Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371976 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
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.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Alexander Heim-Riether, Steven J. Taylor, Shuang Liang, Donghong Amy Gao, Zhaoming Xiong, E. Michael August, Brandon K. Collins, Bennett T. Farmer II, Kathleen Haverty, Melissa Hill-Drzewi, Hans-Dieter Junker, S. Mariana Margarit, Neil Moss,