Article
Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl.
Cancer cell - 1 Feb 2005
Weisberg Ellen, Manley Paul W, Breitenstein Werner, Brüggen Josef, Cowan-Jacob Sandra W, Ray Arghya, Huntly Brian, Fabbro Doriano, Fendrich Gabriele, Hall-Meyers Elizabeth, Kung Andrew L, Mestan Jürgen, Daley George Q, Callahan Linda, Catley Laurie, Cavazza Cara, Azam Mohammad, Mohammed Azam, Neuberg Donna, Wright Renee D, Gilliland D Gary, Griffin James D
Abstract excerpt
The Bcr-Abl tyrosine kinase oncogene causes chronic myelogenous leukemia (CML) and Philadelphia chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL). We describe a novel selective inhibitor of Bcr-Abl, AMN107 (IC50 <30 nM), which is significantly more potent than imatinib, and active against a number of imatinib-resistant Bcr-Abl mutants. Crystallographic analysis of Abl-AMN107 complexes provides a...
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