Effect of Alkynyl Group on Reactivity in Photoaffinity Labeling with 2‐Thienyl‐Substituted α‐Ketoamide
Effect of Alkynyl Group on Reactivity in Photoaffinity Labeling with 2‐Thienyl‐Substituted α‐Ketoamide
复制标题
炔基对 2-噻吩基取代的 α-酮酰胺光亲和标记反应活性的影响
DOI：
10.1002/chem.202103925
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发表时间：
2022
期刊：
影响因子：
--
通讯作者：
Hirai Go
中科院分区：
文献类型：
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作者：
Moriyama Takahiro;Mizukami Daiki;Yoritate Makoto;Usui Kazuteru;Takahashi Daisuke;Ota Eisuke;Sodeoka Mikiko;Ueda Tadashi;Karasawa Satoru;Hirai Go
极简光反应探针由一个光反应基团和一个用于检测目标蛋白的标签组成，是化学生物学中有用的工具。虽然有几种基于重氮嘧啶和芳基叠氮化物的极简探针可用，但尚未有基于酮的极简探针的报道。在这里，我们描述了基于2 -噻吩基取代α -酮酰胺的极简探针，该探针在噻吩环上带有炔基。3炔探针显示出最高的光亲和标记效率。
Minimalist photo‐reactive probes, which consist of a photo‐reactive group and a tag for detection of target proteins, are useful tools in chemical biology. Although several diazirine‐based and aryl azide‐based minimalist probes are available, no keto‐based minimalist probe has yet been reported. Here we describe minimalist probes based on a 2‐thienyl‐substituted α‐ketoamide bearing an alkyne group on the thiophene ring. The 3‐alkyne probe showed the highest photo‐affinity labeling efficiency.