Volume 52, Issue 33 pp. 8551-8556
Communication

Design and Synthesis of Minimalist Terminal Alkyne-Containing Diazirine Photo-Crosslinkers and Their Incorporation into Kinase Inhibitors for Cell- and Tissue-Based Proteome Profiling

Dr. Zhengqiu Li

Dr. Zhengqiu Li

Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543 (Singapore) http://staff.science.nus.edu.sg/∼syao

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Piliang Hao

Piliang Hao

School of Biological Sciences, Nanyang Technological University, 60 Nanyang Drive, Singapore 637551 (Singapore)

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Dr. Lin Li

Dr. Lin Li

Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543 (Singapore) http://staff.science.nus.edu.sg/∼syao

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Chelsea Y. J. Tan

Chelsea Y. J. Tan

Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543 (Singapore) http://staff.science.nus.edu.sg/∼syao

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Xiamin Cheng

Xiamin Cheng

Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543 (Singapore) http://staff.science.nus.edu.sg/∼syao

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Grace Y. J. Chen

Grace Y. J. Chen

Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543 (Singapore) http://staff.science.nus.edu.sg/∼syao

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Prof. Dr. Siu Kwan Sze

Prof. Dr. Siu Kwan Sze

School of Biological Sciences, Nanyang Technological University, 60 Nanyang Drive, Singapore 637551 (Singapore)

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Prof. Dr. Han-Ming Shen

Prof. Dr. Han-Ming Shen

Department of Physiology, National University of Singapore, 16 Medical Drive, Singapore 11794 (Singapore)

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Prof. Dr. Shao Q. Yao

Corresponding Author

Prof. Dr. Shao Q. Yao

Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543 (Singapore) http://staff.science.nus.edu.sg/∼syao

Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543 (Singapore) http://staff.science.nus.edu.sg/∼syaoSearch for more papers by this author
First published: 10 June 2013
Citations: 319

Funding was provided by the National Medical Research Council (NMRC/1260/2010) to H.-M.S. and S.Q.Y. and the Ministry of Education (MOE2012-T2-1-116). We thank Dr. Andrew Emili (Toronto) for helpful discussions of MS results.

Graphical Abstract

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.

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