Reference on EC 3.4.22.38 - cathepsin K
Please use the Reference Search for a specific query.
Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
REF. 
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Bossard, M.J.; Tomaszek, T.A.; Thompson, S.K.; Amegadzie, B.Y.; Hanning, C.R.; Jones, C.J.; Kurdyla, J.T.; McNulty, D.E.; Drake, F.H.; Gowen, M.; Levy, M.A.
Proteolytic activity of human osteoclast cathepsin K. Expression, purification, activation and substrate identification
J. Biol. Chem.
271
12517-12524
1996
Homo sapiens
Brömme, D.; Klaus, J.L.; Okamoto, K.; Rasnik, D.; Palmer, J.T.
Peptidyl vinly sulphones: a new class of potent and selective cysteine proteinase inhibitors
Biochem. J.
315
85-89
1996
Homo sapiens
Inaoka, T.; Bilbe, G.; Ishibashi, O.; Tezuka, K.; Kumegawa, M.; Kokubo, T.
Molecular cloning of human cDNA for cathepsin K: novel cysteine proteinase predominantly expressed in bone
Biochem. Biophys. Res. Commun.
206
89-96
1995
Homo sapiens
McGrath, M.E.; Klaus, J.L.; Barnes, M.G.; Brömme, D.
Crystal structure of human cathepsin K complexed with a potent inhibitor
Nature Struct. Biol.
4
105-109
1997
Homo sapiens
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.; Abdel-Meguid, S.S.
Crystal structure of human osteoclast cathepsin K complexed with E-64
Nature Struct. Biol.
4
109-111
1997
Homo sapiens
Aibe, K.; Yazawa, H.; Abe, K.; Teramura, K.; Kumegawa, M.; Kawashima, H.; Honda, K.
Substrate specificity of recombinant osteoclast cathepsin K from rabbits
Biol. Pharm. Bull.
19
1026-1031
1996
Oryctolagus cuniculus
Schick, C.; Pemberton, P.A.; Shi, G.P.; Kamachi, Y.; Cataltepe, S.; Bartuski, A.J.; Gornstein, E.R.; Brömme, D.; Chapman, H.A.; Silverman, G.A.
Cross-class inhibition of the cysteine proteinases cathepsins K, L, and S by the serpin squamous cell carcinoma antigen I: a kinetic analysis
Biochemistry
37
5258-5266
1998
Homo sapiens
Linnevers, C.J.; McGrath, M.E.; Armstrong, R.; Mistry, F.R.; Barnes, M.G.; Klaus, J.L.; Palmer, J.T.; Katz, B.A.; Brömme, D.
Expression of human cathepsin K in Pichia pastoris and preliminary crystallographic studies of an inhibitor complex
Protein Sci.
6
919-921
1997
Homo sapiens
Littlewood-Evans, A.J.; Bilbe, G.; Bowler, W.B.; Farley, D.; Wlodarski, B.; Kokubo, T.; Inaoka, T.; Sloane, J.; Evans, D.B.; Gallagher, J.A.
The osteoclast-associated protease cathepsin K is expressed in human breast carcinoma
Cancer Res.
57
5386-5390
1997
Homo sapiens
Kamiya, T.; Kobayashi, Y.; Kanaoka, K.; Nakashima, T.; Kato, Y.; Mizuno, A.; Sakai, H.
Fluorescence microscopic demonstration of cathepsin K activity a the major lysosomal cystein proteinase in osteoclasts
J. Biochem.
123
752-759
1998
Mus musculus, Oryctolagus cuniculus
Kafienah, W.; Brömme, D.; Buttle, D.J.; Croucher, L.J.; Hollander, A.P.
Human cathepsin K cleaves native type I and II collagens at the N-terminal end of the triple helix
Biochem. J.
331
727-732
1996
Homo sapiens
-
McQueney, M.S.; Amegadzie, B.Y.; D'Alessio, K.; Hanning, C.R.; McLaughlin, M.M.; McNulty, D.; Carr, S.A.; Ijames, C.; Kurdyla, J.; Jones, C.S.
Autocatalytic activation of human cathepsin K
J. Biol. Chem.
272
13955-13960
1997
Homo sapiens
Brömme, D.; Okamoto, K.; Wang, B.B.; Biroc, S.
Human cathepsin O2, a matrix protein-degrading cysteine protease expressed in osteoclasts
J. Biol. Chem.
271
2126-2132
1996
Homo sapiens
Drake, F.H.; Dodds, R.A.; James, I.E.; Connor, J.R.; Debouck, C.; Richardson, S.; Lee-Rykaczewski, E.; Coleman, L.; Rieman, D.; Barthlow, R.; Hastings, G.; Gowen, M.
Cathepsin K, but no cathepsins B, L, or S, is abundantly expressed in human osteoclasts
J. Biol. Chem.
271
12511-12516
1996
Homo sapiens
Thomson, S.K.; Halbert, S.M.; Bossard, M.J.; Tomaszek, T.A.; Levy, M.A.; Zhao, B.; Smith, W.W.; Abdel- Meguid, S.S.; Janson, C.A.; D'Alessio, K.J.; McQueney, M.S.; Amegadzie, B.Y.; Hanning, C.R.; DesJarlais, R.L.; Briand, J.; Sakkar, S.K.; Huddleston, M.J.; Ijames, C.F.; Carr, S.A; Garnes, K.T.; Shu, A.; Heys, J.R.; Bradbeer, J.; Zembryki, D.; Lee-Rykyczewski, L.; James, I.E.; Lark, M.W.; Drake, F.H.; Gowen, M.; Gleason, J.G.; Veber, D.F.
Design of potent and selective human cathepsin K inhibitors that span the active site
Proc. Natl. Acad. Sci. USA
94
1429-1454
1997
Homo sapiens
-
Brömme, D.; Okamoto, K.
Human cathepsin O2, a novel cystein protease highly expressed in osteoclastomas and ovary. Molecular cloning, sequencing and tissue distribution
Biol. Chem. Hoppe-Seyler
376
379-384
1995
Homo sapiens
Rantakokko, J.; Aro, H.T.; Savontaus, M.; Vuorio, E.
Mouse cathepsin K: cDNA cloning and predominant expression of the gene in osteoclasts, and in some hypertrophing chondrocytes during mouse development
FEBS Lett.
393
307-313
1996
Mus musculus
Marquis, R.W.; Ru, Y.; LoCastro, S.M.; Zeng, J.; et al.
Azepanone-based Inhibitors of human and rat cathepsin K
J. Med. Chem.
44
1380-1395
2001
Homo sapiens, Rattus norvegicus
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.; Palmer, J.T.
A novel class of nonpeptidic biaryl inhibitors of human cathepsin K
J. Med. Chem.
46
3709-3727
2003
Oryctolagus cuniculus, Homo sapiens
Guay, J.; Falgueyret, J.P.; Ducret, A.; Percival, M.D.; Mancini, J.A.
Potency and selectivity of inhibition of cathepsin K, L and S by their respective propeptides
Eur. J. Biochem.
267
6311-6318
2000
Homo sapiens
Falgueyret, J.P.; Oballa, R.M.; Okamoto, O.; Wesolowski, G.; Aubin, Y.; Rydzewski, R.M.; Prasit, P.; Riendeau, D.; Rodan, S.B.; Percival, M.D.
Novel, nonpeptidic cyanamides as potent and reversible inhibitors of human cathepsins K and L
J. Med. Chem.
44
94-104
2001
Homo sapiens
Katunuma, N.; Matsui, A.; Inubushi, T.; Murata, E.; Kakegawa, H.; Ohba, Y.; Turk, D.; Turk, V.; Tada, Y.; Asao, T.
Structure-based development of pyridoxal propionate derivatives as specific inhibitors of cathepsin K in vitro and in vivo
Biochem. Biophys. Res. Commun.
267
850-854
2000
Rattus norvegicus
Billington, C.J.; Mason, P.; Magny, M.C.; Mort, J.S.
The slow-binding inhibition of cathepsin K by its propeptide
Biochem. Biophys. Res. Commun.
276
924-929
2000
Homo sapiens
Bossard, M.J.; Tomaszek, T.A.; Levy, M.A.; Ijames, C.F.; Huddleston, M.J.; Briand, J.; Thompson, S.; Halpert, S.; Veber, D.F.; Carr, S.A.; Meek, T.D.; Tew, D.G.
Mechanism of inhibition of cathepsin K by potent, selective 1,5-Diacylcarbohydrazides: A new class of mechanism-based inhibitors of thiol proteases
Biochemistry
38
15893-15902
1999
Homo sapiens
Wang, D.; Pechar, M.; Li, W.; Kopeckova, P.; Bromme, D.; Kopecek, J.
Inhibition of cathepsin K with lysosomotropic macromolecular inhibitors
Biochemistry
41
8849-8859
2002
Homo sapiens (P43235)
McGrath, M.E.; Sprengeler, P.A.; Hill, C.M.; Martichonok, V.; Cheung, H.; Somoza, J.R.; Palmer, J.T.; Janc, J.W.
Peptide ketobenzoxazole inhibitors bound to cathepsin K
Biochemistry
42
15018-15028
2003
Oryctolagus cuniculus, Homo sapiens
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.; Veber, D.F.
Cyclic ketone inhibitors of the cysteine protease cathepsin K
J. Med. Chem.
44
725-736
2001
Homo sapiens
Altmann, E.; Renaud, J.; Green, J.; Farley, D.; Cutting, B.; Jahnke, W.
Arylaminoethyl amides as novel non-covalent cathepsin K inhibitors
J. Med. Chem.
45
2352-2354
2002
Oryctolagus cuniculus, Homo sapiens
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.; Zhou, H.Q.
Design of potent, selective, and orally bioavailable inhibitors of cysteine protease cathepsin k
J. Med. Chem.
47
588-599
2004
Homo sapiens, Rattus norvegicus
Hwang, H.S.; Chung, H.S.
Preparation of active recombinant cathepsin K expressed in bacteria as inclusion body
Protein Expr. Purif.
25
541-546
2002
Homo sapiens
Rapa, I.; Volante, M.; Cappia, S.; Rosas, R.; Scagliotti, G.V.; Papotti, M.
Cathepsin K is selectively expressed in the stroma of lung adenocarcinoma but not in bronchioloalveolar carcinoma. A useful marker of invasive growth
Am. J. Clin. Pathol.
125
847-854
2006
Homo sapiens
Buehling, F.; Roecken, C.; Brasch, F.; Hartig, R.; Yasuda, Y.; Saftig, P.; Broemme, D.; Welte, T.
Pivotal role of cathepsin K in lung fibrosis
Am. J. Pathol.
164
2203-2216
2004
Homo sapiens, Mus musculus
Lindeman, J.H.; Hanemaaijer, R.; Mulder, A.; Dijkstra, P.D.; Szuhai, K.; Bromme, D.; Verheijen, J.H.; Hogendoorn, P.C.
Cathepsin K is the principal protease in giant cell tumor of bone
Am. J. Pathol.
165
593-600
2004
Homo sapiens
Godat, E.; Lecaille, F.; Desmazes, C.; Duchene, S.; Weidauer, E.; Saftig, P.; Broemme, D.; Vandier, C.; Lalmanach, G.
Cathepsin K: a cysteine protease with unique kinin-degrading properties
Biochem. J.
383
501-506
2004
Mus musculus
Altmann, E.; Aichholz, R.; Betschart, C.; Buhl, T.; Green, J.; Lattmann, R.; Missbach, M.
Dipeptide nitrile inhibitors of cathepsin K
Bioorg. Med. Chem. Lett.
16
2549-2554
2006
Homo sapiens
Mandelin, J.; Hukkanen, M.; Li, T.F.; Korhonen, M.; Liljestroem, M.; Sillat, T.; Hanemaaijer, R.; Salo, J.; Santavirta, S.; Konttinen, Y.T.
Human osteoblasts produce cathepsin K
Bone
38
769-777
2006
Homo sapiens (P43235), Homo sapiens
Troen, B.R.
The role of cathepsin K in normal bone resorption
Drug News Perspect.
17
19-28
2004
Homo sapiens
Ljusberg, J.; Wang, Y.; Lang, P.; Norgard, M.; Dodds, R.; Hultenby, K.; Ek-Rylander, B.; Andersson, G.
Proteolytic excision of a repressive loop domain in tartrate-resistant acid phosphatase by cathepsin K in osteoclasts
J. Biol. Chem.
280
28370-28381
2005
Homo sapiens
Giraudeau, F.S.; McGinnis, R.E.; Gray, I.C.; OBrien, E.J.; Doncaster, K.E.; Spurr, N.K.; Ralston, S.H.; Reid, D.M.; Wood, J.
Characterization of common genetic variants in cathepsin K and testing for association with bone mineral density in a large cohort of perimenopausal women from Scotland
J. Bone Miner. Res.
19
31-41
2004
Homo sapiens
Xiao, Y.; Junfeng, H.; Tianhong, L.; Lu, W.; Shulin, C.; Yu, Z.; Xiaohua, L.; Weixia, J.; Sheng, Z.; Yanyun, G.; Guo, L.; Min, L.
Cathepsin K in adipocyte differentiation and its potential role of the pathogenesis of obesity
J. Clin. Endocrinol. Metab.
91
4520-4527
2006
Homo sapiens
Holzer, G.; Noske, H.; Lang, T.; Holzer, L.; Willinger, U.
Soluble cathepsin K: a novel marker for the prediction of nontraumatic fractures?
J. Lab. Clin. Med.
146
13-17
2005
Homo sapiens
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.; et al
Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K
J. Med. Chem.
48
7520-7534
2005
Homo sapiens
Yamashita, D.S.; Xie, R.; Lin, H.; Wang, B.; Shi, S.D.; Quinn, C.J.; Hemling, M.E.; Hissong, C.; Tomaszek, T.A.; Veber, D.F.
Benzodioxocin-3-ones and N-acyl-3-amino-3-buten-2-ones: novel classes of cathepsin K cysteine protease inhibitors
J. Pept. Res.
63
265-269
2004
Homo sapiens
van den Brule, S.; Misson, P.; Buehling, F.; Lison, D.; Huaux, F.
Overexpression of cathepsin K during silica-induced lung fibrosis and control by TGF-beta
Respir. Res.
6
84
2005
Homo sapiens, Mus musculus
Lecaille, F.; Vandier, C.; Godat, E.; Herve-Grepinet, V.; Broemme, D.; Lalmanach, G.
Modulation of hypotensive effects of kinins by cathepsin K
Arch. Biochem. Biophys.
459
129-136
2007
Homo sapiens, Rattus norvegicus
Samokhin, A.O.; Wong, A.; Saftig, P.; Broemme, D.
Role of cathepsin K in structural changes in brachiocephalic artery during progression of atherosclerosis in apoE-deficient mice
Atherosclerosis
200
58-68
2008
Mus musculus
Lecaille, F.; Broemme, D.; Lalmanach, G.
Biochemical properties and regulation of cathepsin K activity
Biochimie
90
208-226
2008
Homo sapiens
Jaffer, F.A.; Kim, D.E.; Quinti, L.; Tung, C.H.; Aikawa, E.; Pande, A.N.; Kohler, R.H.; Shi, G.P.; Libby, P.; Weissleder, R.
Optical visualization of cathepsin K activity in atherosclerosis with a novel, protease-activatable fluorescence sensor
Circulation
115
2292-2298
2007
Homo sapiens
Ruenger, T.M.; Quintanilla-Dieck, M.J.; Bhawan, J.
Role of cathepsin K in the turnover of the dermal extracellular matrix during scar formation
J. Invest. Dermatol.
127
293-297
2007
Homo sapiens
Quintanilla-Dieck, M.J.; Codriansky, K.; Keady, M.; Bhawan, J.; Ruenger, T.M.
Cathepsin K in Melanoma Invasion
J. Invest. Dermatol.
128
2281-2288
2008
Homo sapiens
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.; Takayanagi, H.
Cathepsin K-dependent toll-like receptor 9 signaling revealed in experimental arthritis
Science
319
624-627
2008
Mus musculus, Rattus norvegicus
Shinozuka, T.; Shimada, K.; Matsui, S.; Yamane, T.; Ama, M.; Fukuda, T.; Taki, M.; Naito, S.
4-Aminophenoxyacetic acids as a novel class of reversible cathepsin K inhibitors
Bioorg. Med. Chem. Lett.
16
1502-1505
2006
Homo sapiens
Palmer, J.T.; Hirschbein, B.L.; Cheung, H.; McCarter, J.; Janc, J.W.; Yu, Z.W.; Wesolowski, G.
Keto-1,3,4-oxadiazoles as cathepsin K inhibitors
Bioorg. Med. Chem. Lett.
16
2909-2914
2006
Homo sapiens
Setti, E.L.; Venkatraman, S.; Palmer, J.T.; Xie, X.; Cheung, H.; Yu, W.; Wesolowski, G.; Robichaud, J.
Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K
Bioorg. Med. Chem. Lett.
16
4296-4299
2006
Homo sapiens
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.; Wright, L.L.
Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?
Bioorg. Med. Chem. Lett.
16
978-983
2006
Homo sapiens
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.; Zhou, H.Q.
Acyclic, orally bioavailable ketone-based cathepsin K inhibitors
Bioorg. Med. Chem. Lett.
17
22-27
2007
Homo sapiens
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.; Crane, S.N.
Beta-substituted cyclohexanecarboxamide cathepsin K inhibitors: modification of the 1,2-disubstituted aromatic core
Bioorg. Med. Chem. Lett.
17
3146-3151
2007
Oryctolagus cuniculus, Homo sapiens
Leger, S.; Bayly, C.I.; Black, W.C.; Desmarais, S.; Falgueyret, J.P.; Masse, F.; Percival, M.D.; Truchon, J.F.
Primary amides as selective inhibitors of cathepsin K
Bioorg. Med. Chem. Lett.
17
4328-4332
2007
Homo sapiens
Altmann, E.; Aichholz, R.; Betschart, C.; Buhl, T.; Green, J.; Irie, O.; Teno, N.; Lattmann, R.; Tintelnot-Blomley, M.; Missbach, M.
2-Cyano-pyrimidines: a new chemotype for inhibitors of the cysteine protease cathepsin K
J. Med. Chem.
50
591-594
2007
Homo sapiens
Dejica, V.M.; Mort, J.S.; Laverty, S.; Percival, M.D.; Antoniou, J.; Zukor, D.J.; Poole, A.R.
Cleavage of type II collagen by cathepsin K in human osteoarthritic cartilage
Am. J. Pathol.
173
161-169
2008
Homo sapiens
Neidhart, M.; Baraliakos, X.; Seemayer, C.; Zelder, C.; Gay, R.E.; Michel, B.A.; Boehm, H.; Gay, S.; Braun, J.
Expression of cathepsin K and MMP-1 indicate persistent osteodestruktive activity in longstanding ankylosing spondylitis
Ann. Rheum. Dis.
68
1334-1339
2008
Homo sapiens
Tsuchiya, M.; Akiba, Y.; Takahashi, I.; Sasano, Y.; Kashiwazaki, J.; Tsuchiya, S.; Watanabe, M.
Comparison of expression patterns of cathepsin K and MMP-9 in odontoclasts and osteoclasts in physiological root resorption in the rat molar
Arch. Histol. Cytol.
71
89-100
2008
Rattus norvegicus (O35186)
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.; Shi, G.P.
Deficiency and inhibition of cathepsin K reduce body weight gain and increase glucose metabolism in mice
Arterioscler. Thromb. Vasc. Biol.
28
2202-2208
2008
Homo sapiens, Mus musculus
Schurigt, U.; Hummel, K.M.; Petrow, P.K.; Gajda, M.; Stoeckigt, R.; Middel, P.; Zwerina, J.; Janik, T.; Bernhardt, R.; Schueler, S.; Scharnweber, D.; Beckmann, F.; Saftig, P.; Kollias, G.; Schett, G.; Wiederanders, B.; Braeuer, R.
Cathepsin K deficiency partially inhibits, but does not prevent, bone destruction in human tumor necrosis factor-transgenic mice
Arthritis Rheum.
58
422-434
2008
Mus musculus
Zhao, Q.; Jia, Y.; Xiao, Y.
Cathepsin K: a therapeutic target for bone diseases
Biochem. Biophys. Res. Commun.
380
721-723
2009
Homo sapiens
Teno, N.; Irie, O.; Miyake, T.; Gohda, K.; Horiuchi, M.; Tada, S.; Nonomura, K.; Kometani, M.; Iwasaki, G.; Betschart, C.
New chemotypes for cathepsin K inhibitors
Bioorg. Med. Chem. Lett.
18
2599-2603
2008
Homo sapiens
Irie, O.; Ehara, T.; Iwasaki, A.; Yokokawa, F.; Sakaki, J.; Hirao, H.; Kanazawa, T.; Teno, N.; Horiuchi, M.; Umemura, I.; Gunji, H.; Masuya, K.; Hitomi, Y.; Iwasaki, G.; Nonomura, K.; Tanabe, K.; Fukaya, H.; Kosaka, T.; Snell, C.R.; Hallett, A.
Discovery of selective and nonpeptidic cathepsin S inhibitors
Bioorg. Med. Chem. Lett.
18
3959-3962
2008
Homo sapiens
Kim, S.H.; Jhon, D.J.; Song, J.H.; No, J.S.; Kang, N.S.
Effect of novel N-cyano-tetrahydro-pyridazine compounds, a class of cathepsin K inhibitors, on the bone resorptive activity of mature osteoclasts
Bioorg. Med. Chem. Lett.
18
3988-3991
2008
Homo sapiens
Irie, O.; Yokokawa, F.; Ehara, T.; Iwasaki, A.; Iwaki, Y.; Hitomi, Y.; Konishi, K.; Kishida, M.; Toyao, A.; Masuya, K.; Gunji, H.; Sakaki, J.; Iwasaki, G.; Hirao, H.; Kanazawa, T.; Tanabe, K.; Kosaka, T.; Hart, T.W.; Hallett, A.
4-Amino-2-cyanopyrimidines: novel scaffold for nonpeptidic cathepsin S inhibitors
Bioorg. Med. Chem. Lett.
18
4642-4646
2008
Homo sapiens (P43235)
Gauthier, J.Y.; Chauret, N.; Cromlish, W.; Desmarais, S.; Duong, l.e..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.
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K
Bioorg. Med. Chem. Lett.
18
923-928
2008
Canis lupus familiaris, Oryctolagus cuniculus, Macaca fascicularis, Homo sapiens, Macaca mulatta, Rattus norvegicus
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.; Wilkinson, T.J.
5-Aminopyrimidin-2-ylnitriles as cathepsin K inhibitors
Bioorg. Med. Chem. Lett.
19
1658-1661
2009
Homo sapiens
Boyd, M.J.; Crane, S.N.; Robichaud, J.; Scheigetz, J.; Black, W.C.; Chauret, N.; Wang, Q.; Masse, F.; Oballa, R.M.
Investigation of ketone warheads as alternatives to the nitrile for preparation of potent and selective cathepsin K inhibitors
Bioorg. Med. Chem. Lett.
19
675-679
2009
Oryctolagus cuniculus, Homo sapiens, Rattus norvegicus
Ayesa, S.; Lindquist, C.; Agback, T.; Benkestock, K.; Classon, B.; Henderson, I.; Hewitt, E.; Jansson, K.; Kallin, A.; Sheppard, D.; Samuelsson, B.
Solid-phase parallel synthesis and SAR of 4-amidofuran-3-one inhibitors of cathepsin S: effect of sulfonamides P3 substituents on potency and selectivity
Bioorg. Med. Chem.
17
1307-1324
2009
Homo sapiens
Yamane, H.; Sakai, A.; Mori, T.; Tanaka, S.; Moridera, K.; Nakamura, T.
The anabolic action of intermittent PTH in combination with cathepsin K Inhibitor or alendronate differs depending on the remodeling status in bone in ovariectomized mice
Bone
44
1055-1062
2008
Mus musculus
Kozloff, K.M.; Quinti, L.; Patntirapong, S.; Hauschka, P.V.; Tung, C.H.; Weissleder, R.; Mahmood, U.
Non-invasive optical detection of cathepsin K-mediated fluorescence reveals osteoclast activity in vitro and in vivo
Bone
44
190-198
2009
Homo sapiens, Mus musculus
Pennypacker, B.; Shea, M.; Liu, Q.; Masarachia, P.; Saftig, P.; Rodan, S.; Rodan, G.; Kimmel, D.
Bone density, strength, and formation in adult cathepsin K (-/-) mice
Bone
44
199-207
2009
Mus musculus
Morko, J.; Kiviranta, R.; Mulari, M.T.; Ivaska, K.K.; Vaeaenaenen, H.K.; Vuorio, E.; Laitala-Leinonen, T.
Overexpression of cathepsin K accelerates the resorption cycle and osteoblast differentiation in vitro
Bone
44
717-728
2009
Mus musculus
Boskey, A.L.; Gelb, B.D.; Pourmand, E.; Kudrashov, V.; Doty, S.B.; Spevak, L.; Schaffler, M.B.
Ablation of cathepsin K activity in the young mouse causes hypermineralization of long bone and growth plates
Calcif. Tissue Int.
84
229-239
2009
Mus musculus, Mus musculus C57Bl6/J
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.; Van Berkel, T.J.
Leucocyte cathepsin K affects atherosclerotic lesion composition and bone mineral density in low-density lipoprotein receptor deficient mice
Cardiovasc. Res.
81
278-285
2009
Mus musculus
Ravikumar, M.; Pavan, S.; Bairy, S.; Pramod, A.B.; Sumakanth, M.; Kishore, M.; Sumithra, T.
Virtual screening of cathepsin K inhibitors using docking and pharmacophore models
Chem. Biol. Drug Des.
72
79-90
2008
Homo sapiens
Kleer, C.G.; Bloushtain-Qimron, N.; Chen, Y.H.; Carrasco, D.; Hu, M.; Yao, J.; Kraeft, S.K.; Collins, L.C.; Sabel, M.S.; Argani, P.; Gelman, R.; Schnitt, S.J.; Krop, I.E.; Polyak, K.
Epithelial and stromal cathepsin K and CXCL14 expression in breast tumor progression
Clin. Cancer Res.
14
5357-5367
2008
Homo sapiens
Han, J.; Luo, T.; Gu, Y.; Li, G.; Jia, W.; Luo, M.
Cathepsin K regulates adipocyte differentiation: possible involvement of type I collagen degradation
Endocr. J.
56
55-63
2009
Mus musculus
Svelander, L.; Erlandsson-Harris, H.; Astner, L.; Grabowska, U.; Klareskog, L.; Lindstrom, E.; Hewitt, E.
Inhibition of cathepsin K reduces bone erosion, cartilage degradation and inflammation evoked by collagen-induced arthritis in mice
Eur. J. Pharmacol.
613
155-162
2009
Homo sapiens, Mus musculus, Mus musculus DBA/1J
Tada, S.; Tsutsumi, K.; Ishihara, H.; Suzuki, K.; Gohda, K.; Teno, N.
Species differences between human and rat in the substrate specificity of cathepsin K
J. Biochem.
144
499-506
2008
Rattus norvegicus (O35186), Homo sapiens (P43235), Homo sapiens
Wilson, S.R.; Peters, C.; Saftig, P.; Broemme, D.
Cathepsin K activity-dependent regulation of osteoclast actin ring formation and bone resorption
J. Biol. Chem.
284
2584-2592
2009
Homo sapiens, Mus musculus, Mus musculus C57BL/6
Li, H.Y.; Ma, H.W.; Wang, H.Q.; Ma, W.H.
Molecular analysis of a novel cathepsin K gene mutation in a Chinese child with pycnodysostosis
J. Int. Med. Res.
37
264-269
2009
Homo sapiens
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.; Kometani, M.
Effect of cathepsin K inhibitors on bone resorption
J. Med. Chem.
51
5459-5462
2008
Homo sapiens, Rattus norvegicus
Irie, O.; Kosaka, T.; Ehara, T.; Yokokawa, F.; Kanazawa, T.; Hirao, H.; Iwasaki, A.; Sakaki, J.; Teno, N.; Hitomi, Y.; Iwasaki, G.; Fukaya, H.; Nonomura, K.; Tanabe, K.; Koizumi, S.; Uchiyama, N.; Bevan, S.J.; Malcangio, M.; Gentry, C.; Fox, A.J.; Yaqoob, M.; Culshaw, A.J.; Allan Hallett, A.J.
Discovery of orally bioavailable cathepsin S inhibitors for the reversal of neuropathic pain
J. Med. Chem.
51
5502-5505
2008
Homo sapiens, Rattus norvegicus
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.; Crane, S.N.
Identification of a nonbasic, nitrile-containing cathepsin K inhibitor (MK-1256) that is efficacious in a monkey model of osteoporosis
J. Med. Chem.
51
6410-6420
2008
Oryctolagus cuniculus
Li, Z.; Kienetz, M.; Cherney, M.M.; James, M.N.; Broemme, D.
The crystal and molecular structures of a cathepsin K:chondroitin sulfate complex
J. Mol. Biol.
383
78-91
2008
Homo sapiens
O'Shea, P.D.; Chen, C.Y.; Gauvreau, D.; Gosselin, F.; Hughes, G.; Nadeau, C.; Volante, R.P.
A practical enantioselective synthesis of odanacatib, a potent Cathepsin K inhibitor, via triflate displacement of an alpha-trifluoromethylbenzyl triflate
J. Org. Chem.
74
1605-1610
2009
Homo sapiens
Wendling, D.; Cedoz, J.P.; Racadot, E.
Serum levels of MMP-3 and cathepsin K in patients with ankylosing spondylitis: effect of TNFalpha antagonist therapy
Joint Bone Spine
75
559-562
2008
Homo sapiens
Aydin, H.M.; Piskin, E.
Cathepsin K/TRAP: Can they be used to induce osteogenesis?
Med. Hypotheses
72
464-465
2009
Homo sapiens
Connor, J.R.; Lepage, C.; Swift, B.A.; Yamashita, D.; Bendele, A.M.; Maul, D.; Kumar, S.
Protective effects of a cathepsin K inhibitor, SB-553484, in the canine partial medial meniscectomy model of osteoarthritis
Osteoarthritis Cartilage
17
1236-1243
2009
Canis lupus familiaris
Vinardell, T.; Dejica, V.; Poole, A.R.; Mort, J.S.; Richard, H.; Laverty, S.
Evidence to suggest that cathepsin K degrades articular cartilage in naturally occurring equine osteoarthritis
Osteoarthritis Cartilage
17
375-383
2009
Equus caballus
Kim, K.W.; Park, J.S.; Kim, K.S.; Jin, U.H.; Kim, J.K.; Suh, S.J.; Kim, C.H.
Inhibition of Ulmus davidiana Planch (Ulmaceae) on bone resorption mediated by processing of cathepsin K in cultured mouse osteoclasts
Phytother. Res.
22
511-517
2008
Mus musculus
Park, Y.; Kong, J.Y.; Cho, H.
A furanquinone from Paulownia tomentosa stem for a new cathepsin K inhibitor
Phytother. Res.
23
1485-1488
2009
Homo sapiens
Srivastava, M.; Steinwede, K.; Kiviranta, R.; Morko, J.; Hoymann, H.G.; Laenger, F.; Buhling, F.; Welte, T.; Maus, U.A.
Overexpression of cathepsin K in mice decreases collagen deposition and lung resistance in response to bleomycin-induced pulmonary fibrosis
Respir. Res.
9
54
2008
Mus musculus, Mus musculus FVB/N
Mikosch, P.; Kerschan-Schindl, K.; Woloszczuk, W.; Stettner, H.; Kudlacek, S.; Kresnik, E.; Gallowitsch, H.J.; Lind, P.; Pietschmann, P.
High cathepsin K levels in men with differentiated thyroid cancer on suppressive L-thyroxine therapy
Thyroid
18
27-33
2008
Homo sapiens
Veber, D.
Factors that influence oral bioavailability: a cathepsin K inhibitor for human studies
Adv. Exp. Med. Biol.
611
607-610
2009
Rattus norvegicus
Li, W.A.; Barry, Z.T.; Cohen, J.D.; Wilder, C.L.; Deeds, R.J.; Keegan, P.M.; Platt, M.O.
Detection of femtomole quantities of mature cathepsin K with zymography
Anal. Biochem.
401
91-98
2010
Homo sapiens
Garg, G.; Pradeep, A.R.; Thorat, M.K.
Effect of nonsurgical periodontal therapy on crevicular fluid levels of Cathepsin K in periodontitis
Arch. Oral Biol.
54
1046-1051
2009
Homo sapiens
Takahashi, D.; Iwasaki, N.; Kon, S.; Matsui, Y.; Majima, T.; Minami, A.; Uede, T.
Down-regulation of cathepsin K in synovium leads to progression of osteoarthritis in rabbits
Arthritis Rheum.
60
2372-2380
2009
Oryctolagus cuniculus
Bai, L.; Beckers, L.; Wijnands, E.; Lutgens, S.P.; Herias, M.V.; Saftig, P.; Daemen, M.J.; Cleutjens, K.; Lutgens, E.; Biessen, E.A.; Heeneman, S.
Cathepsin K gene disruption does not affect murine aneurysm formation
Atherosclerosis
209
96-103
2010
Mus musculus
Desmarais, S.; Masse, F.; Percival, M.D.
Pharmacological inhibitors to identify roles of cathepsin K in cell-based studies: a comparison of available tools
Biol. Chem.
390
941-948
2009
Oryctolagus cuniculus, Homo sapiens, Mus musculus, Rattus norvegicus
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.; van Zeeland, M.
Dioxo-triazines as a novel series of cathepsin K inhibitors
Bioorg. Med. Chem. Lett.
20
1488-1490
2010
Homo sapiens
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 Z, v.a.n..Z.e.
Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors
Bioorg. Med. Chem. Lett.
20
1524-1527
2010
Homo sapiens
Isabel, E.; Bateman, K.P.; Chauret, N.; Cromlish, W.; Desmarais, S.; Duong, l.e..T.; Falgueyret, J.P.; Gauthier, J.Y.; Lamontagne, S.; Lau, C.K.; Leger, S.; LeRiche, T.; Levesque, J.F.; Li, C.S.; Masse, F.; McKay, D.J.; Mellon, C.; Nicoll-Griffith, D.A.; Oballa, R.M.; Percival, M.D.; Riendeau, D.; Robichaud,
The discovery of MK-0674, an orally bioavailable cathepsin K inhibitor
Bioorg. Med. Chem. Lett.
20
887-892
2010
Homo sapiens
Li, J.; Petrassi, H.; Tumanut, C.; Masick, B.; Trussell, C.; Harris, J.
Substrate optimization for monitoring cathepsin C activity in live cells
Bioorg. Med. Chem.
17
1064-1070
2009
Homo sapiens
Barascuk, N.; Skjot-Arkil, H.; Register, T.C.; Larsen, L.; Byrjalsen, I.; Christiansen, C.; Karsdal, M.A.
Human macrophage foam cells degrade atherosclerotic plaques through cathepsin K mediated processes
BMC Cardiovasc. Disord.
10
19
2010
Homo sapiens
Fuller, K.; Lindstrom, E.; Edlund, M.; Henderson, I.; Grabowska, U.; Szewczyk, K.A.; Moss, R.; Samuelsson, B.; Chambers, T.J.
The resorptive apparatus of osteoclasts supports lysosomotropism and increases potency of basic versus non-basic inhibitors of cathepsin K
Bone
46
1400-1407
2010
Homo sapiens
Stroup, G.B.; Kumar, S.; Jerome, C.P.
Treatment with a potent cathepsin K inhibitor preserves cortical and trabecular bone mass in ovariectomized monkeys
Calcif. Tissue Int.
85
344-355
2009
Macaca fascicularis
Sun, Y.; Ishibashi, M.; Seimon, T.; Lee, M.; Sharma, S.M.; Fitzgerald, K.A.; Samokhin, A.O.; Wang, Y.; Sayers, S.; Aikawa, M.; Jerome, W.G.; Ostrowski, M.C.; Bromme, D.; Libby, P.; Tabas, I.A.; Welch, C.L.; Tall, A.R.
Free cholesterol accumulation in macrophage membranes activates Toll-like receptors and p38 mitogen-activated protein kinase and induces cathepsin K
Circ. Res.
104
455-465
2009
Mus musculus
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.; Wagner, J.A.
Effect of the cathepsin K inhibitor odanacatib on bone resorption biomarkers in healthy postmenopausal women: two double-blind, randomized, placebo-controlled phase I studies
Clin. Pharmacol. Ther.
86
175-182
2009
Homo sapiens
Je, J.E.; Ahn, S.J.; Kim, N.Y.; Seo, J.S.; Kim, M.S.; Park, N.G.; Kim, J.K.; Chung, J.K.; Lee, H.H.
Molecular cloning, expression analysis and enzymatic characterization of cathepsin K from olive flounder (Paralichthys olivaceus)
Comp. Biochem. Physiol. A
154
474-485
2009
Paralichthys olivaceus (B2Z447), Paralichthys olivaceus
Kometani, M.; Nonomura, K.; Tomoo, T.; Niwa, S.
Hurdles in the drug discovery of cathepsin K inhibitors
Curr. Top. Med. Chem.
10
733-744
2010
Homo sapiens
Black, W.C.
Peptidomimetic inhibitors of cathepsin K
Curr. Top. Med. Chem.
10
745-751
2010
Homo sapiens
Teno, N.; Masuya, K.
Orally bioavailable cathepsin K inhibitors with pyrrolopyrimidine scaffold
Curr. Top. Med. Chem.
10
752-766
2010
Homo sapiens
Pan, X.; Tan, N.; Zeng, G.; Huang, H.; Yan, H.
3D QSAR studies on ketoamides of human cathepsin K inhibitors based on two different alignment methods
Eur. J. Med. Chem.
45
667-681
2010
Homo sapiens
Yamaguchi, M.; Hayashi, M.; Fujita, S.; Yoshida, T.; Utsunomiya, T.; Yamamoto, H.; Kasai, K.
Low-energy laser irradiation facilitates the velocity of tooth movement and the expressions of matrix metalloproteinase-9, cathepsin K, and alpha(v) beta(3) integrin in rats
Eur. J. Orthod.
32
131-139
2010
Rattus norvegicus
Quintanilla-Dieck, M.J.; Codriansky, K.; Keady, M.; Bhawan, J.; Ruenger, T.M.
Expression and regulation of cathepsin K in skin fibroblasts
Exp. Dermatol.
18
596-602
2009
Homo sapiens
Golovatch, P.; Mercer, B.A.; Lemaitre, V.; Wallace, A.; Foronjy, R.F.; D'Armiento, J.
Role for cathepsin K in emphysema in smoke-exposed guinea pigs
Exp. Lung Res.
35
631-645
2009
Cavia porcellus, Homo sapiens
Broemme, D.; Lecaille, F.
Cathepsin K inhibitors for osteoporosis and potential off-target effects
Expert Opin. Investig. Drugs
18
585-600
2009
Homo sapiens
Harikrishnan, R.; Kim, M.C.; Kim, J.S.; Han, Y.J.; Jang, I.S.; Balasundaram, C.; Heo, M.S.
Immune response and expression analysis of cathepsin K in goldfish during Aeromonas hydrophila infection
Fish Shellfish Immunol.
28
511-516
2010
Carassius auratus (A4PBJ5), Carassius auratus
Naumnik, W.; Niklinska, W.; Ossolinska, M.; Chyczewska, E.
Serum cathepsin K and cystatin C concentration in patients with advanced non-small-cell lung cancer during chemotherapy
Folia Histochem. Cytobiol.
47
207-213
2009
Homo sapiens
Podgorski, I.
Future of anticathepsin K drugs: dual therapy for skeletal disease and atherosclerosis?
Future Med. Chem.
1
21-34
2009
Homo sapiens
Balkan, W.; Martinez, A.F.; Fernandez, I.; Rodriguez, M.A.; Pang, M.; Troen, B.R.
Identification of NFAT binding sites that mediate stimulation of cathepsin K promoter activity by RANK ligand
Gene
446
90-98
2009
Rattus norvegicus
Lewiecki, E.M.
Odanacatib, a cathepsin K inhibitor for the treatment of osteoporosis and other skeletal disorders associated with excessive bone remodeling
IDrugs
12
799-809
2009
Homo sapiens
Yan, X.; Takahara, M.; Xie, L.; Oda, Y.; Nakahara, T.; Uchi, H.; Takeuchi, S.; Tu, Y.; Moroi, Y.; Furue, M.
Stromal expression of cathepsin K in squamous cell carcinoma
J. Eur. Acad. Dermatol. Venereol.
25
362-365
2011
Homo sapiens
Khan, B.; Ahmed, Z.; Ahmad, W.
A novel missense mutation in cathepsin K (CTSK) gene in a consanguineous Pakistani family with pycnodysostosis
J. Investig. Med.
58
720-724
2010
Homo sapiens
Munoz-Torres, M.; Reyes-Garcia, R.; Mezquita-Raya, P.; Fernandez-Garcia, D.; Alonso, G.; Luna, J.d.e..D.; Ruiz-Requena, M.E.; Escobar-Jimenez, F.
Serum cathepsin K as a marker of bone metabolism in postmenopausal women treated with alendronate
Maturitas
64
188-192
2009
Homo sapiens
Chappard, D.; Libouban, H.; Mindeholm, L.; Basle, M.F.; Legrand, E.; Audran, M.
The cathepsin K inhibitor AAE581 induces morphological changes in osteoclasts of treated patients
Microsc. Res. Tech.
73
726-732
2009
Homo sapiens
Fontanesi, L.; Scotti, E.; Buttazzoni, L.; DallOlio, S.; Davoli, R.; Russo, V.
A single nucleotide polymorphism in the porcine cathepsin K (CTSK) gene is associated with back fat thickness and production traits in Italian Duroc pigs
Mol. Biol. Rep.
37
491-495
2010
Sus scrofa
Lendeckel, U.; Kaehne, T.; Ten Have, S.; Bukowska, A.; Wolke, C.; Bogerts, B.; Keilhoff, G.; Bernstein, H.G.
Cathepsin K generates enkephalin from beta-endorphin: a new mechanism with possible relevance for schizophrenia
Neurochem. Int.
54
410-417
2009
Homo sapiens
Codriansky, K.A.; Quintanilla-Dieck, M.J.; Gan, S.; Keady, M.; Bhawan, J.; Ruenger, T.M.
Intracellular degradation of elastin by cathepsin K in skin fibroblasts--a possible role in photoaging
Photochem. Photobiol.
85
1356-1363
2009
Homo sapiens
Wilder, C.L.; Park, K.Y.; Keegan, P.M.; Platt, M.O.
Manipulating substrate and pH in zymography protocols selectively distinguishes cathepsins K, L, S, and V activity in cells and tissues
Arch. Biochem. Biophys.
516
52-57
2011
Homo sapiens
Novinec, M.; Kovacic, L.; Lenarcic, B.; Baici, A.
Conformational flexibility and allosteric regulation of cathepsin K
Biochem. J.
429
379-389
2010
Homo sapiens
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.; Percival, M.D.; Roy, B.; Scheigetz, J.; Therien, M.; Truong, V.L.; Wesolowski, G.; Young, R.N.; Zamboni, R.; Black, W.C.
Difluoroethylamines as an amide isostere in inhibitors of cathepsin K
Bioorg. Med. Chem. Lett.
21
920-923
2011
Oryctolagus cuniculus
Cherney, M.M.; Lecaille, F.; Kienitz, M.; Nallaseth, F.S.; Li, Z.; James, M.N.; Broemme, D.
Structure-activity analysis of cathepsin K/chondroitin 4-sulfate interactions
J. Biol. Chem.
286
8988-8998
2011
Homo sapiens (P43235)
Schmit, J.M.; Pondenis, H.C.; Barger, A.M.; Borst, L.B.; Garrett, L.D.; Wypij, J.M.; Neumann, Z.L.; Fan, T.M.
Cathepsin K expression and activity in canine osteosarcoma
J. Vet. Intern. Med.
26
126-134
2012
Canis lupus familiaris
Sharma, V.; Panwar, P.; O'Donoghue, A.J.; Cui, H.; Guido, R.V.; Craik, C.S.; Broemme, D.
Structural requirements for the collagenase and elastase activity of cathepsin K and its selective inhibition by an exosite inhibitor
Biochem. J.
465
163-173
2015
Homo sapiens (P43235), Homo sapiens
Borel, O.; Gineyts, E.; Bertholon, C.; Garnero, P.
Cathepsin K preferentially solubilizes matured bone matrix
Calcif. Tissue Int.
91
32-39
2012
Homo sapiens
Hu, L.; Cheng, X.W.; Song, H.; Inoue, A.; Jiang, H.; Li, X.; Shi, G.P.; Kozawa, E.; Okumura, K.; Kuzuya, M.
Cathepsin K activity controls injury-related vascular repair in mice
Hypertension
63
607-615
2014
Mus musculus
Novinec, M.; Korenc, M.; Caflisch, A.; Ranganathan, R.; Lenarcic, B.; Baici, A.
A novel allosteric mechanism in the cysteine peptidase cathepsin K discovered by computational methods
Nat. Commun.
5
3287
2014
Homo sapiens (P43235)
Rodnick, M.E.; Shao, X.; Kozloff, K.M.; Scott, P.J.; Kilbourn, M.R.
Carbon-11 labeled cathepsin K inhibitors: syntheses and preliminary in vivo evaluation
Nucl. Med. Biol.
41
384-389
2014
Rattus norvegicus
Bitu, C.C.; Kauppila, J.H.; Bufalino, A.; Nurmenniemi, S.; Teppo, S.; Keinaenen, M.; Vilen, S.T.; Lehenkari, P.; Nyberg, P.; Coletta, R.D.; Salo, T.
Cathepsin K is present in invasive oral tongue squamous cell carcinoma in vivo and in vitro
PLoS ONE
8
e70925
2013
Homo sapiens
Novinec, M.; Lenarcic, B.; Baici, A.
Probing the activity modification space of the cysteine peptidase cathepsin K with novel allosteric modifiers
PLoS ONE
9
e106642
2014
Homo sapiens
Roy, S.; Dattagupta, J.; Biswas, S.
Expression of recombinant human cathepsin K is enhanced by codon optimization
Process Biochem.
47
1944-1947
2012
Homo sapiens (P43235)
-
Law, S.; Du, X.; Panwar, P.; Honson, N.S.; Pfeifer, T.; Roberge, M.; Broemme, D.
Identification of substrate-specific inhibitors of cathepsin K through high-throughput screening
Biochem. J.
476
499-512
2019
Homo sapiens (P43235)
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.; Lah, T.T.
Cathepsin K cleavage of SDF-1alpha inhibits its chemotactic activity towards glioblastoma stem-like cells
Biochim. Biophys. Acta Mol. Cell Res.
1864
594-603
2017
Homo sapiens (P43235), Homo sapiens
Keegan, P.M.; Anbazhakan, S.; Kang, B.; Pace, B.S.; Platt, M.O.
Biomechanical and biochemical regulation of cathepsin K expression in endothelial cells converge at AP-1 and NF-kappaB
Biol. Chem.
397
459-468
2016
Homo sapiens (P43235), Homo sapiens
Petek, N.; Stefane, B.; Novinec, M.; Svete, J.
Synthesis and biological evaluation of 7-(aminoalkyl)pyrazolo[1,5-a]pyrimidine derivatives as cathepsin K inhibitors
Bioorg. Chem.
84
226-238
2019
Homo sapiens (P43235)
Yuan, X.Y.; Ren, Z.; Wu, Y.; Bougault, C.; Brizuela, L.; Magne, D.; Buchet, R.; Mebarek, S.
Design, synthesis and biological evaluation of inhibitors of cathepsin K on dedifferentiated chondrocytes
Bioorg. Med. Chem.
27
1034-1042
2019
Homo sapiens (P43235), Homo sapiens, Mus musculus (P55097), Mus musculus
Kruglyak, N.; Williams, D.E.; Chen, H.; Law, S.; Kaleta, J.; Villanueva, I.; Davies, J.E.; Andersen, R.J.; Broemme, D.
Leupeptazin, a highly modified tripeptide isolated from cultures of a Streptomyces sp. inhibits cathepsin K
Bioorg. Med. Chem. Lett.
27
1397-1400
2017
Homo sapiens
Christensen, J.; Shastri, V.P.
Matrix-metalloproteinase-9 is cleaved and activated by cathepsin K
BMC Res. Notes
8
322
2015
Homo sapiens (P43235)
Gu, X.; Peng, Y.; Zhao, Y.; Liang, X.; Tang, Y.; Liu, J.
A novel derivative of artemisinin inhibits cell proliferation and metastasis via down-regulation of cathepsin K in breast cancer
Eur. J. Pharmacol.
858
172382
2019
Homo sapiens (P43235)
Tian, M.; Cao, M.; Zhang, L.; Fu, Q.; Yang, N.; Tan, F.; Song, L.; Su, B.; Li, C.
Characterization and initial functional analysis of cathepsin K in turbot (Scophthalmus maximus L.)
Fish Shellfish Immunol.
93
153-160
2019
Scophthalmus maximus (A0A1X9T5Z5), Scophthalmus maximus
Qiu, Z.C.; Dong, X.L.; Dai, Y.; Xiao, G.K.; Wang, X.L.; Wong, K.C.; Wong, M.S.; Yao, X.S.
Discovery of a new class of cathepsin K inhibitors in Rhizoma Drynariae as potential candidates for the treatment of osteoporosis
Int. J. Mol. Sci.
17
E2116
2016
Homo sapiens (P43235)
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.; Ovaa, H.
The Alkyne moiety as a latent electrophile in irreversible covalent small molecule inhibitors of cathepsin K
J. Am. Chem. Soc.
141
3507-3514
2019
Homo sapiens (P43235), Homo sapiens
Lu, J.; Wang, M.; Wang, Z.; Fu, Z.; Lu, A.; Zhang, G.
Advances in the discovery of cathepsin K inhibitors on bone resorption
J. Enzyme Inhib. Med. Chem.
33
890-904
2018
Homo sapiens (P43235)
Hussein, H.; Boyaka, P.; Dulin, J.; Russell, D.; Smanik, L.; Azab, M.; Bertone, A.L.
Cathepsin K localizes to equine bone in vivo and inhibits bone marrow atem and progenitor cells differentiation in vitro
J. Stem Cells Regen. Med.
13
45-53
2017
Equus caballus (F7A8R5), Equus caballus
html completed
