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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 |