메뉴 건너뛰기




Volumn 81, Issue 6, 2011, Pages 691-702

Strategies for the identification of allosteric modulators of G-protein-coupled receptors

Author keywords

Allosteric modulators; Ca2+ signaling; G protein coupled receptors; High throughput screening

Indexed keywords

2 AMINO 3 (3,4 DICHLOROBENZOYL) 4,5,6,7 TETRAHYDROBENZO[B]THIOPHENE; 2 AMINO 4,5 DIMETHYL 3 (3 TRIFLUOROMETHYLBENZOYL)THIOPHENE; 2,6 DI TERT BUTYL 4 (3 HYDROXY 2,2 DIMETHYLPROPYL)PHENOL; 4 ANILINO 2 CYCLOPENTYLIMIDAZO[4,5 C]QUINOLINE; 5 CHLORO 4 [N (CYCLOPROPYLMETHYL) N PROPYLAMINO] 2 METHYL 6 (2,4,6 TRICHLOROANILINO)PYRIMIDINE; 8 (2,4 DICHLOROPHENYL) 4 [2 METHOXY 1 (METHOXYMETHYL)ETHYLAMINO] 2,7 DIMETHYLPYRAZOLO[1,5 A][1,3,5]TRIAZINE; AMILORIDE DERIVATIVE; ANTALARMIN; CHEMOKINE RECEPTOR CCR5; CINACALCET; G PROTEIN COUPLED RECEPTOR; GLYCOPROTEIN GP 100; MACROPHAGE INFLAMMATORY PROTEIN 1ALPHA; MARAVIROC; N,N' DICYCLOPENTYL 2 METHYLTHIO 5 NITRO 4,6 PYRIMIDINEDIAMINE; OLCEGEPANT; QUINOXALINE DERIVATIVE; RANTES; REPARIXIN; TRICHOSANTHIN;

EID: 79951958713     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bcp.2010.12.012     Document Type: Note
Times cited : (73)

References (107)
  • 3
    • 33947375174 scopus 로고    scopus 로고
    • Physiological roles of G protein-coupled receptor kinases and arrestins
    • DOI 10.1146/annurev.physiol.69.022405.154731
    • Premont RT, Gainetdinov RR. Physiological roles of G-protein-coupled receptor kinases and arrestins. Annu Rev Physiol 2007;69:511-34. (Pubitemid 46457653)
    • (2007) Annual Review of Physiology , vol.69 , pp. 511-534
    • Premont, R.T.1    Gainetdinov, R.R.2
  • 4
    • 0030671469 scopus 로고    scopus 로고
    • Agonist-specific receptor conformations
    • DOI 10.1016/S0165-6147(97)01127-9, PII S0165614797011279
    • Kenakin T. Agonist-specific receptor conformations. Trends Pharmacol Sci 1997;18:416-7. (Pubitemid 27521058)
    • (1997) Trends in Pharmacological Sciences , vol.18 , Issue.11 , pp. 416-417
    • Kenakin, T.1
  • 5
    • 77949534717 scopus 로고    scopus 로고
    • Allosteric receptors: From electric organ to cognition
    • Changeux JP. Allosteric receptors: from electric organ to cognition. Annu Rev Pharmacol Toxicol 2010;50:1-38.
    • (2010) Annu Rev Pharmacol Toxicol , vol.50 , pp. 1-38
    • Changeux, J.P.1
  • 6
    • 53449093828 scopus 로고    scopus 로고
    • G-protein-coupled receptors: From classical modes of modulation to allosteric mechanisms
    • Bridges TM, Lindsley CW. G-protein-coupled receptors: from classical modes of modulation to allosteric mechanisms. ACS Chem Biol 2008;3:530-41.
    • (2008) ACS Chem Biol , vol.3 , pp. 530-541
    • Bridges, T.M.1    Lindsley, C.W.2
  • 7
    • 58149193205 scopus 로고    scopus 로고
    • Allosteric modulators of GPCRs: A novel approach for the treatment of CNS disorders
    • Conn PJ, Christopoulos A, Lindsley CW. Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders. Nat Rev Drug Discov 2009;8:41-54.
    • (2009) Nat Rev Drug Discov , vol.8 , pp. 41-54
    • Conn, P.J.1    Christopoulos, A.2    Lindsley, C.W.3
  • 8
    • 34447632041 scopus 로고    scopus 로고
    • Allosteric GPCR modulators: Taking advantage of permissive receptor pharmacology
    • DOI 10.1016/j.tips.2007.06.004, PII S0165614707001496, Allosterism and Collateral Efficacy
    • Leach K, Sexton PM, Christopoulos A. Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology. Trends Pharmacol Sci 2007;28:382-9. (Pubitemid 47087967)
    • (2007) Trends in Pharmacological Sciences , vol.28 , Issue.8 , pp. 382-389
    • Leach, K.1    Sexton, P.M.2    Christopoulos, A.3
  • 9
    • 77951985712 scopus 로고    scopus 로고
    • Allosteric ligands for G-protein-coupled receptors: A novel strategy with attractive therapeutic opportunities
    • De Amici M, Dallanoce C, Holzgrabe U, Trankle C, Mohr K. Allosteric ligands for G-protein-coupled receptors: a novel strategy with attractive therapeutic opportunities. Med Res Rev 2009;30:463-549.
    • (2009) Med Res Rev , vol.30 , pp. 463-549
    • De Amici, M.1    Dallanoce, C.2    Holzgrabe, U.3    Trankle, C.4    Mohr, K.5
  • 10
    • 0038024615 scopus 로고    scopus 로고
    • The G-protein-coupled receptors in the human genome form five main families. Phylogenetic analysis, paralogon groups, and fingerprints
    • Fredriksson R, Lagerstrom MC, Lundin LG, Schioth HB. The G-protein-coupled receptors in the human genome form five main families. Phylogenetic analysis, paralogon groups, and fingerprints. Mol Pharmacol 2003;63: 1256-72.
    • (2003) Mol Pharmacol , vol.63 , pp. 1256-1272
    • Fredriksson, R.1    Lagerstrom, M.C.2    Lundin, L.G.3    Schioth, H.B.4
  • 12
    • 0027964227 scopus 로고
    • Cyclothiazide differentially modulates desensitization of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor splice variants
    • Partin KM, Patneau DK, Mayer ML. Cyclothiazide differentially modulates desensitization of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor splice variants. Mol Pharmacol 1994;46:129-38.
    • (1994) Mol Pharmacol , vol.46 , pp. 129-138
    • Partin, K.M.1    Patneau, D.K.2    Mayer, M.L.3
  • 13
    • 0028885504 scopus 로고
    • Interactions among GYKI-52466, cyclothiazide, and aniracetam at recombinant AMPA and kainate receptors
    • Johansen TH, Chaudhary A, Verdoorn TA. Interactions among GYKI-52466, cyclothiazide, and aniracetam at recombinant AMPA and kainate receptors. Mol Pharmacol 1995;48:946-55.
    • (1995) Mol Pharmacol , vol.48 , pp. 946-955
    • Johansen, T.H.1    Chaudhary, A.2    Verdoorn, T.A.3
  • 14
    • 33645796458 scopus 로고    scopus 로고
    • Ago-allosteric modulation and other types of allostery in dimeric 7TM receptors
    • Schwartz TW, Holst B. Ago-allosteric modulation and other types of allostery in dimeric 7TM receptors. J Recept Signal Transduct Res 2006;26:107-28.
    • (2006) J Recept Signal Transduct Res , vol.26 , pp. 107-128
    • Schwartz, T.W.1    Holst, B.2
  • 15
    • 0025603686 scopus 로고
    • Allosteric enhancement of adenosine A1 receptor binding and function by 2-amino-3-benzoylthiophenes
    • Bruns RF, Fergus JH. Allosteric enhancement of adenosine A1 receptor binding and function by 2-amino-3-benzoylthiophenes. Mol Pharmacol 1990;38:939-49.
    • (1990) Mol Pharmacol , vol.38 , pp. 939-949
    • Bruns, R.F.1    Fergus, J.H.2
  • 16
    • 34447638166 scopus 로고    scopus 로고
    • Allosteric enhancers, allosteric agonists and ago-allosteric modulators: Where do they bind and how do they act?
    • Schwartz TW, Holst B. Allosteric enhancers, allosteric agonists and ago-allosteric modulators: where do they bind and how do they act? Trends Pharmacol Sci 2007;28:366-73.
    • (2007) Trends Pharmacol Sci , vol.28 , pp. 366-373
    • Schwartz, T.W.1    Holst, B.2
  • 17
    • 77953485027 scopus 로고    scopus 로고
    • Structural determinants of allosteric agonism and modulation at the M4 muscarinic acetylcholine receptor: Identification of ligand-specific and global activation mechanisms
    • Nawaratne V, Leach K, Felder CC, Sexton PM, Christopoulos A. Structural determinants of allosteric agonism and modulation at the M4 muscarinic acetylcholine receptor: identification of ligand-specific and global activation mechanisms. J Biol Chem 2010;285:19012-21.
    • (2010) J Biol Chem , vol.285 , pp. 19012-19021
    • Nawaratne, V.1    Leach, K.2    Felder, C.C.3    Sexton, P.M.4    Christopoulos, A.5
  • 18
    • 34250743762 scopus 로고    scopus 로고
    • Allosteric approaches to the targeting of G-protein-coupled receptors for novel drug discovery: A critical assessment
    • DOI 10.1016/j.bcp.2007.05.007, PII S0006295207002997
    • Raddatz R, Schaffhauser H, Marino MJ. Allosteric approaches to the targeting of G-protein-coupled receptors for novel drug discovery: a critical assessment. Biochem Pharmacol 2007;74:383-91. (Pubitemid 46963242)
    • (2007) Biochemical Pharmacology , vol.74 , Issue.3 , pp. 383-391
    • Raddatz, R.1    Schaffhauser, H.2    Marino, M.J.3
  • 19
    • 1942517868 scopus 로고    scopus 로고
    • Principles. Receptor theory in pharmacology
    • Kenakin T, Principles. Receptor theory in pharmacology. Trends Pharmacol Sci 2004;25:186-92.
    • (2004) Trends Pharmacol Sci , vol.25 , pp. 186-192
    • Kenakin, T.1
  • 20
    • 1842333847 scopus 로고    scopus 로고
    • Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors
    • Jakubik J, Bacakova L, El-Fakahany EE, Tucek S. Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors. Mol Pharmacol 1997;52:172-9. (Pubitemid 27318633)
    • (1997) Molecular Pharmacology , vol.52 , Issue.1 , pp. 172-179
    • Jakubik, J.1    Bacakova, L.2    El-Fakahany, E.E.3    Tucek, S.4
  • 21
    • 69649097791 scopus 로고    scopus 로고
    • '7TM receptor allostery: Putting numbers to shapeshifting proteins
    • Kenakin TP. '7TM receptor allostery: putting numbers to shapeshifting proteins. Trends Pharmacol Sci 2009;30:460-9.
    • (2009) Trends Pharmacol Sci , vol.30 , pp. 460-469
    • Kenakin, T.P.1
  • 22
    • 0036462446 scopus 로고    scopus 로고
    • Allosteric modulators of group I metabotropic glutamate receptors: Novel subtype-selective ligands and therapeutic perspectives
    • Gasparini F, Kuhn R, Pin JP. Allosteric modulators of group I metabotropic glutamate receptors: novel subtype-selective ligands and therapeutic perspectives. Curr Opin Pharmacol 2002;2:43-9.
    • (2002) Curr Opin Pharmacol , vol.2 , pp. 43-49
    • Gasparini, F.1    Kuhn, R.2    Pin, J.P.3
  • 24
    • 27844482134 scopus 로고    scopus 로고
    • A close structural analog of 2-methyl-6-(phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators
    • DOI 10.1124/mol.105.016139
    • Rodriguez AL, Nong Y, Sekaran NK, Alagille D, Tamagnan GD, Conn PJ. A close structural analog of 2-methyl-6-(phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators. Mol Pharmacol 2005; 68:1793-802. (Pubitemid 41654362)
    • (2005) Molecular Pharmacology , vol.68 , Issue.6 , pp. 1793-1802
    • Rodriguez, A.L.1    Nong, Y.2    Sekaran, N.K.3    Alagille, D.4    Tamagnan, G.D.5    Conn, P.J.6
  • 25
    • 35048840600 scopus 로고    scopus 로고
    • Maraviroc
    • discussion 89-90
    • Carter NJ, Keating GM. Maraviroc. Drugs 2007;67:2277-88 [discussion 89-90].
    • (2007) Drugs , vol.67 , pp. 2277-2288
    • Carter, N.J.1    Keating, G.M.2
  • 26
    • 70349482329 scopus 로고    scopus 로고
    • New antiretroviral drugs: A review of the efficacy, safety, pharmacokinetics, and resistance profile of tipranavir, darunavir, etravirine, rilpivirine, maraviroc, and raltegravir
    • Hughes CA, Robinson L, Tseng A, MacArthur RD. New antiretroviral drugs: a review of the efficacy, safety, pharmacokinetics, and resistance profile of tipranavir, darunavir, etravirine, rilpivirine, maraviroc, and raltegravir. Expert Opin Pharmacother 2009;10:2445-66.
    • (2009) Expert Opin Pharmacother , vol.10 , pp. 2445-2466
    • Hughes, C.A.1    Robinson, L.2    Tseng, A.3    MacArthur, R.D.4
  • 27
    • 1342346546 scopus 로고    scopus 로고
    • Homology Modeling of the Transmembrane Domain of the Human Calcium Sensing Receptor and Localization of an Allosteric Binding Site
    • DOI 10.1074/jbc.M307191200
    • Miedlich SU, Gama L, Seuwen K, Wolf RM, Breitwieser GE. Homology modeling of the transmembrane domain of the human calcium sensing receptor and localization of an allosteric binding site. J Biol Chem 2004;279:7254-63. (Pubitemid 38248875)
    • (2004) Journal of Biological Chemistry , vol.279 , Issue.8 , pp. 7254-7263
    • Miedlich, S.U.1    Gama, L.2    Seuwen, K.3    Wolf, R.M.4    Breitwieser, G.E.5
  • 31
    • 27844597919 scopus 로고    scopus 로고
    • Functional assays for screening GPCR targets
    • DOI 10.1016/j.copbio.2005.10.008, PII S0958166905001680, Chemical Biotechnology/Pharmaceutical Biotechnology
    • Thomsen W, Frazer J, Unett D. Functional assays for screening GPCR targets. Curr Opin Biotechnol 2005;16:655-65. (Pubitemid 41654645)
    • (2005) Current Opinion in Biotechnology , vol.16 , Issue.6 , pp. 655-665
    • Thomsen, W.1    Frazer, J.2    Unett, D.3
  • 32
    • 46149110286 scopus 로고    scopus 로고
    • 2b receptor in evaluation of aequorin detection of calcium mobilization for miniaturized GPCR high-throughput screening
    • DOI 10.1177/1087057108319212
    • Gilchrist 2nd MA, Cacace A, Harden DG. Characterization of the 5-HT2b receptor in evaluation of aequorin detection of calcium mobilization for miniaturized GPCR high-throughput screening. J Biomol Screen 2008;13: 486-93. (Pubitemid 351905080)
    • (2008) Journal of Biomolecular Screening , vol.13 , Issue.6 , pp. 486-493
    • Gilchrist II, M.A.1    Cacace, A.2    Harden, D.G.3
  • 33
    • 27144434813 scopus 로고    scopus 로고
    • Techniques: Promiscuous Galpha proteins in basic research and drug discovery
    • DOI 10.1016/j.tips.2005.09.007, PII S0165614705002397
    • Kostenis E, Waelbroeck M, Milligan G. Techniques: Promiscuous G[alpha] proteins in basic research and drug discovery. Trends Pharmacol Sci 2005;26:595-602. (Pubitemid 41505228)
    • (2005) Trends in Pharmacological Sciences , vol.26 , Issue.11 , pp. 595-602
    • Kostenis, E.1    Waelbroeck, M.2    Milligan, G.3
  • 34
    • 0030666738 scopus 로고    scopus 로고
    • Desensitization of thyrotropin-releasing hormone receptor-mediated responses involves multiple steps
    • DOI 10.1074/jbc.272.45.28301
    • Yu R, Hinkle PM. Desensitization of thyrotropin-releasing hormone receptor-mediated responses involves multiple steps. J Biol Chem 1997;272:28301-7. (Pubitemid 27517773)
    • (1997) Journal of Biological Chemistry , vol.272 , Issue.45 , pp. 28301-28307
    • Yu, R.1    Hinkle, P.M.2
  • 37
    • 0029162109 scopus 로고
    • Pharmacological proteus?
    • Kenakin T. Pharmacological proteus? Trends Pharmacol Sci 1995;16:256-8.
    • (1995) Trends Pharmacol Sci , vol.16 , pp. 256-258
    • Kenakin, T.1
  • 40
    • 36348946976 scopus 로고    scopus 로고
    • Functional selectivity through protean and biased agonism: Who steers the ship?
    • Kenakin T. Functional selectivity through protean and biased agonism: who steers the ship? Mol Pharmacol 2007;72:1393-401.
    • (2007) Mol Pharmacol , vol.72 , pp. 1393-1401
    • Kenakin, T.1
  • 41
    • 77956249652 scopus 로고    scopus 로고
    • Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner; implications for drug screening
    • Koole C, Wootten D, Simms J, Valant C, Sridhar R, Woodman OL, et al. Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner; implications for drug screening. Mol Pharmacol 2010;78:456-65.
    • (2010) Mol Pharmacol , vol.78 , pp. 456-465
    • Koole, C.1    Wootten, D.2    Simms, J.3    Valant, C.4    Sridhar, R.5    Woodman, O.L.6
  • 42
    • 67650436176 scopus 로고    scopus 로고
    • Drug discovery and natural products: End of an era or an endless frontier?
    • Li J-W, Vederas JC. Drug discovery and natural products: end of an era or an endless frontier? Science 2009;325:161-5.
    • (2009) Science , vol.325 , pp. 161-165
    • Li, J.-W.1    Vederas, J.C.2
  • 47
    • 0033003760 scopus 로고    scopus 로고
    • A simple statistical parameter for use in evaluation and validation of high throughput screening assays
    • DOI 10.1177/108705719900400206
    • Zhang JH, Chung TD, Oldenburg KR. A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J Biomol Screen 1999;4:67-73. (Pubitemid 29278954)
    • (1999) Journal of Biomolecular Screening , vol.4 , Issue.2 , pp. 67-73
    • Zhang, J.-H.1    Chung, T.D.Y.2    Oldenburg, K.R.3
  • 48
    • 77149174796 scopus 로고    scopus 로고
    • Context-dependent pharmacology exhibited by negative allosteric modulators of metabotropic glutamate receptor 7
    • Niswender CM, Johnson KA, Miller NR, Ayala JE, Luo Q, Williams R, et al. Context-dependent pharmacology exhibited by negative allosteric modulators of metabotropic glutamate receptor 7. Mol Pharmacol 2010;77: 459-68.
    • (2010) Mol Pharmacol , vol.77 , pp. 459-468
    • Niswender, C.M.1    Johnson, K.A.2    Miller, N.R.3    Ayala, J.E.4    Luo, Q.5    Williams, R.6
  • 49
    • 77952546520 scopus 로고    scopus 로고
    • Impact of new technologies for cellular screening along the drug value chain
    • Moller C, Slack M. Impact of new technologies for cellular screening along the drug value chain. Drug Discov Today 2010;15:384-90.
    • (2010) Drug Discov Today , vol.15 , pp. 384-390
    • Moller, C.1    Slack, M.2
  • 50
    • 33750822293 scopus 로고    scopus 로고
    • G Protein-Coupled Receptor Internalization Assays in the High-Content Screening Format
    • DOI 10.1016/S0076-6879(06)14008-2, PII S0076687906140082, Measuring Biological Responses with Automated Microscopy
    • Haasen D, Schnapp A, Valler MJ, Heilker R, James I. G-Protein-coupled receptor internalization assays in the high-content screening format. Methods Enzymol 2006;414:121-39. (Pubitemid 44716220)
    • (2006) Methods in Enzymology , vol.414 , pp. 121-139
    • Haasen, D.1    Schnapp, A.2    Valler, M.J.3    Heilker, R.4
  • 51
    • 73149088166 scopus 로고    scopus 로고
    • Differential regulation of muscarinic M1 receptors by orthosteric and allosteric ligands
    • Davis C, Bradley S, Schiffer H, Friberg M, Koch K, Tolf B-R, et al. Differential regulation of muscarinic M1 receptors by orthosteric and allosteric ligands. BMC Pharmacol 2009;9:14.
    • (2009) BMC Pharmacol , vol.9 , pp. 14
    • Davis, C.1    Bradley, S.2    Schiffer, H.3    Friberg, M.4    Koch, K.5    Tolf, B.-R.6
  • 52
    • 77955887321 scopus 로고    scopus 로고
    • Differential effects of allosteric M1 muscarinic acetylcholine receptor agonists on receptor activation, arrestin 3 recruitment, and receptor down-regulation
    • Davis AA, Heilman CJ, Brady AE, Miller NR, Fuerstenau-Sharp M, Hanson BJ, et al. Differential effects of allosteric M1 muscarinic acetylcholine receptor agonists on receptor activation, arrestin 3 recruitment, and receptor down-regulation. ACS Chem Neurosci 2010;1:542-51.
    • (2010) ACS Chem Neurosci , vol.1 , pp. 542-551
    • Davis, A.A.1    Heilman, C.J.2    Brady, A.E.3    Miller, N.R.4    Fuerstenau-Sharp, M.5    Hanson, B.J.6
  • 53
    • 75449117290 scopus 로고    scopus 로고
    • High-content screening for the discovery of pharmacological compounds: Advantages, challenges and potential benefits of recent technological developments
    • Soleilhac E, Nadon R, Lafanechere L. High-content screening for the discovery of pharmacological compounds: advantages, challenges and potential benefits of recent technological developments. Expert Opin Drug Discov 2010;5:135-44.
    • (2010) Expert Opin Drug Discov , vol.5 , pp. 135-144
    • Soleilhac, E.1    Nadon, R.2    Lafanechere, L.3
  • 55
    • 35248895259 scopus 로고    scopus 로고
    • Impedance-based cellular assay technologies: Recent advances, future promise
    • DOI 10.1016/j.coph.2007.08.004, PII S1471489207001324, Anti-Infective/New Technologies
    • McGuinness R. Impedance-based cellular assay technologies: recent advances, future promise. Curr Opin Pharmacol 2007;7:535-40. (Pubitemid 47560223)
    • (2007) Current Opinion in Pharmacology , vol.7 , Issue.5 , pp. 535-540
    • McGuinness, R.1
  • 57
    • 79951959893 scopus 로고    scopus 로고
    • Characterization of GABA-B receptor allosteric modulators using the CellKey® system
    • San Francisco: MDS Sciex
    • Sturchler E. Characterization of GABA-B receptor allosteric modulators using the CellKey® system. In: Benefits of Label-Free Impedance Analysis for Complex GPCR Biology. San Francisco: MDS Sciex; 2010 , https://danaher. webex.com/ec0600l/eventcenter/recording/recordAction.do?siteurl=danaher &theAction=poprecord&path=pop-program-info&recordID=44910047.
    • (2010) Benefits of Label-Free Impedance Analysis for Complex GPCR Biology
    • Sturchler, E.1
  • 59
    • 69249206623 scopus 로고    scopus 로고
    • G-protein-coupled receptor hetero-dimerization: Contribution to pharmacology and function
    • Milligan G. G-protein-coupled receptor hetero-dimerization: contribution to pharmacology and function. Br J Pharmacol 2009;158:5-14.
    • (2009) Br J Pharmacol , vol.158 , pp. 5-14
    • Milligan, G.1
  • 60
    • 0038497887 scopus 로고    scopus 로고
    • Frizzled receptor dimerization is sufficient to activate the Wnt/β-catenin pathway
    • DOI 10.1242/jcs.00451
    • Carron C, Pascal A, Djiane A, Boucaut J-C, Shi D-L, Umbhauer M. Frizzled receptor dimerization is sufficient to activate the Wnt/β-catenin pathway. J Cell Sci 2003;116:2541-50. (Pubitemid 36790135)
    • (2003) Journal of Cell Science , vol.116 , Issue.12 , pp. 2541-2550
    • Carron, C.1    Pascal, A.2    Djiane, A.3    Boucaut, J.-C.4    Shi, D.-L.5    Umbhauer, M.6
  • 61
    • 34848813593 scopus 로고    scopus 로고
    • The role of receptor oligomerization in modulating the expression and function of leukocyte adhesion-G-protein-coupled receptors
    • Davies JQ, Chang G-W, Yona S, Gordon S, Stacey M, Lin H-H. The role of receptor oligomerization in modulating the expression and function of leukocyte adhesion-G-protein-coupled receptors. J Biol Chem 2007;282: 27343-5.
    • (2007) J Biol Chem , vol.282 , pp. 27343-27345
    • Davies, J.Q.1    Chang, G.-W.2    Yona, S.3    Gordon, S.4    Stacey, M.5    Lin, H.-H.6
  • 63
    • 78650147139 scopus 로고    scopus 로고
    • Allostery at G-protein-coupled receptor homo- and heteromers: Uncharted pharmacological landscapes
    • Smith NJ, Milligan G. Allostery at G-protein-coupled receptor homo- and heteromers: uncharted pharmacological landscapes. Pharmacol Rev 2010; 62:701-25.
    • (2010) Pharmacol Rev , vol.62 , pp. 701-725
    • Smith, N.J.1    Milligan, G.2
  • 64
    • 77951668878 scopus 로고    scopus 로고
    • Heterodimerisation of G-protein-coupled receptors: Implications for drug design and ligand screening
    • del Burgo LS, Milligan G. Heterodimerisation of G-protein-coupled receptors: implications for drug design and ligand screening. Expert Opin Drug Discov 2010;5:461-74.
    • (2010) Expert Opin Drug Discov , vol.5 , pp. 461-474
    • Del Burgo, L.S.1    Milligan, G.2
  • 65
    • 67650489125 scopus 로고    scopus 로고
    • Orthosteric/allosteric bitopic ligands: Going hybrid at GPCRs
    • Valant C, Sexton PM, Christopoulos A. Orthosteric/allosteric bitopic ligands: going hybrid at GPCRs. Mol Interv 2009;9:125-35.
    • (2009) Mol Interv , vol.9 , pp. 125-135
    • Valant, C.1    Sexton, P.M.2    Christopoulos, A.3
  • 67
    • 57649170953 scopus 로고    scopus 로고
    • A novel mechanism of G-protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand
    • Valant C, Gregory KJ, Hall NE, Scammells PJ, Lew MJ, Sexton PM, et al. A novel mechanism of G-protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand. J Biol Chem 2008;283:29312-21.
    • (2008) J Biol Chem , vol.283 , pp. 29312-29321
    • Valant, C.1    Gregory, K.J.2    Hall, N.E.3    Scammells, P.J.4    Lew, M.J.5    Sexton, P.M.6
  • 71
    • 56749103466 scopus 로고    scopus 로고
    • The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist
    • Jaakola VP, Griffith MT, Hanson MA, Cherezov V, Chien EY, Lane JR, et al. The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist. Science 2008;322:1211-7.
    • (2008) Science , vol.322 , pp. 1211-1217
    • Jaakola, V.P.1    Griffith, M.T.2    Hanson, M.A.3    Cherezov, V.4    Chien, E.Y.5    Lane, J.R.6
  • 72
    • 47049130668 scopus 로고    scopus 로고
    • Crystal structure of the ligand-free G-protein-coupled receptor opsin
    • DOI 10.1038/nature07063, PII NATURE07063
    • Park JH, Scheerer P, Hofmann KP, Choe HW, Ernst OP. Crystal structure of the ligand-free G-protein-coupled receptor opsin. Nature 2008;454:183-7. (Pubitemid 351969893)
    • (2008) Nature , vol.454 , Issue.7201 , pp. 183-187
    • Park, J.H.1    Scheerer, P.2    Hofmann, K.P.3    Choe, H.-W.4    Ernst, O.P.5
  • 74
    • 85027927015 scopus 로고    scopus 로고
    • Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists
    • Wu B, Chien EY, Mol CD, Fenalti G, Liu W, Katritch V, et al. Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists. Science 2010;330:1066-71.
    • (2010) Science , vol.330 , pp. 1066-1071
    • Wu, B.1    Chien, E.Y.2    Mol, C.D.3    Fenalti, G.4    Liu, W.5    Katritch, V.6
  • 75
    • 78449305788 scopus 로고    scopus 로고
    • Structure of the human dopamine D3 receptor in complex with a D2/D3 selective antagonist
    • Chien EY, Liu W, Zhao Q, Katritch V, Han GW, Hanson MA, et al. Structure of the human dopamine D3 receptor in complex with a D2/D3 selective antagonist. Science 2010;330:1091-5.
    • (2010) Science , vol.330 , pp. 1091-1095
    • Chien, E.Y.1    Liu, W.2    Zhao, Q.3    Katritch, V.4    Han, G.W.5    Hanson, M.A.6
  • 76
    • 74049158987 scopus 로고    scopus 로고
    • Design of phosphodiesterase 4D (PDE4D) allosteric modulators for enhancing cognition with improved safety
    • Burgin AB, Magnusson OT, Singh J, Witte P, Staker BL, Bjornsson JM, et al. Design of phosphodiesterase 4D (PDE4D) allosteric modulators for enhancing cognition with improved safety. Nat Biotechnol 2010;28:63-70.
    • (2010) Nat Biotechnol , vol.28 , pp. 63-70
    • Burgin, A.B.1    Magnusson, O.T.2    Singh, J.3    Witte, P.4    Staker, B.L.5    Bjornsson, J.M.6
  • 78
    • 0023214801 scopus 로고
    • 2-adrenergic receptors
    • Howard MJ, Hughes RJ, Motulsky HJ, Mullen MD, Insel PA. Interactions of amiloride with alpha- and beta-adrenergic receptors: amiloride reveals an allosteric site on alpha 2-adrenergic receptors. Mol Pharmacol 1987;32: 53-8. (Pubitemid 17112315)
    • (1987) Molecular Pharmacology , vol.32 , Issue.1 , pp. 53-58
    • Howard, M.J.1    Hughes, R.J.2    Motulsky, H.J.3
  • 79
    • 0032705772 scopus 로고    scopus 로고
    • Binding, partial agonism, and potentiation of alpha(1)-adrenergic receptor function by benzodiazepines: A potential site of allosteric modulation
    • Waugh DJ, Gaivin RJ, Damron DS, Murray PA, Perez DM. Binding, partial agonism, and potentiation of alpha(1)-adrenergic receptor function by benzodiazepines: a potential site of allosteric modulation. J Pharmacol Exp Ther 1999;291:1164-71.
    • (1999) J Pharmacol Exp Ther , vol.291 , pp. 1164-1171
    • Waugh, D.J.1    Gaivin, R.J.2    Damron, D.S.3    Murray, P.A.4    Perez, D.M.5
  • 81
    • 0036006695 scopus 로고    scopus 로고
    • Allosteric modulation of beta2-adrenergic receptor by Zn(2+)
    • Swaminath G, Steenhuis J, Kobilka B, Lee TW. Allosteric modulation of beta2-adrenergic receptor by Zn(2+). Mol Pharmacol 2002;61:65-72.
    • (2002) Mol Pharmacol , vol.61 , pp. 65-72
    • Swaminath, G.1    Steenhuis, J.2    Kobilka, B.3    Lee, T.W.4
  • 84
    • 0034714211 scopus 로고    scopus 로고
    • A small molecule antagonist of chemokine receptors CCR1 and CCR3. Potent inhibition of eosinophil function and CCR3-mediated HIV-1 entry
    • Sabroe I, Peck MJ, Van Keulen BJ, Jorritsma A, Simmons G, Clapham PR, et al. A small molecule antagonist of chemokine receptors CCR1 and CCR3. Potent inhibition of eosinophil function and CCR3-mediated HIV-1 entry. J Biol Chem 2000;275:25985-92.
    • (2000) J Biol Chem , vol.275 , pp. 25985-25992
    • Sabroe, I.1    Peck, M.J.2    Van Keulen, B.J.3    Jorritsma, A.4    Simmons, G.5    Clapham, P.R.6
  • 85
    • 48649101575 scopus 로고    scopus 로고
    • Involvement of the second extracellular loop and transmembrane residues of CCR5 in inhibitor binding and HIV-1 fusion: Insights into the mechanism of allosteric inhibition
    • Maeda K, Das D, Yin PD, Tsuchiya K, Ogata-Aoki H, Nakata H, et al. Involvement of the second extracellular loop and transmembrane residues of CCR5 in inhibitor binding and HIV-1 fusion: insights into the mechanism of allosteric inhibition. J Mol Biol 2008;381:956-74.
    • (2008) J Mol Biol , vol.381 , pp. 956-974
    • Maeda, K.1    Das, D.2    Yin, P.D.3    Tsuchiya, K.4    Ogata-Aoki, H.5    Nakata, H.6
  • 86
    • 15744391870 scopus 로고    scopus 로고
    • The CCR5 receptor-based mechanism of action of 873140, a potent allosteric noncompetitive HIV entry inhibitor
    • DOI 10.1124/mol.104.008565
    • Watson C, Jenkinson S, Kazmierski W, Kenakin T. The CCR5 receptor-based mechanism of action of 873140, a potent allosteric noncompetitive HIV entry inhibitor. Mol Pharmacol 2005;67:1268-82. (Pubitemid 40410427)
    • (2005) Molecular Pharmacology , vol.67 , Issue.4 , pp. 1268-1282
    • Watson, C.1    Jenkinson, S.2    Kazmierski, W.3    Kenakin, T.4
  • 87
    • 0030992175 scopus 로고    scopus 로고
    • 2 dopamine receptors
    • Schetz JA, Sibley DR. Zinc allosterically modulates antagonist binding to cloned D1 and D2 dopamine receptors. J Neurochem 1997;68:1990-7. (Pubitemid 27176135)
    • (1997) Journal of Neurochemistry , vol.68 , Issue.5 , pp. 1990-1997
    • Schetz, J.A.1    Sibley, D.R.2
  • 88
    • 0035144450 scopus 로고    scopus 로고
    • 4 dopamine receptor is coupled to three distinct sites of allosteric modulation
    • Schetz JA, Sibley DR. The binding-site crevice of the D4 dopamine receptor is coupled to three distinct sites of allosteric modulation. J Pharmacol Exp Ther 2001;296:359-63. (Pubitemid 32112461)
    • (2001) Journal of Pharmacology and Experimental Therapeutics , vol.296 , Issue.2 , pp. 359-363
    • Schetz, J.A.1    Sibley, D.R.2
  • 89
    • 19944402189 scopus 로고    scopus 로고
    • Allosteric modulation of dopamine receptors
    • DOI 10.2174/1389557054023260
    • Schetz JA. Allosteric modulation of dopamine receptors. Mini Rev Med Chem 2005;5:555-61. (Pubitemid 40754169)
    • (2005) Mini-Reviews in Medicinal Chemistry , vol.5 , Issue.6 , pp. 555-561
    • Schetz, J.A.1
  • 91
    • 0033922586 scopus 로고    scopus 로고
    • Regulation of human D(1), d(2(long)), d(2(short)), D(3) and D(4) dopamine receptors by amiloride and amiloride analogues
    • Hoare SR, Coldwell MC, Armstrong D, Strange PG. Regulation of human D(1), d(2(long)), d(2(short)), D(3) and D(4) dopamine receptors by amiloride and amiloride analogues. Br J Pharmacol 2000;130:1045-59.
    • (2000) Br J Pharmacol , vol.130 , pp. 1045-1059
    • Hoare, S.R.1    Coldwell, M.C.2    Armstrong, D.3    Strange, P.G.4
  • 92
    • 54449102284 scopus 로고    scopus 로고
    • Allosteric modulators of glycoprotein hormone receptors: Discovery and therapeutic potential
    • Arey BJ. Allosteric modulators of glycoprotein hormone receptors: discovery and therapeutic potential. Endocrine 2008;34:1-10.
    • (2008) Endocrine , vol.34 , pp. 1-10
    • Arey, B.J.1
  • 93
    • 0037375881 scopus 로고    scopus 로고
    • Allosteric drugs acting at muscarinic acetylcholine receptors
    • DOI 10.1023/A:1022888332221
    • Waelbroeck M. Allosteric drugs acting at muscarinic acetylcholine receptors. Neurochem Res 2003;28:419-22. (Pubitemid 36314827)
    • (2003) Neurochemical Research , vol.28 , Issue.3-4 , pp. 419-422
    • Waelbroeck, M.1
  • 94
    • 19944401545 scopus 로고    scopus 로고
    • Allosterism at muscarinic receptors: Ligands and mechanisms
    • DOI 10.2174/1389557054023251
    • Birdsall NJ, Lazareno S. Allosterism at muscarinic receptors: ligands and mechanisms. Mini Rev Med Chem 2005;5:523-43. (Pubitemid 40754167)
    • (2005) Mini-Reviews in Medicinal Chemistry , vol.5 , Issue.6 , pp. 523-543
    • Birdsall, N.J.M.1    Lazareno, S.2
  • 95
    • 61349093537 scopus 로고    scopus 로고
    • Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders
    • Conn PJ, Jones CK, Lindsley CW. Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders. Trends Pharmacol Sci 2009;30:148-55.
    • (2009) Trends Pharmacol Sci , vol.30 , pp. 148-155
    • Conn, P.J.1    Jones, C.K.2    Lindsley, C.W.3
  • 97
    • 45749127879 scopus 로고    scopus 로고
    • Allosteric modulators of class B G-protein-coupled receptors
    • DOI 10.2174/157015907781695928
    • Hoare SR. Allosteric modulators of class B G-protein-coupled receptors. Curr Neuropharmacol 2007;5:168-79. (Pubitemid 351863858)
    • (2007) Current Neuropharmacology , vol.5 , Issue.3 , pp. 168-179
    • Hoare, S.R.J.1
  • 98
    • 11244302448 scopus 로고    scopus 로고
    • Noncompetitive antagonism of BIBN4096BS on CGRP-induced responses in human subcutaneous arteries
    • DOI 10.1038/sj.bjp.0705967
    • Sheykhzade M, Lind H, Edvinsson L. Noncompetitive antagonism of BIBN4096BS on CGRP-induced responses in human subcutaneous arteries. Br J Pharmacol 2004;143:1066-73. (Pubitemid 40065508)
    • (2004) British Journal of Pharmacology , vol.143 , Issue.8 , pp. 1066-1073
    • Sheykhzade, M.1    Lind, H.2    Edvinsson, L.3
  • 99
    • 31144473816 scopus 로고    scopus 로고
    • Pharmacological and clinical properties of calcimimetics: Calcium receptor activators that afford an innovative approach to controlling hyperparathyroidism
    • DOI 10.1016/j.pharmthera.2005.06.019, PII S016372580500152X
    • Nagano N. Pharmacological and clinical properties of calcimimetics: calcium receptor activators that afford an innovative approach to controlling hyperparathyroidism. Pharmacol Ther 2006;109:339-65. (Pubitemid 43132817)
    • (2006) Pharmacology and Therapeutics , vol.109 , Issue.3 , pp. 339-365
    • Nagano, N.1
  • 100
    • 13844275284 scopus 로고    scopus 로고
    • B receptors by CGP7930 and GS39783: Effects on affinities and efficacies of orthosteric ligands with distinct intrinsic properties
    • DOI 10.1016/j.neuropharm.2004.10.013
    • Urwyler S, Gjoni T, Koljatic J, Dupuis DS. Mechanisms of allosteric modulation at GABAB receptors by CGP7930 and GS39783: effects on affinities and efficacies of orthosteric ligands with distinct intrinsic properties. Neuropharmacology 2005;48:343-53. (Pubitemid 40249997)
    • (2005) Neuropharmacology , vol.48 , Issue.3 , pp. 343-353
    • Urwyler, S.1    Gjoni, T.2    Koljatic, J.3    Dupuis, D.S.4
  • 101
    • 0034760504 scopus 로고    scopus 로고
    • b receptors by 2,6-Di-tert-butyl-4-(3-hydroxy- 2,2-dimethyl-propyl)-phenol (CGP7930) and its aldehyde analog CGP13501
    • Urwyler S, Mosbacher J, Lingenhoehl K, Heid J, Hofstetter K, Froestl W, et al. Positive allosteric modulation of native and recombinant gamma-aminobutyric acid(B) receptors by 2,6-Di-tert-butyl-4-(3-hydroxy-2,2- dimethyl-propyl)-phenol (CGP7930) and its aldehyde analog CGP13501. Mol Pharmacol 2001;60:963-71. (Pubitemid 33027431)
    • (2001) Molecular Pharmacology , vol.60 , Issue.5 , pp. 963-971
    • Urwyler, S.1    Mosbacher, J.2    Lingenhoehl, K.3    Heid, J.4    Hofstetter, K.5    Froestl, W.6    Bettler, B.7    Kaupmann, K.8
  • 102
    • 8744227147 scopus 로고    scopus 로고
    • Allosteric modulators of metabotropic glutamate receptors: Lessons learnt from mGlu1, mGlu2 and mGlu5 potentiators and antagonists
    • DOI 10.1042/BST0320881
    • Johnson MP, Nisenbaum ES, Large TH, Emkey R, Baez M, Kingston AE. Allosteric modulators of metabotropic glutamate receptors: lessons learnt from mGlu1, mGlu2 and mGlu5 potentiators and antagonists. Biochem Soc Trans 2004;32:881-7. (Pubitemid 39524404)
    • (2004) Biochemical Society Transactions , vol.32 , Issue.5 , pp. 881-887
    • Johnson, M.P.1    Nisenbaum, E.S.2    Large, T.H.3    Emkey, R.4    Baez, M.5    Kingston, A.E.6
  • 103
    • 30844432624 scopus 로고    scopus 로고
    • Glutamate-based therapeutic approaches: Allosteric modulators of metabotropic glutamate receptors
    • DOI 10.1016/j.coph.2005.09.006, PII S1471489205001839
    • Marino MJ, Conn PJ. Glutamate-based therapeutic approaches: allosteric modulators of metabotropic glutamate receptors. Curr Opin Pharmacol 2006;6:98-102. (Pubitemid 43103825)
    • (2006) Current Opinion in Pharmacology , vol.6 , Issue.1 SPEC. ISS , pp. 98-102
    • Marino, M.J.1    Conn, P.J.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.