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1ztq

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(New page: 200px<br /> <applet load="1ztq" size="450" color="white" frame="true" align="right" spinBox="true" caption="1ztq, resolution 2.00&Aring;" /> '''Crystal structure o...)
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Revision as of 18:34, 12 November 2007

Image:1ztq.gif

1ztq, resolution 2.00Å

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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 with ZN, CA and 033 as ligands. 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 Mon Nov 12 20:41:23 2007

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