Protein Information

Name Cathepsin K
Synonyms CTS02; CTSK; CTSK protein; CTSO; CTSO 1; CTSO 2; CTSO1; CTSO2…

Compound Information

Name biphenyl
CAS 1,1′-biphenyl

Reference List

PubMed Abstract RScore(About this table)
18685424 Le Gall C, Bonnelye E, Clezardin P: Cathepsin K inhibitors as treatment of bone metastasis. . Curr Opin Support Palliat Care. 2008 Sep;2(3):218-22.

8(0,0,0,8) Details
18511517 Dejica VM, Mort JS, Laverty S, Percival MD, Antoniou J, Zukor DJ, Poole AR: Cleavage of type II collagen by cathepsin K in human osteoarthritic cartilage. Am J Pathol. 2008 Jul;173(1):161-9. Epub 2008 May 29.

6(0,0,0,6) Details
17940194 Desmarais S, Black WC, Oballa R, Lamontagne S, Riendeau D, Tawa P, Duong le T, Pickarski M, Percival MD: Effect of cathepsin k inhibitor basicity on in vivo off-target activities. Mol Pharmacol. 2008 Jan;73(1):147-56. Epub 2007 Oct 16.

No such increase in these tissue cathepsins was detected at the same dose of N-(cyanomethyl)-N (2)-{(1S)-2,2,2-trifluoro-1-[4'-methylsulfonyl) biphenyl-4 -yl] ethyl}-l-leucinamide (L-873724), a potent nonbasic cathepsin K inhibitor with a similar off-target profile, although all three inhibitors provided similar plasma exposures.
4(0,0,0,4) Details
19943223 Lewiecki EM: Odanacatib, a cathepsin K inhibitor for the treatment of osteoporosis and other skeletal disorders associated with excessive bone remodeling. IDrugs. 2009 Dec;12(12):799-809.

4(0,0,0,4) Details
19252249 Kadono Y, Tanaka S: [Prevention of joint destruction by osteoclast-targeting therapy in search of new tools, such as OPG or cathepsin K inhibitor]. Clin Calcium. 2009 Mar;19(3):387-93.

2(0,0,0,2) Details
18226527 Gauthier JY, Chauret N, Cromlish W, Desmarais S, Duong le T, Falgueyret JP, Kimmel DB, Lamontagne S, Leger S, LeRiche T, Li CS, Masse F, McKay DJ, Nicoll-Griffith DA, Oballa RM, Palmer JT, Percival MD, Riendeau D, Robichaud J, Rodan GA, Rodan SB, Seto C, Therien M, Truong VL, Venuti MC, Wesolowski G, Young RN, Zamboni R, Black WC: The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8. Epub 2008 Jan 15.

2(0,0,0,2) Details
19421185 Stoch SA, Zajic S, Stone J, Miller DL, Van Dyck K, Gutierrez MJ, De Decker M, Liu L, Liu Q, Scott BB, Panebianco D, Jin B, Duong LT, Gottesdiener K, Wagner JA: Effect of the cathepsin K inhibitor odanacatib on bone resorption biomarkers in healthy postmenopausal women: two double-blind, randomized, placebo-controlled phase I studies. Clin Pharmacol Ther. 2009 Aug;86(2):175-82. Epub 2009 May 6.

2(0,0,0,2) Details
19759519 Iwasawa M, Miyazaki T, Nagase Y, Akiyama T, Kadono Y, Nakamura M, Oshima Y, Yasui T, Matsumoto T, Nakamura T, Kato S, Hennighausen L, Nakamura K, Tanaka S: The antiapoptotic protein Bcl-xL negatively regulates the bone-resorbing activity of osteoclasts in mice. J Clin Invest. 2009 Oct;119(10):3149-59. doi: 10.1172/JCI39819. Epub 2009 Sep 14.


To investigate the role of Bcl-xL in osteoclasts, we generated mice with osteoclast-specific conditional deletion of Bcl-x (referred to herein as Bcl-x cKO mice) by mating Bcl-xfl/fl mice with mice in which the gene encoding the Cre recombinase has been knocked into the cathepsin K locus and specifically expressed in mature osteoclasts.
1(0,0,0,1) Details
19626933 Ferrari S: [Bone remodeling: new therapeutic approaches] . Rev Med Suisse. 2009 Jun 10;5(207):1325-8.


Better understanding of the molecular processes of bone remodeling has led to the development of agents to inhibit bone resorption, such as the human monoclonal antibody Denosumab targeting osteoclast-activating factor RANK Ligand, and odanacatib targeting the collagen-degrading enzyme cathepsin K.
1(0,0,0,1) Details
19453281 Desmarais S, Masse F, Percival MD: Pharmacological inhibitors to identify roles of cathepsin K in cell-based studies: a comparison of available tools. Biol Chem. 2009 Sep;390(9):941-8.

2(0,0,0,2) Details
19140725 O'Shea PD, Chen CY, Gauvreau D, Gosselin F, Hughes G, Nadeau C, Volante RP: A practical enantioselective synthesis of odanacatib, a potent Cathepsin K inhibitor, via triflate displacement of an alpha-trifluoromethylbenzyl triflate. J Org Chem. 2009 Feb 20;74(4):1605-10.

2(0,0,0,2) Details