James Lindsey I, Frye Stephen V
Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, 125 Mason Farm Road, Marsico Hall, UNC-Chapel Hill, NC 27599-7363, United States.
Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, 125 Mason Farm Road, Marsico Hall, UNC-Chapel Hill, NC 27599-7363, United States.
Curr Opin Chem Biol. 2016 Aug;33:135-41. doi: 10.1016/j.cbpa.2016.06.004. Epub 2016 Jun 25.
The primary intent of a chemical probe is to establish the relationship between a molecular target, usually a protein whose function is modulated by the probe, and the biological consequences of that modulation. In order to fulfill this purpose, a chemical probe must be profiled for selectivity, mechanism of action, and cellular activity, as the cell is the minimal system in which 'biology' can be explored. This review provides a brief overview of progress towards chemical probes for methyl lysine reader domains with a focus on recent progress targeting chromodomains.
化学探针的主要目的是建立分子靶点(通常是一种其功能可被探针调节的蛋白质)与该调节作用的生物学后果之间的关系。为了实现这一目的,必须对化学探针的选择性、作用机制和细胞活性进行分析,因为细胞是能够探索“生物学”的最小系统。本综述简要概述了针对甲基赖氨酸识别结构域的化学探针的研究进展,重点关注靶向色域结构域的最新进展。