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

Diabetes

Volumn 62, Issue 6, 2013, Pages 2106-2111

  Wagner, Robert ^a   Kaiser, Gabriele ^a   Gerst, Felicia ^a   Christiansen, Elisabeth ^c   Due Hansen, Maria E ^c   Grundmann, Manuel ^b   Machicao, Fausto ^a   Peter, Andreas ^a   Kostenis, Evi ^b   Ulven, Trond ^c   Fritsche, Andreas ^a   Har̈ing, Hans Ulrich ^a   Ullrich, Susanne ^a  

^a UNIVERSITY OF TÜBINGEN   (Germany)

^b UNIVERSITY OF BONN   (Germany)

^c UNIVERSITY OF SOUTHERN DENMARK   (Denmark)

Author keywords

[No Author keywords available]

Indexed keywords

FATTY ACID DERIVATIVE; G PROTEIN COUPLED RECEPTOR 40; GLUCOSE; INSULIN; PALMITIC ACID; TUG 469; UNCLASSIFIED DRUG;

ADULT; ANIMAL EXPERIMENT; APOPTOSIS; ARTICLE; CONTROLLED STUDY; DRUG TARGETING; FEMALE; GENETIC VARIABILITY; GENOTYPE; HUMAN; IN VITRO STUDY; IN VIVO STUDY; INSULIN RELEASE; MAJOR CLINICAL STUDY; MALE; MOUSE; NONHUMAN; PANCREAS ISLET BETA CELL; PHENOTYPE; PRIORITY JOURNAL; STIMULATION;

ANIMALS; CELL LINE; CELLS, CULTURED; FATTY ACIDS, NONESTERIFIED; GENOTYPE; HUMANS; INSULIN; INSULIN-SECRETING CELLS; ISLETS OF LANGERHANS; MICE; PALMITATES; RECEPTORS, G-PROTEIN-COUPLED;

EID: 84878230795     PISSN: 00121797     EISSN: 1939327X     Source Type: Journal    
DOI: 10.2337/db12-1249     Document Type: Article

References (26)

1. Briscoe CP, Tadayyon M, Andrews JL, et al. The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids. J Biol Chem 2003;278:11303-11311 (Pubitemid 36792687)
2. Itoh Y, Kawamata Y, Harada M, et al. Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40. Nature 2003;422:173-176 (Pubitemid 36362750)
3. Nolan CJ, Madiraju MS, Delghingaro-Augusto V, Peyot ML, Prentki M. Fatty acid signaling in the beta-cell and insulin secretion. Diabetes 2006;55(Suppl 2):S16-S23 (Pubitemid 44927028)
4. Burant CF, Viswanathan P, Marcinak J, et al. TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: a phase 2, randomised, doubleblind, placebo-controlled trial. Lancet 2012;379:1403-1411
5. Christiansen E, Urban C, Grundmann M, et al. Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties. J Med Chem 2011;54:6691-6703
6. Christiansen E, Urban C, Merten N, et al. Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes. J Med Chem 2008;51:7061-7064
7. Scott RA, Lagou V, Welch RP, et al DIAbetes Genetics Replication and Meta-analysis (DIAGRAM) Consortium. Large-scale association analyses identify new loci influencing glycemic traits and provide insight into the underlying biological pathways. Nat Genet 2012;44:991-1005
8. Maedler K, Spinas GA, Dyntar D, Moritz W, Kaiser N, Donath MY. Distinct effects of saturated and monounsaturated fatty acids on beta-cell turnover and function. Diabetes 2001;50:69-76 (Pubitemid 32047983)
9. Sargsyan E, Bergsten P. Lipotoxicity is glucose-dependent in INS-1E cells but not in human islets and MIN6 cells. Lipids Health Dis 2011;10:115-121
10. Eitel K, Staiger H, Brendel MD, et al. Different role of saturated and unsaturated fatty acids in beta-cell apoptosis. Biochem Biophys Res Commun 2002;299:853-856 (Pubitemid 36034564)
11. Paolisso G, Gambardella A, Amato L, et al. Opposite effects of short- and long-term fatty acid infusion on insulin secretion in healthy subjects. Diabetologia 1995;38:1295-1299
12. Carpentier A, Mittelman SD, Lamarche B, Bergman RN, Giacca A, Lewis GF. Acute enhancement of insulin secretion by FFA in humans is lost with prolonged FFA elevation. Am J Physiol 1999;276:E1055-E1066 (Pubitemid 29323421)
13. Carpentier A, Mittelman SD, Bergman RN, Giacca A, Lewis GF. Prolonged elevation of plasma free fatty acids impairs pancreatic beta-cell function in obese nondiabetic humans but not in individuals with type 2 diabetes. Diabetes 2000;49:399-408 (Pubitemid 30131785)
14. Kashyap S, Belfort R, Gastaldelli A, et al. A sustained increase in plasma free fatty acids impairs insulin secretion in nondiabetic subjects genetically predisposed to develop type 2 diabetes. Diabetes 2003;52:2461-2474 (Pubitemid 37210533)
15. Lan H, Hoos LM, Liu L, et al. Lack of FFAR1/GPR40 does not protect mice from high-fat diet-induced metabolic disease. Diabetes 2008;57:2999-3006
16. Ranta F, Avram D, Berchtold S, et al. Dexamethasone induces cell death in insulin-secreting cells, an effect reversed by exendin-4. Diabetes 2006;55:1380-1390 (Pubitemid 44195377)
17. Ullrich S, Berchtold S, Ranta F, et al. Serum- and glucocorticoid- inducible kinase 1 (SGK1) mediates glucocorticoid-induced inhibition of insulin secretion. Diabetes 2005;54:1090-1099 (Pubitemid 40446323)
18. Christiansen E, Due-Hansen ME, Urban C, et al. Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties. J Med Chem 2012;55:6624-6628
19. Matsuda M, DeFronzo RA. Insulin sensitivity indices obtained from oral glucose tolerance testing: comparison with the euglycemic insulin clamp. Diabetes Care 1999;22:1462-1470 (Pubitemid 29418240)
20. Herzberg-Schäfer SA, Staiger H, Heni M, et al. Evaluation of fasting state-/oral glucose tolerance test-derived measures of insulin release for the detection of genetically impaired b-cell function. PLoS ONE 2010;5:e14194
21. Gauderman W, Morrison J. QUANTO 1.1: A computer program for power and sample size calculations for genetic-epidemiology studies. Available at: http://hydra.usc.edu/gxe/
22. Christiansen E, Due-Hansen ME, Urban C, et al. Structure-activity study of dihydrocinnamic acids and discovery of the potent FFA1 (GPR40) agonist TUG-469. ACS Med Chem Lett 2010;1:345-349
23. Kalis M, Levéen P, Lyssenko V, Almgren P, Groop L, Cilio CM. Variants in the FFAR1 gene are associated with beta cell function. PLoS ONE 2007;2:e1090
24. Dupuis J, Langenberg C, Prokopenko I, et al.; DIAGRAM Consortium; GIANT Consortium; Global BPgen Consortium; Anders Hamsten on behalf of Procardis Consortium; MAGIC investigators. New genetic loci implicated in fasting glucose homeostasis and their impact on type 2 diabetes risk. Nat Genet 2010;42:105-116
25. Zhang Y, Xu M, Zhang S, et al. The role of G protein-coupled receptor 40 in lipoapoptosis in mouse beta-cell line NIT-1. J Mol Endocrinol 2007;38:651-661 (Pubitemid 47019065)
26. Salgin B, Ong KK, Thankamony A, Emmett P, Wareham NJ, Dunger DB. Higher fasting plasma free fatty acid levels are associated with lower insulin secretion in children and adults and a higher incidence of type 2 diabetes. J Clin Endocrinol Metab 2012;97:3302-3309