Selective non zinc binding inhibitors of MMP13

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• 作者：Chris De Savi^a ; Andrew D. Morley ; ^a ; ^{andy.morley@astrazeneca.com"" rel=""nofollow} ; Attilla Ting^a ; Ian Nash^a ; Kostas Karabelas^a ; Christine M. Wood^a ; Michael James^a ; Stephen J. Norris^a ; Galith Karoutchi^a ; Neil Rankine^a ; Gordon Hamlin^a ; Philip A. MacFaul^a ; David Ryan^a ; Sarah V. Baker^a ; David Hargreaves^a ; Stefan Gerhardt^a
• 关键词：MMP13 ; Selectivity ; Non zinc binder ; Lead Generation
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2011
• 出版时间：15 July 2011
• 年：2011
• 卷：21
• 期：14
• 页码：4215-4219
• 全文大小：1686 K

文摘

Directed screening has identified a novel series of MMP13 inhibitors that possess good levels of activity whilst possessing excellent selectivity over related MMPs. The binding mode of the series has been solved by co-crystallisation and demonstrates an interesting mode of inhibition without interaction with the catalytic zinc atom.