1KYN
 
 | | Cathepsin-G | | Descriptor: | (2-NAPHTHALEN-2-YL-1-NAPHTHALEN-1-YL-2-OXO-ETHYL)-PHOSPHONIC ACID, cathepsin G | | Authors: | Greco, M.N, Hawkins, M.J, Powell, E.T, Almond Jr, H.R, Corcoran, T.W, De Garavilla, L, Kauffman, J.A, Recacha, R, Chattopadhyay, D, Andrade-Gordon, P, Maryanoff, B.E. | | Deposit date: | 2002-02-05 | | Release date: | 2002-05-01 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (3.5 Å) | | Cite: | Nonpeptide inhibitors of cathepsin G: optimization of a novel beta-ketophosphonic acid lead by structure-based drug design.
J.Am.Chem.Soc., 124, 2002
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2HVX
 | | Discovery of Potent, Orally Active, Nonpeptide Inhibitors of Human Mast Cell Chymase by Using Structure-Based Drug Design | | Descriptor: | Chymase, [(1S)-1-(5-CHLORO-1-BENZOTHIEN-3-YL)-2-(2-NAPHTHYLAMINO)-2-OXOETHYL]PHOSPHONIC ACID | | Authors: | Greco, M.N, Hawkins, M.J, Powell, E.T, Almond, H.R, de Garavilla, L, Wang, Y, Minor, L.A, Wells, G.I, Di Cera, E, Cantwell, A.M, Savvides, S.N, Damiano, B.P, Maryanoff, B.E. | | Deposit date: | 2006-07-31 | | Release date: | 2007-06-12 | | Last modified: | 2021-10-20 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase.
J.Med.Chem., 50, 2007
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3N7O
 | | X-ray structure of human chymase in complex with small molecule inhibitor. | | Descriptor: | (S)-[(1S)-1-(5-chloro-1-benzothiophen-3-yl)-2-{[(E)-2-(3,4-difluorophenyl)ethenyl]amino}-2-oxoethyl]methylphosphinic acid, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Chymase, ... | | Authors: | Abad, M.C, Kervinen, J, Crysler, C, Bayoumy, S, Spurlino, J, Deckman, I, Greco, M.N, Maryanoff, B.E, Degaravilla, L. | | Deposit date: | 2010-05-27 | | Release date: | 2010-07-21 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Potency variation of small-molecule chymase inhibitors across species.
Biochem. Pharmacol., 80, 2010
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1T31
 | | A Dual Inhibitor of the Leukocyte Proteases Cathepsin G and Chymase with Therapeutic Efficacy in Animals Models of Inflammation | | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 2-[3-({METHYL[1-(2-NAPHTHOYL)PIPERIDIN-4-YL]AMINO}CARBONYL)-2-NAPHTHYL]-1-(1-NAPHTHYL)-2-OXOETHYLPHOSPHONIC ACID, 2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | Authors: | de Garavilla, L, Greco, M.N, Giardino, E.C, Wells, G.I, Haertlein, B.J, Kauffman, J.A, Corcoran, T.W, Derian, C.K, Eckardt, A.J, Abraham, W.M, Sukumar, N, Chen, Z, Pineda, A.O, Mathews, F.S, Di Cera, E, Andrade-Gordon, P, Damiano, B.P, Maryanoff, B.E, Pereira, P.J.B, Wang, Z.M, Rubin, H, Huber, R, Bode, W, Schechter, N.M, Strobl, S. | | Deposit date: | 2004-04-23 | | Release date: | 2005-03-01 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | A novel, potent dual inhibitor of the leukocyte proteases cathepsin G and chymase: molecular mechanisms and anti-inflammatory activity in vivo.
J.Biol.Chem., 280, 2005
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1T32
 | | A Dual Inhibitor of the Leukocyte Proteases Cathepsin G and Chymase with Therapeutic Efficacy in Animals Models of Inflammation | | Descriptor: | 2-[3-({METHYL[1-(2-NAPHTHOYL)PIPERIDIN-4-YL]AMINO}CARBONYL)-2-NAPHTHYL]-1-(1-NAPHTHYL)-2-OXOETHYLPHOSPHONIC ACID, Cathepsin G, SULFATE ION | | Authors: | de Garavilla, L, Greco, M.N, Giardino, E.C, Wells, G.I, Haertlein, B.J, Kauffman, J.A, Corcoran, T.W, Derian, C.K, Eckardt, A.J, Abraham, W.M, Sukumar, N, Chen, Z, Pineda, A.O, Mathews, F.S, Di Cera, E, Andrade-Gordon, P, Damiano, B.P, Maryanoff, B.E. | | Deposit date: | 2004-04-23 | | Release date: | 2005-03-01 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (1.85 Å) | | Cite: | A novel, potent dual inhibitor of the leukocyte proteases cathepsin G and chymase: molecular mechanisms and anti-inflammatory activity in vivo.
J.Biol.Chem., 280, 2005
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