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基质金属蛋白酶抑制的结构基础。

The structural basis of matrix metalloproteinase inhibition.

作者信息

Borkakoti N

机构信息

Roche Discovery Welwyn, Broadwater Road, Welwyn Garden City, Hertfordshire AL7 3AY, UK.

出版信息

Curr Opin Drug Discov Devel. 1999 Sep;2(5):449-62.

PMID:19649972
Abstract

Over the last decade, the potential utility of matrix metalloproteinase (MMP) inhibitors as novel therapeutic agents for diseases such as arthritis, cancer and multiple sclerosis has lead to an abundance of three-dimensional structural information on this family of enzymes. This review describes the spatial features of the conserved three-dimensional scaffold of the MMPs, discusses enzyme-inhibitor interactions and relates these data to the characteristics of individual MMPs which influence the potency and selectivity of inhibitors.

摘要

在过去十年中,基质金属蛋白酶(MMP)抑制剂作为关节炎、癌症和多发性硬化症等疾病的新型治疗药物的潜在效用,已产生了关于该酶家族的大量三维结构信息。本综述描述了MMPs保守三维支架的空间特征,讨论了酶与抑制剂的相互作用,并将这些数据与影响抑制剂效力和选择性的各个MMPs的特征联系起来。

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