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Effect of Alkynyl Group on Reactivity in Photoaffinity Labeling with 2-Thienyl-Substituted α-Ketoamide |
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| Authors: | Takahiro Moriyama Daiki Mizukami Dr Makoto Yoritate Dr Kazuteru Usui Dr Daisuke Takahashi Dr Eisuke Ota Prof?Dr Mikiko Sodeoka Prof?Dr Tadashi Ueda Prof?Dr Satoru Karasawa Prof?Dr Go Hirai |
| Institution: | 1. Graduate School of Pharmaceutical Sciences, Kyushu University Maidashi Higashi-ku, Fukuoka, 812-8582 Japan
These authors contributed equally to this work.;2. Graduate School of Pharmaceutical Sciences, Kyushu University Maidashi Higashi-ku, Fukuoka, 812-8582 Japan;3. RIKEN Cluster for Pioneering Research, 2-1, Hirosawa, Wako, Saitama, 351-0198 Japan;4. Faculty of Pharmaceutical Sciences, Showa Pharmaceutical University Higashi-Tamagawagakuen, Machida, Tokyo, 194-8543 Japan |
| Abstract: | 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. |
| Keywords: | α-ketoamides alkynes photo-affinity labeling spin density thiophenes |