Improving potency and selectivity of a new class of non-Zn-chelating MMP-13 inhibitors.
Bioorganic & Medicinal Chemistry Letters(2009)
摘要
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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关键词
MMP-13,Non-Zn-chelating inhibitor,SAR
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