| Literature DB >> 19692239 |
Alexander Heim-Riether1, Steven J Taylor, Shuang Liang, Donghong Amy Gao, Zhaoming Xiong, E Michael August, Brandon K Collins, Bennett T Farmer, Kathleen Haverty, Melissa Hill-Drzewi, Hans-Dieter Junker, S Mariana Margarit, Neil Moss, Thomas Neumann, John R Proudfoot, Lana Smith Keenan, Renate Sekul, Qiang Zhang, Jun Li, Neil A Farrow.
Abstract
Discovery and optimization of potency and selectivity of a non-Zn-chelating MMP-13 inhibitor with the aid of protein co-crystal structural information is reported. This inhibitor was observed to have a binding mode distinct from previously published MMP-13 inhibitors. Potency and selectivity were improved by extending the hit structure out from the active site into the S1' pocket.Entities:
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Year: 2009 PMID： 19692239 DOI： 10.1016/j.bmcl.2009.07.151
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823