Novel pharmacological applications of G-protein-coupled receptor-G protein fusions

Current Opinion in Pharmacology

Volumn 7, Issue 5, 2007, Pages 521-526

  Milligan, Graeme ^a   Parenty, Geraldine ^a   Stoddart, Leigh A ^a   Lane, J Robert ^a  

^a UNIVERSITY OF GLASGOW   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

DIPRENORPHINE; DOPAMINE; DOPAMINE 2 RECEPTOR; G PROTEIN COUPLED RECEPTOR; GUANINE NUCLEOTIDE BINDING PROTEIN ALPHA SUBUNIT; HYBRID PROTEIN; OPIATE AGONIST; PRECLAMOL; QUINPIROLE; TYRAMINE;

ALLOSTERISM; BINDING AFFINITY; BINDING SITE; DIMERIZATION; DRUG MECHANISM; DRUG RECEPTOR BINDING; DRUG RESEARCH; DRUG SYNTHESIS; GENE MUTATION; GENETIC CODE; HUMAN; LIGAND BINDING; OLIGOMERIZATION; PHENOTYPE; PRIORITY JOURNAL; PROTEIN BINDING; PROTEIN CONFORMATION; PROTEIN DETERMINATION; PROTEIN DOMAIN; PROTEIN EXPRESSION; PROTEIN PROCESSING; PROTEIN PROTEIN INTERACTION; PROTEIN VARIANT; RECEPTOR BINDING; REVIEW; SIGNAL TRANSDUCTION;

DIMERIZATION; GTP-BINDING PROTEIN ALPHA SUBUNITS; HUMANS; RECEPTORS, G-PROTEIN-COUPLED; RECOMBINANT FUSION PROTEINS;

EID: 35248877040     PISSN: 14714892     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.coph.2007.06.007     Document Type: Review

References (41)

1. 2A-adrenoceptor. Biochemistry 37 (1998) 11555-11562
2. Wise A., Sheehan M., Rees S., Lee M., and Milligan G. Comparative analysis of the efficacy of A1 adenosine receptor activation of Gi/oα G proteins following co-expression of receptor and G protein and expression of A1 adenosine receptor-Gi/oα fusion proteins. Biochemistry 38 (1999) 2272-2278
3. Milligan G. Altering the relative stoichiometry of receptors. G-proteins and effectors: effects on agonist function. Handb Exp Pharm 148 (2000) 363-389
4. Bertin B., Freissmuth M., Jockers R., Strosberg A.D., and Marullo S. Cellular signaling by an agonist-activated receptor/Gs alpha fusion protein. Proc Natl Acad Sci USA 91 (1994) 8827-8831
5. i1α fusion protein. Biochem J 325 (1997) 17-21
6. Colquhoun D. Binding, gating, affinity and efficacy: the interpretation of structure-activity relationships for agonists and of the effects of mutating receptors. Br J Pharmacol 125 (1998) 924-947
7. Milligan G., Feng G.-J., Ward R.J., Sartania N., Ramsay D., McLean A.J., and Carrillo J.J. G protein-coupled receptor fusion proteins in drug discovery. Curr Pharmaceut Des 10 (2004) 1989-2001. A recent review highlighting the range of ways in which GPCR fusions might be used in drug discovery.
8. Hildebrandt J.D. Bring your own G protein. Mol Pharmacol 69 (2006) 1079-1082. An excellent recent 'perspective' that collects together much of the available literature on GPCR-G protein fusions and comments on reference [19].
9. Kostenis E., Waelbroeck M., and Milligan G. Promiscuous Gα proteins in basic research and drug discovery. Trends Pharmacol Sci 26 (2005) 595-602
10. Fong C.W., and Milligan G. Analysis of agonist function at fusion proteins between the IP prostanoid receptor and cognate, unnatural and chimaeric G proteins. Biochem J 342 (1999) 457-463
11. o1 fusion protein dynamically regulates the palmitoylation status of the G protein but not of the receptor. Biochem J 385 (2005) 197-206
12. 11 are compromised by de-palmitoylation of the G protein but not of the receptor. Cell Signal 18 (2006) 1244-1251
13. Perez D.M., and Karnik S.S. Multiple signaling states of G-protein-coupled receptors. Pharmacol Rev 57 (2005) 147-161
14. Kenakin T. Drug efficacy at G protein-coupled receptors. Annu Rev Pharmacol Toxicol 42 (2002) 349-379
15. Urban J.D., Clarke W.P., von Zastrow M., Nichols D.E., Kobilka B., Weinstein H., Javitch J.A., Roth B.L., Christopoulos A., Sexton P.M., et al. Functional selectivity and classical concepts of quantitative pharmacology. J Pharmacol Exp Ther 320 (2007) 1-13
16. Swaminath G., Deupi X., Lee T.W., Zhu W., Thian F.S., Kobilka T.S., and Kobilka B. Probing the beta2 adrenoceptor binding site with catechol reveals differences in binding and activation by agonists and partial agonists. J Biol Chem 280 (2005) 22165-22171
17. Siefert R., Wenzel-Seifert K., Gether U., and Kokilka B.K. Functional differences between full and partial agonists: evidence for ligand-specific receptor conformations. J Pharmacol Exp Ther 297 (2001) 1218-1226
18. i3. Mol Pharmacol 71 (2007) 1349-1359. The first use of a set of GPCR-G protein fusions in which the same receptor is linked to each member of a subfamily of G proteins to examine whether ligands can selectively activate or block activation of closely related G proteins.
19. Neubig R.R. Missing links: mechanisms of protean agonism. Mol Pharmacol 71 (2007) 1200-1202
20. 13 G proteins and indications that agonists at the thromboxane A2 receptor do not activate them equally.
21. Meyer B.H., Segura J.-M., Martinez K.L., Hovius R., George N., and Johnsson K. FRET imaging reveals that functional neurokinin-1 receptors are monomeric and reside in membrane microdomains of live cells. Proc Natl Acad Sci USA 103 (2006) 2138-2143
22. Milligan G. G protein-coupled receptor dimerisation: molecular basis and relevance to function. Biochim Biophys Acta Biomemb 1768 (2007) 825-835
23. Pin J.P., Kniazeff J., Liu J., Binet V., Goudet C., Rondard P., and Prezeau L. Allosteric functioning of dimeric class C G-protein-coupled receptors. FEBS J 272 (2005) 2947-2955
24. Albizu L., Balestre M.N., Breton C., Pin J.P., Manning M., Mouillac B., Barberis C., and Durroux T. Probing the existence of G protein-coupled receptor dimers by positive and negative ligand-dependent cooperative binding. Mol Pharmacol 70 (2006) 1783-1791
25. El-Asmar L., Springael J.Y., Ballet S., Andrieu E.U., Vassart G., and Parmentier M. Evidence for negative binding cooperativity within CCR5-CCR2b heterodimers. Mol Pharmacol 67 (2005) 460-469
26. Springael J.Y., Le Minh P.N., Urizar E., Costagliola S., Vassart G., and Parmentier M. Allosteric modulation of binding properties between units of chemokine receptor homo- and hetero-oligomers. Mol Pharmacol 69 (2006) 1652-1661
27. Damian M., Martin A., Mesnier D., Pin J.P., and Baneres J.L. Asymmetric conformational changes in a GPCR dimer controlled by G-proteins. EMBO J 25 (2006) 5693-5702
28. Carrillo J.J., Pediani J., and Milligan G. Dimers of class A G protein-coupled receptors function via agonist-mediated trans-activation of associated G proteins. J Biol Chem 278 (2003) 42578-42587
29. Pascal G., and Milligan G. Functional complementation and the analysis of opioid receptor homo-dimerization. Mol Pharmacol 68 (2005) 905-915. Description of how pairs of non-functonal (but potentially complementary) GPCR-G proteins may be used to explore GPCR dimerisation.
30. 1L-adrenoceptor. Mol Pharmacol 66 (2004) 228-239
31. Milligan G. GPCR hetero-dimers: pharmacology, function and relevance to drug discovery. Drug Discov Today 11 (2006) 541-549
32. Covington D.K., Briscoe C.A., Brown A.J., and Jayawickreme C.K. The G-protein-coupled receptor 40 family (GPR40-GPR43) and its role in nutrient sensing. Biochem Soc Trans 34 (2006) 770-773
33. Milligan G., Stoddart L.A., and Brown A.J. G protein-coupled receptors for free fatty acids. Cell Signal 18 (2006) 1360-1365
34. q fusion to demonstrate that high apparent 'constitutive' activity at this receptor is an artefact because of the presence of bound endogenous agonist.
35. Hosoi T., Koguchi Y., Sugikawa E., Chikada A., Ogawa K., Tsuda N., Suto N., Tsunoda S., Taniguchi T., and Ohnuki T. Identification of a novel human eicosanoid receptor coupled to G(i/o). J Biol Chem 277 (2002) 31459-31465
36. Takeda S., Yamamoto A., Okada T., Matsumura E., Nose E., Kogure K., Kojima S., and Haga T. Identification of surrogate ligands for orphan G protein-coupled receptors. Life Sci 74 (2003) 367-377
37. Watanabe M., Houten S.M., Mataki C., Christoffolete M.A., Kim B.W., Sato H., Messaddeq N., Harney J.W., Ezaki O., Kodama T., et al. Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation. Nature 439 (2006) 484-489
38. Robas N., Mead E., and Fidock M. MrgX2 is a high potency cortistatin receptor expressed in dorsal root ganglion. J Biol Chem 278 (2003) 44400-44404
39. 389-beta1-adrenoceptor-Gsalpha fusion proteins. Receptors Channels 9 (2003) 315-323. Only current example of the use of GPCR-G protein fusions to explore the functional significance of polymorphic variants in a GPCR open-reading frame.
40. Liggett S.B., Mialet-Perez J., Thaneemit-Chen S., Weber S.A., Greene S.M., Hodne D., Nelson B., Morrison J., Domanski M.J., Wagoner L.E., et al. A polymorphism within a conserved beta(1)-adrenergic receptor motif alters cardiac function and beta-blocker response in human heart failure. Proc Natl Acad Sci USA 103 (2006) 11288-11293
41. Akhtar S.A., D'Souza K.M., Petrashevskaya N.N., Mialet-Perez J., and Liggett S.B. Myocardial beta1-adrenergic receptor polymorphisms affect functional recovery after ischemic injury. Am J Physiol Heart Circ Physiol 290 (2006) H1427-H1432