Functional Complementation and the Analysis of GPCR Dimerization

Contemporary Clinical Neuroscience

Volumn , Issue , 2005, Pages 267-285

  Milligan, Graeme ^a   Carrillo, Juan J ^b   Pascal, Geraldine ^c  

^a UNIVERSITY OF GLASGOW   (United Kingdom)

^b ASTRAZENECA   (United Kingdom)

^c UNIVERSITY OF GLASGOW   (United Kingdom)

Author keywords

Bioluminescence Resonance Energy Transfer; Functional Complementation; Fusion Protein; GPCR Dimerization; Opioid Receptor

Indexed keywords

EID: 33645426435     PISSN: 2627535X     EISSN: 26275341     Source Type: Book Series    
DOI: 10.1007/978-1-59259-919-6_12     Document Type: Chapter

References (66)

1. Salahpour A, Angers S, Bouvier M. Functional significance of oligomerization of G-protein-coupled receptors. Trends Endocrinol Metab 2000;11:163–168.
2. Hebert TE, Moffett S, Morello JP, et al. A peptide derived from a beta2-adrenergic receptor transmembrane domain inhibits both receptor dimerization and activation. J Biol Chem 1996;271:16,384–16,392.
3. Ng GYK, O’Dowd BF, Lee SP, et al. Dopamine D2 receptor dimers and receptor-blocking peptides. Biochem Biophys Res Comm 1996;227:200–204.
4. Nimchinsky EA, Hof PR, Janssen WG, Morrison JH, Schmauss C. Expression of dopamine D3 receptor dimers and tetramers in brain and in transfected cells. J Biol Chem 1997;272:29,229–29,237.
5. Cvejic S, Devi LA. Dimerization of the delta opioid receptor: implication for a role in receptor internalization. J Biol Chem 1997;272:26,959–26,964.
6. George SR, O’Dowd BF, Lee SP. G-protein-coupled receptor oligomerization and its potential for drug discovery. Nat Rev Drug Discov 2002;1:808–820.
7. Devi LA. Heterodimerization of G-protein-coupled receptors: pharmacology, signaling and trafficking. Trends Pharmacol Sci 2001;22:532–537.
8. Salim K, Fenton T, Bacha J, et al. Oligomerization of G-protein-coupled receptors shown by selective co-immunoprecipitation. J Biol Chem 2002;277:15,482–15,485.
9. Angers S, Salahpour A, Joly E, et al. Detection of beta 2-adrenergic receptor dimerization in living cells using bioluminescence resonance energy transfer (BRET). Proc Natl Acad Sci USA 2000;97:3684–3689.
10. McVey M, Ramsay D, Kellett E, et al. Monitoring receptor oligomerization using time-resolved fluorescence resonance energy transfer and bioluminescence resonance energy transfer. The human delta-opioid receptor displays constitutive oligomerization at the cell surface, which is not regulated by receptor occupancy. J Biol Chem 2001;276:14,092–14,099.
11. Mercier JF, Salahpour A, Angers S, Breit A, Bouvier M. Quantitative assessment of beta 1-and beta 2-adrenergic receptor homo-and heterodimerization by bioluminescence resonance energy transfer. J Biol Chem 2002;277:44,925–44,931.
12. Overton MC, Blumer KJ. The extracellular N-terminal domain and transmembrane domains 1 and 2 mediate oligomerization of a yeast G protein-coupled receptor. J Biol Chem 2002;277:41,463–41,472.
13. Ramsay D, Kellett E, McVey M, Rees S, Milligan G. Homo-and hetero-oligomeric interactions between G-protein-coupled receptors in living cells monitored by two variants of bioluminescence resonance energy transfer (BRET): hetero-oligomers between receptor subtypes form more efficiently than between less closely related sequences. Biochem J 2002;365:429–440.
14. 1β-adrenergic receptor subtypes. J Biol Chem 2003;278:40,239–40,251.
15. Eidne KA, Kroeger KM, Hanyaloglu AC. Applications of novel resonance energy transfer techniques to study dynamic hormone receptor interactions in living cells. Trends Endocrinol Metabol 2002;13:415–421.
16. Milligan G. Applications of bioluminescence and fluorescence resonance energy transfer to drug discovery at G protein-coupled receptors. Eur J Pharm Sci 2004;21:397–405.
17. Kroeger KM, Pfleger KDG, Eidne KA. Biophysical and biochemical methods to study G protein-coupled receptor oligomerization. In Devi LA, ed., The G Protein-Coupled Receptors Handbook. Humana, Totowa, NJ: 2005; pp. 217–241.
18. Martin NP, Leavitt LM, Sommers CM, Dumont ME. Assembly of G proteincoupled receptors from fragments: identification of functional receptors with discontinuities in each of the loops connecting transmembrane segments. Biochemistry 1999;38:682–695.
19. Dean MK, Higgs C, Smith RE, et al. Dimerization of G-protein-coupled receptors. J Med Chem 2001;44:4595–4614.
20. Gouldson PR, Dean MK, Snell CR, Bywater RP, Gkoutos G, Reynolds CA. Lipid-facing correlated mutations and dimerization in G-protein coupled receptors. Protein Eng 2001;14:759–767.
21. Maggio R, Scarselli M, Novi F, Millan MJ, Corsini GU. Potent activation of dopamine D3/D2 heterodimers by the antiparkinsonian agents, S32504, pramipexole and ropinirole. J Neurochem 2003;87:631–641.
22. Maggio R, Vogel Z, Wess J. Coexpression studies with mutant muscarinic/ adrenergic receptors provide evidence for intermolecular “cross-talk” between G-protein-linked receptors. Proc Natl Acad Sci USA 1993;90:3103–3107.
23. Monnot C, Bihoreau C, Conchon S, Curnow KM, Corvol P, Clauser E. Polar residues in the transmembrane domains of the type 1 angiotensin II receptor are required for binding and coupling. Reconstitution of the binding site by coexpression of two deficient mutants. J Biol Chem 1996;271:1507–1513.
24. B receptors make it to the top—as dimers. Trends Pharmacol Sci 1999;20:87–89.
25. B receptors—the first 7TM heterodimers. Trends Pharmacol Sci 1999;20:396–399.
26. Parmentier ML, Prezeau L, Bockaert J, Pin JP. A model for the functioning of family 3 GPCRs. Trends Pharmacol Sci 2002;23:268–274.
27. Lee C, Ji I, Ryu K, Song Y, Conn PM, Ji TH. Two defective heterozygous luteinizing hormone receptors can rescue hormone action. J Biol Chem. 2002;277:15,795–15,800.
28. Lee C, Ji IJ, Ji TH. Use of defined-function mutants to access receptor–receptor interactions. Methods 2002;27:318–323.
29. Ji I, Lee C, Song Y, Conn PM, Ji TH. Cis-and trans-activation of hormone receptors: the LH receptor. Mol Endocrinol 2002;16:1299–1308.
30. Nakanishi-Matsui M, Zheng YW, Sulciner DJ, Weiss EJ, Ludeman MJ, Coughlin SR. PAR3 is a cofactor for PAR4 activation by thrombin. Nature 2000;404:609–613.
31. O’Brien PJ, Prevost N, Molino M, et al. Thrombin responses in human endothelial cells. Contributions from receptors other than PAR1 include the transactivation of PAR2 by thrombin-cleaved PAR1. J Biol Chem 2000;275:13,502–13,509.
32. Bertin B, Freissmuth M, Jockers R, Strosberg AD, Marullo S. Cellular signaling by an agonist-activated receptor/Gs alpha fusion protein. Proc Natl Acad Sci USA 1994;91:8827–8831.
33. Milligan G. Insights into ligand pharmacology using receptor–G protein fusion proteins. Trends Pharmacol Sci 2000;21:24–28.
34. Milligan G. Construction and analysis of function of GPCR–G protein fusion proteins. Methods Enzymol 2002;343:260–273.
35. o1 α. J Neurochem 2001;76:1805–1813.
36. Ugur O, Onaran HO, Jones TL. Partial rescue of functional interactions of a nonpalmitoylated mutant of the G-protein G alpha s by fusion to the beta-adrenergic receptor. Biochemistry 2003;42:2607–2615.
37. Loisel TP, Ansanay H, Adam L, et al. Activation of the beta(2)-adrenergic receptor-Galpha(s) complex leads to rapid depalmitoylation and inhibition of repalmitoylation of both the receptor and Galpha(s). J Biol Chem 1999;274:31,014–31,019.
38. 11 alpha is not required for interaction with beta/gamma complex. J Biol Chem 2001;276:35,883–35,890.
39. Hosoi T, Koguchi Y, Sugikawa E, et al. Identification of a novel human eicosanoid receptor coupled to G(i/o). J Biol Chem 2002;277:31,459–31,465.
40. Takeda S, Yamamoto A, Okada T, et al. Identification of surrogate ligands for orphan G protein-coupled receptors. Life Sci 2003;74:367–377.
41. Carrillo JJ, Pediani J, Milligan G. Dimers of class A G protein-coupled receptors function via agonist-mediated trans-activation of associated G proteins. J Biol Chem 2003;278:42,578–42,587.
42. Gether U. Uncovering molecular mechanisms involved in activation of G protein-coupled receptors. Endocr Rev 2000;21:90–113.
43. 2A adrenoceptor. Biochemistry 1998;37:11,555–11,562.
44. Dupuis DS, Wurch T, Tardif S, Colpaert FC, Pauwels PJ. Modulation of 5-HT(1A) receptor activation by its interaction with wild-type and mutant g(alphai3) proteins. Neuropharmacology 2001;40:36–47.
45. i1 α. Mol Pharmacol 1999;55:195–201.
46. Milligan G. The use of receptor-G protein fusion proteins for the study of ligand activity. Receptors Channels 2002;8:309–317.
47. 11 α requires both β/γ interactions and an aromatic group 4 amino acid from the C-terminus of the G protein. J Biol Chem 2002;277:25,707–25,714.
48. Sullivan KA, Miller RT, Masters SB, Beiderman B, Heideman W, Bourne HR. Identification of receptor contact site involved in receptor–G protein coupling. Nature 1987;330:758–760.
49. Waldhoer M, Wise A, Milligan G, Freissmuth M, Nanoff C. Kinetics of ternary complex formation with fusion proteins composed of the A1-adenosine receptor and G protein α-subunits. J Biol Chem 1999;274:30,571–30,579.
50. 35 S]GTPγS binding assays. Trends Pharmacol Sci 2003;24:87–90.
51. i1 α fusion protein results in activation of both receptor-linked and endogenous G proteins: comparisons of their contributions to GTPase activity and signal transduction and analysis of receptor–G protein activation stoichiometry. J Biol Chem 1998;273:10,367–10,375.
52. Molinari P, Ambrosio C, Riitano D, Sbraccia M, Gro MC, Costa T. Promiscuous coupling at receptor–Galpha fusion proteins. The receptor of one covalent complex interacts with the alpha-subunit of another. J Biol Chem 2003;278:15,778–15,788.
53. Carrillo JJ, Stevens PA, Milligan G. Measurement of agonist-dependent and independent signal initiation of alpha(1b)-adrenoceptor mutants by direct analysis of guanine nucleotide exchange on the G protein γalpha(11). J Pharmacol Exp Ther 2002;302:1080–1088.
54. George SR, Fan T, Xie Z, et al. Oligomerization of μ-and δ-opioid receptors. J Biol Chem 2000;275:26,128–26,135.
55. Jordan BA, Devi LA. G-protein-coupled receptor heterodimerization modulates receptor function. Nature 1999;399:697–700.
56. Wenzel-Seifert K, Seifert R. Molecular analysis of beta(2)-adrenoceptor coupling to G(s)-, G(i)-, and G(q)-proteins. Mol Pharmacol 2000;58:954–966.
57. Yu R, Hinkle PM. Signal transduction and hormone-dependent internalization of the thyrotropin-releasing hormone receptor in cells lacking Gq and G11. J Biol Chem 1999;274:15,745–15,750.
58. Milligan G, Marshall F, Rees S. G16 as a universal G protein adapter: implications for agonist screening strategies. Trends Pharmacol Sci 1996;17:235–237.
59. Pauwels PJ, Colpaert FC. Disparate ligand-mediated Ca(2+) responses by wildtype, mutant Ser(200)Ala and Ser(204)Ala alpha(2A)-adrenoceptor: G(alpha15) fusion proteins: evidence for multiple ligand-activation binding sites. Br J Pharmacol 2000;130:1505–1512.
60. Pauwels PJ, Tardif S, Finana F, Wurch T, Colpaert FC. Ligand-receptor interactions as controlled by wild-type and mutant Thr(370)Lys alpha2Badrenoceptor–Galpha15 fusion proteins. J Neurochem 2000;74:375–384.
61. Martin RS, Reynen PH, Calixto JJ, et al. Pharmacological comparison of a recombinant CB1 cannabinoid receptor with its G(alpha 16) fusion product. J Biomol Screen 2002;7:281–289.
62. Milligan G, Rees S. Chimaeric G alpha proteins: their potential use in drug discovery. Trends Pharmacol Sci 1999;20:118–124.
63. Coward P, Chan SD, Wada HG, Humphries GM, Conklin BR. Chimeric G proteins allow a high-throughput signaling assay of Gi-coupled receptors. Anal Biochem 1999;270:242–248.
64. Liu AM, Ho MK, Wong CS, Chan JH, Pau AH, Wong YH. Galpha(16/z) chimeras efficiently link a wide range of G protein-coupled receptors to calcium mobilization. J Biomol Screen 2003;8:39–49.
65. Feng GJ, Cavalli A, Milligan G. Engineering a V(2) vasopressin receptor agonistand regulator of G-protein-signaling-sensitive G protein. Anal Biochem 2002;300:212–220.
66. Fong CW, Milligan G. Analysis of agonist function at fusion proteins between the IP prostanoid receptor and cognate, unnatural and chimaeric G-proteins. Biochem J 1999;342:457–463.