The activation of the CGRP receptor

Biochemical Society Transactions

Volumn 41, Issue 1, 2013, Pages 180-184

  Barwell, James ^a   Wheatley, Mark ^b   Conner, Alex C ^c   Taddese, Bruck ^d   Vohra, Shabana ^d   Reynolds, Christopher A ^d   Poyner, David R ^a  

^a ASTON UNIVERSITY   (United Kingdom)

^b UNIVERSITY OF BIRMINGHAM   (United Kingdom)

^c UNIVERSITY OF WARWICK   (United Kingdom)

^d UNIVERSITY OF ESSEX   (United Kingdom)

Author keywords

Alanine scan; Family A GPCRs; Family B GPCRs; Mutagenesis; Secretin like GPCR; Structure activity relationship

Indexed keywords

BETA ADRENERGIC RECEPTOR; CALCITONIN GENE RELATED PEPTIDE RECEPTOR; CORTICOTROPIN RELEASING FACTOR; GASTRIC INHIBITORY POLYPEPTIDE; GLUCAGON; GLUCAGON LIKE PEPTIDE 1; PARATHYROID HORMONE; PITUITARY ADENYLATE CYCLASE ACTIVATING PEPTIDE; SECRETIN; UNCLASSIFIED DRUG; VASOACTIVE INTESTINAL POLYPEPTIDE;

AMINO TERMINAL SEQUENCE; CONFERENCE PAPER; CRYSTAL STRUCTURE; ENZYME ACTIVATION; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN CONFORMATION; PROTEIN STRUCTURE; SITE DIRECTED MUTAGENESIS;

CRYSTALLOGRAPHY, X-RAY; PROTEIN BINDING; RECEPTORS, CALCITONIN GENE-RELATED PEPTIDE;

EID: 84873158298     PISSN: 03005127     EISSN: 14708752     Source Type: Journal    
DOI: 10.1042/BST20120251     Document Type: Conference Paper

References (41)

1. Durham, P. L. and Vause, C. V. (2010) Calcitonin gene-related peptide (CGRP) receptor antagonists in the treatment of migraine. CNS Drugs 24, 539-548
2. McLatchie, L. M., Fraser, N. J., Main, M. J., Wise, A., Brown, J., Thompson, N., Solari, R., Lee, M. G. and Foord, S. M. (1998) RAMPs regulate the transport and ligand specificity of the calcitonin-receptor-like receptor. Nature 393, 333-339 (Pubitemid 28269699)
3. Barwell, J., Gingell, J. J., Watkins, H. A., Archbold, J. K., Poyner, D. R. and Hay, D. L. (2011) Calcitonin and calcitonin receptor-like receptors: common themes with family B GPCRs? Br. J. Pharmacol. 166, 51-65
4. Prado, M. A., Evans-Bain, B. and Dickerson, I. M. (2002) Receptor component protein (RCP): a member of a multi-protein complex required for G-protein-coupled signal transduction. Biochem. Soc. Trans. 30, 460-464 (Pubitemid 35001577)
5. Fredriksson, R., Lagerstrom, M. C., Lundin, L. G. and Schioth, H. B. (2003) The G-protein-coupled receptors in the human genome form five main families. Phylogenetic analysis, paralogon groups, and fingerprints. Mol. Pharmacol. 63, 1256-1272 (Pubitemid 36627220)
6. Archbold, J. K., Flanagan, J. U., Watkins, H. A., Gingell, J. J. and Hay, D. L. (2011) Structural insights into RAMP modification of secretin family G protein-coupled receptors: implications for drug development. Trends Pharmacol. Sci. 32, 591-600
7. Hoare, S. R. (2005) Mechanisms of peptide and nonpeptide ligand binding to class B G-protein-coupled receptors. Drug Discovery Today 10, 417-427 (Pubitemid 40450272)
8. Katritch, V., Cherezov, V. and Stevens, R. C. (2012) Diversity and modularity of G protein-coupled receptor structures. Trends Pharmacol. Sci. 33, 17-27
9. Conner, M., Hicks, M. R., Dafforn, T., Knowles, T. J., Ludwig, C., Staddon, S., Overduin, M., Gunther, U. L., Thome, J., Wheatley, M. et al. (2008) Functional and biophysical analysis of the C-terminus of the CGRP-receptor; a family B GPCR. Biochemistry 47, 8434-8444
10. Vohra, S., Chintapalli, S. V., Illingworth, C. J., Reeves, P. J., Mullineaux, P. M., Clark, H. S., Dean, M. K., Upton, G. J. and Reynolds, C. A. (2007) Computational studies of family A and family B GPCRs. Biochem. Soc. Trans. 35, 749-754 (Pubitemid 47310360)
11. Wu, B., Chien, E. Y., Mol, C. D., Fenalti, G., Liu, W., Katritch, V., Abagyan, R., Brooun, A., Wells, P., Bi, F. C. et al. (2010) Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists. Science 330, 1066-1071
12. Thompson, A. A., Liu, W., Chun, E., Katritch, V., Wu, H., Vardy, E., Huang, X. P., Trapella, C., Guerrini, R., Calo, G. et al. (2012) Structure of the nociceptin/orphanin FQ receptor in complex with a peptide mimetic. Nature 485, 395-399
13. Wu, H., Wacker, D., Mileni, M., Katritch, V., Han, G. W., Vardy, E., Liu, W., Thompson, A. A., Huang, X. P., Carroll, F. I. et al. (2012) Structure of the human κ-opioid receptor in complex with JDTic. Nature 485, 327-332
14. Granier, S., Manglik, A., Kruse, A. C., Kobilka, T. S., Thian, F. S., Weis, W. I. and Kobilka, B. K. (2012) Structure of the delta-opioid receptor bound to naltrindole. Nature 485, 400-404
15. Manglik, A., Kruse, A. C., Kobilka, T. S., Thian, F. S., Mathiesen, J. M., Sunahara, R. K., Pardo, L., Weis, W. I., Kobilka, B. K. and Granier, S. (2012) Crystal structure of the μ-opioid receptor bound to a morphinan antagonist. Nature 485, 321-326
16. Watkins, H. A., Au, M. and Hay, D. L. (2012) The structure of secretin family GPCR peptide ligands: implications for receptor pharmacology and drug development. Drug Discovery Today 17, 1006-1014
17. ter Haar, E., Koth, C. M., Abdul-Manan, N., Swenson, L., Coll, J. T., Lippke, J. A., Lepre, C. A., Garcia-Guzman, M. and Moore, J. M. (2010) Crystal structure of the ectodomain complex of the CGRP receptor, a class-B GPCR, reveals the site of drug antagonism. Structure 18, 1083-1093
18. Barwell, J., Miller, P. S., Donnelly, D. and Poyner, D. R. (2010) Mapping interaction sites within the N-terminus of the calcitonin gene-related peptide receptor; the role of residues 23-60 of the calcitonin receptor-like receptor. Peptides 31, 170-176
19. Moore, E. L., Gingell, J. J., Kane, S. A., Hay, D. L. and Salvatore, C. A. (2010) Mapping the CGRP receptor ligand binding domain: tryptophan-84 of RAMP1 is critical for agonist and antagonist binding. Biochem. Biophys. Res. Commun. 394, 141-145
20. Dong, M., Pinon, D. I., Asmann, Y. W. and Miller, L. J. (2006) Possible endogenous agonist mechanism for the activation of secretin family G protein-coupled receptors. Mol. Pharmacol. 70, 206-213
21. Dong, M., Lam, P. C., Pinon, D. I., Orry, A., Sexton, P. M., Abagyan, R. and Miller, L. J. (2010) Secretin occupies a single protomer of the homodimeric secretin receptor complex: insights from photoaffinity labeling studies using dual sites of covalent attachment. J. Biol. Chem. 285, 9919-9931
22. Koth, C. M., Murray, J. M., Mukund, S., Madjidi, A., Minn, A., Clarke, H. J., Wong, T., Chiang, V., Luis, E., Estevez, A. et al. (2012) Molecular basis for negative regulation of the glucagon receptor. Proc. Natl. Acad. Sci. U. S. A. 109, 14393-14398
23. Koth, C. M., Abdul-Manan, N., Lepre, C. A., Connolly, P. J., Yoo, S., Mohanty, A. K., Lippke, J. A., Zwahlen, J., Coll, J., Doran, J. D. et al. (2010) Refolding and in vitro characterization of a soluble antagonist binding domain of the CGRP receptor. Biochemistry 49, 1862-1872
24. Koole, C., Wootten, D., Simms, J., Miller, L. J., Christopoulos, A. and Sexton, P. M. (2012) Second extracellular loop of human glucagon-like peptide-1 receptor (GLP-1R) has a critical role in GLP-1 peptide binding and receptor activation. J. Biol. Chem. 287, 3642-3658
25. Barwell, J., Conner, A. and Poyner, D. R. (2011) Extracellular loops 1 and 3 and their associated transmembrane regions of calcitonin receptor-like receptor are needed for CGRP receptor function. Biochim. Biophys. Acta 1813, 1906-1916
26. Kuwasako, K., Hay, D. L., Nagata, S., Hikosaka, T., Kitamura, K. and Kato, J. (2012) The third extracellular loop of the human calcitonin receptor-like receptor is crucial for the activation of adrenomedullin signalling. Br. J. Pharmacol. 166, 137-150
27. Barwell, J., Woolley, M. J., Wheatley, M., Conner, A. C. and Poyner, D. R. (2012) The role of the extracellular loops of the CGRP receptor, a family B GPCR. Biochem. Soc. Trans. 40, 433-437
28. Wheatley, M., Wootten, D., Conner, M. T., Simms, J., Kendrick, R., Logan, R. T., Poyner, D. R. and Barwell, J. (2012) Lifting the lid on GPCRs: the role of extracellular loops. Br. J. Pharmacol. 165, 1688-1703
29. Roberts, D. J., Vertongen, P. and Waelbroeck, M. (2011) Analysis of the glucagon receptor first extracellular loop by the substituted cysteine accessibility method. Peptides 32, 1593-1599
30. Hay, D. L., Conner, A. C., Howitt, S. G., Takhshid, M. A., Simms, J., Mahmoud, K. and Poyner, D. R. (2004) The pharmacology of CGRP-responsive receptors in cultured and transfected cells. Peptides 25, 2019-2026 (Pubitemid 39389199)
31. Conner, A. C., Hay, D. L., Simms, J., Howitt, S. G., Schindler, M., Smith, D. M., Wheatley, M. and Poyner, D. R. (2005) A key role for transmembrane prolines in calcitonin receptor-like receptor agonist binding and signalling: implications for family B G-protein-coupled receptors. Mol. Pharmacol. 67, 20-31 (Pubitemid 40069963)
32. Tams, J. W., Knudsen, S. M. and Fahrenkrug, J. (2001) Characterization of a G protein coupling 'YL' motif of the human VPAC1 receptor, equivalent to the first two amino acids in the 'DRY' motif of the rhodopsin family. J. Mol. Neurosci. 17, 325-330 (Pubitemid 34123949)
33. Conner, A. C., Simms, J., Conner, M. T., Wootten, D. L., Wheatley, M. and Poyner, D. R. (2006) Diverse functional motifs within the three intracellular loops of the CGRP1 receptor. Biochemistry 45, 12976-12985 (Pubitemid 44763420)
34. Conner, A. C., Simms, J., Howitt, S. G., Wheatley, M. and Poyner, D. R. (2006) The second intracellular loop of the calcitonin gene-related peptide receptor provides molecular determinants for signal transduction and cell surface expression. J. Biol. Chem. 281, 1644-1651
35. Frimurer, T. M. and Bywater, R. P. (1999) Structure of the integral membrane domain of the GLP1 receptor. Proteins 35, 375-386 (Pubitemid 29264834)
36. Mathi, S. K., Chan, Y., Li, X. and Wheeler, M. B. (1997) Scanning of the glucagon-like peptide-1 receptor localizes G protein-activating determinants primarily to the N terminus of the third intracellular loop. Mol Endocrinol. 11, 424-432 (Pubitemid 27147010)
37. Turner, P. R., Bambino, T. and Nissenson, R. A. (1996) Mutations of neighboring polar residues on the second transmembrane helix disrupt signaling by the parathyroid hormone receptor. Mol. Endocrinol. 10, 132-139 (Pubitemid 26042545)
38. Holtmann, M. H., Ganguli, S., Hadac, E. M., Dolu, V. and Miller, L. J. (1996) Multiple extracellular loop domains contribute critical determinants for agonist binding and activation of the secretin receptor. J. Biol. Chem. 271, 14944-14949 (Pubitemid 26197574)
39. Couvineau, A., Lacapere, J. J., Tan, Y. V., Rouyer-Fessard, C., Nicole, P. and Laburthe, M. (2003) Identification of cytoplasmic domains of hVPAC1 receptor required for activation of adenylyl cyclase. Crucial role of two charged amino acids strictly conserved in class II G protein-coupled receptors. J. Biol. Chem. 278, 24759-24766 (Pubitemid 37548633)
40. Schipani, E., Langman, C., Hunzelman, J., Le Merrer, M., Loke, K. Y., Dillon, M. J., Silve, C. and Juppner, H. (1999) A novel parathyroid hormone (PTH)/PTH-related peptide receptor mutation in Jansen's metaphyseal chondrodysplasia. J. Clin. Endocrinol. Metab. 84, 3052-3057 (Pubitemid 30646922)
41. Chugunov, A. O., Simms, J., Poyner, D. R., Dehouck, Y., Rooman, M., Gilis, D. and Langer, I. (2010) Evidence that interaction between conserved residues in transmembrane helices 2, 3, and 7 are crucial for human VPAC1 receptor activation. Mol. Pharmacol. 78, 394-401