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Christiansen E, Hansen SV, Urban C, et al. Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes. ACS Med Chem Lett. 2013;4(5):441-445doi: 10.1021/ml4000673.
Christiansen, E., Hansen, S. V., Urban, C., Hudson, B. D., Wargent, E. T., Grundmann, M., Jenkins, L., Zaibi, M., Stocker, C. J., Ullrich, S., Kostenis, E., Kassack, M. U., Milligan, G., Cawthorne, M. A., & Ulven, T. (2013). Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes. ACS medicinal chemistry letters, 4(5), 441-445. https://doi.org/10.1021/ml4000673
Christiansen, Elisabeth, et al. "Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes." ACS medicinal chemistry letters vol. 4,5 (2013): 441-445. doi: https://doi.org/10.1021/ml4000673
Christiansen E, Hansen SV, Urban C, Hudson BD, Wargent ET, Grundmann M, Jenkins L, Zaibi M, Stocker CJ, Ullrich S, Kostenis E, Kassack MU, Milligan G, Cawthorne MA, Ulven T. Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes. ACS Med Chem Lett. 2013 May 09;4(5):441-445. doi: 10.1021/ml4000673. Epub 2013 Apr 08. PMID: 23687558; PMCID: PMC3654565.
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ACS Med Chem Lett. 2013 May 09;4(5):441-445. doi: 10.1021/ml4000673. Epub 2013 Apr 08.

Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes.

ACS medicinal chemistry letters

Elisabeth Christiansen, Steffen V F Hansen, Christian Urban, Brian D Hudson, Edward T Wargent, Manuel Grundmann, Laura Jenkins, Mohamed Zaibi, Claire J Stocker, Susanne Ullrich, Evi Kostenis, Matthias U Kassack, Graeme Milligan, Michael A Cawthorne, Trond Ulven

Affiliations

  1. Department of Physics, Chemistry and Pharmacy, University of Southern Denmark , Campusvej 55, DK-5230 Odense M, Denmark.

PMID: 23687558 PMCID: PMC3654565 DOI: 10.1021/ml4000673

Abstract

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.

Keywords: FFA1 agonist; GPR40 agonist; TUG-770; Type 2 diabetes; free fatty acid receptor; insulin secretagogue

References

  1. ACS Med Chem Lett. 2010 Jul 02;1(7):345-9 - PubMed
  2. Lancet. 2012 Apr 14;379(9824):1403-11 - PubMed
  3. ACS Med Chem Lett. 2010 Jun 18;1(6):290-4 - PubMed
  4. J Med Chem. 2012 Jul 26;55(14):6624-8 - PubMed
  5. Front Endocrinol (Lausanne). 2012 Jan 03;2:112 - PubMed
  6. J Med Chem. 2013 Feb 14;56(3):982-92 - PubMed
  7. Biochem Biophys Res Commun. 2003 Feb 7;301(2):406-10 - PubMed
  8. J Med Chem. 2008 Nov 27;51(22):7061-4 - PubMed
  9. J Med Chem. 2011 Oct 13;54(19):6691-703 - PubMed
  10. J Med Chem. 2012 May 10;55(9):4511-5 - PubMed
  11. J Biol Chem. 2003 Mar 28;278(13):11303-11 - PubMed
  12. J Org Chem. 2010 Feb 19;75(4):1301-4 - PubMed
  13. J Med Chem. 2011 Mar 10;54(5):1365-78 - PubMed
  14. Drug Discov Today. 2004 May 15;9(10):430-1 - PubMed
  15. Nature. 2003 Mar 13;422(6928):173-6 - PubMed
  16. Nat Rev Drug Discov. 2007 Nov;6(11):881-90 - PubMed
  17. Nat Rev Drug Discov. 2012 Aug;11(8):603-19 - PubMed

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