Article ID Journal Published Year Pages File Type
1371976 Bioorganic & Medicinal Chemistry Letters 2009 4 Pages PDF
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.

Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide

Keywords
Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
Authors
, , , , , , , , , , , , ,