Issue 91, 2014

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

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

Supplementary files

Article information

Article type
Communication
Submitted
29 7 2014
Accepted
17 9 2014
First published
17 9 2014

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

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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