University of Notre Dame, United States.
University of Notre Dame, United States.
Biochim Biophys Acta Mol Cell Res. 2017 Nov;1864(11 Pt A):2001-2014. doi: 10.1016/j.bbamcr.2017.04.011. Epub 2017 Apr 20.
The focus of this article is to highlight novel inhibitors and current examples where the use of selective small-molecule inhibitors has been critical in defining the roles of matrix metalloproteinases (MMPs) in disease. Selective small-molecule inhibitors are surgical chemical tools that can inhibit the targeted enzyme; they are the method of choice to ascertain the roles of MMPs and complement studies with knockout animals. This strategy can identify targets for therapeutic development as exemplified by the use of selective small-molecule MMP inhibitors in diabetic wound healing, spinal cord injury, stroke, traumatic brain injury, cancer metastasis, and viral infection. This article is part of a Special Issue entitled: Matrix Metalloproteinases edited by Rafael Fridman.
本文的重点是强调新型抑制剂,并举例说明选择性小分子抑制剂在确定基质金属蛋白酶(MMPs)在疾病中的作用方面的重要性。选择性小分子抑制剂是手术化学工具,可以抑制靶向酶;它们是确定 MMP 作用的首选方法,并补充了基因敲除动物的研究。这种策略可以确定治疗开发的靶点,例如在糖尿病伤口愈合、脊髓损伤、中风、创伤性脑损伤、癌症转移和病毒感染中使用选择性小分子 MMP 抑制剂。本文是由 Rafael Fridman 编辑的特刊“基质金属蛋白酶”的一部分。