Functional coupling of Cys-226 and Cys-296 in the glucagon-like peptide-1 (GLP-1) receptor indicates a disulfide bond that is close to the activation pocket

Peptides

Volumn 31, Issue 12, 2010, Pages 2289-2293

  Mann, Rosalind J ^a   Al Sabah, Suleiman ^a   De Maturana, Rakel López ^a   Sinfield, John K ^a   Donnelly, Dan ^a  

^a UNIVERSITY OF LEEDS   (United Kingdom)

Author keywords

Agonist; GLP 1; GPCR; Mutagenesis; Receptor

Indexed keywords

ALANINE; CYSTEINE; EXTRACELLULAR LOOP 2 PROTEIN; G PROTEIN COUPLED RECEPTOR; GLUCAGON LIKE PEPTIDE 1 RECEPTOR; HELIX LOOP HELIX PROTEIN; MEMBRANE PROTEIN; TRANSMEMBRANE HELIX 3; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DISULFIDE BOND; EMBRYO; HUMAN; HUMAN CELL; MUTAGENESIS; MUTATION; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN DOMAIN; PROTEIN INTERACTION; SEQUENCE ANALYSIS;

CELL LINE; CYCLIC AMP; CYSTEINE; DISULFIDES; GENE EXPRESSION; GLUCAGON-LIKE PEPTIDE 1; HUMANS; MUTAGENESIS; RECEPTORS, GLUCAGON; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 78049465517     PISSN: 01969781     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.peptides.2010.09.015     Document Type: Article

References (36)

1. 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 British Journal of Pharmacology 140 2003 339 346
2. 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 Letters 553 2003 342 346
3. M. Castro, V.O. Nikolaev, D. Palm, M.J. Lohse, and J.P. Vilardaga Turn-on switch in parathyroid hormone receptor by a two-step parathyroid hormone binding mechanism Proceedings of the National Academy of Sciences of the United States of America 102 2005 16084 16089
4. V. Cherezov, D.M. Rosenbaum, M.A. Hanson, S.G.F. Rasmussen, F.S. Thian, and T.S. Kobilka High-resolution crystal structure of an engineered human beta(2)-adrenergic G protein-coupled receptor Science 318 2007 1258 1265
5. R.A. DeFronzo, R.E. Ratner, J. Han, D.D. Kim, M.S. Fineman, and A.D. Baron Effects of exenatide (exendin-4) on glycemic control and weight over 30 weeks in metformin-treated patients with type 2 diabetes Diabetes Care 28 2005 1092 1100
6. H.G. Dohlman, M.G. Caron, A. Deblasi, T. Frielle, and R.J. Lefkowitz Role of extracellular disulfide-bonded cysteines in the ligand-binding function of the beta-2-adrenergic receptor Biochemistry 29 1990 2335 2342
7. D.J. Drucker Minireview: the glucagon-like peptides Endocrinology 142 2001 521 527
8. R.W. Gelling, M.B. Wheeler, J.P. Xue, S. Gyomorey, C.L. Nian, and R.A. Pederson Localization of the domains involved in ligand binding and activation of the glucose-dependent insulinotropic polypeptide receptor Endocrinology 138 1997 2640 2643
9. U. Gether Uncovering molecular mechanisms involved in activation of G protein-coupled receptors Endocrine Reviews 21 2000 90 113
10. C.R.R. Grace, M.H. Perrin, J. Gulyas, M.R. DiGruccio, J.P. Cantle, and J.E. Rivier Structure of the N-terminal domain of a type B1 G protein-coupled receptor in complex with a peptide ligand Proceedings of the National Academy of Sciences of the United States of America 104 2007 4858 4863
11. S.R.J. Hoare, and T.B. Usdin Quantitative cell membrane-based radioligand binding assays for parathyroid hormone receptors Journal of Pharmacological and Toxicological Methods 41 1999 83 90
12. M.H. Holtmann, E.M. Hadac, and L.J. Miller Critical contributions of amino-terminal extracellular domains in agonist binding and activation of secretin and vasoactive intestinal polypeptide receptors - studies of chimeric receptors Journal of Biological Chemistry 270 1995 14394 14398
13. V.P. Jaakola, M.T. Griffith, M.A. Hanson, V. Cherezov, E.Y.T. Chien, and J.R. Lane The 2.6 Angstrom crystal structure of a human A(2A) adenosine receptor bound to an antagonist Science 322 2008 1211 1217
14. S.S. Karnik, and H.G. Khorana Assembly of functional rhodopsin requires a disulfide bond between cysteine residue-110 and residue-187 Journal of Biological Chemistry 265 1990 17520 17524
15. S.S. Karnik, T.P. Sakmar, H.B. Chen, and H.G. Khorana Cysteine residues 110 and 187 are essential for the formation of correct structure in bovine rhodopsin Proceedings of the National Academy of Sciences of the United States of America 85 1988 8459 8463
16. T.J. Kieffer, and J.L. Habener The glucagon-like peptides Endocrine Reviews 20 1999 876 913
17. L.B. Knudsen, H. Agerso, C. Bjenning, S. Bregenholt, R.D. Carr, and C. Godtfredsen GLP-1 derivatives as novel compounds for the treatment of type 2 diabetes: selection of NN2211 for clinical development Drugs of the Future 26 2001 677 685
18. S.M. Knudsen, J.W. Tams, B.S. Wulff, and J. Fahrenkrug A disulfide bond between conserved cysteines in the extracellular loops of the human VIP receptor is required for binding and activation FEBS Letters 412 1997 141 143
19. C.W. Lee, T.J. Gardella, A.B. Abousamra, S.R. Nussbaum, G.V. Segre, and J.T. Potts Role of the extracellular regions of the parathyroid-hormone (Pth) Pth-related peptide receptor in hormone-binding Endocrinology 135 1994 1488 1495
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 Letters 530 2002 244 248
21. R. Lopez de Maturana, J. Treece-Birch, F. Abidi, J.B.C. Findlay, and D. Donnelly Met-204 and Tyr-205 are together important for binding GLP-1 receptor agonists but not their N-terminally truncated analogues Protein and Peptide Letters 11 2004 15 22
22. R. Lopez de Maturana, A. Willshaw, A. Kuntzsch, R. Rudolph, and D. Donnelly The isolated N-terminal domain of the glucagon-like peptide-1 (GLP-1) receptor binds exendin peptides with much higher affinity than GLP-1 Journal of Biological Chemistry 278 2003 10195 10200
23. J.E. Matthews, M.W. Stewart, E.H. De Boever, R.L. Dobbins, R.J. Hodge, and S.E. Walker Pharmacodynamics, pharmacokinetics, safety, and tolerability of albiglutide, a long-acting glucagon-like peptide-1 mimetic, in patients with type 2 diabetes Journal of Clinical Endocrinology & Metabolism 93 2008 4810 4817
24. K. Noda, Y. Saad, R.M. Graham, and S.S. Karnik The high-affinity state of the beta-2-adrenergic receptor requires unique interaction between conserved and nonconserved extracellular loop cysteines Journal of Biological Chemistry 269 1994 6743 6752
25. C. Orskov, J.J. Holst, and O.V. Nielsen Effect of truncated glucagon-like peptide-1 [proglucagon-(78-107) amide] on endocrine secretion from pig pancreas, antrum, and nonantral stomach Endocrinology 123 1988 2009 2013
26. K. Palczewski, T. Kumasaka, T. Hori, C.A. Behnke, H. Motoshima, and B.A. Fox Crystal structure of rhodopsin: a G protein-coupled receptor Science 289 2000 739 745
27. C. Parthier, M. Kleinschmidt, P. Neumann, R. Rudolph, S. Manhart, and D. Schlenzig Crystal structure of the incretin-bound extracellular domain of a G protein-coupled receptor Proceedings of the National Academy of Sciences of the United States of America 104 2007 13942 13947
28. A.A. Pioszak, N.R. Parker, K. Suino-Powell, and H.E. Xu Molecular recognition of corticotropin-releasing factor by Its G-protein-coupled receptor CRFR1 Journal of Biological Chemistry 283 2008 32900 32912
29. A.A. Pioszak, and H.E. Xu Molecular recognition of parathyroid hormone by its G protein-coupled receptor Proceedings of the National Academy of Sciences of the United States of America 105 2008 5034 5039
30. S. Runge, H. Thogersen, K. Madsen, J. Lau, and R. Rudolph Crystal structure of the ligand-bound glucagon-like peptide-1 receptor extracellular domain Journal of Biological Chemistry 283 2008 11340 11347
31. Y. Salomon, C. Londos, and M. Rodbell Highly sensitive adenylate cyclase assay Analytical Biochemistry 58 1974 541 548
32. D.J. Scholl, and J.N. Wells Serine and alanine mutagenesis of the nine native cysteine residues of the human A(1) adenosine receptor Biochemical Pharmacology 60 2000 1647 1654
33. M.D. Turton, D. Oshea, I. Gunn, S.A. Beak, C.M.B. Edwards, and K. Meeran A role for glucagon-like peptide-1 in the central regulation of feeding Nature 379 1996 69 72
34. J.P. Vilardaga, E. DiPaolo, C. Bialek, P. DeNeef, M. Waelbroeck, and A. Bollen Mutational analysis of extracellular cysteine residues of rat secretin receptor shows that disulfide bridges are essential for receptor function European Journal of Biochemistry 246 1997 173 180
35. T. Warne, M.J. Serrano-Vega, J.G. Baker, R. Moukhametzianov, P.C. Edwards, and R. Henderson Structure of a beta(1)-adrenergic G-protein-coupled receptor Nature 454 2008 486 492
36. M. Zander, S. Madsbad, J.L. Madsen, and J.J. Holst Effect of 6-week course of glucagon-like peptide 1 on glycaemic control, insulin sensitivity, and beta-cell function in type 2 diabetes: a parallel-group study Lancet 359 2002 824 830