title: 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.
authors.affiliation: Graduate School of Engineering, Department of Synthetic Chemistry and Biological Chemistry, Kyoto University, Katsura, Nishikyo-ku, Kyoto 615-8510, Japan. ihamachi@sbchem.kyoto-u.ac.jp.
authors.forename: Kei
authors.initials: K
authors.lastname: Yamaura
authors.forename: Keiko
authors.initials: K
authors.lastname: Kuwata
authors.forename: Tomonori
authors.initials: T
authors.lastname: Tamura
authors.forename: Yoshiyuki
authors.initials: Y
authors.lastname: Kioi
authors.forename: Yousuke
authors.initials: Y
authors.lastname: Takaoka
authors.forename: Shigeki
authors.initials: S
authors.lastname: Kiyonaka
authors.forename: Itaru
authors.initials: I
authors.lastname: Hamachi
mesh_terms: D045744:Cell Line, Tumor; D002470:Cell Survival; D006801:Humans; D000077341:Lapatinib; D008024:Ligands; D015394:Molecular Structure; D019704:Protein Disulfide-Isomerases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011799:Quinazolines / Q000737:chemistry / Q000494:pharmacology*; D018719:Erb-b2 Receptor Tyrosine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D014105:Tosyl Compounds / Q000737:chemistry*
chemical_list: D000077341:Lapatinib; D008024:Ligands; D019704:Protein Disulfide-Isomerases; D011799:Quinazolines; D018719:Erb-b2 Receptor Tyrosine Kinases; D014105:Tosyl Compounds; C508053:ERBB2 protein, human