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Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes
[Image: see text] Free fatty acid receptor 1 (FFA1 or GPR40) enhances glucose-stimulated insulin secretion from pancreatic β-cells and currently attracts high interest as a new target for the treatment of type 2 diabetes. We here report the discovery of a highly potent FFA1 agonist with favorable ph...
| Autores principales: | , , , , , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
American Chemical Society
2013
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| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3654565/ https://www.ncbi.nlm.nih.gov/pubmed/23687558 http://dx.doi.org/10.1021/ml4000673 |
| _version_ | 1782269579974672384 |
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| author | Christiansen, Elisabeth Hansen, Steffen V. F. Urban, Christian Hudson, Brian D. Wargent, Edward T. Grundmann, Manuel Jenkins, Laura Zaibi, Mohamed Stocker, Claire J. Ullrich, Susanne Kostenis, Evi Kassack, Matthias U. Milligan, Graeme Cawthorne, Michael A. Ulven, Trond |
| author_facet | Christiansen, Elisabeth Hansen, Steffen V. F. Urban, Christian Hudson, Brian D. Wargent, Edward T. Grundmann, Manuel Jenkins, Laura Zaibi, Mohamed Stocker, Claire J. Ullrich, Susanne Kostenis, Evi Kassack, Matthias U. Milligan, Graeme Cawthorne, Michael A. Ulven, Trond |
| author_sort | Christiansen, Elisabeth |
| collection | PubMed |
| description | [Image: see text] Free fatty acid receptor 1 (FFA1 or GPR40) enhances glucose-stimulated insulin secretion from pancreatic β-cells and currently attracts high interest as a new target for the treatment of type 2 diabetes. We here report the discovery of a highly potent FFA1 agonist with favorable physicochemical and pharmacokinetic properties. The compound efficiently normalizes glucose tolerance in diet-induced obese mice, an effect that is fully sustained after 29 days of chronic dosing. |
| format | Online Article Text |
| id | pubmed-3654565 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2013 |
| publisher | American Chemical Society |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-36545652013-05-15 Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes Christiansen, Elisabeth Hansen, Steffen V. F. Urban, Christian Hudson, Brian D. Wargent, Edward T. Grundmann, Manuel Jenkins, Laura Zaibi, Mohamed Stocker, Claire J. Ullrich, Susanne Kostenis, Evi Kassack, Matthias U. Milligan, Graeme Cawthorne, Michael A. Ulven, Trond ACS Med Chem Lett [Image: see text] Free fatty acid receptor 1 (FFA1 or GPR40) enhances glucose-stimulated insulin secretion from pancreatic β-cells and currently attracts high interest as a new target for the treatment of type 2 diabetes. We here report the discovery of a highly potent FFA1 agonist with favorable physicochemical and pharmacokinetic properties. The compound efficiently normalizes glucose tolerance in diet-induced obese mice, an effect that is fully sustained after 29 days of chronic dosing. American Chemical Society 2013-04-08 /pmc/articles/PMC3654565/ /pubmed/23687558 http://dx.doi.org/10.1021/ml4000673 Text en Copyright © 2013 American Chemical Society Terms of Use (http://pubs.acs.org/page/policy/authorchoice_termsofuse.html) |
| spellingShingle | Christiansen, Elisabeth Hansen, Steffen V. F. Urban, Christian Hudson, Brian D. Wargent, Edward T. Grundmann, Manuel Jenkins, Laura Zaibi, Mohamed Stocker, Claire J. Ullrich, Susanne Kostenis, Evi Kassack, Matthias U. Milligan, Graeme Cawthorne, Michael A. Ulven, Trond Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes |
| title | Discovery of TUG-770: A Highly Potent Free Fatty Acid
Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes |
| title_full | Discovery of TUG-770: A Highly Potent Free Fatty Acid
Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes |
| title_fullStr | Discovery of TUG-770: A Highly Potent Free Fatty Acid
Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes |
| title_full_unstemmed | Discovery of TUG-770: A Highly Potent Free Fatty Acid
Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes |
| title_short | Discovery of TUG-770: A Highly Potent Free Fatty Acid
Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes |
| title_sort | discovery of tug-770: a highly potent free fatty acid
receptor 1 (ffa1/gpr40) agonist for treatment of type 2 diabetes |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3654565/ https://www.ncbi.nlm.nih.gov/pubmed/23687558 http://dx.doi.org/10.1021/ml4000673 |
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