Allosteric activation of plasma membrane receptors - Physiological implications and structural origins

Progress in Biophysics and Molecular Biology

Volumn 81, Issue 3, 2003, Pages 219-240

  Conigrave, Arthur D ^a   Franks, Alison H ^a  

^a UNIVERSITY OF SYDNEY   (Australia)

Author keywords

Agonist; Allosteric modulator; Conformational induction; Conformational selection; G protein coupled receptor; Metabotropic receptor; Plasma membrane; Receptor

Indexed keywords

EID: 0038026057     PISSN: 00796107     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0079-6107(03)00020-8     Document Type: Review

References (81)

1. Alberts G.L., Chio C.L., Im W.B. Allosteric modulation of the human 5-HT7A receptor by lipidic amphipathic compounds. Mol. Pharmacol. 60:2001;1349-1355.
2. Altenbach C., Cai K., Klein-Seetharaman J., Khorana H.G., Hubbell W.L. Structure and function in rhodopsin. mapping light-dependent changes in distance between residue 65 in helix TM1 and residues in the sequence 306-319 at the cytoplasmic end of helix TM7 and in helix H8 Biochemistry. 40:2001;15483-15492.
3. Anderson D.J., Crossland J., Shaw G.G. The actions of spermidine and spermine on the central nervous system. Neuropharmacology. 14:1975;571-577.
4. Bai M., Trivedi S., Kifor O., Quinn S.J., Brown E.M. Intermolecular interactions between dimeric calcium-sensing receptor monomers are important for its normal function. Proc. Natl. Acad. Sci. USA. 96:1999;2834-2839.
5. Bhattacharya S., Linden J. The allosteric enhancer, PD 81,723 stabilizes human A1 adenosine receptor coupling to G proteins. Biochim. Biophys. Acta. 1265:1995;15-21.
6. + and GTP Proc. Natl. Acad. Sci. USA. 76:1979;5626-5630.
7. Brauner-Osborne H., Jensen A.A., Sheppard P.O., O'Hara P., Krogsgaard-Larsen P. The agonist-binding domain of the calcium-sensing receptor is located at the amino-terminal domain. J. Biol. Chem. 274:1999;18382-18386.
8. 2+-sensing receptor from bovine parathyroid. Nature. 366:1993;575-580.
9. Bruns R.F., Fergus J.H. Allosteric enhancement of adenosine A1 receptor binding and function by 2-amino-3-benzoylthiophenes. Mol. Pharmacol. 38:1990;939-949.
10. Ceresa B.P., Limbird L.E. Mutation of an aspartate residue highly conserved among G-protein-coupled receptors results in nonreciprocal disruption of α2-adrenergic-G-protein interactions. J. Biol. Chem. 269:1994;29557-29564.
11. 2+-sensing receptor mediate efficient coupling to phospholipase. C. J. Biol. Chem. 275:2000;19955-19963.
12. Chatterton J.E., Awobuluyi M., Premkumar L.S., Takahashi H., Talantova M., Shin Y., Cui J., Tu S., Sevarino K.A., Nakanishi N., Tong G., Lipton S.A., Zhang D. Excitatory glycine receptors containing the NR3 family of NMDA receptor subunits. Nature. 415:2002;793-798.
13. Christopoulos A. Allosteric binding sites on cell-surface receptors. novel targets for drug discovery Nat. Rev. Drug Discov. 1:2002;198-210.
14. Christopoulos A., Kenakin T. G protein-coupled receptor allosterism and complexing. Pharmacol. Rev. 54:2002;323-374.
15. Colson A., Perlman J.H., Jinsi-Parimoo A., Nussenzeig D.R., Osman R., Gershengorn M.C. Minireview. insights into G protein-coupled receptor function using molecular models Endocrinology. 142:2001;2-10.
16. 2+-sensing receptor. Trends Pharm. Sci. 21:2000;401-407.
17. 2+-sensing receptor. Proc. Natl. Acad. Sci. USA. 97:2000;4814-4819.
18. Conigrave A.D., Franks A.H., Brown E.M., Quinn S.J. L-amino acid sensing by the calcium-sensing receptor. a general mechanism for coupling protein and calcium metabolism? Eur. J. Clin. Nutr. 56:2002;1072-1080.
19. Costa E., Guidotti A., Mao C.C., Suria A. New concepts on the mechanism of action of benzodiazepines. Life Sci. 17:1975;167-185.
20. Cravatt B.F., Prospero-Garcia O., Siuzdak G., Gilula N.B., Henriksen S.J., Boger D.L., Lerner R.A. Chemical characterization of a family of brain lipids that induce sleep. Science. 268:1995;1506-1509.
21. Daaka Y., Luttrell L.M., Lefkowitz R.J. Switching of the coupling of the b2-adrenergic receptor to different G proteins by protein kinase A. Nature. 390:1997;88-91.
22. Ellis J., Seidenberg M. Interactions between gallamine and muscarinic receptors. allosterism and subpopulation specificity are separate phenomena Eur. J. Pharmacol. 144:1987;39-44.
23. Ellis J., Seidenberg M. Interactions of alcuronium, TMB-8, and other allosteric ligands with muscarinic acetylcholine receptors. studies with chimeric receptors Mol. Pharmacol. 58:2000;1451-1460.
24. Farrens D.L., Altenbach C., Yang K., Hubbell W.L., Khorana H.G. Requirement of rigid-body motion of transmembrane helices for light activation of rhodopsin. Science. 274:1996;768-770.
25. Gao Z.G., Kim S.G., Soltysiak K.A., Melman N., Ijzerman A.P., Jacobson K.A. Selective allosteric enhancement of agonist binding and function at human A3 adenosine receptors by a series of imidazoquinoline derivatives. Mol. Pharmacol. 62:2002;81-89.
26. Gershengorn M.C., Osman R. Minireview. insights into G-protein coupled receptor function using molecular models Endocrinology. 142:2000;2-10.
27. Gether U., Kobilka B.K. G protein-coupled receptors. II. Mechanisms of agonist activation. J. Biol. Chem. 273:1998;17979-17982.
28. Gether U., Lin S., Ghanouni P., Ballesteros J.A., Weinstein H., Kobilka B.K. Agonists induce conformational changes in transmembrane domains III and VI of the beta2 adrenoceptor. EMBO J. 16:1997;6737-6747.
29. Goodman R.R., Cooper M.J., Gavish M., Snyder S.H. Guanine nucleotide and cation regulation of the binding of [H]cyclohexyladenosine and [H]diethylphenylxanthine to adenosine A1 receptors in brain membranes. Mol. Pharmacol. 21:1982;329-335.
30. Hammerland L.G., Garrett J.E., Krapcho K.J., Simin R., Capuano I.V., Alasti N., Nemeth E.F., Fuller F.H. NPS R-467 activation of chimeric calcium-metabotropic glutamate receptors and a calcium receptor deletion mutant indicates a site of action within the transmembrane domain of the calcium receptor. J. Bone Miner. Res. 11:1996;P272.
31. 2+ receptor/metabotrophic glutamate chimeric receptors. Endocrinology. 141:2000;4156-4163.
32. Han M., Lin S.W., Minkova M., Smith S.O., Sakmar T.P. Functional interaction of transmembrane helices 3 and 6 in rhodopsin. Replacement of phenylalanine 261 by alanine causes reversion of phenotype of a glycine 121 replacement mutant. J. Biol. Chem. 271:1996;32337-32342.
33. Hirai H., Kirsch J., Laube B., Betz H., Kuhse J. The glycine binding site of the N-methyl-D-aspartate receptor subunit NR1. identification of novel determinants of co-agonist potentiation in the extracellular M3-M4 loop region Proc. Natl. Acad. Sci. USA. 93:1996;6031-6036.
34. Hoare S.R.J., Strange P.G. Regulation of D2 dopamine receptors by amiloride and amiloride analogs. Mol. Pharmacol. 50:1996;1295-1308.
35. 2+ receptor cysteine-rich domain. Analysis of function of mutant and chimeric receptors. J. Biol. Chem. 275:2000;16382-16389.
36. Huang R.R., Dehaven R.N., Cheung A.H., Diehl R.E., Dixon R.A., Strader C.D. Identification of allosteric antagonists of receptor-guanine nucleotide-binding protein interactions. Mol. Pharmacol. 37:1990;304-310.
37. Janulis M., Wong M.S., Favus M.J. Structure-function requirements of parathyroid hormone for stimulation of 1,25-dihydroxyvitamin D3 production by rat renal proximal tubules. Endocrinology. 133:1993;713-719.
38. Jensen A.D., Guarnieri F., Rasmussen S.G., Asmar F., Ballesteros J.A., Gether U. Agonist-induced conformational changes at the cytoplasmic side of transmembrane segment 6 in the beta 2 adrenergic receptor mapped by site-selective fluorescent labeling. J. Biol. Chem. 276:2001;9279-9290.
39. Johnson J.W., Ascher P. Glycine potentiates the NMDA response in cultured mouse brain neurons. Nature. 325:1987;529-531.
40. Jouishomme H., Whitfield J.F., Chakravarthy B., Durkin J.P., Gagnon L., Isaacs R.J., MacLean S., Neugebauer W., Willick G., Rixon R.H. The protein kinase-C activation domain of the parathyroid hormone. Endocrinology. 130:1992;53-60.
41. Kaupmann K., Malitschek B., Schuler V., Heid J., Froestl W., Beck P., Mosbacher J., Bischoff S., Kulik A., Shigemoto R., Karschin A., Bettler B. GABA(B)-receptor subtypes assemble into functional heteromeric complexes. Nature. 396:1998;683-687.
42. Knoflach F., Mutel V., Jolidon S., Kew J.N.C., Malherbe P., Vieira E., Wichmann J., Kemp J.A. Positive allosteric modulators of metabotropic glutamate 1 receptor. characterization, mechansim of action, and binding site Proc. Natl. Acad. Sci. USA. 98:2001;13402-13407.
43. Kroiggard M., Thams P., Thorn N.A. Polyamines in nerve terminals and secretory granules isolated from neurohyophyses. Acta Physiol. Scand. 146:1992;233-239.
44. Kunishima N., Shimada Y., Tsuji Y., Sato T., Yamamoto M., Kumasaka T., Nakanishi S., Jingami H., Morikawa K. Structural basis of glutamate recognition by a dimeric metabotropic glutamate receptor. Nature. 407:2000;971-977.
45. Laube B., Hirai H., Sturgess M., Betz H., Kuhse J. Molecular determinants of agonist discrimination by NMDA receptor subunits. analysis of the glutamate binding site on the NR2B subunit Neuron. 18:1997;493-503.
46. Lawler O.A., Miggin S.M., Kinsella B.T. Protein kinase A-mediated phosphorylation of 357 serine of the mouse prostacyclin receptor regulates its coupling to G(s)-, to G(i)-, and to G(q)-coupled effector signaling. J. Biol. Chem. 276:2001;33596-33607.
47. Leppik R.A., Miller R.C., Eck M., Paquet J.L. Role of acidic amino acids in the allosteric modulation by gallamine of antagonist binding at the m2 muscarinic acetylcholine receptor. Mol. Pharmacol. 45:1994;983-990.
48. Liang M., Freedman N.J., Theiss C.T., Liggett S.B. Serine 232 of the alpha(2A)-adrenergic receptor is a protein kinase C-sensitive effector coupling switch. Biochemistry. 40:2001;15031-15037.
49. 2+ and spermine on the NMDA receptors of rat hippocampal CA1 pyramidal neurones. J. Physiol. 512:1998;29-46.
50. Maas A., Kostenis E., Mohr K. Potentiation by alcuronium of the antimuscarinic effect of N-methylscopolamine in guinea pig left atria. Eur. J. Pharmacol. 272:1995;103-106.
51. Menon S.T., Han M., Sakmar T.P. Rhodopsin. structural basis of molecular physiology Physiol. Rev. 81:2001;1659-1688.
52. + and guanine nucleotides. Nature. 288:1980;709-711.
53. Motulsky H.J., Insel P.A. Influence of sodium on the α2-adrenergic receptor system of human platelets. Role for intraplatelet sodium in receptor binding. J. Biol. Chem. 258:1983;3913-3919.
54. Nedoma J., Tucek S., Danilov A.F., Shelkovnikov S.A. Stabilization of antagonist binding to cardiac muscarinic acetylcholine receptors by gallamine and other neuromuscular blocking drugs. J. Pharmacol. Exp. Ther. 236:1986;219-223.
55. Nelson G., Chandrashekar J., Hoon M.A., Feng L., Zhao G., Ryba N.J.P., Zuker C.S. An amino-acid taste receptor. Nature. 416:2002;199-202.
56. Nemeth E.F., Steffey M.E., Hammerland L.G., Hung B.C.P., van Wagenen B.C., Delmar E.G., Balandrin M.F. Calcimimetics with potent and selective activity on the parathyroid calcium receptor. Proc. Natl. Acad. Sci. USA. 95:1998;4040-4045.
57. 2+ receptor antagonists that stimulate secretion of parathyroid hormone J. Pharmacol. Exp. Therap. 299:2001;323-331.
58. Neve K.A., Cox B.A., Henningsen R.A., Spanoyannis A., Neve R.L. Pivotal role for aspartate-80 in the regulation of dopamine D2 receptor affinity for drugs and inhibition of adenylyl cyclase. Mol. Pharmacol. 39:1991;733-739.
59. Okada T., Ernst O.P., Palczewski K., Hofmann K.P. Activation of rhodopsin. new insights from structural and biochemical studies Trends Biochem. Sci. 26:2001;319-324.
60. Palczewski K., Kumasaka T., Hori T., Behnke C.A., Motoshima H., Fox B.A., Trong I.L., Teller D.C., Okada T., Stenkamp R.E., Yamamoto M., Miyano M. Crystal structure of rhodopsin. a G protein-coupled receptor Science. 289:2000;739-745.
61. Paterson S.J., Robson L.E., Kosterlitz H.W. Control by cations of opioid binding in guinea pig brain membranes. Proc. Natl. Acad. Sci. USA. 83:1986;6216-6220.
62. Pert C.B., Snyder S.H. Opiate receptor binding of agonists and antagonists affected differentially by sodium. Mol. Pharmacol. 10:1974;868-879.
63. Pierce K.L., Lefkowitz R.J. Classical and new roles of beta-arrestins in the regulation of G-protein-coupled receptors. Nat. Rev. Neurosci. 2:2001;727-733.
64. 2+-sensing receptor. a target for polyamines Am. J. Physiol. 273:1997;C1315-1323.
65. Ransom R.W., Stec N.L. Cooperative modulation of [3H]MK-801 binding to the N-methyl-D-aspartate receptor-ion channel complex by L-glutamate, glycine, and polyamines. J. Neurochem. 51:1988;830-836.
66. Rios C.D., Jordan B.A., Gomes I., Devi L.A. G-protein-coupled receptor dimerization. modulation of receptor function Pharmacol. Therap. 92:2001;71-87.
67. Schetz J.A., Sibley D.R. The binding site crevice of the D4 dopamine receptor is coupled to three distinct sites of allosteric modulation. J. Pharmacol. Exp. Therap. 296:2001;359-363.
68. Schetz J.A., Chu A., Sibley D.R. Zinc modulates antagonist interactions with D2-like dopamine receptors through distinct molecular mechanisms. J. Pharmacol. Exp. Ther. 289:1999;956-964.
69. Schulz A., Bruns K., Henklein P., Krause G., Schubert M., Gudermann T., Wray V., Schultz G., Schoneberg T. Requirement of specific intrahelical interactions for stabilizing the inactive conformation of glycoprotein hormone receptors. J. Biol. Chem. 275:2000;37860-37869.
70. 2+ in two enteroendocrine cell lines, STC-1 and GLUTag. J. Physiol. 528:2000;165-176.
71. Sun Y., Olson R., Horning M., Armstrong N., Mayer M., Gouaux E. Mechanism of glutamate receptor desensitization. Nature. 417:2002;245-253.
72. 2+. Mol. Pharmacol. 61:2002;65-72.
73. Takasu, H., Gardella, T.J., Luck, M.D., Potts, J.T.P. Jr, Bringhurst, F.R., 1999. Amino-terminal modifications of human parathyroid hormone (PTH) selectivley alter phospholipase C signaling via the type 1 PTH receptor: implications for design of signal-specific PTH ligands. Biochemistry 38, 13453-13460.
74. Thomas E.A., Carson M.J., Neal M.J., Sutcliffe J.G. Unique allosteric regulation of 5-hydroxytryptamine receptor-mediated signal transduction by oleamide. Proc. Natl. Acad. Sci. USA. 94:1997;14115-14119.
75. Tsai B.S., Lefkowitz R.J. Agonist-specific effects of monovalent and divalent cations on adenylate cyclase-coupled alpha adrenergic receptors in rabbit platelets. Mol. Pharmacol. 14:1978;540-548.
76. 3+. Proc. Natl. Acad. Sci. USA. 99:2002;2660-2665.
77. Tucek S., Musilkova J., Nedoma J., Proska J., Shelkovnikov S., Vorlicek J. Positive cooperativity in the binding of alcuronium and N-methylscopolamine to muscarinic acetylcholine receptors. Mol. Pharmacol. 38:1990;674-680.
78. Ward S.D.C., Hamdan F.F., Bloodworth L.M., Wess J. Conformational changes that occur during M3 muscarinic acetylcholine receptor activation probed by the use of an in situ disulfide cross-linking strategy. J. Biol. Chem. 277:2002;2247-2257.
79. Wonerow P., Neumann S., Gudermann T., Paschke R. Thyrotropin receptor mutations as a tool to understand thyrotropin receptor action. J. Mol. Med. 79:2001;707-721.
80. Zahn K., Eckstein N., Trankle C., Sadee W., Mohr K. Allosteric modulation of muscarinic receptor signaling. alcuronium-induced conversion of pilocarpine from an agonist into an antagonist J. Pharmacol. Exp. Therap. 301:2002;720-728.
81. Zhang Z., Qiu W., Quinn S.J., Conigrave A.D., Brown E.M., Bai M. Three adjacent serines in the extracellular domains of the CaR are required for L-amino acid-mediated potentiation of receptor function. J. Biol. Chem. 277:2002;33727-33735.