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Design and Synthesis of Minimalist Terminal Alkyne‐Containing Diazirine Photo‐Crosslinkers and Their Incorporation into Kinase Inhibitors for Cell‐ and Tissue‐Based Proteome Profiling
Author(s) -
Li Zhengqiu,
Hao Piliang,
Li Lin,
Tan Chelsea Y. J.,
Cheng Xiamin,
Chen Grace Y. J.,
Sze Siu Kwan,
Shen HanMing,
Yao Shao Q.
Publication year - 2013
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201300683
Subject(s) - diazirine , linker , click chemistry , chemistry , proteome , derivatization , covalent bond , chemical biology , drug discovery , small molecule , photoaffinity labeling , combinatorial chemistry , bioorthogonal chemistry , kinase , chemical library , biochemistry , biophysics , computational biology , receptor , mass spectrometry , biology , computer science , operating system , organic chemistry , chromatography
Less is more : A minimalist “clickable” photo‐crosslinker (see scheme) was incorporated with numerous small‐molecule kinase inhibitors. The resulting probes were used for both in vitro (cell lysates) and in situ (live cells) proteome profiling, for large‐scale identification of their potential cellular kinase targets and shows improved outcomes over previous probes.