Novel Allosteric Kinase Inhibitors

Title
Novel Allosteric Kinase Inhibitors
Authors
심태보
Issue Date
2010-05
Publisher
International 2010 KSBMB Annual Meeting
Abstract
Chronic myelogenous leukemia (CML) is a hematological malignancy caused by a chromosomal rearrangement that generates a fusion protein, Bcr-Abl, with deregulated tyrosine kinase activity. Although clinical remission is usually achieved in early-stage disease with the ATP-site targeting drug imatinib, advanced-stage patients may relapse due to the emergence of clones expressing inhibitor-resistant forms of Bcr-Abl. To address these relapses, two more potent ATPsite directed agents: nilotinib (AMN107)[1] and dasatinib (BMS-354825)[2],[3] have recently received clinical approval. Although both compounds inhibit most of the mutations that induce resistance to imatinib, neither is capable of inhibiting the “gatekeeper” T315I mutation, which is situated in the middle of the ATP-binding cleft[4],[5].
URI
http://pubs.kist.re.kr/handle/201004/39188
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KIST Publication > Conference Paper
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