The identification of β-hydroxy carboxylic acids as selective MMP-12 inhibitors

Ian P. Holmes,Simon Gaines,Steve P. Watson,Olivier Lorthioir,Adam Walker,Suzanne J. Baddeley,Shane Herbert,Danielle Egan,Máire A. Convery,Onkar M.P. Singh,Jeffrey W. Gross,John M. Strelow, Robert H. Smith,Augustin J. Amour,David Brown,Stephen L. Martin

Bioorganic & Medicinal Chemistry Letters（2009）

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摘要

A new class of selective MMP-12 inhibitors have been identified via high throughput screening. Crystallization with MMP-12 confirmed the mode of binding and allowed initial optimization to be carried out using classical structure based design.

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关键词

Inhibitor,MMP-12,Macrophage metalloelastase,Metalloproteinase,COPD,Rheumatoid arthritis,Angiogenesis

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