TY - JOUR
T1 - Effect of Alkynyl Group on Reactivity in Photoaffinity Labeling with 2-Thienyl-Substituted α-Ketoamide
AU - Moriyama, Takahiro
AU - Mizukami, Daiki
AU - Yoritate, Makoto
AU - Usui, Kazuteru
AU - Takahashi, Daisuke
AU - Ota, Eisuke
AU - Sodeoka, Mikiko
AU - Ueda, Tadashi
AU - Karasawa, Satoru
AU - Hirai, Go
N1 - Funding Information:
This study was partially supported by PRIME and the Platform Project for Supporting Drug Discovery and Life Science Research (BINDS) from the Japan Agency for Medical Research and Development, AMED, the JSPS KAKENHI (grants no. 21K19053, 21H02070, and 20K15957), and the Sumitomo Foundation.
Publisher Copyright:
© 2022 Wiley-VCH GmbH
PY - 2022
Y1 - 2022
N2 - 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.
AB - 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.
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U2 - 10.1002/chem.202103925
DO - 10.1002/chem.202103925
M3 - Article
C2 - 35023607
AN - SCOPUS:85123892376
SN - 0947-6539
JO - Chemistry - A European Journal
JF - Chemistry - A European Journal
ER -