Target spectrum of the BCR-ABL inhibitors imatinib, nilotinib and dasatinib.
Following the initial success of imatinib as frontline therapy for chronic myeloid leukemia (CML), several second-generation therapeutics have been developed with increased potency and the ability to inhibit the majority of imatinib-resistant mutations. Here, we review the current knowledge about the target specificity of the two new inhibitors nilotinib and dasatinib in comparison to imatinib, including the recent large-scale chemical proteomics screens.
Hantschel
Oliver
O
CeMM-Center for Molecular Medicine of the Austrian Academy of Sciences, Vienna, Austria.
Rix
Uwe
U
Superti-Furga
Giulio
G
D001549:Benzamides; D000069439:Dasatinib; D016503:Drug Delivery Systems / Q000379:methods*; D016044:Fusion Proteins, bcr-abl / Q000037:antagonists & inhibitors*; D006801:Humans; D000068877:Imatinib Mesylate; D015464:Leukemia, Myelogenous, Chronic, BCR-ABL Positive / Q000188:drug therapy; D010879:Piperazines; D047428:Protein Kinase Inhibitors / Q000627:therapeutic use*; D011743:Pyrimidines; D013844:Thiazoles
D001549:Benzamides; D010879:Piperazines; D047428:Protein Kinase Inhibitors; D011743:Pyrimidines; D013844:Thiazoles; D000068877:Imatinib Mesylate; D016044:Fusion Proteins, bcr-abl; C498826:nilotinib; D000069439:Dasatinib