Johnson L L, Dyer R, Hupe D J
Department of Biochemistry, Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, MI 48105, USA.
Curr Opin Chem Biol. 1998 Aug;2(4):466-71. doi: 10.1016/s1367-5931(98)80122-1.
Matrix metalloproteinases are a family of highly regulated peptidases that are collectively responsible for the degradation of extracellular matrix during tissue remodeling. Dysregulated activity has long been implicated in the pathologies of cancer and arthritis, and the number of diseases more recently associated with these enzymes has been increasing. In the past year, new transgenic models of matrix metalloproteinase knockouts have been described, allowing the direct assessment of specific enzyme activity in particular disease models. In addition, more selective inhibitors with improved pharmacokinetic profiles have entered clinical trials, allowing the assessment of the safety and efficacy of this strategy.
基质金属蛋白酶是一类受到高度调控的肽酶家族，它们共同负责组织重塑过程中细胞外基质的降解。长期以来，活性失调一直与癌症和关节炎的病理过程有关，最近与这些酶相关的疾病数量也在增加。在过去的一年里，已经描述了新的基质金属蛋白酶基因敲除转基因模型，这使得在特定疾病模型中能够直接评估特定酶的活性。此外，具有改善药代动力学特征的更具选择性的抑制剂已进入临床试验阶段，从而可以评估该策略的安全性和有效性。
