PROTAC-induced proteolytic targeting.
PROTAC-induced proteolytic targeting.
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DOI：
10.1007/978-1-61779-474-2_44
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发表时间：
2012
期刊：
影响因子：
--
通讯作者：
Kim, Kyung-Bo
中科院分区：
文献类型：
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作者：
Carmony, Kimberly Cornish;Kim, Kyung-Bo
蛋白质活性的小分子调节剂越来越多地被用作研究蛋白质功能作用的工具。在翻译后水平上操作，这些分子提供增强的时间和空间控制，并与经典的遗传方法相比减轻代偿反应的潜力。蛋白水解靶向嵌合分子，或PROTAC，是通过靶向它们以被泛素蛋白酶体系统（UPS）降解来抑制它们的靶蛋白的功能的小分子。本章总结了PROTAC制备和表征的策略。
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 (UPS). This chapter summarizes strategies for PROTAC preparation and characterization.