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An approach to enzyme inhibition employing reversible boronate ester formation

Abstract:

Dynamic combinatorial chemistry (DCC) is a potentially useful method for the identification of biomacromolecule ligands; however, the number of reactions applicable to DCC in aqueous solution is limited. We report studies that investigate the reversible reaction of boronic acids with alcohols as an approach to enzyme inhibition, employing α-chymotrypsin as a model system. NMR techniques (11B NMR and 1H waterLOGSY) were used to observe ternary complexes of boronic acids, ...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1039/c1md00011j

Authors


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Institution:
University of Oxford
Oxford college:
St Peter's College
Department:
Oxford, MPLS, Chemistry, Organic Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Department:
Oxford, MPLS, Chemistry, Organic Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Department:
Oxford, MPLS, Chemistry, Organic Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Department:
Oxford, MPLS, Chemistry, Organic Chemistry
Role:
Author
Biotechnology and Biological Sciences Research Council More from this funder
Engineering and Physical Sciences Research Council More from this funder
Publisher:
Royal Society of Chemistry Publisher's website
Journal:
MEDCHEMCOMM Journal website
Volume:
2
Issue:
5
Pages:
390-395
Publication date:
2011-05-05
DOI:
EISSN:
2040-2511
ISSN:
2040-2503
URN:
uuid:35b7f824-d875-4f66-852c-816894d813d6
Source identifiers:
159326
Local pid:
pubs:159326

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