Cellular targets of gefitinib.
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.
Brehmer
Dirk
D
Axxima Pharmaceuticals AG, Munich, Germany.
Greff
Zoltán
Z
Godl
Klaus
K
Blencke
Stephanie
S
Kurtenbach
Alexander
A
Weber
Martina
M
Müller
Stefan
S
Klebl
Bert
B
Cotten
Matt
M
Kéri
György
G
Wissing
Josef
J
Daub
Henrik
H
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
D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D011799:Quinazolines; D066246:ErbB Receptors; D000077156:Gefitinib