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

Actions

Email

Email this record

Send the bibliographic details of this record to your email address.

Your Email
Please enter the email address that the record information will be sent to.

-
Your message (optional)
Please add any additional information to be included within the email.
Share
Cite

Cite this record

APA Style

Conejo-Garcia, A., McDonough, M., Loenarz, C., Schofield, C., & Clifton, I. (2010). Structural basis for binding of cyclic 2-oxoglutarate analogues to factor-inhibiting hypoxia-inducible factor. Bioorganic & Medicinal Chemistry Letters, 20(20), 6125–6128 .

MLA Style

Conejo-Garcia, A, et al. “Structural Basis for Binding of Cyclic 2-Oxoglutarate Analogues to Factor-Inhibiting Hypoxia-Inducible Factor.” Bioorganic & Medicinal Chemistry Letters, Accepted Manuscript, vol. 20, no. 20, 2010, pp. 6125–28 .

Chicago Style

Conejo-Garcia, A, M McDonough, C Loenarz, C Schofield, and I Clifton. 2010. “Structural Basis for Binding of Cyclic 2-Oxoglutarate Analogues to Factor-Inhibiting Hypoxia-Inducible Factor.” Bioorganic & Medicinal Chemistry Letters 20 (20): 6125–28 .
Print

Access Document

Files:: Figures

(Accepted manuscript, bin, 393.7KB, Terms of use)

Supplementary Material

(Accepted manuscript, bin, 384.1KB, Terms of use)

Text of article

(Accepted manuscript, bin, 70.2KB, Terms of use)

Publisher copy:: 10.1016/j.bmcl.2010.08.032

Authors

+ Conejo-Garcia, A More by this author

Institution:: University of Oxford
Division:: MPLS
Department:: Chemistry
Sub department:: Chemistry Research Laboratory
Role:: Author

+ McDonough, M More by this author

Institution:: University of Oxford
Division:: MPLS
Department:: Chemistry
Sub department:: Chemistry Research Laboratory
Role:: Author

+ Loenarz, C More by this author

Institution:: University of Oxford
Division:: MPLS
Department:: Chemistry
Sub department:: Chemistry Research Laboratory
Role:: Author

+ Schofield, C More by this author

Institution:: University of Oxford
Division:: MPLS
Department:: Chemistry
Sub department:: Chemistry Research Laboratory
Oxford college:: Hertford College
Role:: Author

+ Clifton, I 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

+ European Commision : Marie Curie programme More from this funder

Funding agency for:: Conejo-Garcia, A
Grant:: MEIF-CT-2003-500525

+ BBSCR More from this funder

+ European Union More from this funder

Publisher:: Elsevier
Journal:: Bioorganic & Medicinal Chemistry Letters More from this journal
Volume:: 20
Issue:: 20
Pages:: 6125-6128
Publication date:: 2010-10-01
Edition:: Accepted Manuscript
DOI:: 10.1016/j.bmcl.2010.08.032
ISSN:: 0960-894X

Language:: English
Keywords:: factor inhibiting hypoxia-inducible factor

2-oxoglutarate analogue

oxygenase

hypoxic response

hydroxamic acid
Subjects:: Chemical biology
UUID:: uuid:64146860-e31b-481f-9ff8-28a593a0b108
Local pid:: ora:5447
Deposit date:: 2011-06-14
ARK identifier:: ark:/29072/ora_64146860e31b481f9ff828a593a0b108

Terms of use

Copyright holder:: Elsevier
Copyright date:: 2010

Licence:: Terms and Conditions of Use for Oxford University Research Archive

Views and Downloads

About views and downloads

If you are the owner of this record, you can report an update to it here: Report update to this record

TO TOP