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1ztq

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Template:STRUCTURE 1ztq

Crystal structure of the catalytic domain of MMP-13 complexed with WAY-033


Overview

A potent, selective series of MMP-13 inhibitors has been derived from a weak (3.2 microM) inhibitor that did not bear a zinc chelator. Structure-based drug design strategies were employed to append a Zn-chelating group to one end of the molecule and functionality to enhance selectivity to the other. A compound from this series demonstrated rat oral bioavailability and efficacy in a bovine articular cartilage explant model.

About this Structure

1ZTQ is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Identification of potent and selective MMP-13 inhibitors., Wu J, Rush TS 3rd, Hotchandani R, Du X, Geck M, Collins E, Xu ZB, Skotnicki J, Levin JI, Lovering FE, Bioorg Med Chem Lett. 2005 Sep 15;15(18):4105-9. PMID:16005220 Page seeded by OCA on Sat May 3 18:03:43 2008

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