메뉴 건너뛰기




Volumn 10, Issue 7, 2015, Pages 763-780

Quantitative analysis of receptor allosterism and its implication for drug discovery

Author keywords

Agonism; Allosteric two state model; Bitopic or dualsteric agonist; Full agonist; G protein couple receptor; Global curve fitting; Monte Carlo simulation; Negative allosteric modulators; Operational model; Orthosterism; Partial agonist; Positive allosteric modulator; Receptor allosterism; Silent allosteric modulator; supremacy

Indexed keywords

G PROTEIN COUPLED RECEPTOR; LIGAND;

EID: 84932115371     PISSN: 17460441     EISSN: 1746045X     Source Type: Journal    
DOI: 10.1517/17460441.2015.1041498     Document Type: Review
Times cited : (17)

References (72)
  • 1
    • 0036453601 scopus 로고    scopus 로고
    • GPCR drug discovery through the exploitation of allosteric drug binding sites
    • Rees S, Morrow D, Kenakin T. GPCR drug discovery through the exploitation of allosteric drug binding sites. Receptors Channels 2002;8(5-6): 261-8
    • (2002) Receptors Channels , vol.8 , Issue.5-6 , pp. 261-268
    • Rees, S.1    Morrow, D.2    Kenakin, T.3
  • 2
    • 33747754105 scopus 로고    scopus 로고
    • Comprehensive repertoire and phylogenetic analysis of the G protein-coupled receptors in human and mouse
    • Bjarnadottir TK, Gloriam DE, Hellstrand SH, et al. Comprehensive repertoire and phylogenetic analysis of the G protein-coupled receptors in human and mouse. Genomics 2006;88(3):263-73
    • (2006) Genomics , vol.88 , Issue.3 , pp. 263-273
    • Bjarnadottir, T.K.1    Gloriam, D.E.2    Hellstrand, S.H.3
  • 4
    • 84903818726 scopus 로고    scopus 로고
    • Muscarinic acetylcholine receptors: Novel opportunities for drug development
    • Kruse AC, Kobilka BK, Gautam D, et al. Muscarinic acetylcholine receptors: novel opportunities for drug development. Nat Rev 2014;13(7):549-60
    • (2014) Nat Rev , vol.13 , Issue.7 , pp. 549-560
    • Kruse, A.C.1    Kobilka, B.K.2    Gautam, D.3
  • 5
    • 84893980520 scopus 로고    scopus 로고
    • The role of protein dynamics in GPCR function: Insights from the beta2AR and rhodopsin
    • Manglik A, Kobilka B. The role of protein dynamics in GPCR function: insights from the beta2AR and rhodopsin. Cur Opin Cell Biol 2014;27:136-43
    • (2014) Cur Opin Cell Biol , vol.27 , pp. 136-143
    • Manglik, A.1    Kobilka, B.2
  • 6
    • 84893642127 scopus 로고    scopus 로고
    • G protein-coupled receptor oligomerization revisited: Functional and pharmacological perspectives
    • Ferre S, Casado V, Devi LA, et al. G protein-coupled receptor oligomerization revisited: functional and pharmacological perspectives. Pharmacol Rev 2014;66(2):413-34
    • (2014) Pharmacol Rev , vol.66 , Issue.2 , pp. 413-434
    • Ferre, S.1    Casado, V.2    Devi, L.A.3
  • 7
    • 84890157678 scopus 로고    scopus 로고
    • Role of beta-arrestins and arrestin domaincontaining proteins in G protein-coupled receptor trafficking
    • Kang DS, Tian X, Benovic JL. Role of beta-arrestins and arrestin domaincontaining proteins in G protein-coupled receptor trafficking. Cur Opin Cell Biol 2014;27:63-71
    • (2014) Cur Opin Cell Biol , vol.27 , pp. 63-71
    • Kang, D.S.1    Tian, X.2    Benovic, J.L.3
  • 8
    • 84892367339 scopus 로고    scopus 로고
    • Defining and characterizing drug/compound function
    • Kenakin T, Williams M. Defining and characterizing drug/compound function. Biochem Pharmacol 2014;87(1):40-63
    • (2014) Biochem Pharmacol , vol.87 , Issue.1 , pp. 40-63
    • Kenakin, T.1    Williams, M.2
  • 9
    • 0001169515 scopus 로고
    • Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins
    • Costa T, Herz A. Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins. Proc Natl Acad Sci USA 1989;86(19):7321-5
    • (1989) Proc Natl Acad Sci USA , vol.86 , Issue.19 , pp. 7321-7325
    • Costa, T.1    Herz, A.2
  • 10
    • 0347627709 scopus 로고    scopus 로고
    • Constitutive activity and inverse agonists of G protein-coupled receptors: A current perspective
    • Milligan G. Constitutive activity and inverse agonists of G protein-coupled receptors: a current perspective. Mol Pharmacol 2003;64(6):1271-6
    • (2003) Mol Pharmacol , vol.64 , Issue.6 , pp. 1271-1276
    • Milligan, G.1
  • 11
    • 84871806221 scopus 로고    scopus 로고
    • Bridging the gap: Bitopic ligands of G-protein-coupled receptors
    • Lane JR, Sexton PM, Christopoulos A. Bridging the gap: bitopic ligands of G-protein-coupled receptors. Trends Pharmacol Sci 2013;34(1):59-66
    • (2013) Trends Pharmacol Sci , vol.34 , Issue.1 , pp. 59-66
    • Lane, J.R.1    Sexton, P.M.2    Christopoulos, A.3
  • 12
    • 84871980480 scopus 로고    scopus 로고
    • Molecular alliance-from orthosteric and allosteric ligands to dualsteric/bitopic agonists at G protein coupled receptors
    • Mohr K, Schmitz J, Schrage R, et al. Molecular alliance-from orthosteric and allosteric ligands to dualsteric/bitopic agonists at G protein coupled receptors. Angew Chem Int Ed Engl 2013;52(2):508-16
    • (2013) Angew Chem Int Ed Engl , vol.52 , Issue.2 , pp. 508-516
    • Mohr, K.1    Schmitz, J.2    Schrage, R.3
  • 13
    • 84855879360 scopus 로고    scopus 로고
    • The best of both worlds? Bitopic orthosteric/allosteric ligands of g proteincoupled receptors
    • Valant C, Robert Lane J, Sexton PM, et al. The best of both worlds? Bitopic orthosteric/allosteric ligands of g proteincoupled receptors. Annu Rev Pharmacol Toxicol 2012;52:153-78
    • (2012) Annu Rev Pharmacol Toxicol , vol.52 , pp. 153-178
    • Valant, C.1    Robert Lane, J.2    Sexton, P.M.3
  • 14
    • 84904301809 scopus 로고    scopus 로고
    • International Union of Basic and Clinical Pharmacology. XC. Multisite pharmacology: Recommendations for the nomenclature of receptor allosterism and allosteric ligands
    • Christopoulos A, Changeux JP, Catterall WA, et al. International Union of Basic and Clinical Pharmacology. XC. multisite pharmacology: recommendations for the nomenclature of receptor allosterism and allosteric ligands. Pharmacol Rev 2014;66(4):918-47
    • (2014) Pharmacol Rev , vol.66 , Issue.4 , pp. 918-947
    • Christopoulos, A.1    Changeux, J.P.2    Catterall, W.A.3
  • 15
    • 0036258990 scopus 로고    scopus 로고
    • G proteincoupled receptor allosterism and complexing
    • Christopoulos A, Kenakin T. G proteincoupled receptor allosterism and complexing. Pharmacol Rev 2002;54(2):323-74
    • (2002) Pharmacol Rev , vol.54 , Issue.2 , pp. 323-374
    • Christopoulos, A.1    Kenakin, T.2
  • 16
    • 73649152457 scopus 로고
    • Allosteric proteins and cellular control systems
    • Monod J, Changeux JP, Jacob F. Allosteric proteins and cellular control systems. J Mol Biol 1963;6:306-29
    • (1963) J Mol Biol , vol.6 , pp. 306-329
    • Monod, J.1    Changeux, J.P.2    Jacob, F.3
  • 17
    • 73049167504 scopus 로고
    • General conclusions: Teleonomic mechanisms in cellular metabolism, growth and differentiation
    • Monod J, Jacob F. General conclusions: teleonomic mechanisms in cellular metabolism, growth and differentiation. Cold Spring Harbor Symp Quant Biol 1961;26:389-401
    • (1961) Cold Spring Harbor Symp Quant Biol , vol.26 , pp. 389-401
    • Monod, J.1    Jacob, F.2
  • 18
    • 78651189765 scopus 로고
    • On the nature of allosteric transitions: A plausible model
    • Monod J, Wyman J, Changeux JP. On the Nature of Allosteric Transitions: a Plausible Model. J Mol Biol 1965;12:88-118
    • (1965) J Mol Biol , vol.12 , pp. 88-118
    • Monod, J.1    Wyman, J.2    Changeux, J.P.3
  • 19
    • 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
  • 20
    • 84929941469 scopus 로고    scopus 로고
    • Endogenous allosteric modulators of G protein-coupled receptors
    • van der Westhuizen ET, Valant C, Sexton PM, et al. Endogenous allosteric modulators of G protein-coupled receptors. J Pharmacol Exp Ther 2015;353(2):246-60
    • (2015) J Pharmacol Exp Ther , vol.353 , Issue.2 , pp. 246-260
    • Van Der Westhuizen, E.T.1    Valant, C.2    Sexton, P.M.3
  • 21
    • 84879514548 scopus 로고    scopus 로고
    • Discovery of positive allosteric modulators and silent allosteric modulators of the mu-opioid receptor
    • Burford NT, Clark MJ, Wehrman TS, et al. Discovery of positive allosteric modulators and silent allosteric modulators of the mu-opioid receptor. Proc Natl Acad Sci USA 2013;110(26):10830-5
    • (2013) Proc Natl Acad Sci USA , vol.110 , Issue.26 , pp. 10830-10835
    • Burford, N.T.1    Clark, M.J.2    Wehrman, T.S.3
  • 22
    • 78650379605 scopus 로고    scopus 로고
    • Chemical switch of a metabotropic glutamate receptor 2 silent allosteric modulator into dual metabotropic glutamate receptor 2/3 negative/positive allosteric modulators
    • Schann S, Mayer S, Franchet C, et al. Chemical switch of a metabotropic glutamate receptor 2 silent allosteric modulator into dual metabotropic glutamate receptor 2/3 negative/positive allosteric modulators. J Med Chem 2010;53(24):8775-9
    • (2010) J Med Chem , vol.53 , Issue.24 , pp. 8775-8779
    • Schann, S.1    Mayer, S.2    Franchet, C.3
  • 23
    • 70449143838 scopus 로고
    • Interaction at end-plate receptors between different choline derivatives
    • Del Castillo J, Katz B. Interaction at end-plate receptors between different choline derivatives. Proc R Soc Lond B Biol Sci 1957;146(924):369-81
    • (1957) Proc R Soc Lond B Biol Sci , vol.146 , Issue.924 , pp. 369-381
    • Del Castillo, J.1    Katz, B.2
  • 24
    • 0033669603 scopus 로고    scopus 로고
    • Modeling the functional effects of allosteric modulators at pharmacological receptors: An extension of the two-state model of receptor activation
    • Hall DA. Modeling the functional effects of allosteric modulators at pharmacological receptors: an extension of the two-state model of receptor activation. Mol Pharmacol 2000;58(6):1412-23
    • (2000) Mol Pharmacol , vol.58 , Issue.6 , pp. 1412-1423
    • Hall, D.A.1
  • 25
    • 84873906998 scopus 로고    scopus 로고
    • Application of receptor theory to allosteric modulation of receptors
    • Hall DA. Application of receptor theory to allosteric modulation of receptors. Prog Mol Biol Transl Sci 2013;115:217-90
    • (2013) Prog Mol Biol Transl Sci , vol.115 , pp. 217-290
    • Hall, D.A.1
  • 26
    • 0021058380 scopus 로고
    • Operational models of pharmacological agonism
    • Black JW, Leff P. Operational models of pharmacological agonism. Proc R Soc Lond B Biol Sci 1983;220(1219):141-62
    • (1983) Proc R Soc Lond B Biol Sci , vol.220 , Issue.1219 , pp. 141-162
    • Black, J.W.1    Leff, P.2
  • 27
    • 0021990306 scopus 로고
    • An operational model of pharmacological agonism: The effect of E/[A] curve shape on agonist dissociation constant estimation
    • Black JW, Leff P, Shankley NP, et al. An operational model of pharmacological agonism: the effect of E/[A] curve shape on agonist dissociation constant estimation. Br J Pharmacol 1985;84(2):561-71
    • (1985) Br J Pharmacol , vol.84 , Issue.2 , pp. 561-571
    • Black, J.W.1    Leff, P.2    Shankley, N.P.3
  • 28
    • 27144491979 scopus 로고    scopus 로고
    • Analysis of allosterism in functional assays
    • Ehlert FJ. Analysis of allosterism in functional assays. J Pharmacol Exp Ther 2005;315(2):740-54
    • (2005) J Pharmacol Exp Ther , vol.315 , Issue.2 , pp. 740-754
    • Ehlert, F.J.1
  • 29
    • 27844519281 scopus 로고    scopus 로고
    • New concepts in drug discovery: Collateral efficacy and permissive antagonism
    • Kenakin T. New concepts in drug discovery: collateral efficacy and permissive antagonism. Nat Rev 2005;4(11):919-27
    • (2005) Nat Rev , vol.4 , Issue.11 , pp. 919-927
    • Kenakin, T.1
  • 30
    • 34447632041 scopus 로고    scopus 로고
    • Allosteric GPCR modulators: Taking advantage of permissive receptor pharmacology
    • Leach K, Sexton PM, Christopoulos A. Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology. Trends Pharmacol Sci 2007;28(8):382-9
    • (2007) Trends Pharmacol Sci , vol.28 , Issue.8 , pp. 382-389
    • Leach, K.1    Sexton, P.M.2    Christopoulos, A.3
  • 31
    • 24044539957 scopus 로고    scopus 로고
    • Allosteric modulation of the cannabinoid CB1 receptor
    • Price MR, Baillie GL, Thomas A, et al. Allosteric modulation of the cannabinoid CB1 receptor. Mol Pharmacol 2005;68(5):1484-95
    • (2005) Mol Pharmacol , vol.68 , Issue.5 , pp. 1484-1495
    • Price, M.R.1    Baillie, G.L.2    Thomas, A.3
  • 32
    • 84863224949 scopus 로고    scopus 로고
    • Development of operational models of receptor activation including constitutive receptor activity and their use to determine the efficacy of the chemokine CCL17 at the CC chemokine receptor CCR4
    • Slack RJ, Hall DA. Development of operational models of receptor activation including constitutive receptor activity and their use to determine the efficacy of the chemokine CCL17 at the CC chemokine receptor CCR4. Br J Pharmacol 2012;166(6):1774-92
    • (2012) Br J Pharmacol , vol.166 , Issue.6 , pp. 1774-1792
    • Slack, R.J.1    Hall, D.A.2
  • 33
    • 0010673662 scopus 로고
    • A modification of receptor theory
    • Stephenson RP. A modification of receptor theory. Br J Pharmacol Chemother 1956;11(4):379-93
    • (1956) Br J Pharmacol Chemother , vol.11 , Issue.4 , pp. 379-393
    • Stephenson, R.P.1
  • 34
    • 0002134457 scopus 로고
    • Affinity, efficacy and receptor classification: Is the classical theory still useful?
    • Black JW, Jenkinson DH, Gerskowitch VP, Alan R, editors, Liss Inc; New York
    • Colquhoun D. Affinity, efficacy and receptor classification: is the classical theory still useful? In: Black JW, Jenkinson DH, Gerskowitch VP, Alan R, editors. Perspectives on hormone receptor classification. Liss Inc; New York: 1987. p. 103-14
    • (1987) Perspectives on Hormone Receptor Classification , pp. 103-114
    • Colquhoun, D.1
  • 35
    • 0032199006 scopus 로고    scopus 로고
    • Binding, gating, affinity and efficacy: The interpretation of structure-activity relationships for agonists and of the effects of mutating receptors
    • 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 1998;125(5):924-47
    • (1998) Br J Pharmacol , vol.125 , Issue.5 , pp. 924-947
    • Colquhoun, D.1
  • 36
    • 84879339183 scopus 로고    scopus 로고
    • Mechanistic analysis of the function of agonists and allosteric modulators: Reconciling two-state and operational models
    • Roche D, Gil D, Giraldo J. Mechanistic analysis of the function of agonists and allosteric modulators: reconciling two-state and operational models. Br J Pharmacol 2013;169(6): 1189-202
    • (2013) Br J Pharmacol , vol.169 , Issue.6 , pp. 1189-1202
    • Roche, D.1    Gil, D.2    Giraldo, J.3
  • 37
    • 84895745240 scopus 로고    scopus 로고
    • A unified view of "how allostery works"
    • Tsai CJ, Nussinov R. A unified view of "how allostery works". PLoS Comput Biol 2014;10(2): e1003394
    • (2014) PLoS Comput Biol , vol.10 , Issue.2 , pp. e1003394
    • Tsai, C.J.1    Nussinov, R.2
  • 38
    • 30444460582 scopus 로고    scopus 로고
    • The quantitative analysis of drug-receptor interactions: A short history
    • Colquhoun D. The quantitative analysis of drug-receptor interactions: a short history. Trends Pharmacol Sci 2006;27(3):149-57
    • (2006) Trends Pharmacol Sci , vol.27 , Issue.3 , pp. 149-157
    • Colquhoun, D.1
  • 40
    • 78651175536 scopus 로고
    • The uptake of atropine and related drugs by intestinal smooth muscle of the Guinea-pig in relation to acetylcholine receptors
    • Paton WD, Rang HP. The Uptake of Atropine and Related Drugs by Intestinal Smooth Muscle of the Guinea-Pig in Relation to Acetylcholine Receptors. Proc R Soc Lond B Biol Sci 1965;163:1-44
    • (1965) Proc R Soc Lond B Biol Sci , vol.163 , pp. 1-44
    • Paton, W.D.1    Rang, H.P.2
  • 41
    • 10044248233 scopus 로고    scopus 로고
    • Single-channel behavior of heteromeric alpha1beta glycine receptors: An attempt to detect a conformational change before the channel opens
    • Burzomato V, Beato M, Groot-Kormelink PJ, et al. Single-channel behavior of heteromeric alpha1beta glycine receptors: an attempt to detect a conformational change before the channel opens. J Neurosci 2004;24(48):10924-40
    • (2004) J Neurosci , vol.24 , Issue.48 , pp. 10924-10940
    • Burzomato, V.1    Beato, M.2    Groot-Kormelink, P.J.3
  • 42
    • 84875729319 scopus 로고    scopus 로고
    • Multiple active receptor conformation, agonist efficacy and maximum effect of the system: The conformation-based operational model of agonism
    • Roche D, Gil D, Giraldo J. Multiple active receptor conformation, agonist efficacy and maximum effect of the system: the conformation-based operational model of agonism. Drug Discov Today 2013;18(7-8):365-71
    • (2013) Drug Discov Today , vol.18 , Issue.7-8 , pp. 365-371
    • Roche, D.1    Gil, D.2    Giraldo, J.3
  • 43
    • 78149496159 scopus 로고    scopus 로고
    • Allosteric modulation of G proteincoupled receptors: A pharmacological perspective
    • Keov P, Sexton PM, Christopoulos A. Allosteric modulation of G proteincoupled receptors: a pharmacological perspective. Neuropharmacology 2011;60(1):24-35
    • (2011) Neuropharmacology , vol.60 , Issue.1 , pp. 24-35
    • Keov, P.1    Sexton, P.M.2    Christopoulos, A.3
  • 44
    • 76749144987 scopus 로고    scopus 로고
    • Molecular mechanisms of action and in vivo validation of an M4 muscarinic acetylcholine receptor allosteric modulator with potential antipsychotic properties
    • Leach K, Loiacono RE, Felder CC, et al. Molecular mechanisms of action and in vivo validation of an M4 muscarinic acetylcholine receptor allosteric modulator with potential antipsychotic properties. Neuropsychopharmacology 2010;35(4):855-69
    • (2010) Neuropsychopharmacology , vol.35 , Issue.4 , pp. 855-869
    • Leach, K.1    Loiacono, R.E.2    Felder, C.C.3
  • 45
    • 84874232168 scopus 로고    scopus 로고
    • The apelin receptor inhibits the angiotensin II type 1 receptor via allosteric trans-inhibition
    • Siddiquee K, Hampton J, McAnally D, et al. The apelin receptor inhibits the angiotensin II type 1 receptor via allosteric trans-inhibition. Br J Pharmacol 2012;168(5):1104-17
    • (2012) Br J Pharmacol , vol.168 , Issue.5 , pp. 1104-1117
    • Siddiquee, K.1    Hampton, J.2    McAnally, D.3
  • 46
    • 79959309348 scopus 로고    scopus 로고
    • Extracellular loop 2 of the free fatty acid receptor 2 mediates allosterism of a phenylacetamide ago-allosteric modulator
    • Smith NJ, Ward RJ, Stoddart LA, et al. Extracellular loop 2 of the free fatty acid receptor 2 mediates allosterism of a phenylacetamide ago-allosteric modulator. Mol Pharmacol 2011;80(1):163-73
    • (2011) Mol Pharmacol , vol.80 , Issue.1 , pp. 163-173
    • Smith, N.J.1    Ward, R.J.2    Stoddart, L.A.3
  • 47
    • 84891438084 scopus 로고    scopus 로고
    • Selective actions of novel allosteric modulators reveal functional heteromers of metabotropic glutamate receptors in the CNS
    • Yin S, Noetzel MJ, Johnson KA, et al. Selective actions of novel allosteric modulators reveal functional heteromers of metabotropic glutamate receptors in the CNS. J Neurosci 2014;34(1):79-94
    • (2014) J Neurosci , vol.34 , Issue.1 , pp. 79-94
    • Yin, S.1    Noetzel, M.J.2    Johnson, K.A.3
  • 48
    • 84879086561 scopus 로고    scopus 로고
    • Allosteric controls of nuclear receptor function in the regulation of transcription
    • Billas I, Moras D. Allosteric controls of nuclear receptor function in the regulation of transcription. J Mol Biol 2013;425(13):2317-29
    • (2013) J Mol Biol , vol.425 , Issue.13 , pp. 2317-2329
    • Billas, I.1    Moras, D.2
  • 49
    • 84858775788 scopus 로고    scopus 로고
    • A simple method for quantifying functional selectivity and agonist bias
    • Kenakin T, Watson C, Muniz-Medina V, et al. A simple method for quantifying functional selectivity and agonist bias. ACS Chem Neurosci 2012;3(3):193-203
    • (2012) ACS Chem Neurosci , vol.3 , Issue.3 , pp. 193-203
    • Kenakin, T.1    Watson, C.2    Muniz-Medina, V.3
  • 50
    • 84857497773 scopus 로고    scopus 로고
    • Biased signalling and allosteric machines: New vistas and challenges for drug discovery
    • Kenakin TP. Biased signalling and allosteric machines: new vistas and challenges for drug discovery. Br J Pharmacol 2012;165(6):1659-69
    • (2012) Br J Pharmacol , vol.165 , Issue.6 , pp. 1659-1669
    • Kenakin, T.P.1
  • 51
    • 34447638166 scopus 로고    scopus 로고
    • Allosteric enhancers, allosteric agonists and agoallosteric modulators: Where do they bind and how do they act?
    • Schwartz TW, Holst B. Allosteric enhancers, allosteric agonists and agoallosteric modulators: where do they bind and how do they act? Trends Pharmacol Sci 2007;28(8):366-73
    • (2007) Trends Pharmacol Sci , vol.28 , Issue.8 , pp. 366-373
    • Schwartz, T.W.1    Holst, B.2
  • 52
    • 84862964996 scopus 로고    scopus 로고
    • Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function
    • Noetzel MJ, Rook JM, Vinson PN, et al. Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function. Mol Pharmacol 2011;81(2):120-33
    • (2011) Mol Pharmacol , vol.81 , Issue.2 , pp. 120-133
    • Noetzel, M.J.1    Rook, J.M.2    Vinson, P.N.3
  • 53
    • 77949407879 scopus 로고    scopus 로고
    • Ligand detection in the allosteric world
    • Kenakin T. Ligand detection in the allosteric world. J Biomolec screen 2010;15(2):119-30
    • (2010) J Biomolec Screen , vol.15 , Issue.2 , pp. 119-130
    • Kenakin, T.1
  • 54
    • 84920101808 scopus 로고    scopus 로고
    • Operational models of allosteric modulation: Caution is needed
    • Giraldo J. Operational models of allosteric modulation: caution is needed. Trends Pharmacol Sci 2015;36(1):1-2
    • (2015) Trends Pharmacol Sci , vol.36 , Issue.1 , pp. 1-2
    • Giraldo, J.1
  • 55
    • 0002355204 scopus 로고
    • The use of betahaloalkylamines in the differentiation of receptors and in the determination of dissociation constants of receptor-agonist complexes
    • Harper NJ, editor, Academic Press; New York
    • Furchgott RF. The use of betahaloalkylamines in the differentiation of receptors and in the determination of dissociation constants of receptor-agonist complexes. In: Harper NJ, editor. Advances in Drug Research. Academic Press; New York: 1966. p. 21-55
    • (1966) Advances in Drug Research , pp. 21-55
    • Furchgott, R.F.1
  • 56
    • 0021355975 scopus 로고
    • The relative contribution of affinity and efficacy to agonist activity: Organ selectivity of noradrenaline and oxymetazoline with reference to the classification of drug receptors
    • Kenakin TP. The relative contribution of affinity and efficacy to agonist activity: organ selectivity of noradrenaline and oxymetazoline with reference to the classification of drug receptors. Br J Pharmacol 1984;81(1):131-41
    • (1984) Br J Pharmacol , vol.81 , Issue.1 , pp. 131-141
    • Kenakin, T.P.1
  • 57
    • 84857482783 scopus 로고    scopus 로고
    • Constitutive formation of an RXFP1-signalosome: A novel paradigm in GPCR function and regulation
    • Halls ML. Constitutive formation of an RXFP1-signalosome: a novel paradigm in GPCR function and regulation. Br J Pharmacol 2012;165(6):1644-58
    • (2012) Br J Pharmacol , vol.165 , Issue.6 , pp. 1644-1658
    • Halls, M.L.1
  • 58
    • 0036597671 scopus 로고    scopus 로고
    • Constitutive activity of G-protein coupled receptors: Emphasis on serotonin receptors
    • Teitler M, Herrick-Davis K, Purohit A. Constitutive activity of G-protein coupled receptors: emphasis on serotonin receptors. Curr Top Med Chem 2002;2(6):529-38
    • (2002) Curr Top Med Chem , vol.2 , Issue.6 , pp. 529-538
    • Teitler, M.1    Herrick-Davis, K.2    Purohit, A.3
  • 59
    • 77950197835 scopus 로고    scopus 로고
    • The dynamics of drugtarget interactions: Drug-target residence time and its impact on efficacy and safety
    • Copeland RA. The dynamics of drugtarget interactions: drug-target residence time and its impact on efficacy and safety. Expert Opin Drug Discov 2010;5(4):305-10
    • (2010) Expert Opin Drug Discov , vol.5 , Issue.4 , pp. 305-310
    • Copeland, R.A.1
  • 60
    • 84901827515 scopus 로고    scopus 로고
    • Drug-target residence time-A case for G protein-coupled receptors
    • Guo D, Hillger JM, AP IJ, et al. Drug-target residence time-a case for G protein-coupled receptors. Med Res Rev 2014;34(4):856-92
    • (2014) Med Res Rev , vol.34 , Issue.4 , pp. 856-892
    • Guo, D.1    Hillger, J.M.2    Ij, A.P.3
  • 61
    • 84903211679 scopus 로고    scopus 로고
    • A study of the molecular mechanism of binding kinetics and long residence times of human CCR5 receptor small molecule allosteric ligands
    • Swinney DC, Beavis P, Chuang KT, et al. A study of the molecular mechanism of binding kinetics and long residence times of human CCR5 receptor small molecule allosteric ligands. Br J Pharmacol 2014;171(14): 3364-75
    • (2014) Br J Pharmacol , vol.171 , Issue.14 , pp. 3364-3375
    • Swinney, D.C.1    Beavis, P.2    Chuang, K.T.3
  • 63
    • 84907692805 scopus 로고    scopus 로고
    • Kinetic analysis of antagonistoccupied adenosine-A3 receptors within membrane microdomains of individual cells provides evidence of receptor dimerization and allosterism
    • Corriden R, Kilpatrick LE, Kellam B, et al. Kinetic analysis of antagonistoccupied adenosine-A3 receptors within membrane microdomains of individual cells provides evidence of receptor dimerization and allosterism. Faseb J 2014;28(10):4211-22
    • (2014) Faseb J , vol.28 , Issue.10 , pp. 4211-4222
    • Corriden, R.1    Kilpatrick, L.E.2    Kellam, B.3
  • 64
    • 84895161057 scopus 로고    scopus 로고
    • Allosteric interactions at adenosine A(1) and A(3) receptors: New insights into the role of small molecules and receptor dimerization
    • Hill SJ, May LT, Kellam B, et al. Allosteric interactions at adenosine A(1) and A(3) receptors: new insights into the role of small molecules and receptor dimerization. Br J Pharmacol 2014;171(5):1102-13
    • (2014) Br J Pharmacol , vol.171 , Issue.5 , pp. 1102-1113
    • Hill, S.J.1    May, L.T.2    Kellam, B.3
  • 65
    • 80053906571 scopus 로고    scopus 로고
    • Allosteric interactions across native adenosine-A3 receptor homodimers: Quantification using single-cell ligandbinding kinetics
    • May LT, Bridge LJ, Stoddart LA, et al. Allosteric interactions across native adenosine-A3 receptor homodimers: quantification using single-cell ligandbinding kinetics. Faseb J 2011;25(10):3465-76
    • (2011) Faseb J , vol.25 , Issue.10 , pp. 3465-3476
    • May, L.T.1    Bridge, L.J.2    Stoddart, L.A.3
  • 66
    • 84915747589 scopus 로고    scopus 로고
    • Kinetics of the early events of GPCR signalling
    • Adamson RJ, Watts A. Kinetics of the early events of GPCR signalling. FEBS Lett 2014;588(24):4701-7
    • (2014) FEBS Lett , vol.588 , Issue.24 , pp. 4701-4707
    • Adamson, R.J.1    Watts, A.2
  • 67
    • 84922438756 scopus 로고    scopus 로고
    • Interhelical interaction and receptor phosphorylation regulate the activation kinetics of different human beta1-adrenoceptor variants
    • Ahles A, Rodewald F, Rochais F, et al. Interhelical interaction and receptor phosphorylation regulate the activation kinetics of different human beta1-adrenoceptor variants. J Biol Chem 2015;290(3):1760-9
    • (2015) J Biol Chem , vol.290 , Issue.3 , pp. 1760-1769
    • Ahles, A.1    Rodewald, F.2    Rochais, F.3
  • 68
    • 78649837764 scopus 로고    scopus 로고
    • Kinetics of G-protein-coupled receptor endosomal trafficking pathways revealed by single quantum dots
    • Fichter KM, Flajolet M, Greengard P, et al. Kinetics of G-protein-coupled receptor endosomal trafficking pathways revealed by single quantum dots. Proc Natl Acad Sci USA 2010;107(43):18658-63
    • (2010) Proc Natl Acad Sci USA , vol.107 , Issue.43 , pp. 18658-18663
    • Fichter, K.M.1    Flajolet, M.2    Greengard, P.3
  • 69
    • 77951035803 scopus 로고    scopus 로고
    • Regulators of G-protein signaling accelerate GPCR signaling kinetics and govern sensitivity solely by accelerating GTPase activity
    • Lambert NA, Johnston CA, Cappell SD, et al. Regulators of G-protein signaling accelerate GPCR signaling kinetics and govern sensitivity solely by accelerating GTPase activity. Proc Natl Acad Sci USA 2010;107(15):7066-71
    • (2010) Proc Natl Acad Sci USA , vol.107 , Issue.15 , pp. 7066-7071
    • Lambert, N.A.1    Johnston, C.A.2    Cappell, S.D.3
  • 70
    • 23944505054 scopus 로고    scopus 로고
    • Kinetics of the initial steps of G proteincoupled receptor-mediated cellular signaling revealed by single-molecule imaging
    • Lill Y, Martinez KL, Lill MA, et al. Kinetics of the initial steps of G proteincoupled receptor-mediated cellular signaling revealed by single-molecule imaging. ChemPhysChem 2005;6(8):1633-40
    • (2005) ChemPhysChem , vol.6 , Issue.8 , pp. 1633-1640
    • Lill, Y.1    Martinez, K.L.2    Lill, M.A.3
  • 71
    • 77957068671 scopus 로고    scopus 로고
    • Theme and variations on kinetics of GPCR activation/deactivation
    • Vilardaga JP. Theme and variations on kinetics of GPCR activation/deactivation. J Recept Signal Transduct Res 2010;30(5):304-12
    • (2010) J Recept Signal Transduct Res , vol.30 , Issue.5 , pp. 304-312
    • Vilardaga, J.P.1
  • 72
    • 84873383490 scopus 로고    scopus 로고
    • Kinetics and dynamics in the G protein-coupled receptor signaling cascade
    • Vilardaga JP, Romero G, Feinstein TN, et al. Kinetics and dynamics in the G protein-coupled receptor signaling cascade. Methods Enzymol 2013;522:337-63
    • (2013) Methods Enzymol , vol.522 , pp. 337-363
    • Vilardaga, J.P.1    Romero, G.2    Feinstein, T.N.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.