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Items: 1 to 20 of 135

1.

Reevaluation of fatty acid receptor 1 as a drug target for the stimulation of insulin secretion in humans.

Wagner R, Kaiser G, Gerst F, Christiansen E, Due-Hansen ME, Grundmann M, Machicao F, Peter A, Kostenis E, Ulven T, Fritsche A, Häring HU, Ullrich S.

Diabetes. 2013 Jun;62(6):2106-11. doi: 10.2337/db12-1249. Epub 2013 Feb 1.

2.

Activation of extracellular signal-regulated protein kinases 1 and 2 (ERK1/2) by free fatty acid receptor 1 (FFAR1/GPR40) protects from palmitate-induced beta cell death, but plays no role in insulin secretion.

Panse M, Gerst F, Kaiser G, Teutsch CA, Dölker R, Wagner R, Häring HU, Ullrich S.

Cell Physiol Biochem. 2015;35(4):1537-45. doi: 10.1159/000373969. Epub 2015 Mar 12.

3.

FFAR1 is involved in both the acute and chronic effects of palmitate on insulin secretion.

Kristinsson H, Smith DM, Bergsten P, Sargsyan E.

Endocrinology. 2013 Nov;154(11):4078-88. doi: 10.1210/en.2013-1352. Epub 2013 Sep 13.

PMID:
24035997
4.

Lack of GPR40/FFAR1 does not induce diabetes even under insulin resistance condition.

Matsuda-Nagasumi K, Takami-Esaki R, Iwachidow K, Yasuhara Y, Tanaka H, Ogi K, Nakata M, Yano T, Hinuma S, Taketomi S, Odaka H, Kaisho Y.

Diabetes Obes Metab. 2013 Jun;15(6):538-45. doi: 10.1111/dom.12065. Epub 2013 Feb 6.

PMID:
23331570
5.

Free fatty acid receptor 1 (FFAR1/GPR40) signaling affects insulin secretion by enhancing mitochondrial respiration during palmitate exposure.

Kristinsson H, Bergsten P, Sargsyan E.

Biochim Biophys Acta. 2015 Dec;1853(12):3248-57. doi: 10.1016/j.bbamcr.2015.09.022. Epub 2015 Sep 25.

PMID:
26408932
6.

A novel antidiabetic drug, fasiglifam/TAK-875, acts as an ago-allosteric modulator of FFAR1.

Yabuki C, Komatsu H, Tsujihata Y, Maeda R, Ito R, Matsuda-Nagasumi K, Sakuma K, Miyawaki K, Kikuchi N, Takeuchi K, Habata Y, Mori M.

PLoS One. 2013 Oct 10;8(10):e76280. doi: 10.1371/journal.pone.0076280. eCollection 2013.

7.

Identification and pharmacological characterization of multiple allosteric binding sites on the free fatty acid 1 receptor.

Lin DC, Guo Q, Luo J, Zhang J, Nguyen K, Chen M, Tran T, Dransfield PJ, Brown SP, Houze J, Vimolratana M, Jiao XY, Wang Y, Birdsall NJ, Swaminath G.

Mol Pharmacol. 2012 Nov;82(5):843-59. doi: 10.1124/mol.112.079640. Epub 2012 Aug 2.

8.

In vitro and mouse in vivo characterization of the potent free fatty acid 1 receptor agonist TUG-469.

Urban C, Hamacher A, Partke HJ, Roden M, Schinner S, Christiansen E, Due-Hansen ME, Ulven T, Gohlke H, Kassack MU.

Naunyn Schmiedebergs Arch Pharmacol. 2013 Dec;386(12):1021-30. doi: 10.1007/s00210-013-0899-3. Epub 2013 Jul 17.

PMID:
23861168
9.

Selective small-molecule agonists of G protein-coupled receptor 40 promote glucose-dependent insulin secretion and reduce blood glucose in mice.

Tan CP, Feng Y, Zhou YP, Eiermann GJ, Petrov A, Zhou C, Lin S, Salituro G, Meinke P, Mosley R, Akiyama TE, Einstein M, Kumar S, Berger JP, Mills SG, Thornberry NA, Yang L, Howard AD.

Diabetes. 2008 Aug;57(8):2211-9. doi: 10.2337/db08-0130. Epub 2008 May 13.

10.

Potentiation of insulin secretion and improvement of glucose intolerance by combining a novel G protein-coupled receptor 40 agonist DS-1558 with glucagon-like peptide-1 receptor agonists.

Nakashima R, Yano T, Ogawa J, Tanaka N, Toda N, Yoshida M, Takano R, Inoue M, Honda T, Kume S, Matsumoto K.

Eur J Pharmacol. 2014 Aug 15;737:194-201. doi: 10.1016/j.ejphar.2014.05.014. Epub 2014 May 22.

PMID:
24858371
11.

Peroxisome proliferator-activated receptor gamma (PPARG) modulates free fatty acid receptor 1 (FFAR1) dependent insulin secretion in humans.

Wagner R, Hieronimus A, Lamprinou A, Heni M, Hatziagelaki E, Ullrich S, Stefan N, Staiger H, Häring HU, Fritsche A.

Mol Metab. 2014 Jul 7;3(6):676-80. doi: 10.1016/j.molmet.2014.07.001. eCollection 2014 Sep.

12.

The effects of TAK-875, a selective G protein-coupled receptor 40/free fatty acid 1 agonist, on insulin and glucagon secretion in isolated rat and human islets.

Yashiro H, Tsujihata Y, Takeuchi K, Hazama M, Johnson PR, Rorsman P.

J Pharmacol Exp Ther. 2012 Feb;340(2):483-9. doi: 10.1124/jpet.111.187708. Epub 2011 Nov 21.

13.

Lack of FFAR1/GPR40 does not protect mice from high-fat diet-induced metabolic disease.

Lan H, Hoos LM, Liu L, Tetzloff G, Hu W, Abbondanzo SJ, Vassileva G, Gustafson EL, Hedrick JA, Davis HR.

Diabetes. 2008 Nov;57(11):2999-3006. doi: 10.2337/db08-0596. Epub 2008 Aug 4.

14.

GPR40 protein levels are crucial to the regulation of stimulated hormone secretion in pancreatic islets. Lessons from spontaneous obesity-prone and non-obese type 2 diabetes in rats.

Meidute Abaraviciene S, Muhammed SJ, Amisten S, Lundquist I, Salehi A.

Mol Cell Endocrinol. 2013 Dec 5;381(1-2):150-9. doi: 10.1016/j.mce.2013.07.025. Epub 2013 Aug 2.

PMID:
23911664
15.

β-Arrestin Recruitment and Biased Agonism at Free Fatty Acid Receptor 1.

Mancini AD, Bertrand G, Vivot K, Carpentier É, Tremblay C, Ghislain J, Bouvier M, Poitout V.

J Biol Chem. 2015 Aug 21;290(34):21131-40. doi: 10.1074/jbc.M115.644450. Epub 2015 Jul 8.

16.

Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules.

Briscoe CP, Peat AJ, McKeown SC, Corbett DF, Goetz AS, Littleton TR, McCoy DC, Kenakin TP, Andrews JL, Ammala C, Fornwald JA, Ignar DM, Jenkinson S.

Br J Pharmacol. 2006 Jul;148(5):619-28. Epub 2006 May 15.

17.

GPR40 is necessary but not sufficient for fatty acid stimulation of insulin secretion in vivo.

Latour MG, Alquier T, Oseid E, Tremblay C, Jetton TL, Luo J, Lin DC, Poitout V.

Diabetes. 2007 Apr;56(4):1087-94.

18.

Alteration of the glucagon axis in GPR120 (FFAR4) knockout mice: a role for GPR120 in glucagon secretion.

Suckow AT, Polidori D, Yan W, Chon S, Ma JY, Leonard J, Briscoe CP.

J Biol Chem. 2014 May 30;289(22):15751-63. doi: 10.1074/jbc.M114.568683. Epub 2014 Apr 17.

19.

Deletion of GPR40 impairs glucose-induced insulin secretion in vivo in mice without affecting intracellular fuel metabolism in islets.

Alquier T, Peyot ML, Latour MG, Kebede M, Sorensen CM, Gesta S, Ronald Kahn C, Smith RD, Jetton TL, Metz TO, Prentki M, Poitout V.

Diabetes. 2009 Nov;58(11):2607-15. doi: 10.2337/db09-0362. Epub 2009 Aug 31.

20.

Overexpression of GPR40 in pancreatic beta-cells augments glucose-stimulated insulin secretion and improves glucose tolerance in normal and diabetic mice.

Nagasumi K, Esaki R, Iwachidow K, Yasuhara Y, Ogi K, Tanaka H, Nakata M, Yano T, Shimakawa K, Taketomi S, Takeuchi K, Odaka H, Kaisho Y.

Diabetes. 2009 May;58(5):1067-76. doi: 10.2337/db08-1233. Erratum in: Diabetes. 2009 Jul;58(7):1721.

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