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Development and application of ligand-based NMR screening assays for γ-butyrobetaine hydroxylase

Abstract:

γ-Butyrobetaine hydroxylase (BBOX) is a 2-oxoglutarate (2OG) dependent oxygenase that catalyses the stereoselective C-3 hydroxylation of γ-butyrobetaine (GBB) to give L-carnitine. L-carnitine is involved in fatty acid metabolism in all animals and in some prokaryotes, and BBOX is a current drug target for the treatment of myocardial infarction. We describe the development and application of 1 H NMR GBB/2OG reporter based assays employing paramagnetic relaxation enhancement to monitor inhibito...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1039/C6MD00004E

Authors


More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Organic Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Role:
Author
Wellcome Trust More from this funder
Cancer Research UK More from this funder
British Heart Foundation More from this funder
Biotechnology and Biological Sciences Research Council More from this funder
Publisher:
Royal Society of Chemistry Publisher's website
Journal:
MedChemComm Journal website
Publication date:
2016-02-17
Acceptance date:
2016-02-15
DOI:
EISSN:
2040-2511
ISSN:
2040-2503
Pubs id:
pubs:604478
UUID:
uuid:aa427c2c-74cf-4d55-9d44-acd76a526391
Local pid:
pubs:604478
Source identifiers:
604478
Deposit date:
2016-02-16

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