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Second Generation Abl Kinase Inhibitors and Novel Compounds to Eliminate the Bcr-Abl/T315I Clone

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The first line therapy for chronic myeloid leukemia (CML) was dramatically altered within a few years of the introduction of Abl specific tyrosine kinase inhibitor, imatinib mesylate to the clinic. However, refractoriness and early relapse have frequently been reported, particularly in patients with advanced-stage disease. Point mutations within the Abl kinase domain that interfere with imatinib mesylate binding are most critical cause of imatinib resistance. To override resistance, several second generation ATP competitive Abl kinase inhibitors such as dasatinib, nilotinib and INNO-406 have been developed. Although, these novel inhibitors can inhibit the phosphorylation of most mutated Bcr-Abl except T315I, no ATP competitive Abl kinase inhibitors, which can inhibit the phosphorylation of Bcr-Abl/T315I, has been developed. Thus, Bcr-Abl/T315I is an important and challenging target for discovery of CML therapeutics. This review is focused on the three novel compounds reported in the recent patents (2004-2006) which claim the efficacy against Bcr- Abl/T315I.





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Keywords: Bcr-Abl; SGX; cyclin dependent kinase; hydrazine derivatives; imatinib mesylate

Document Type: Research Article

Affiliations: Department of Transfusion Medicine and Cell Therapy, Kyoto University Hospital, 54 Kawahara-cho Shogoin, Sakyo-ku, Kyoto 606-8507, Japan.

Publication date: November 1, 2006

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  • Recent Patents on Anti-Cancer Drug Discovery publishes review articles on recent patents in the field of anti-cancer drug discovery e.g. novel bioactive compounds, analogs & targets. A selection of important and recent patents on anti-cancer drug discovery is also included in the journal. The journal is essential reading for all researchers involved in anti-cancer drug design and discovery.
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