A human glucagon-like peptide-1 receptor polymorphism results in reduced agonist responsiveness

Regulatory Peptides

Volumn 130, Issue 1-2, 2005, Pages 1-6

  Beinborn, Martin ^a   Worrall, Christine I ^a   McBride, Edward W ^a   Kopin, Alan S ^a  

^a TUFTS MEDICAL CENTER   (United States)

Author keywords

Affinity; Cyclic adenosine monophosphate; Diabetes; G protein coupled receptor; Incretin; Potency

Indexed keywords

CYCLIC AMP; EXENDIN 4; GLUCAGON LIKE PEPTIDE 1 [9-36] AMIDE; GLUCAGON LIKE PEPTIDE 1 DERIVATIVE; GLUCAGON LIKE PEPTIDE 1 RECEPTOR; GLUCOSE; METHIONINE; RECOMBINANT GLUCAGON; THREONINE; UNCLASSIFIED DRUG;

AGONIST; AMINO ACID SUBSTITUTION; ANIMAL CELL; ARTICLE; BINDING AFFINITY; CELL STRAIN COS7; CELL STRAIN HEK293; CONTROLLED STUDY; DISEASE PREDISPOSITION; DNA POLYMORPHISM; DRUG EFFICACY; DRUG POTENCY; DRUG RECEPTOR BINDING; FUNCTIONAL ASSESSMENT; GENETIC ASSOCIATION; GENETIC VARIABILITY; GLUCOSE BLOOD LEVEL; GLUCOSE HOMEOSTASIS; HETEROZYGOSITY LOSS; HUMAN; HUMAN CELL; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; PRIORITY JOURNAL; PROTEIN DOMAIN; PROTEIN EXPRESSION; RECEPTOR AFFINITY; RECEPTOR INTRINSIC ACTIVITY; WILD TYPE;

AMINO ACID SEQUENCE; ANIMALS; CELL LINE; COS CELLS; CYCLIC AMP; DNA, COMPLEMENTARY; DOSE-RESPONSE RELATIONSHIP, DRUG; GENETIC PREDISPOSITION TO DISEASE; GLUCOSE; HOMEOSTASIS; HUMANS; LIGANDS; MOLECULAR SEQUENCE DATA; MUTAGENESIS, SITE-DIRECTED; MUTATION; PEPTIDES; POLYMORPHISM, GENETIC; RECEPTORS, G-PROTEIN-COUPLED; RECEPTORS, GLUCAGON; RECOMBINANT PROTEINS; SEQUENCE HOMOLOGY, AMINO ACID; SIGNAL TRANSDUCTION; SOFTWARE; TRANSCRIPTION, GENETIC; VARIATION (GENETICS); VENOMS;

EID: 22044446844     PISSN: 01670115     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.regpep.2005.05.001     Document Type: Article

References (27)

1. T.J. Kieffer, and J.F. Habener The glucagon-like peptides Endocr Rev 20 1999 876 913
2. D.J. Drucker Glucagon-like peptides Diabetes 47 1998 159 169
3. D.J. Drucker Glucagon-like peptides: regulators of cell proliferation, differentiation, and apoptosis Mol Endocrinol 17 2003 161 171
4. I.A. Urusova, L. Farilla, H. Hui, E. D'Amico, and R. Perfetti GLP-1 inhibition of pancreatic islet cell apoptosis Trend Endocrinol Metab 15 2004 27 33
5. J.J. Holst Therapy of type 2 diabetes mellitus based on the actions of glucagon-like peptide-1 Diabetes/Metab Res Rev 18 2002 430 441
6. K.E. Mayo, L.J. Miller, D. Bataille, S. Dalle, B. Göke, B. Thorens International Union of Pharmacology XXXV The glucagon receptor family Pharmacol Rev 55 2003 167 194
7. G.G. Holz, and O.G. Chepurny Glucagon-like peptide-1 synthetic analogs: new therapeutic agents for use in the treatment of diabetes mellitus Curr Med Chem 10 2003 2471 2484
8. L.B. Knudsen Glucagon-like peptide-1: the basis of a new class of treatment for type 2 diabetes J Med Chem 47 2004 4128 4134
9. J.P. Raufman Bioactive peptides from lizard venoms Regul Pept 61 1996 1 18
10. C.F. Deacon, B. Ahren, and J.J. Holst Inhibitors of dipeptidyl peptidase IV: a novel approach for the prevention and treatment of type 2 diabetes? Expert Opin Investig Drugs 13 2004 1091 1102
11. Y. Tokuyama, K. Matsui, T. Egashira, O. Nozaki, T. Ishizuka, and A. Kanatsuka Five missense mutations in glucagon-like peptide 1 receptor gene in Japanese population Diabetes Res Clin Pract 66 2004 63 69
12. B. Thorens, A. Porret, L. Buhler, S.P. Deng, P. Morel, and C. Widmann 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 1993 1678 1682
13. E.C. Tibaduiza, C. Chen, and M. Beinborn A small molecule ligand of the glucagon-like peptide 1 receptor targets its amino-terminal hormone binding domain J Biol Chem 276 2001 37787 37793
14. A.S. Kopin, Y.M. Lee, E.W. McBride, L.J. Miller, M. Lu, H.Y. Lin, and M. Beinborn Expression cloning and characterization of the canine parietal cell gastrin receptor Proc Natl Acad Sci U S A 89 1992 3605 3609
15. M.G. Hearn, Y. Ren, E.W. McBride, I. Reveillaud, M. Beinborn, and A.S. Kopin A Drosophila dopamine 2-like receptor: molecular characterization and identification of multiple alternatively spliced variants Proc Natl Acad Sci U S A 99 2002 14554 14559
16. R. Göke, H.C. Fehmann, T. Linn, H. Schmidt, M. Krause, and J. Eng 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 beta-cells J Biol Chem 268 1993 19650 19655
17. L.B. Knudsen, and L. Pridal Glucagon-like peptide-1-(9-36) amide is a major metabolite of glucagon-like peptide-1-(7-36) amide after in vivo administration to dogs, and it acts as an antagonist on the pancreatic receptor Eur J Pharmacol 318 1996 429 435
18. C. Montrose-Rafizadeh, H. Yang, B.D. Rodgers, A. Beday, L.A. Pritchette, and J. Eng High potency antagonists of the pancreatic glucagon-like peptide-1 receptor J Biol Chem 272 1997 21201 21206
19. S. Al-Sabah, and D. Donnelly The positive charge at Lys-288 of the glucagon-like peptide-1 (GLP-1) receptor is important for binding the N-terminus of peptide agonists FEBS Lett 553 2003 342 346
20. R. Lopez de Maturana, and D. Donnelly The glucagon-like peptide-1 receptor binding site for the N-terminus of GLP-1 requires polarity at Asp198 rather than negative charge FEBS Lett 530 2002 244 248
21. R. Lopez de Maturana, J. Treece-Birch, F. Abidi, J.B. Findlay, D. Donnelly, and S. Al-Sabah Met-204 and Tyr-205 are together important for binding GLP-1 receptor agonists but not their N-terminally truncated analogues Prot Peptide Letters 11 2004 15 22
22. Q. Xiao, W. Jeng, and M.B. Wheeler Characterization of glucagon-like peptide-1 receptor-binding determinants J Mol Endocrinol 25 2000 321 335
23. S. Al-Sabah, and D. Donnelly A model for receptor-peptide binding at the glucagon-like peptide-1 (GLP-1) receptor through the analysis of truncated ligands and receptors Br J Pharmacol 140 2003 339 346
24. M. Bläker, Y. Ren, M.C. Gordon, J.E. Hsu, M. Beinborn, and A.S. Kopin Mutations within the cholecystokinin-B/gastrin receptor ligand "pocket" interconvert the functions of nonpeptide agonists and antagonists Mol Pharmacol 54 1998 857 863
25. A. Bisello, M. Chorev, M. Rosenblatt, L. Monticelli, D.F. Mierke, and S.L. Ferrari Selective ligand-induced stabilization of active and desensitized parathyroid hormone type 1 receptor conformations J Biol Chem 277 2002 38524 38530
26. V. Behar, A. Bisello, G. Bitan, M. Rosenblatt, and M. Chorev Photoaffinity cross-linking identifies differences in the interactions of an agonist and an antagonist with the parathyroid hormone/parathyroid hormone-related protein receptor J Biol Chem 275 2000 9 17
27. M. Chorev Parathyroid hormone 1 receptor: insights into structure and function Recept Channels 8 2002 219 242