Discovery of a potent free fatty acid 1 receptor agonist with low lipophilicity, low polar surface area and robust in vivo efficacy

Hansen, S. V.F. et al. (2016) Discovery of a potent free fatty acid 1 receptor agonist with low lipophilicity, low polar surface area and robust in vivo efficacy. Journal of Medicinal Chemistry, 59, pp. 2841-2846. (doi: 10.1021/acs.jmedchem.5b01962)

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Abstract

The free fatty acid receptor 1 (FFA1 or GPR40) is established as an interesting potential target for treatment of type 2 diabetes. However, to obtain optimal ligands, it may be necessary to limit both lipophilicity and polar surface area, translating to a need for small compounds. We here describe the identification of 24, a potent FFA1 agonist with low lipophilicity and very high ligand efficiency that exhibit robust glucose lowering effect.

Item Type:Articles
Additional Information:Funding sources: Danish Council for Independent Research, Technology and Production (grant 09-070364) and the Danish Council for Strategic Research (grant 11-116196) and the University of Southern Denmark (SDU2020) for financial support.
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Milligan, Professor Graeme and Hudson, Dr Brian
Authors: Hansen, S. V.F., Christiansen, E., Urban, C., Hudson, B. D., Stocker, C. J., Due-Hansen, M. E., Wargent, E. T., Shimpukade, B., Almeida, R., Ejsing, C. S., Cawthorne, M. A., Kassack, M. U., Milligan, G., and Ulven, T.
College/School:College of Medical Veterinary and Life Sciences > Institute of Molecular Cell and Systems Biology
Journal Name:Journal of Medicinal Chemistry
Publisher:American Chemical Society
ISSN:0022-2623
ISSN (Online):1520-4804
Published Online:01 March 2016

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