1yt7
From Proteopedia
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| , resolution 2.3Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | and | ||||||
| Gene: | CTSK, CTSO, CTSO2 (Homo sapiens) | ||||||
| Activity: | Cathepsin K, with EC number 3.4.22.38 | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Cathepsin K complexed with a constrained ketoamide inhibitor
Contents |
Overview
An orally bioavailable series of ketoamide-based cathepsin K inhibitors with good pharmacokinetic properties has been identified. Starting from a potent inhibitor endowed with poor drug properties, conformational constraint of the P(2)-P(3) linker and modifications to P(1') elements led to an enhancement in potency, solubility, clearance, and bioavailability. These optimized inhibitors attenuated bone resorption in a rat TPTX hypocalcemic bone resorption model.
Disease
Known disease associated with this structure: Pycnodysostosis OMIM:[601105]
About this Structure
1YT7 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K., Barrett DG, Boncek VM, Catalano JG, Deaton DN, Hassell AM, Jurgensen CH, Long ST, McFadyen RB, Miller AB, Miller LR, Payne JA, Ray JA, Samano V, Shewchuk LM, Tavares FX, Wells-Knecht KJ, Willard DH Jr, Wright LL, Zhou HQ, Bioorg Med Chem Lett. 2005 Aug 1;15(15):3540-6. PMID:15982880
Page seeded by OCA on Thu Mar 20 15:27:09 2008
Categories: Cathepsin K | Homo sapiens | Single protein | 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. | Wright, L L. | Zhou, H Q. | 3FC | SO4 | Cathepsin | Cysteine protease
