一种非异羟肟酸类双基质金属蛋白酶（MMP）-7/-13抑制剂的研发
Development of a Non-Hydroxamate Dual Matrix Metalloproteinase (MMP)-7/-13 Inhibitor.
作者信息
Fischer Thomas, Riedl Rainer
机构信息
Center for Organic and Medicinal Chemistry, Institute of Chemistry and Biotechnology, Zurich University of Applied Sciences ZHAW, Einsiedlerstrasse 31, 8820 Wädenswil, Switzerland.
出版信息
Molecules. 2017 Sep 14;22(9):1548. doi: 10.3390/molecules22091548.
Matrix metalloproteinase 7 (MMP-7) is a member of the MMP superfamily and is able to degrade extracellular matrix proteins such as casein, gelatin, fibronectin and proteoglycan. MMP-7 is a validated target for the development of small molecule drugs against cancer. MMP-13 is within the enzyme class the most efficient contributor to type II collagen degeneration and is a validated target in arthritis and cancer. We have developed the dual MMP-7/-13 inhibitor ZHAWOC6941 with IC-values of 2.2 μM (MMP-7) and 1.2 μM (MMP-13) that is selective over a broad range of MMP isoforms. It spares MMP-1, -2, -3, -8, -9, -12 and -14, making it a valuable modulator for targeted polypharmacology approaches.
基质金属蛋白酶7（MMP - 7）是MMP超家族的成员，能够降解细胞外基质蛋白，如酪蛋白、明胶、纤连蛋白和蛋白聚糖。MMP - 7是开发抗癌小分子药物的一个经过验证的靶点。MMP - 13是酶类中对II型胶原蛋白降解最有效的贡献者，是关节炎和癌症的一个经过验证的靶点。我们已经开发出双MMP - 7/-13抑制剂ZHAWOC6941，其对MMP - 7的IC值为2.2 μM，对MMP - 13的IC值为1.2 μM，对多种MMP亚型具有选择性。它对MMP - 1、-2、-3、-8、-9、-12和-14没有影响，使其成为靶向多药理学方法的一个有价值的调节剂。
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