Defining the molecular basis for the first potent and selective orthosteric agonists of the FFA2 free fatty acid receptor

Hudson, B.D. et al. (2013) Defining the molecular basis for the first potent and selective orthosteric agonists of the FFA2 free fatty acid receptor. Journal of Biological Chemistry, 288(24), pp. 17296-17312. (doi: 10.1074/jbc.M113.455337)

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Abstract

Background: Understanding the function of FFA2 has been slowed by a lack of selective orthosteric ligands. Results: Residues within FFA2 that dictate the recognition and function of potent and selective orthosteric agonists are described. Conclusion: Key aspects of ligand interaction with the orthosteric binding pocket of FFA2 are defined. Significance: This work will be invaluable in future drug development at the FFA2 receptor.

Item Type:Articles
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Ward, Dr Richard and Marquez, Dr Rudi and Hudson, Dr Brian and Murdoch, Dr Hannah and Milligan, Professor Graeme
Authors: Hudson, B.D., Due-Hansen, M.E., Christiansen, E., Hansen, A.M., Mackenzie, A.E., Murdoch, H., Pandey, S.K., Ward, R.J., Marquez, R., Tikhonova, I.G., Ulven, T., and Milligan, G.
College/School:College of Medical Veterinary and Life Sciences > Institute of Molecular Cell and Systems Biology
College of Science and Engineering > School of Chemistry
Journal Name:Journal of Biological Chemistry
Publisher:American Society for Biochemistry and Molecular Biology, Inc.
ISSN:0021-9258
ISSN (Online):1083-351X
Copyright Holders:Copyright © 2013 The The American Society for Biochemistry and Molecular Biology, Inc.
First Published:First published in Journal of Biological Chemistry 288(24):17296-17312
Publisher Policy:Reproduced under a Creative Commons License
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Project CodeAward NoProject NamePrincipal InvestigatorFunder's NameFunder RefLead Dept
519861Developing selective ligands for Free Fatty Acid Receptor 2 with novel pharmacological propertiesGraeme MilliganWellcome Trust (WELLCOME)089600/Z/09/ZRI NEUROSCIENCE & PSYCHOLOGY