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Crystal structures of ABL-related gene (ABL2) in complex with imatinib, tozasertib (VX-680), and a type I inhibitor of the triazole carbothioamide class.

Abstract:

ABL2 (also known as ARG (ABL related gene)) is closely related to the well-studied Abelson kinase cABL. ABL2 is involved in human neoplastic diseases and is deregulated in solid tumors. Oncogenic gene translocations occur in acute leukemia. So far no structural information for ABL2 has been reported. To elucidate structural determinants for inhibitor interaction, we determined the cocrystal structure of ABL2 with the oncology drug imatinib. Interestingly, imatinib not only interacted with the...

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Journal:
Journal of medicinal chemistry
Volume:
54
Issue:
7
Pages:
2359-2367
Publication date:
2011-01-01
ISSN:
1520-4804
URN:
uuid:f17a651f-9ca9-453e-8b2f-419bbe584e0f
Local pid:
SGC:21417343

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