Journal article
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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(Accepted manuscript, pdf, 393.7KB)
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(Accepted manuscript, pdf, 384.1KB)
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(Accepted manuscript, pdf, 70.2KB)
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- Publisher copy:
- 10.1016/j.bmcl.2010.08.032
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Authors
Contributors
+ McNeill, L
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Chemistry Research Laboratory
Role:
Researcher
+ Hewitson, K
Institution:
University of Oxford
Oxford college:
St Edmund Hall
Role:
Researcher
+ Ge, W
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Chemistry Research Laboratory
Role:
Researcher
+ Liénard, B
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Chemistry Research Laboratory
Role:
Researcher
Funding
+ European Commision : Marie Curie programme
More from this funder
Funding agency for:
Conejo-Garcia, A
Grant:
MEIF-CT-2003-500525
European Union
More from this funder
BBSCR
More from this funder
Bibliographic Details
- 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
Item Description
- Language:
- English
- Keywords:
- Subjects:
- UUID:
-
uuid:64146860-e31b-481f-9ff8-28a593a0b108
- Local pid:
- ora:5447
- Deposit date:
- 2011-06-14
Related Items
Terms of use
- Copyright holder:
- Elsevier
- Copyright date:
- 2010
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