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Structural basis for binding of cyclic 2-oxoglutarate analogues to factor-inhibiting hypoxia-inducible factor

Abstract:
Aromatic analogues of the 2-oxoglutarate cosubstrate of the hypoxia-inducible factor hydroxylases are shown to bind at the active site iron: Pyridine-2,4-dicarboxylate binds as anticipated with a single molecule chelating the iron in a bidentate manner. The binding mode of a hydroxamic acid analogue, at least in the crystalline state, is unusual because two molecules of the inhibitor are observed at the active site and partial displacement of the iron binding aspartyl residue was observed.
Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1016/j.bmcl.2010.08.032

Authors


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Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Chemistry Research Laboratory
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Chemistry Research Laboratory
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Chemistry Research Laboratory
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Chemistry Research Laboratory
Oxford college:
Hertford College
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Chemistry Research Laboratory
Oxford college:
Linacre College
Role:
Author

Contributors

Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Chemistry Research Laboratory
Role:
Researcher
Institution:
University of Oxford
Oxford college:
St Edmund Hall
Role:
Researcher
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Chemistry Research Laboratory
Role:
Researcher
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Chemistry Research Laboratory
Role:
Researcher
More from this funder
Funding agency for:
Conejo-Garcia, A
Grant:
MEIF-CT-2003-500525
European Union More from this funder
Publisher:
Elsevier Publisher's website
Journal:
Bioorganic & Medicinal Chemistry Letters Journal website
Volume:
20
Issue:
20
Pages:
6125-6128
Publication date:
2010-10-01
DOI:
ISSN:
0960-894X
Language:
English
Keywords:
Subjects:
UUID:
uuid:64146860-e31b-481f-9ff8-28a593a0b108
Local pid:
ora:5447
Deposit date:
2011-06-14

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