PROTAC诱导的蛋白水解靶向作用。
PROTAC-induced proteolytic targeting.
作者信息
Carmony Kimberly Cornish, Kim Kyung-Bo
机构信息
Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY, USA.
出版信息
Methods Mol Biol. 2012;832:627-38. doi: 10.1007/978-1-61779-474-2_44.
Abstract
Small-molecule modulators of protein activity are increasingly being utilized as tools to examine the functional roles of proteins. Operating at the post-translational level, these molecules provide enhanced temporal and spatial control and mitigate the potential for compensatory responses in comparison with classical genetic approaches. Proteolysis targeting chimeric molecules, or PROTACs, are small molecules that inhibit the function of their target proteins by targeting them for degradation by the ubiquitin proteasome system. This chapter summarizes strategies for PROTAC preparation and characterization.
摘要
蛋白质活性的小分子调节剂正越来越多地被用作研究蛋白质功能作用的工具。这些分子在翻译后水平起作用，与传统的遗传方法相比，它们提供了更强的时间和空间控制，并降低了补偿反应的可能性。靶向嵌合分子的蛋白酶解（PROTAC）是一类小分子，通过将其靶蛋白靶向泛素蛋白酶体系统进行降解来抑制其功能。本章总结了PROTAC制备和表征的策略。
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