环丙烯
生物正交化学
电泳剂
化学
半胱氨酸
谷胱甘肽
立体化学
组合化学
生物化学
酶
有机化学
催化作用
点击化学
作者
Gustav J. Wørmer,Bente K. Hansen,Johan Palmfeldt,Thomas B. Poulsen
标识
DOI:10.1002/anie.201907520
摘要
Abstract Cyclopropenes are an important new addition to the portfolio of functional groups that can be used for bioorthogonal couplings. The inert nature of these highly strained compounds in complex biological systems is almost counterintuitive given their established electrophilic properties in organic synthesis. Here we provide the first demonstration of a cyclopropene that is capable of direct conjugation to protein targets in cells and show that this compound preferentially alkylates the active site cysteine of glutathione S‐transferase omega‐1 (GSTO1).
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