1yt7

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Revision as of 18:17, 12 November 2007

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spinqualitylabelsall models 1yt7, resolution 2.3Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

Cathepsin K complexed with a constrained ketoamide inhibitor

Contents 1 Overview 2 Disease 3 About this Structure 4 Reference

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 with SO4 and 3FC as ligands. Active as Cathepsin K, with EC number 3.4.22.38 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

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