Issue 91, 2014
From the journal:

Chemical Communications

Live cell off-target identification of lapatinib using ligand-directed tosyl chemistry†‡

Kei Yamaura,a   Keiko Kuwata,b   Tomonori Tamura,a   Yoshiyuki Kioi,a   Yousuke Takaoka,a   Shigeki Kiyonakaa  and  Itaru Hamachi*ac  

* Corresponding authors

a Graduate School of Engineering, Department of Synthetic Chemistry and Biological Chemistry, Kyoto University, Katsura, Nishikyo-ku, Kyoto 615-8510, Japan
E-mail: ihamachi@sbchem.kyoto-u.ac.jp

b Institute of Transformative Bio-Molecules (ITbM), Nagoya University, Chikusa, Nagoya 464-8602, Japan

c Core Research for Evolutional Science and Technology (CREST), Japan Science and Technology Agency, 5 Sanbancho, Chiyoda-ku, Tokyo 102-0075, Japan

Abstract

We demonstrate that ligand-directed tosyl (LDT) chemistry is applicable to off-target identification in live cells. Lapatinib (Lap)-based LDT reagents not only labeled a receptor tyrosine kinase, HER2, target protein, but also the protein disulfide isomerase (PDI) that should be an off-target protein for Lap.

Graphical abstract: Live cell off-target identification of lapatinib using ligand-directed tosyl chemistry

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Article information

DOI
https://doi.org/10.1039/C4CC05885B
Article type
Communication
Submitted
29 7 2014
Accepted
17 9 2014
First published
17 9 2014

Chem. Commun., 2014,50, 14097-14100

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Live cell off-target identification of lapatinib using ligand-directed tosyl chemistry

K. Yamaura, K. Kuwata, T. Tamura, Y. Kioi, Y. Takaoka, S. Kiyonaka and I. Hamachi, Chem. Commun., 2014, 50, 14097 DOI: 10.1039/C4CC05885B

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