4.7 Article

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

Journal

CHEMICAL COMMUNICATIONS
Volume 50, Issue 91, Pages 14097-14100

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c4cc05885b

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Funding

  1. Grants-in-Aid for Scientific Research [25282238, 25708026] Funding Source: KAKEN

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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.

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