title: Cellular targets of gefitinib.
abstract: Targeted inhibition of protein kinases with small molecule drugs has evolved into a viable approach for anticancer therapy. However, the true selectivity of these therapeutic agents has remained unclear. Here, we used a proteomic method to profile the cellular targets of the clinical epidermal growth factor receptor kinase inhibitor gefitinib. Our data suggest alternative cellular modes of action for gefitinib and provide rationales for the development of related drugs.
authors.affiliation: Axxima Pharmaceuticals AG, Munich, Germany.
authors.forename: Dirk
authors.initials: D
authors.lastname: Brehmer
authors.forename: Zoltán
authors.initials: Z
authors.lastname: Greff
authors.forename: Klaus
authors.initials: K
authors.lastname: Godl
authors.forename: Stephanie
authors.initials: S
authors.lastname: Blencke
authors.forename: Alexander
authors.initials: A
authors.lastname: Kurtenbach
authors.forename: Martina
authors.initials: M
authors.lastname: Weber
authors.forename: Stefan
authors.initials: S
authors.lastname: Müller
authors.forename: Bert
authors.initials: B
authors.lastname: Klebl
authors.forename: Matt
authors.initials: M
authors.lastname: Cotten
authors.forename: György
authors.initials: G
authors.lastname: Kéri
authors.forename: Josef
authors.initials: J
authors.lastname: Wissing
authors.forename: Henrik
authors.initials: H
authors.lastname: Daub
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D019556:COS Cells; D002522:Chlorocebus aethiops; D066246:ErbB Receptors / Q000037:antagonists & inhibitors; D000077156:Gefitinib; D006367:HeLa Cells; D006801:Humans; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*; D040901:Proteomics / Q000379:methods; D011799:Quinazolines / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D011799:Quinazolines; D066246:ErbB Receptors; D000077156:Gefitinib