-
1
-
-
84903543514
-
Cysteine cathepsins and extracellular matrix degradation
-
Fonovic, M.; Turk, B. Cysteine cathepsins and extracellular matrix degradation Biochim. Biophys. Acta, Gen. Subj. 2014, 1840, 2560-2570 10.1016/j.bbagen.2014.03.017
-
(2014)
Biochim. Biophys. Acta, Gen. Subj.
, vol.1840
, pp. 2560-2570
-
-
Fonovic, M.1
Turk, B.2
-
2
-
-
84881539601
-
Cathepsin K: A unique collagenolytic cysteine peptidase
-
Novinec, M.; Lenarcic, B. Cathepsin K: a unique collagenolytic cysteine peptidase Biol. Chem. 2013, 394, 1163-1179 10.1515/hsz-2013-0134
-
(2013)
Biol. Chem.
, vol.394
, pp. 1163-1179
-
-
Novinec, M.1
Lenarcic, B.2
-
3
-
-
4444344451
-
6. Cathepsin K inhibitors: Their potential as anti-osteoporosis agents
-
Deaton, D. M.; Kumar, S. 6. Cathepsin K inhibitors: their potential as anti-osteoporosis agents Prog. Med. Chem. 2004, 42, 245-375 10.1016/S0079-6468(04)42006-2
-
(2004)
Prog. Med. Chem.
, vol.42
, pp. 245-375
-
-
Deaton, D.M.1
Kumar, S.2
-
4
-
-
79951613664
-
Structure-based development of specific inhibitors for individual cathepsins and their medical applications
-
Katunuma, N. Structure-based development of specific inhibitors for individual cathepsins and their medical applications Proc. Jpn. Acad., Ser. B 2011, 87, 29-39 10.2183/pjab.87.29
-
(2011)
Proc. Jpn. Acad., Ser. B
, vol.87
, pp. 29-39
-
-
Katunuma, N.1
-
5
-
-
15544384612
-
Involvement of cathepsins in the invasion, metastasis and proliferation of cancer cells
-
Nomura, T.; Katunuma, N. Involvement of cathepsins in the invasion, metastasis and proliferation of cancer cells J. Med. Invest. 2005, 52, 1-9 10.2152/jmi.52.1
-
(2005)
J. Med. Invest.
, vol.52
, pp. 1-9
-
-
Nomura, T.1
Katunuma, N.2
-
6
-
-
0035801514
-
Lysosomal cysteine proteases: Facts and opportunities
-
Turk, V.; Turk, B.; Turk, D. Lysosomal cysteine proteases: facts and opportunities EMBO J. 2001, 20, 4629-4633 10.1093/emboj/20.17.4629
-
(2001)
EMBO J.
, vol.20
, pp. 4629-4633
-
-
Turk, V.1
Turk, B.2
Turk, D.3
-
7
-
-
82755161948
-
Cysteine cathepsins: From structure, function and regulation to new frontiers
-
Turk, V.; Stoka, V.; Vasiljeva, O.; Renko, M.; Sun, T.; Turk, B.; Turk, D. Cysteine cathepsins: from structure, function and regulation to new frontiers Biochim. Biophys. Acta, Proteins Proteomics 2012, 1824, 68-88 10.1016/j.bbapap.2011.10.002
-
(2012)
Biochim. Biophys. Acta, Proteins Proteomics
, vol.1824
, pp. 68-88
-
-
Turk, V.1
Stoka, V.2
Vasiljeva, O.3
Renko, M.4
Sun, T.5
Turk, B.6
Turk, D.7
-
8
-
-
84918557552
-
Structural basis of collagen fiber degradation by cathepsin K
-
Aguda, A. H.; Panwar, P.; Du, X.; Nguyen, N. T.; Brayer, G. D.; Brömme, D. Structural basis of collagen fiber degradation by cathepsin K Proc. Natl. Acad. Sci. U. S. A. 2014, 111, 17474-17479 10.1073/pnas.1414126111
-
(2014)
Proc. Natl. Acad. Sci. U. S. A.
, vol.111
, pp. 17474-17479
-
-
Aguda, A.H.1
Panwar, P.2
Du, X.3
Nguyen, N.T.4
Brayer, G.D.5
Brömme, D.6
-
9
-
-
84919794346
-
Proteases in cardiometabolic diseases: Pathophysiology, molecular mechanisms and clinical applications
-
Hua, Y.; Nair, S. Proteases in cardiometabolic diseases: Pathophysiology, molecular mechanisms and clinical applications Biochim. Biophys. Acta, Mol. Basis Dis. 2015, 1852, 195-208 10.1016/j.bbadis.2014.04.032
-
(2015)
Biochim. Biophys. Acta, Mol. Basis Dis.
, vol.1852
, pp. 195-208
-
-
Hua, Y.1
Nair, S.2
-
10
-
-
84892771725
-
Bone turnover markers and pharmacokinetics of a new sustained-release formulation of the cathepsin K inhibitor, ONO-5334, in healthy post-menopausal women
-
Nagase, S.; Ohyama, M.; Hashimoto, Y.; Small, M.; Sharpe, J.; Manako, J.; Kuwayama, T.; Deacon, S. Bone turnover markers and pharmacokinetics of a new sustained-release formulation of the cathepsin K inhibitor, ONO-5334, in healthy post-menopausal women J. Bone Miner. Metab. 2015, 33, 93-100 10.1007/s00774-013-0558-2
-
(2015)
J. Bone Miner. Metab.
, vol.33
, pp. 93-100
-
-
Nagase, S.1
Ohyama, M.2
Hashimoto, Y.3
Small, M.4
Sharpe, J.5
Manako, J.6
Kuwayama, T.7
Deacon, S.8
-
11
-
-
84859061110
-
Role for cysteine protease cathepsins in heart disease: Focus on biology and mechanisms with clinical implication
-
Cheng, X. W.; Shi, G. P.; Kuzuya, M.; Sasaki, T.; Okumura, K.; Murohara, T. Role for cysteine protease cathepsins in heart disease: focus on biology and mechanisms with clinical implication Circulation 2012, 125, 1551-1562 10.1161/CIRCULATIONAHA.111.066712
-
(2012)
Circulation
, vol.125
, pp. 1551-1562
-
-
Cheng, X.W.1
Shi, G.P.2
Kuzuya, M.3
Sasaki, T.4
Okumura, K.5
Murohara, T.6
-
12
-
-
67649628133
-
Cathepsin K inhibitors for osteoporosis and potential off-target effects
-
Brömme, D.; Lecaille, F. Cathepsin K inhibitors for osteoporosis and potential off-target effects Expert Opin. Invest. Drugs 2009, 18, 585-600 10.1517/13543780902832661
-
(2009)
Expert Opin. Invest. Drugs
, vol.18
, pp. 585-600
-
-
Brömme, D.1
Lecaille, F.2
-
13
-
-
84876786964
-
Cathepsin K - A classical bone biomarker in cardiovascular disease: The heart is not alone anymore
-
Vassalle, C.; Iervasi, G. Cathepsin K-A classical bone biomarker in cardiovascular disease: The heart is not alone anymore Atherosclerosis 2013, 228, 36-37 10.1016/j.atherosclerosis.2013.01.042
-
(2013)
Atherosclerosis
, vol.228
, pp. 36-37
-
-
Vassalle, C.1
Iervasi, G.2
-
14
-
-
84873025790
-
Cathepsin K knockout mitigates high-fat diet-induced cardiac hypertrophy and contractile dysfunction
-
Hua, Y.; Zhang, Y.; Dolence, J.; Shi, G. P.; Ren, J.; Nair, S. Cathepsin K knockout mitigates high-fat diet-induced cardiac hypertrophy and contractile dysfunction Diabetes 2013, 62, 498-509 10.2337/db12-0350
-
(2013)
Diabetes
, vol.62
, pp. 498-509
-
-
Hua, Y.1
Zhang, Y.2
Dolence, J.3
Shi, G.P.4
Ren, J.5
Nair, S.6
-
15
-
-
77949483288
-
Development of Nitrile-Based Peptidic Inhibitors of Cysteine Cathepsins
-
Frizler, M.; Stirnberg, M.; Sisay, M. T.; Gütschow, M. Development of Nitrile-Based Peptidic Inhibitors of Cysteine Cathepsins Curr. Top. Med. Chem. 2010, 10, 294-322 10.2174/156802610790725452
-
(2010)
Curr. Top. Med. Chem.
, vol.10
, pp. 294-322
-
-
Frizler, M.1
Stirnberg, M.2
Sisay, M.T.3
Gütschow, M.4
-
16
-
-
80053049819
-
Inhibitors of cathepsin K: A patent review (2004 - 2010)
-
Wijkmans, J.; Gossen, J. Inhibitors of cathepsin K: a patent review (2004-2010) Expert Opin. Ther. Pat. 2011, 21, 1611-1629 10.1517/13543776.2011.616283
-
(2011)
Expert Opin. Ther. Pat.
, vol.21
, pp. 1611-1629
-
-
Wijkmans, J.1
Gossen, J.2
-
17
-
-
84893639104
-
Treatment of postmenopausal osteoporosis with odanacatib
-
Chapurlat, R. D. Treatment of postmenopausal osteoporosis with odanacatib Expert Opin. Pharmacother. 2014, 15, 559-564 10.1517/14656566.2014.881470
-
(2014)
Expert Opin. Pharmacother.
, vol.15
, pp. 559-564
-
-
Chapurlat, R.D.1
-
18
-
-
84894435615
-
The Effect of the Cathepsin K Inhibitor ONO-5334 on Trabecular and Cortical Bone in Postmenopausal Osteoporosis: The OCEAN Study
-
Engelke, K.; Nagase, S.; Fuerst, T.; Small, M.; Kuwayama, T.; Deacon, S.; Eastell, R.; Genant, H. K. The Effect of the Cathepsin K Inhibitor ONO-5334 on Trabecular and Cortical Bone in Postmenopausal Osteoporosis: The OCEAN Study J. Bone Miner. Res. 2014, 29, 629-638 10.1002/jbmr.2080
-
(2014)
J. Bone Miner. Res.
, vol.29
, pp. 629-638
-
-
Engelke, K.1
Nagase, S.2
Fuerst, T.3
Small, M.4
Kuwayama, T.5
Deacon, S.6
Eastell, R.7
Genant, H.K.8
-
19
-
-
84917705814
-
Efficacy of a Cathepsin K Inhibitor in a Preclinical Model for Prevention and Treatment of Breast Cancer Bone Metastasis
-
Duong, L. T.; Wesolowski, G. A.; Leung, P.; Oballa, R.; Pickarski, M. Efficacy of a Cathepsin K Inhibitor in a Preclinical Model for Prevention and Treatment of Breast Cancer Bone Metastasis Mol. Cancer Ther. 2014, 13, 2898-2909 10.1158/1535-7163.MCT-14-0253
-
(2014)
Mol. Cancer Ther.
, vol.13
, pp. 2898-2909
-
-
Duong, L.T.1
Wesolowski, G.A.2
Leung, P.3
Oballa, R.4
Pickarski, M.5
-
20
-
-
84891839676
-
Effect of the cathepsin K inhibitor odanacatib administered once weekly on bone mineral density in Japanese patients with osteoporosis-a double-blind, randomized, dose-finding study
-
Nakamura, T.; Shiraki, M.; Fukunaga, M.; Tomomitsu, T.; Santora, A. C.; Tsai, R.; Fujimoto, G.; Nakagomi, M.; Tsubouchi, H.; Rosenberg, E.; Uchida, S. Effect of the cathepsin K inhibitor odanacatib administered once weekly on bone mineral density in Japanese patients with osteoporosis-a double-blind, randomized, dose-finding study Osteoporosis Int. 2014, 25, 367-376 10.1007/s00198-013-2398-2
-
(2014)
Osteoporosis Int.
, vol.25
, pp. 367-376
-
-
Nakamura, T.1
Shiraki, M.2
Fukunaga, M.3
Tomomitsu, T.4
Santora, A.C.5
Tsai, R.6
Fujimoto, G.7
Nakagomi, M.8
Tsubouchi, H.9
Rosenberg, E.10
Uchida, S.11
-
21
-
-
84873684246
-
Bone density, turnover, and estimated strength in postmenopausal women treated with odanacatib: A randomized trial
-
Brixen, K.; Chapurlat, R.; Cheung, A. M.; Keaveny, T. M.; Fuerst, T.; Engelke, K.; Recker, R.; Dardzinski, B.; Verbruggen, N.; Ather, S.; Rosenberg, E.; de Papp, A. E. Bone density, turnover, and estimated strength in postmenopausal women treated with odanacatib: a randomized trial J. Clin. Endocrinol. Metab. 2013, 98, 571-580 10.1210/jc.2012-2972
-
(2013)
J. Clin. Endocrinol. Metab.
, vol.98
, pp. 571-580
-
-
Brixen, K.1
Chapurlat, R.2
Cheung, A.M.3
Keaveny, T.M.4
Fuerst, T.5
Engelke, K.6
Recker, R.7
Dardzinski, B.8
Verbruggen, N.9
Ather, S.10
Rosenberg, E.11
De Papp, A.E.12
-
22
-
-
84875295907
-
Odanacatib, a Selective Cathepsin K inhibitor to Treat Osteoporosis: Safety, Tolerability, Pharmacokinetics and Pharmacodynamics - Results from Single Oral Dose Studies in Healthy Volunteers
-
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.; Wagner, J. A. Odanacatib, a Selective Cathepsin K inhibitor to Treat Osteoporosis: Safety, Tolerability, Pharmacokinetics and Pharmacodynamics-Results from Single Oral Dose Studies in Healthy Volunteers Br. J. Clin. Pharmacol. 2013, 75, 1240-1254 10.1111/j.1365-2125.2012.04471.x
-
(2013)
Br. J. Clin. Pharmacol.
, vol.75
, pp. 1240-1254
-
-
Stoch, S.A.1
Zajic, S.2
Stone, J.A.3
Miller, D.L.4
Van Bortel, L.5
Lasseter, K.C.6
Pramanik, B.7
Cilissen, C.8
Liu, Q.9
Liu, L.10
Scott, B.B.11
Panebianco, D.12
Ding, Y.13
Gottesdiener, K.14
Wagner, J.A.15
-
23
-
-
84869011778
-
Serum and urine bone resorption markers and pharmacokinetics of the cathepsin K inhibitor ONO-5334 after ascending single doses in post menopausal women
-
Nagase, S.; Hashimoto, Y.; Small, M.; Ohyama, M.; Kuwayama, T.; Deacon, S. Serum and urine bone resorption markers and pharmacokinetics of the cathepsin K inhibitor ONO-5334 after ascending single doses in post menopausal women Br. J. Clin. Pharmacol. 2012, 74, 959-970 10.1111/j.1365-2125.2012.04307.x
-
(2012)
Br. J. Clin. Pharmacol.
, vol.74
, pp. 959-970
-
-
Nagase, S.1
Hashimoto, Y.2
Small, M.3
Ohyama, M.4
Kuwayama, T.5
Deacon, S.6
-
24
-
-
84871692621
-
Potential role of odanacatib in the treatment of osteoporosis
-
Ng, K. W. Potential role of odanacatib in the treatment of osteoporosis Clin. Interventions Aging 2012, 7, 235-247 10.2147/CIA.S26729
-
(2012)
Clin. Interventions Aging
, vol.7
, pp. 235-247
-
-
Ng, K.W.1
-
25
-
-
81355148559
-
Effects of ONO-5334, a novel orally-active inhibitor of cathepsin K, on bone metabolism
-
Ochi, Y.; Yamada, H.; Mori, H.; Nakanishi, Y.; Nishikawa, S.; Kayasuga, R.; Kawada, N.; Kunishige, A.; Hashimoto, Y.; Tanaka, M.; Sugitani, M.; Kawabata, K. Effects of ONO-5334, a novel orally-active inhibitor of cathepsin K, on bone metabolism Bone 2011, 49, 1351-1356 10.1016/j.bone.2011.09.041
-
(2011)
Bone
, vol.49
, pp. 1351-1356
-
-
Ochi, Y.1
Yamada, H.2
Mori, H.3
Nakanishi, Y.4
Nishikawa, S.5
Kayasuga, R.6
Kawada, N.7
Kunishige, A.8
Hashimoto, Y.9
Tanaka, M.10
Sugitani, M.11
Kawabata, K.12
-
26
-
-
84857447754
-
Morphea-like skin reactions in patients treated with the cathepsin K inhibitor balicatib
-
Rünger, T. M.; Adami, S.; Benhamou, C. L.; Czerwiński, E.; Farrerons, J.; Kendler, D. L.; Mindeholm, L.; Realdi, G.; Roux, C.; Smith, V. Morphea-like skin reactions in patients treated with the cathepsin K inhibitor balicatib J. Am. Acad. Dermatol. 2012, 66, e89-e96 10.1016/j.jaad.2010.11.033
-
(2012)
J. Am. Acad. Dermatol.
, vol.66
, pp. 89-e96
-
-
Rünger, T.M.1
Adami, S.2
Benhamou, C.L.3
Czerwiński, E.4
Farrerons, J.5
Kendler, D.L.6
Mindeholm, L.7
Realdi, G.8
Roux, C.9
Smith, V.10
-
27
-
-
28144452675
-
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity
-
Falgueyret, J. P.; Desmarais, S.; Oballa, R.; Black, W. C.; Cromlish, W.; Khougaz, K.; Lamontagne, S.; Massé, F.; Riendeau, D.; Toulmond, S.; Percival, M. D. Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity J. Med. Chem. 2005, 48, 7535-7543 10.1021/jm0504961
-
(2005)
J. Med. Chem.
, vol.48
, pp. 7535-7543
-
-
Falgueyret, J.P.1
Desmarais, S.2
Oballa, R.3
Black, W.C.4
Cromlish, W.5
Khougaz, K.6
Lamontagne, S.7
Massé, F.8
Riendeau, D.9
Toulmond, S.10
Percival, M.D.11
-
28
-
-
0031030808
-
Crystal structure of human cathepsin K complexed with a potent inhibitor
-
McGrath, M. E.; Klaus, J. L.; Barnes, M. G.; Brömme, D. Crystal structure of human cathepsin K complexed with a potent inhibitor Nat. Struct. Biol. 1997, 4, 105-109 10.1038/nsb0297-105
-
(1997)
Nat. Struct. Biol.
, vol.4
, pp. 105-109
-
-
McGrath, M.E.1
Klaus, J.L.2
Barnes, M.G.3
Brömme, D.4
-
29
-
-
0345310073
-
Revised definition of substrate binding sites of papain-like cysteine proteases
-
Turk, D.; Guncar, G.; Podobnik, M.; Turk, B. Revised definition of substrate binding sites of papain-like cysteine proteases Biol. Chem. 1998, 379, 137-147 10.1515/bchm.1998.379.2.137
-
(1998)
Biol. Chem.
, vol.379
, pp. 137-147
-
-
Turk, D.1
Guncar, G.2
Podobnik, M.3
Turk, B.4
-
30
-
-
84861229565
-
Combinatorially-generated library of 6-fluoroquinolone analogs as potential novel antitubercular agents: A chemometric and molecular modeling assessment
-
Minovski, N.; Perdih, A.; Solmajer, T. Combinatorially-generated library of 6-fluoroquinolone analogs as potential novel antitubercular agents: a chemometric and molecular modeling assessment J. Mol. Model. 2012, 18, 1735-1753 10.1007/s00894-011-1179-0
-
(2012)
J. Mol. Model.
, vol.18
, pp. 1735-1753
-
-
Minovski, N.1
Perdih, A.2
Solmajer, T.3
-
31
-
-
84874651628
-
Cluster-based molecular docking study for in silico identification of novel 6-fluoroquinolones as potential inhibitors against mycobacterium tuberculosis
-
Minovski, N.; Perdih, A.; Novic, M.; Solmajer, T. Cluster-based molecular docking study for in silico identification of novel 6-fluoroquinolones as potential inhibitors against mycobacterium tuberculosis J. Comput. Chem. 2013, 34, 790-801 10.1002/jcc.23205
-
(2013)
J. Comput. Chem.
, vol.34
, pp. 790-801
-
-
Minovski, N.1
Perdih, A.2
Novic, M.3
Solmajer, T.4
-
32
-
-
84897486898
-
Mechanistic interpretation of artificial neural network-based QSAR model for prediction of cathepsin K inhibition potency
-
Borišek, J.; Drgan, V.; Minovski, N.; Novič, M. Mechanistic interpretation of artificial neural network-based QSAR model for prediction of cathepsin K inhibition potency J. Chemom. 2014, 28, 272-281 10.1002/cem.2617
-
(2014)
J. Chemom.
, vol.28
, pp. 272-281
-
-
Borišek, J.1
Drgan, V.2
Minovski, N.3
Novič, M.4
-
33
-
-
84941596671
-
-
Enamine fragment database. URL: (accessed Feb. 15).ontent&task=view&id=117 (accessed Feb., 15, 2013).
-
Enamine fragment database. URL: http://www.enamine.net/index.php?option=com
-
(2013)
-
-
-
34
-
-
0141726877
-
A rule of three for fragment-based lead discovery?
-
Congreve, M.; Carr, R.; Murray, C.; Jhoti, H. A rule of three for fragment-based lead discovery? Drug Discovery Today 2003, 8, 876-877 10.1016/S1359-6446(03)02831-9
-
(2003)
Drug Discovery Today
, vol.8
, pp. 876-877
-
-
Congreve, M.1
Carr, R.2
Murray, C.3
Jhoti, H.4
-
35
-
-
0037030653
-
Molecular properties that influence the oral bioavailability of drug candidates
-
Veber, D. F.; Johnson, S. R.; Cheng, H. Y.; Smith, B. R.; Ward, K. W.; Kopple, K. D. Molecular properties that influence the oral bioavailability of drug candidates J. Med. Chem. 2002, 45, 2615-2623 10.1021/jm020017n
-
(2002)
J. Med. Chem.
, vol.45
, pp. 2615-2623
-
-
Veber, D.F.1
Johnson, S.R.2
Cheng, H.Y.3
Smith, B.R.4
Ward, K.W.5
Kopple, K.D.6
-
36
-
-
84864250242
-
(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
-
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.; Vickers, M. (1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole '2-carbonyl)cyclohexanecarboxamide (AZD4996): a potent and highly selective cathepsin K inhibitor for the treatment of osteoarthritis J. Med. Chem. 2012, 55, 6363-6374 10.1021/jm3007257
-
(2012)
J. Med. Chem.
, vol.55
, pp. 6363-6374
-
-
Dossetter, A.G.1
Beeley, H.2
Bowyer, J.3
Cook, C.R.4
Crawford, J.J.5
Finlayson, J.E.6
Heron, N.M.7
Heyes, C.8
Highton, A.J.9
Hudson, J.A.10
Jestel, A.11
Kenny, P.W.12
Krapp, S.13
Martin, S.14
MacFaul, P.A.15
McGuire, T.M.16
Gutierrez, P.M.17
Morley, A.D.18
Morris, J.J.19
Page, K.M.20
Ribeiro, L.R.21
Sawney, H.22
Steinbacher, S.23
Smith, C.24
Vickers, M.25
more..
-
37
-
-
28144433007
-
Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K
-
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.; Rodan, G. Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K J. Med. Chem. 2005, 48, 7520-7534 10.1021/jm058198r
-
(2005)
J. Med. Chem.
, vol.48
, pp. 7520-7534
-
-
Palmer, J.T.1
Bryant, C.2
Wang, D.X.3
Davis, D.E.4
Setti, E.L.5
Rydzewski, R.M.6
Venkatraman, S.7
Tian, Z.Q.8
Burrill, L.C.9
Mendonca, R.V.10
Springman, E.11
McCarter, J.12
Chung, T.13
Cheung, H.14
Janc, J.W.15
McGrath, M.16
Somoza, J.R.17
Enriquez, P.18
Yu, Z.W.19
Strickley, R.M.20
Liu, L.21
Venuti, M.C.22
Percival, M.D.23
Falgueyret, J.P.24
Prasit, P.25
Oballa, R.26
Riendeau, D.27
Young, R.N.28
Wesolowski, G.29
Rodan, S.B.30
Johnson, C.31
Kimmel, D.B.32
Rodan, G.33
more..
-
38
-
-
78651072739
-
Structural Optimization of Azadipeptide Nitriles Strongly Increases Association Rates and Allows the Development of Selective Cathepsin Inhibitors
-
Frizler, M.; Lohr, F.; Furtmann, N.; Kläs, J.; Gütschow, M. Structural Optimization of Azadipeptide Nitriles Strongly Increases Association Rates and Allows the Development of Selective Cathepsin Inhibitors J. Med. Chem. 2011, 54, 396-400 10.1021/jm101272p
-
(2011)
J. Med. Chem.
, vol.54
, pp. 396-400
-
-
Frizler, M.1
Lohr, F.2
Furtmann, N.3
Kläs, J.4
Gütschow, M.5
-
39
-
-
80053188665
-
Facing the gem-Dialkyl Effect in Enzyme Inhibitor Design: Preparation of Homocycloleucine-Based Azadipeptide Nitriles
-
Frizler, M.; Lohr, F.; Lülsdorff, M.; Gütschow, M. Facing the gem-Dialkyl Effect in Enzyme Inhibitor Design: Preparation of Homocycloleucine-Based Azadipeptide Nitriles Chem.-Eur. J. 2011, 17, 11419-11423 10.1002/chem.201101350
-
(2011)
Chem. - Eur. J.
, vol.17
, pp. 11419-11423
-
-
Frizler, M.1
Lohr, F.2
Lülsdorff, M.3
Gütschow, M.4
-
40
-
-
28144452675
-
Lysosomotropism of Basic Cathepsin K Inhibitors Contributes to Increased Cellular Potencies against Off-Target Cathepsins and Reduced Functional Selectivity
-
Falgueyret, J. P.; Desmarais, S.; Oballa, R.; Black, W. C.; Cromlish, W.; Khougaz, K.; Lamontagne, S.; Massé, F.; Riendeau, D.; Toulmond, S.; Percival, M. D. Lysosomotropism of Basic Cathepsin K Inhibitors Contributes to Increased Cellular Potencies against Off-Target Cathepsins and Reduced Functional Selectivity J. Med. Chem. 2005, 48, 7535-43 10.1021/jm0504961
-
(2005)
J. Med. Chem.
, vol.48
, pp. 7535-7543
-
-
Falgueyret, J.P.1
Desmarais, S.2
Oballa, R.3
Black, W.C.4
Cromlish, W.5
Khougaz, K.6
Lamontagne, S.7
Massé, F.8
Riendeau, D.9
Toulmond, S.10
Percival, M.D.11
-
41
-
-
84874602189
-
Docking-based virtual screening of covalently binding ligands: An orthogonal lead discovery approach
-
Schröder, J.; Klinger, A.; Oellien, F.; Marhöfer, R. J.; Duszenko, M.; Selzer, P. M. Docking-based virtual screening of covalently binding ligands: an orthogonal lead discovery approach J. Med. Chem. 2013, 56, 1478-1490 10.1021/jm3013932
-
(2013)
J. Med. Chem.
, vol.56
, pp. 1478-1490
-
-
Schröder, J.1
Klinger, A.2
Oellien, F.3
Marhöfer, R.J.4
Duszenko, M.5
Selzer, P.M.6
-
42
-
-
0019948262
-
L-trans-Epoxysuccinyl-leucylamido(4-guanidino)butane (E-64) and its analogs as inhibitors of cysteine proteinases including cathepsins B, H and L
-
Barrett, A. J.; Kembhavi, A. A.; Brown, M. A.; Kirschke, H.; Knight, C. G.; Tamai, M.; Hanada, K. L-trans-Epoxysuccinyl-leucylamido(4-guanidino)butane (E-64) and its analogs as inhibitors of cysteine proteinases including cathepsins B, H and L Biochem. J. 1982, 201, 189-198 10.1042/bj2010189
-
(1982)
Biochem. J.
, vol.201
, pp. 189-198
-
-
Barrett, A.J.1
Kembhavi, A.A.2
Brown, M.A.3
Kirschke, H.4
Knight, C.G.5
Tamai, M.6
Hanada, K.7
-
43
-
-
0031552362
-
Development and validation of a genetic algorithm for flexible docking
-
Jones, G.; Willett, P.; Glen, R. C.; Leach, A. R.; Taylor, R. Development and validation of a genetic algorithm for flexible docking J. Mol. Biol. 1997, 267, 727-748 10.1006/jmbi.1996.0897
-
(1997)
J. Mol. Biol.
, vol.267
, pp. 727-748
-
-
Jones, G.1
Willett, P.2
Glen, R.C.3
Leach, A.R.4
Taylor, R.5
-
44
-
-
0041919542
-
Improved protein-ligand docking using GOLD
-
Verdonk, M. L.; Cole, J. C.; Hartshorn, M. J.; Murray, C. W.; Taylor, R. D. Improved protein-ligand docking using GOLD Proteins: Struct., Funct., Genet. 2003, 52, 609-623 10.1002/prot.10465
-
(2003)
Proteins: Struct., Funct., Genet.
, vol.52
, pp. 609-623
-
-
Verdonk, M.L.1
Cole, J.C.2
Hartshorn, M.J.3
Murray, C.W.4
Taylor, R.D.5
-
45
-
-
0013133162
-
A new test set for validating predictions of protein-ligand interaction
-
Nissink, J. W.; Murray, C.; Hartshorn, M.; Verdonk, M. L.; Cole, J. C.; Taylor, R. A new test set for validating predictions of protein-ligand interaction Proteins: Struct., Funct., Genet. 2002, 49, 457-471 10.1002/prot.10232
-
(2002)
Proteins: Struct., Funct., Genet.
, vol.49
, pp. 457-471
-
-
Nissink, J.W.1
Murray, C.2
Hartshorn, M.3
Verdonk, M.L.4
Cole, J.C.5
Taylor, R.6
-
46
-
-
41349106585
-
Evaluation of the performance of 3D virtual screening protocols: RMSD comparisons, enrichment assessments, and decoy selection - What can we learn from earlier mistakes?
-
Kirchmair, J.; Markt, P.; Distinto, S.; Wolber, G.; Langer, T. Evaluation of the performance of 3D virtual screening protocols: RMSD comparisons, enrichment assessments, and decoy selection-What can we learn from earlier mistakes? J. Comput.-Aided Mol. Des. 2008, 22, 213-228 10.1007/s10822-007-9163-6
-
(2008)
J. Comput.-Aided Mol. Des.
, vol.22
, pp. 213-228
-
-
Kirchmair, J.1
Markt, P.2
Distinto, S.3
Wolber, G.4
Langer, T.5
-
47
-
-
33645681649
-
1,4-Benzodiazepines as inhibitors of respiratory syncytial virus
-
Carter, M. C.; Alber, D. G.; Baxter, R. C.; Bithell, S. K.; Budworth, J.; Chubb, A.; Cockerill, G. S.; Dowdell, V. C. L.; Henderson, E. A.; Keegan, S. J.; Kelsey, R. D.; Lockyer, M. J.; Stables, J. N.; Wilson, L. J.; Powell, K. L. 1,4-Benzodiazepines as inhibitors of respiratory syncytial virus J. Med. Chem. 2006, 49, 2311-2319 10.1021/jm051185t
-
(2006)
J. Med. Chem.
, vol.49
, pp. 2311-2319
-
-
Carter, M.C.1
Alber, D.G.2
Baxter, R.C.3
Bithell, S.K.4
Budworth, J.5
Chubb, A.6
Cockerill, G.S.7
Dowdell, V.C.L.8
Henderson, E.A.9
Keegan, S.J.10
Kelsey, R.D.11
Lockyer, M.J.12
Stables, J.N.13
Wilson, L.J.14
Powell, K.L.15
-
48
-
-
84879584395
-
-
Bernhart, C.; Bouaboula, M.; Casellas, P.; Duclos, O.; Herbert, J. M.; Jegham, S.; Mccort, G. Antineoplastic derivatives, preparation thereof, and therapeutic use thereof. Patent WO2010004198 A2, 2010.
-
(2010)
Antineoplastic Derivatives, Preparation Thereof, and Therapeutic Use Thereof
-
-
Bernhart, C.1
Bouaboula, M.2
Casellas, P.3
Duclos, O.4
Herbert, J.M.5
Jegham, S.6
Mccort, G.7
-
49
-
-
0015984592
-
Rigid Analogs of Indomethacin
-
Olson, D. R.; Wheeler, W. J.; Wells, J. N. Rigid Analogs of Indomethacin J. Med. Chem. 1974, 17, 167-171 10.1021/jm00248a005
-
(1974)
J. Med. Chem.
, vol.17
, pp. 167-171
-
-
Olson, D.R.1
Wheeler, W.J.2
Wells, J.N.3
-
50
-
-
47249150493
-
Inhibitory fragment from the p41 form of invariant chain can regulate activity of cysteine cathepsins in antigen presentation
-
Mihelic, M.; Dobersek, A.; Guncar, G.; Turk, D. Inhibitory fragment from the p41 form of invariant chain can regulate activity of cysteine cathepsins in antigen presentation J. Biol. Chem. 2008, 283, 14453-60 10.1074/jbc.M801283200
-
(2008)
J. Biol. Chem.
, vol.283
, pp. 14453-14460
-
-
Mihelic, M.1
Dobersek, A.2
Guncar, G.3
Turk, D.4
-
51
-
-
0345862190
-
Production and activation of recombinant papain-like cysteine proteases
-
Brömme, D.; Nallaseth, F. S.; Turk, B. Production and activation of recombinant papain-like cysteine proteases Methods 2004, 32, 199-206 10.1016/S1046-2023(03)00212-3
-
(2004)
Methods
, vol.32
, pp. 199-206
-
-
Brömme, D.1
Nallaseth, F.S.2
Turk, B.3
-
52
-
-
12444315984
-
Inhibition of papain-like cysteine proteases and legumain by caspase-specific inhibitors: When reaction mechanism is more important than specificity
-
Rozman-Pungercar, J.; Kopitar-Jerala, N.; Bogyo, M.; Turk, D.; Vasiljeva, O.; Stefe, I.; Vandenabeele, P.; Brömme, D.; Puizdar, V.; Fonović, M.; Trstenjak-Prebanda, M.; Dolenc, I.; Turk, V.; Turk, B. Inhibition of papain-like cysteine proteases and legumain by caspase-specific inhibitors: when reaction mechanism is more important than specificity Cell Death Differ. 2003, 10, 881-8 10.1038/sj.cdd.4401247
-
(2003)
Cell Death Differ.
, vol.10
, pp. 881-888
-
-
Rozman-Pungercar, J.1
Kopitar-Jerala, N.2
Bogyo, M.3
Turk, D.4
Vasiljeva, O.5
Stefe, I.6
Vandenabeele, P.7
Brömme, D.8
Puizdar, V.9
Fonović, M.10
Trstenjak-Prebanda, M.11
Dolenc, I.12
Turk, V.13
Turk, B.14
-
53
-
-
0018787723
-
Evaluation of methods for estimating the dissociation constant of tight binding enzyme inhibitors
-
Greco, W. R.; Hakala, M. T. Evaluation of methods for estimating the dissociation constant of tight binding enzyme inhibitors J. Biol. Chem. 1979, 254, 12104-9
-
(1979)
J. Biol. Chem.
, vol.254
, pp. 12104-12109
-
-
Greco, W.R.1
Hakala, M.T.2
-
54
-
-
79953217030
-
Structure-activity analysis of cathepsin K/chondroitin 4-sulfate interactions
-
Cherney, M. M.; Lecaille, F.; Kienitz, M.; Nallaseth, F. S.; Li, Z.; James, M. N.; Brömme, D. Structure-activity analysis of cathepsin K/chondroitin 4-sulfate interactions J. Biol. Chem. 2011, 286, 8988-98 10.1074/jbc.M110.126706
-
(2011)
J. Biol. Chem.
, vol.286
, pp. 8988-8998
-
-
Cherney, M.M.1
Lecaille, F.2
Kienitz, M.3
Nallaseth, F.S.4
Li, Z.5
James, M.N.6
Brömme, D.7
-
55
-
-
0029439443
-
Proteinases 1: Lysosomal cysteine proteinases
-
Kirschke, H.; Barrett, A. J.; Rawlings, N. D. Proteinases 1: lysosomal cysteine proteinases Protein Profile 1995, 2, 1581-643
-
(1995)
Protein Profile
, vol.2
, pp. 1581-1643
-
-
Kirschke, H.1
Barrett, A.J.2
Rawlings, N.D.3
-
56
-
-
0028258640
-
Kinetics of inhibition of bovine cathepsin S by bovine stefin B
-
Turk, B.; Colić, A.; Stoka, V.; Turk, V. Kinetics of inhibition of bovine cathepsin S by bovine stefin B FEBS Lett. 1994, 339, 155-159 10.1016/0014-5793(94)80405-2
-
(1994)
FEBS Lett.
, vol.339
, pp. 155-159
-
-
Turk, B.1
Colić, A.2
Stoka, V.3
Turk, V.4
-
57
-
-
0001396685
-
The slow-binding and slow, tight-binding inhibition of enzyme-catalysed reactions
-
Morrison, J. F. The slow-binding and slow, tight-binding inhibition of enzyme-catalysed reactions Trends Biochem. Sci. 1982, 7, 102-105 10.1016/0968-0004(82)90157-8
-
(1982)
Trends Biochem. Sci.
, vol.7
, pp. 102-105
-
-
Morrison, J.F.1
-
58
-
-
84894443190
-
-
Invitrogen.
-
Invitrogen. Pichia Expression Kit. http://tools.thermofisher.com/content/sfs/manuals/pich
-
Pichia Expression Kit
-
-
-
59
-
-
84860129612
-
Facilities for macromolecular crystallography at the Helmholtz-Zentrum Berlin
-
Mueller, U.; Darowski, N.; Fuchs, M. R.; Förster, R.; Hellmig, M.; Paithankar, K. S.; Pühringer, S.; Steffien, M.; Zocher, G.; Weiss, M. S. Facilities for macromolecular crystallography at the Helmholtz-Zentrum Berlin J. Synchrotron Radiat. 2012, 19, 442-449 10.1107/S0909049512006395
-
(2012)
J. Synchrotron Radiat.
, vol.19
, pp. 442-449
-
-
Mueller, U.1
Darowski, N.2
Fuchs, M.R.3
Förster, R.4
Hellmig, M.5
Paithankar, K.S.6
Pühringer, S.7
Steffien, M.8
Zocher, G.9
Weiss, M.S.10
-
60
-
-
84861486823
-
XDSAPP: A graphical user interface for the convenient processing of diffraction data using XDS
-
Krug, M.; Weiss, M. S.; Heinemann, U.; Mueller, U. XDSAPP: a graphical user interface for the convenient processing of diffraction data using XDS J. Appl. Crystallogr. 2012, 45, 568-572 10.1107/S0021889812011715
-
(2012)
J. Appl. Crystallogr.
, vol.45
, pp. 568-572
-
-
Krug, M.1
Weiss, M.S.2
Heinemann, U.3
Mueller, U.4
-
61
-
-
34447508216
-
Phaser crystallographic software
-
Mccoy, A. J.; Grosse-Kunstleve, R. W.; Adams, P. D.; Winn, M. D.; Storoni, L. C.; Read, R. J. Phaser crystallographic software J. Appl. Crystallogr. 2007, 40, 658-674 10.1107/S0021889807021206
-
(2007)
J. Appl. Crystallogr.
, vol.40
, pp. 658-674
-
-
Mccoy, A.J.1
Grosse-Kunstleve, R.W.2
Adams, P.D.3
Winn, M.D.4
Storoni, L.C.5
Read, R.J.6
-
62
-
-
79953763877
-
REFMAC5 for the refinement of macromolecular crystal structures
-
Murshudov, G. N.; Skubák, P.; Lebedev, A. A.; Pannu, N. S.; Steiner, R. A.; Nicholls, R. A.; Winn, M. D.; Long, F.; Vagin, A. A. REFMAC5 for the refinement of macromolecular crystal structures Acta Crystallogr., Sect. D: Biol. Crystallogr. 2011, 67, 355-367 10.1107/S0907444911001314
-
(2011)
Acta Crystallogr., Sect. D: Biol. Crystallogr.
, vol.67
, pp. 355-367
-
-
Murshudov, G.N.1
Skubák, P.2
Lebedev, A.A.3
Pannu, N.S.4
Steiner, R.A.5
Nicholls, R.A.6
Winn, M.D.7
Long, F.8
Vagin, A.A.9
-
63
-
-
84881304302
-
MAIN software for density averaging, model building, structure refinement and validation
-
Turk, D. MAIN software for density averaging, model building, structure refinement and validation Acta Crystallogr., Sect. D: Biol. Crystallogr. 2013, 69, 1342-1357 10.1107/S0907444913008408
-
(2013)
Acta Crystallogr., Sect. D: Biol. Crystallogr.
, vol.69
, pp. 1342-1357
-
-
Turk, D.1
-
64
-
-
77949535720
-
Features and development of Coot
-
Emsley, P.; Lohkamp, B.; Scott, W. G.; Cowtan, K. Features and development of Coot Acta Crystallogr., Sect. D: Biol. Crystallogr. 2010, 66, 486-501 10.1107/S0907444910007493
-
(2010)
Acta Crystallogr., Sect. D: Biol. Crystallogr.
, vol.66
, pp. 486-501
-
-
Emsley, P.1
Lohkamp, B.2
Scott, W.G.3
Cowtan, K.4
|