Discovery of a potent free fatty acid 1 receptor agonist with low lipophilicity, low polar surface area and robust in vivo efficacy (original) (raw)
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: | Hudson, Dr Brian and Milligan, Professor Graeme |
| 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 > School of Molecular Biosciences |
| 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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Deposit and Record Details
| ID Code: | 117104 |
|---|---|
| Depositing User: | Mr Gavin Merrifield |
| Datestamp: | 07 Mar 2016 12:01 |
| Last Modified: | 21 Sep 2022 06:52 |
| Date of acceptance: | 1 March 2016 |
| Date of first online publication: | 1 March 2016 |
| Data Availability Statement: | Yes |