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Journal article

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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Publication status:
Published

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Publisher copy:
10.1021/jm101506n

Authors


More by this author
Institution:
University of Oxford
Division:
MSD
Department:
NDM
Sub department:
Structural Genomics Consortium
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MSD
Department:
NDM
Sub department:
Structural Genomics Consortium
Role:
Author
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Journal:
Journal of medicinal chemistry
Volume:
54
Issue:
7
Pages:
2359-2367
Publication date:
2011-04-01
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
Source identifiers:
127159
Language:
English
Keywords:
Pubs id:
pubs:127159
UUID:
uuid:8cc25c57-5a56-447d-8c6f-c175e2a552f0
Local pid:
pubs:127159
Deposit date:
2012-12-19

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