Comparative effects of the endogenous agonist glucagon-like peptide-1 (GLP-1)-(7-36) amide and the small-molecule ago-allosteric agent "compound 2" at the GLP-1 receptor

Journal of Pharmacology and Experimental Therapeutics

Volumn 334, Issue 3, 2010, Pages 795-808

  Coopman, Karen ^a   Huang, Yan ^a   Johnston, Neil ^a   Bradley, Sophie J ^a   Wilkinson, Graeme F ^b   Willars, Gary B ^a  

^a UNIVERSITY OF LEICESTER   (United Kingdom)

^b ASTRAZENECA   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

6,7 DICHLORO 2 METHYLSULFONYL 3 N TERT BUTYLAMINOQUINOXALINE; CALCIUM ION; EXENDIN [9-39]; GLUCAGON LIKE PEPTIDE; GLUCAGON LIKE PEPTIDE 1 RECEPTOR; GLUCAGON LIKE PEPTIDE 1 RECEPTOR AGONIST; GLUCAGON LIKE PEPTIDE 1 [7-36] AMIDE; HORMONE RECEPTOR AFFECTING AGENT; UNCLASSIFIED DRUG; 3-(TERT-BUTYLAMINO)-6,7-DICHLORO-2-(METHYLSULFONYL)QUINOXALINE; CALCIUM; CYCLIC AMP; GLUCAGON LIKE PEPTIDE 1; GLUCAGON RECEPTOR; GLUCAGON-LIKE PEPTIDE 1 (7-36)AMIDE; GLUCAGON-LIKE PEPTIDE-1 RECEPTOR; GREEN FLUORESCENT PROTEIN; GUANINE NUCLEOTIDE BINDING PROTEIN; LIGAND; PEPTIDE FRAGMENT; QUINOXALINE DERIVATIVE; SULFONE; TRYPAN BLUE;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; CALCIUM CELL LEVEL; CALCIUM SIGNALING; CELL MEMBRANE; CELL STRUCTURE; CELL VIABILITY; CONTROLLED STUDY; CYTOTOXICITY; DRUG MECHANISM; HUMAN; HUMAN CELL; INTERNALIZATION; NONHUMAN; PRIORITY JOURNAL; PROTEIN BINDING; PROTEIN EXPRESSION; SIGNAL TRANSDUCTION; BIOSYNTHESIS; BIOTRANSFORMATION; CELL LINE; CELL SURVIVAL; COMPARATIVE STUDY; DRUG EFFECTS; METABOLISM; STATISTICAL ANALYSIS;

BIOTRANSFORMATION; CALCIUM; CELL LINE; CELL MEMBRANE; CELL SURVIVAL; CYCLIC AMP; DATA INTERPRETATION, STATISTICAL; GLUCAGON-LIKE PEPTIDE 1; GREEN FLUORESCENT PROTEINS; GTP-BINDING PROTEINS; HUMANS; LIGANDS; PEPTIDE FRAGMENTS; QUINOXALINES; RECEPTORS, GLUCAGON; SIGNAL TRANSDUCTION; SULFONES; TRYPAN BLUE;

EID: 77956256197     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.110.166009     Document Type: Article

References (38)

1. i/o activation profiles in CHO cells expressing human muscarinic acetylcholine receptors: dependence on agonist as well as receptor-subtype. Br J Pharmacol 132:950-958.
2. Baggio LL and Drucker DJ (2007) Biology of incretins: GLP-1 and GIP. Gastroenterology 132:2131-2157.
3. Bavec A, Hällbrink M, Langel U, and Zorko M (2003) Different role of intracellular loops of glucagon-like peptide-1 receptor in G-protein coupling. Regul Pept 111:137-144.
4. Bleasdale JE, Thakur NR, Gremban RS, Bundy GL, Fitzpatrick FA, Smith RJ, and Bunting S (1990) Selective inhibition of receptor-coupled phospholipase C-dependent processes in human platelets and polymorphonuclear neutrophils. J Pharmacol Exp Ther 255:756-768.
5. Bradford MM (1976) A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal Biochem 72:248-254.
6. Brown BL, Albano JD, Ekins RP, and Sgherzi AM (1971) A simple and sensitive saturation assay method for the measurement of adenosine 3′:5′-cyclic monophosphate. Biochem J 121:561-562.
7. q/11 in SH-SY5Y human neuroblastoma cells. Br J Pharmacol 134:257-264.
8. Burford NT, Tobin AB, and Nahorski SR (1995) Differential coupling of m1, m2 and m3 muscarinic receptor subtypes to inositol 1,4,5-trisphosphate and adenosine 3′,5′-cyclic monophosphate accumulation in Chinese hamster ovary cells. J Pharmacol Exp Ther 274:134-142.
9. Chen D, Liao J, Li N, Zhou C, Liu Q, Wang G, Zhang R, Zhang S, Lin L, Chen K, et al. (2007) A nonpeptidic agonist of glucagon-like peptide 1 receptors with efficacy in diabetic db/db mice. Proc Nat Acad Sci USA 104:943-948.
10. Dimitriadis GD, Richards SJ, Parry-Billings M, Leighton B, Newsholme EA, and Challiss RA (1991) Beta-adrenoceptor-agonist and insulin actions on glucose metabolism in rat skeletal muscle in different thyroid states. Biochem J 278:587-593.
11. Doyle ME and Egan JM (2007) Mechanisms of action of glucagon-like peptide 1 in the pancreas. Pharmacol Ther 113:546-593.
12. Göke R, Fehmann HC, Linn T, Schmidt H, Krause M, Eng J, and Göke B (1993) Exendin-4 is a high potency agonist and truncated exendin-(9-39)-amide an antagonist at the glucagon-like peptide 1-(7-36)-amide receptor of insulin-secreting β-cells. J Biol Chem 268:19650-19655.
13. o activation. Biochim Biophys Acta 1546:79-86.
14. 2+ signalling exemplified by the NK1 receptor. J Recept Signal Transduct Res 22:241-252.
15. Holst JJ (2007) The physiology of glucagon-like peptide 1. Physiol Rev 87:1409-1439.
16. Holst JJ, Orskov C, Nielsen OV, and Schwartz TW (1987) Truncated glucagon-like peptide I, an insulin-releasing hormone from the distal gut. FEBS Lett 211:169-174.
17. Holz GG 4th, Kühtreiber WM, and Habener JF (1993) Pancreatic beta-cells are rendered glucose-competent by the insulinotropic hormone glucagon-like peptide- 1(7-37). Nature 361:362-365.
18. Jorgensen R, Martini L, Schwartz TW, and Elling CE (2005) Characterization of glucagon-like peptide-1 receptor β-arrestin 2 interaction: a high-affinity receptor phenotype. Mol Endocrinol 19:812-823.
19. Kenakin T (2004) A Pharmacology Primer: Theory, Application, and Methods, Elsevier Academic Press, San Diego, CA.
20. Kieffer TJ, McIntosh CH, and Pederson RA (1995) Degradation of glucose-dependent insulinotropic polypeptide and truncated glucagon-like peptide 1 in vitro and in vivo by dipeptidyl peptidase IV. Endocrinology 136:3585-3596.
21. Knudsen LB, Kiel D, Teng M, Behrens C, Bhumralkar D, Kodra JT, Holst JJ, Jeppesen CB, Johnson MD, de Jong JC, et al. (2007) Small-molecule agonists for the glucagon-like peptide 1 receptor. Proc Natl Acad Sci USA 104:937-942.
22. Lin F and Wang R (2009) Molecular modeling of the three-dimensional structure of GLP-1R and its interactions with several agonists. J Mol Model 15:53-65.
23. Meier JJ and Nauck MA (2005) Glucagon-like peptide 1 (GLP-1) in biology and pathology. Diabetes Metab Res Rev 21:91-117.
24. Mentlein R, Gallwitz B, and Schmidt WE (1993) Dipeptidyl-peptidase IV hydrolyses gastric inhibitory polypeptide, glucagon-like peptide-1(7-36)amide, peptide histidine methionine and is responsible for their degradation in human serum. Eur J Biochem 214:829-835.
25. Montrose-Rafizadeh C, Avdonin P, Garant MJ, Rodgers BD, Kole S, Yang H, Levine MA, Schwindinger W, and Bernier M (1999) Pancreatic glucagon-like peptide-1 receptor couples to multiple G proteins and activates mitogen-activated protein kinase pathways in Chinese hamster ovary cells. Endocrinology 140:1132-1140.
26. Orskov C, Rabenhøj L, Wettergren A, Kofod H, and Holst JJ (1994) Tissue and plasma concentrations of amidated and glycine-extended glucagon-like peptide I in humans. Diabetes 43:535-539.
27. Reimann F, Ward PS, and Gribble FM (2006) Signaling mechanisms underlying the release of glucagon-like peptide 1. Diabetes 55 (Suppl 2):S78-S85.
28. Seidel MG, Klinger M, Freissmuth M, and Höller C (1999) Activation of mitogen-activated protein kinase by the A(2A)-adenosine receptor via a rap1-dependent and via a p21(ras)-dependent pathway. J Biol Chem 274:25833-25841.
29. Shigeto M, Katsura M, Matsuda M, Ohkuma S, and Kaku K (2008) Low, but physiological, concentration of GLP-1 stimulates insulin secretion independent of the cAMP-dependent protein kinase pathway. J Pharmacol Sci 108:274-279.
30. Syme CA, Zhang L, and Bisello A (2006) Caveolin-1 regulates cellular trafficking and function of the glucagon-like peptide 1 receptor. Mol Endocrinol 20:3400-3411.
31. Thorens B, Porret A, Bühler L, Deng SP, Morel P, and Widmann C (1993) Cloning and functional expression of the human islet GLP-1 receptor. Demonstration that exendin-4 is an agonist and exendin-(9-39) an antagonist of the receptor. Diabetes 42:1678-1682.
32. 3 receptor. Mol Pharmacol 66:1453-1464.
33. Vázquez P, Roncero I, Blázquez E, and Alvarez E (2005) The cytoplasmic domain close to the transmembrane region of the glucagon-like peptide-1 receptor contains sequence elements that regulate agonist-dependent internalisation. J Endocrinol 186:221-231.
34. 2+ release in human embryonic kidney cells. J Pharmacol Exp Ther 307:661-669.
35. Wheeler MB, Lu M, Dillon JS, Leng XH, Chen C, and Boyd AE 3rd (1993) Functional expression of the rat glucagon-like peptide-I receptor, evidence for coupling to both adenylyl cyclase and phospholipase-C. Endocrinology 133:57-62.
36. Widmann C, Bürki E, Dolci W, and Thorens B (1994) Signal transduction by the cloned glucagon-like peptide-1 receptor: comparison with signaling by the endogenous receptors of beta cell lines. Mol Pharmacol 45:1029-1035.
37. Widmann C, Dolci W, and Thorens B (1995) Agonist-induced internalization and recycling of the glucagon-like peptide-1 receptor in transfected fibroblasts and in insulinomas. Biochem J 310:203-214.
38. 2+ signalling in human neuroblastoma cells. Br J Pharmacol 114:1133-1142.