem55, 6363-6374. 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
Bone50, 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 Int23, 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 Rheum64, 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
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Roy,S., Dattagupta,J.K. and Biswas,S.
Expression of recombinant human cathepsin K is enhanced by codon optimization
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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 Med26, 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
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Zhang,Y., Li,J., Zhu,J., Zhou,G., Zhang,W.J., Cao,Y. and Liu,W.
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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 Lett21, 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 Res26, 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 Chem286, 8988-8998. PubMed Europe PubMed DOI
Costa,A.G., Cusano,N.E., Silva,B.C., Cremers,S. and Bilezikian,J.P.
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Nat Rev Rheumatol7, 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 Neurosci12, 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 Res26, 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 Chem54, 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
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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
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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
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Knaapi,J., Lukkarinen,H., Kiviranta,R., Vuorio,E. and Kaapa,P.
Cathepsin K deficiency aggravates lung injury in hyperoxia-exposed newborn mice
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[New approach for osteoporosis treatment: cathepsin K inhibitor, ONO-5334]
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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 Res26, 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
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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)
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Wijkmans,J. and Gossen,J.
Inhibitors of cathepsin K: a patent review (2004 - 2010)
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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
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Xue,Y., Cai,T., Shi,S., Wang,W., Zhang,Y., Mao,T. and Duan,X.
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The effect of cathepsin K deficiency on airway development and TGF-beta1 degradation
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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
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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
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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
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Black,W.C.
Peptidomimetic inhibitors of cathepsin K
Curr Top Med Chem10, 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 Rep37, 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 Chem10, 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
Bone46, 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 Med58, 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 Chem10, 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
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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 Chem75, 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 Cartilage18, 1355-1357. PubMed Europe PubMed DOI I
Novinec,M., Kovacic,L., Lenarcic,B. and Baici,A.
Conformational flexibility and allosteric regulation of cathepsin K
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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
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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
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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
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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
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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 Biosyst6, 587-593. PubMed Europe PubMed DOI I
Teno,N. and Masuya,K.
Orally bioavailable cathepsin K inhibitors with pyrrolopyrimidine scaffold
Curr Top Med Chem10, 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 Med3, 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
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2009

Aydin,H.M. and Piskin,E.
Cathepsin K/TRAP: can they be used to induce osteogenesis?
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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 Lett19, 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 Lett19, 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 Drugs18, 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
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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 Cartilage17, 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 Chem390, 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 Res81, 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
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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)
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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
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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 Int54, 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
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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
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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
Bone44, 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
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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
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Podgorski,I.
Future of anticathepsin K drugs: dual therapy for skeletal disease and atherosclerosis?
Future Med Chem1, 21-34. PubMed Europe PubMed DOI I
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 Pathol175, 1255-1269. PubMed Europe PubMed DOI
Quintanilla-Dieck,M.J., Codriansky,K., Keady,M., Bhawan,J. and Runger,T.M.
Expression and regulation of cathepsin K in skin fibroblasts
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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
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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 A106, 14558-14563. PubMed Europe PubMed DOI 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 Ther86, 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 Int85, 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 Pharmacol613, 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
Tetrahedron65, 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 Pathol175, 2053-2062. PubMed Europe PubMed DOI
Zhao,Q., Jia,Y. and Xiao,Y.
Cathepsin K: a therapeutic target for bone diseases
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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
Science319, 624-627. PubMed Europe PubMed DOI T
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Innate immunity: new role for cathepsin K
Nat Rev Immunol8, 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 Pathol173, 161-169. PubMed Europe PubMed DOI
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 Pharmacol73, 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
Bone42, 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 Lett18, 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 Chem389, 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 Carcinog47, 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 Lett18, 3988-3991. PubMed Europe PubMed DOI I
Krieg,A.M. and Lipford,G.B.
Immunology. The toll of cathepsin K deficiency
Science319, 576-577. PubMed Europe PubMed DOI
Lecaille,F., Bromme,D. and Lalmanach,G.
Biochemical properties and regulation of cathepsin K activity
Biochimie90, 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 Biol383, 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
Menopause15, 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 Dermatol128, 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 Des72, 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 Chem51, 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
Atherosclerosis200, 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 Rheum58, 422-434. PubMed Europe PubMed DOI K
Simpson,S.J.
T cell role for cathepsin K
Sci Signal1, 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 Res9, 54-54. PubMed Europe PubMed DOI U
Stoch,S.A. and Wagner,J.A.
Cathepsin K inhibitors: a novel target for osteoporosis therapy
Clin Pharmacol Ther83, 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 Biochem144, 499-506. PubMed Europe PubMed DOI P
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 Chem51, 5459-5462. PubMed Europe PubMed DOI I
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 Lett18, 2599-2603. 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 Biol28, 2202-2208. PubMed Europe PubMed DOI

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 Chem50, 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 Lett17, 22-27. PubMed Europe PubMed DOI I
Cameron Black,W. and David Percival,M.
Chapter 8 Cathepsin K Inhibitors
Annu Rep Med Chem42, 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 Genet16, 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 ONE2, e683-e683. PubMed Europe PubMed DOI 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
Circulation115, 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
Bone40, 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 Res67, 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 Biophys459, 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 Lett17, 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 Soc129, 13633-13645. PubMed Europe PubMed DOI
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
Gene403, 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 Trans35, 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 Lett17, 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 SciUnit 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 Dermatol127, 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 Targets8, 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 Int18, 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 Chem282, 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
Tetrahedron63, 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 Lett17, 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
Bone40, 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 Lett16, 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 Res24, 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 Acta359, 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 Lett16, 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 Chem281, 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 Chem49, 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 Ther318, 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 Chem6, 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 Biol292, 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 Lett16, 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 Res21, 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 Chem387, 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
Circulation113, 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 Pathol210, 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
Bone38, 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 Future31, 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 Lab52, 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 Lett16, 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 Target14, 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 Chem14, 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 Chem71, 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
Biotechniques41, 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 Lett16, 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 Lett16, 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 Chem14, 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 Chem14, 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
Heterocycles67, 549-+.
Troen,B.R.
The regulation of cathepsin K gene expression
Ann N Y Acad Sci1068, 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
Chembiochem7, 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 Metab91, 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 Chem49, 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 Chem41, 1247-1252. PubMed Europe PubMed DOI I

2005

[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 Lett15, 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 Lett15, 3540-3546. PubMed Europe PubMed DOI I
[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 Lett15, 2209-2213. 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 Lett15, 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 Pat15, 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 Lett15, 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 Chem5, 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 Chem48, 7535-7543. PubMed Europe PubMed DOI I
Grabowskal,U., Chambers,T.J. and Shiroo,M.
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Holzer,G., Noske,H., Lang,T., Holzer,L. and Willinger,U.
Soluble cathepsin K: a novel marker for the prediction of nontraumatic fractures?
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[YEAR:31-5-2005]Kerschan-Schindl,K., Hawa,G., Kudlacek,S., Woloszczuk,W. and Pietschmann,P.
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Exp Gerontol40, 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
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[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 Chem280, 28370-28381. 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 Rheum52, 3713-3717. PubMed Europe PubMed DOI K
Morko,J., Kiviranta,R., Hurme,S., Rantakokko,J. and Vuorio,E.
Differential turnover of cortical and trabecular bone in transgenic mice overexpressing cathepsin K
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[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 Chem48, 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
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[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 Lett15, 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
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[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
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[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 Lett15, 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 Res66 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 Rev57, 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 Chem47, 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 Reprod70, 562-569. PubMed Europe PubMed DOI
[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 Lett14, 4897-4902. PubMed Europe PubMed DOI I
[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
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[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
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Bromme,D.
Cathepsin K
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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
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[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
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[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 Lett14, 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 Chem42, 245-375. PubMed Europe PubMed DOI
Fratzl-Zelman,N., Valenta,A., Roschger,P., Nader,A., Gelb,B.D., Fratzl,P. and Klaushofer,K.
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[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
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[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 Lett14, 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 Pathol165, 593-600. PubMed Europe PubMed DOI
Marquis,R.W.
Inhibition of the cysteine protease cathepsin K (EC 3.4.22.38)
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[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 Pharm1, 97-100. PubMed Europe PubMed 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
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[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 Chem12, 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
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[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 Chem47, 5057-5068. 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 Chem47, 5049-5056. 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 Chem47, 588-599. PubMed Europe PubMed DOI I
Troen,B.R.
The role of cathepsin K in normal bone resorption
Drug News Perspect17, 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 Pharm277, 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 Res63, 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 Lett13, 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 J373, 981-986. PubMed Europe PubMed DOI
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 Physiol195, 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 Biochem270, 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 Int73, 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 Chem384, 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 J375, 307-312. PubMed Europe PubMed DOI
[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
Biochemistry42, 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
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[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 Chem46, 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 Lett13, 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 Chem45, 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 Sci72, 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 Rheum46, 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 Purif25, 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 Rheum46, 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
Bone30, 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
Biochemistry41, 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 Chem277, 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
Biochemistry41, 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 Pathol195, 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 Commun285, 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 Res16, 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 Rheumatol28, 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 Pathol159, 2167-2177. PubMed Europe PubMed DOI
[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 Chem276, 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 Res80, 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 Res16, 1444-1452. PubMed Europe PubMed DOI
[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 Chem44, 725-736. PubMed Europe PubMed DOI I
[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 Chem44, 1380-1395. 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 A98, 5798-5803. PubMed Europe PubMed DOI
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 Pathol158, 1029-1038. PubMed Europe PubMed DOI
[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 Rec263, 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 Res16, 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
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[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 Pharmacol60, 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 Metab85, 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 Biochem267, 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 Genet8, 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 Pathol31, 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 Biochem283, 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
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Yamashita,D.S. and Dodds,R.A.
Cathepsin K and the design of inhibitors of cathepsin K
Curr Pharm Des6, 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 Purif15, 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 Lett9, 1907-1910. PubMed Europe PubMed DOI I
Guay,J., Riendeau,D. and Mancini,J.A.
Cloning and expression of rhesus monkey cathepsin K
Bone25, 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 Invest103, 731-738. PubMed Europe PubMed DOI 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
Biochemistry38, 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 Res14, 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
Biopolymers51, 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
Biochemistry38, 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 Biol18, 155-161. PubMed Europe PubMed DOI
Sivaraman,J., Lalumiere,M., Menard,R. and Cygler,M.
Crystal structure of wild-type human procathepsin K
Protein Sci8, 283-290. PubMed Europe PubMed DOI 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 J331, 727-732. PubMed Europe PubMed
[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 Chem41, 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 Chem41, 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 A95, 13453-13458. PubMed Europe PubMed DOI 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 Invest102, 576-583. PubMed Europe PubMed DOI
[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 Chem41, 3923-3927. PubMed Europe PubMed DOI I

1997

Gowen,M.
Inhibition of cathepsin K - a novel approach to antiresorptive therapy
Expert Opin Investig Drugs6, 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 Chem272, 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 Sci6, 919-921. PubMed Europe PubMed DOI 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 Biol4, 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 Chem272, 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)
Genomics41, 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 A94, 14249-14254. PubMed Europe PubMed DOI 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 Soc119, 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 Biol4, 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 Bull19, 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 Chem271, 12517-12524. PubMed Europe PubMed DOI 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 Chem271, 2126-2132. PubMed Europe PubMed
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 J315, 85-89. PubMed Europe PubMed I
Gelb,B.D., Shi,G.P., Chapman,H.A. and Desnick,R.J.
Pycnodysostosis, a lysosomal disease caused by cathepsin K deficiency
Science273, 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 Res6, 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 Lett393, 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 Seyler376, 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 Genet10, 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 Commun206, 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 Res10, 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 Genet10, 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 Lett357, 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 Chem269, 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 Int37, 25-31. PubMed Europe PubMed M