Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site.
作者： Doriano Fabbro , Paul W. Manley , Wolfgang Jahnke , Janis Liebetanz , Alexandra Szyttenholm
DOI: 10.1016/J.BBAPAP.2009.12.009
关键词: Imatinib mesylate 、 Biochemistry 、 Dasatinib 、 Kinase 、 Proto-oncogene tyrosine-protein kinase Src 、 Allosteric regulation 、 Nilotinib 、 Protein kinase domain 、 Biology 、 ABL
摘要: The ATP-competitive inhibitors dasatinib and nilotinib, which bind to catalytically different conformations of the Abl kinase domain, have recently been approved for treatment imatinib-resistant CML. These two new drugs, albeit very efficient against most mutants Bcr-Abl, fail effectively suppress Bcr-Abl activity T315I (or gatekeeper) mutation. Generating ATP site-binding drugs that target in has hampered, amongst others, by selectivity, is frequently an issue when developing inhibitors. Recently, using unbiased cellular screening approach, GNF-2, a non-ATP-competitive inhibitor, identified demonstrates transformed cells. exquisite selectivity GNF-2 due finding it targets myristate binding site located near C-terminus as demonstrated genetic approaches, solution NMR X-ray crystallography. like myristate, able induce and/or stabilize clamped inactive conformation analogous SH2-Y527 interaction Src. molecular mechanism allosteric inhibition inhibitor class, combined effects with such nilotinib imatinib on wild-type mutants, particular gatekeeper mutant, are reviewed.
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