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Volumn , Issue , 2010, Pages 53-68

Use of the [35S]GTPγS Binding Assay to Determine Ligand Efficacy at G Protein-Coupled Receptors

Author keywords

35S GTP S binding assay determining ligand efficacy at G protein coupled receptors; 35S GTP S binding assay under conditions for GPCRs coupled to Gi o proteins; BSA in assays for preventing ligand loss; Chinese hamster ovary (CHO) cells expressing recombinant GPCR; In vitro systems to measure agonist efficacy; Methods for assessing efficacy for agonists for G protein coupled receptors (GPCRs); Other assays for efficacy at GPCRs; Protocol 3.2 determination of concentration of GDP in 35S GTP S binding assay; Protocol 3.3 data analysis of GDP requirements; Understanding and quantifying drug efficacy

Indexed keywords


EID: 84886326028     PISSN: None     EISSN: None     Source Type: Book    
DOI: 10.1002/9780470749210.ch3     Document Type: Chapter
Times cited : (4)

References (30)
  • 1
    • 22344458106 scopus 로고    scopus 로고
    • The place of partial agonism in psychiatry: recent developments
    • Ohlsen, R.I. and Pilowsky, L.S. (2005) The place of partial agonism in psychiatry: recent developments. J. Psychopharmacol., 19, 408-413.
    • (2005) J. Psychopharmacol. , vol.19 , pp. 408-413
    • Ohlsen, R.I.1    Pilowsky, L.S.2
  • 2
    • 20844434337 scopus 로고    scopus 로고
    • A FlAsH-based FRET approach to determine G protein-coupled receptor activation in living cells
    • Hoffmann, C., Gaietta, G., Bunemann, M. et al. (2005) A FlAsH-based FRET approach to determine G protein-coupled receptor activation in living cells. Nat. Methods, 2, 171-176.
    • (2005) Nat. Methods , vol.2 , pp. 171-176
    • Hoffmann, C.1    Gaietta, G.2    Bunemann, M.3
  • 3
    • 0031595716 scopus 로고    scopus 로고
    • 2(long) dopamine receptors: ligand binding and functional assays
    • 2(long) dopamine receptors: ligand binding and functional assays. Br. J. Pharmacol., 124, 978-984.
    • (1998) Br. J. Pharmacol. , vol.124 , pp. 978-984
    • Gardner, B.1    Strange, P.G.2
  • 4
    • 0030613814 scopus 로고    scopus 로고
    • 2(short) dopamine receptors determined in ligand binding and functional assays
    • 2(short) dopamine receptors determined in ligand binding and functional assays. J. Neurochem., 69, 2589-2598.
    • (1997) J. Neurochem. , vol.69 , pp. 2589-2598
    • Gardner, B.R.1    Hall, D.A.2    Strange, P.G.3
  • 5
    • 0021058380 scopus 로고
    • Operational models of pharmacological agonism
    • Black, J.W. and Leff, P. (1983) Operational models of pharmacological agonism. Proc. R. Soc. Lond. B Biol. Sci., 220, 141-162.
    • (1983) Proc. R. Soc. Lond. B Biol. Sci. , vol.220 , pp. 141-162
    • Black, J.W.1    Leff, P.2
  • 7
    • 34548148009 scopus 로고    scopus 로고
    • Mechanisms underlying agonist efficacy
    • A review on the importance of considering different parameters in efficacy assessment
    • Strange, P.G. (2007) Mechanisms underlying agonist efficacy. Biochem. Soc. Trans., 35, 733-736. A review on the importance of considering different parameters in efficacy assessment.
    • (2007) Biochem. Soc. Trans. , vol.35 , pp. 733-736
    • Strange, P.G.1
  • 8
    • 0242552831 scopus 로고    scopus 로고
    • 35S]GTPγ S binding assay: approaches and applications in pharmacology
    • An overview on the GTPγ S binding technique
    • 35S]GTPγ S binding assay: approaches and applications in pharmacology. Life Sci., 74, 489-508. An overview on the GTPγ S binding technique.
    • (2003) Life Sci. , vol.74 , pp. 489-508
    • Harrison, C.1    Traynor, J.R.2
  • 10
    • 32944470681 scopus 로고    scopus 로고
    • The development of an europium-GTP assay to quantitate chemokine antagonist interactions for CXCR4 and CCR5
    • Labrecque, J., Anastassov, V., Lau, G. et al. (2005) The development of an europium-GTP assay to quantitate chemokine antagonist interactions for CXCR4 and CCR5. Assay Drug Dev. Technol., 3, 637-648.
    • (2005) Assay Drug Dev. Technol. , vol.3 , pp. 637-648
    • Labrecque, J.1    Anastassov, V.2    Lau, G.3
  • 11
    • 71849104860 scopus 로고
    • Protein measurement with the folin phenol reagent
    • Lowry, O., Rosebrough, N., Farr, A. and Randall, R. (1951) Protein measurement with the folin phenol reagent. J. Biol. Chem., 193, 265-275.
    • (1951) J. Biol. Chem. , vol.193 , pp. 265-275
    • Lowry, O.1    Rosebrough, N.2    Farr, A.3    Randall, R.4
  • 15
    • 0021741847 scopus 로고
    • Reconstitution of catecholamine-stimulated binding of guanosine 5'-O-(3-thiotriphosphate) to the stimulatory GTP-binding protein of adenylate cyclase
    • Asano, T., Pedersen, S.E., Scott, C.W. and Ross, E.M. (1984) Reconstitution of catecholamine-stimulated binding of guanosine 5'-O-(3-thiotriphosphate) to the stimulatory GTP-binding protein of adenylate cyclase. Biochemistry, 23, 5460-5467.
    • (1984) Biochemistry , vol.23 , pp. 5460-5467
    • Asano, T.1    Pedersen, S.E.2    Scott, C.W.3    Ross, E.M.4
  • 17
    • 0031017050 scopus 로고    scopus 로고
    • μ-Opioid receptor-stimulated guanosine-5'-O-(μ-thio)-triphosphate binding in rat thalamus and cultured cell lines: signal transduction mechanisms underlying agonist efficacy
    • Selley, D.E., Sim, L.J., Xiao, R. et al. (1997) μ-Opioid receptor-stimulated guanosine-5'-O-(μ-thio)-triphosphate binding in rat thalamus and cultured cell lines: signal transduction mechanisms underlying agonist efficacy. Mol. Pharmacol., 51, 87-96.
    • (1997) Mol. Pharmacol. , vol.51 , pp. 87-96
    • Selley, D.E.1    Sim, L.J.2    Xiao, R.3
  • 18
    • 0032479282 scopus 로고    scopus 로고
    • 35S]GTPγ S binding to rat cerebellar membranes correlates with agonist-induced decreases in GDP affinity
    • 35S]GTPγ S binding to rat cerebellar membranes correlates with agonist-induced decreases in GDP affinity. J. Biol. Chem., 273, 16865-16873.
    • (1998) J. Biol. Chem. , vol.273 , pp. 16865-16873
    • Breivogel, C.S.1    Selley, D.E.2    Childers, S.R.3
  • 19
    • 0027525822 scopus 로고
    • Pharmacological characterization of guanine nucleotide exchange reactions in membranes from CHO cells stably transfected with human muscarinic receptors m1-m4
    • Lazareno, S., Farries, T. and Birdsall, N.J. (1993) Pharmacological characterization of guanine nucleotide exchange reactions in membranes from CHO cells stably transfected with human muscarinic receptors m1-m4. Life Sci., 52, 449-456.
    • (1993) Life Sci. , vol.52 , pp. 449-456
    • Lazareno, S.1    Farries, T.2    Birdsall, N.J.3
  • 20
    • 0036191430 scopus 로고    scopus 로고
    • Pharmacological characterization of the chemokine receptor, CCR5
    • Mueller, A., Mahmoud, N.G., Goedecke, M.C. et al. (2002) Pharmacological characterization of the chemokine receptor, CCR5. Br. J. Pharmacol., 135, 1033-1043.
    • (2002) Br. J. Pharmacol. , vol.135 , pp. 1033-1043
    • Mueller, A.1    Mahmoud, N.G.2    Goedecke, M.C.3
  • 22
    • 33749027768 scopus 로고    scopus 로고
    • 2 dopamine receptor
    • This article shows the importance of assay conditions in assessing ligand efficacy
    • 2 dopamine receptor. Br. J. Pharmacol., 149, 291-299. This article shows the importance of assay conditions in assessing ligand efficacy.
    • (2006) Br. J. Pharmacol. , vol.149 , pp. 291-299
    • Lin, H.1    Saisch, S.G.2    Strange, P.G.3
  • 25
    • 34547691003 scopus 로고    scopus 로고
    • Allosteric effects of antagonists on signalling by the chemokine receptor CCR5
    • Haworth, B., Lin, H., Fidock, M. et al. (2007) Allosteric effects of antagonists on signalling by the chemokine receptor CCR5. Biochem. Pharmacol., 74, 891-897.
    • (2007) Biochem. Pharmacol. , vol.74 , pp. 891-897
    • Haworth, B.1    Lin, H.2    Fidock, M.3
  • 26
    • 0027049395 scopus 로고
    • 2 guanine nucleotide-binding protein-coupled receptor: utilization of receptor state binding affinities
    • 2 guanine nucleotide-binding protein-coupled receptor: utilization of receptor state binding affinities. Mol. Pharmacol., 42, 432-438.
    • (1992) Mol. Pharmacol. , vol.42 , pp. 432-438
    • Lahti, R.A.1    Figur, L.M.2    Piercey, M.F.3
  • 28
    • 34247556946 scopus 로고    scopus 로고
    • 2 dopamine receptor: evidence for persistent receptor/G protein interaction after agonist stimulation
    • 2 dopamine receptor: evidence for persistent receptor/G protein interaction after agonist stimulation. Br. J. Pharmacol., 151, 144-152.
    • (2007) Br. J. Pharmacol. , vol.151 , pp. 144-152
    • Quirk, K.1    Roberts, D.J.2    Strange, P.G.3
  • 29
    • 3042630989 scopus 로고    scopus 로고
    • 2L cell line: evidence for induction of ligand-specific receptor states
    • 2L cell line: evidence for induction of ligand-specific receptor states. Mol. Pharmacol., 66, 97-105.
    • (2004) Mol. Pharmacol. , vol.66 , pp. 97-105
    • Gay, E.A.1    Urban, J.D.2    Nichols, D.E.3
  • 30
    • 27844519281 scopus 로고    scopus 로고
    • New concepts in drug discovery: collateral efficacy and permissive antagonism
    • Kenakin, T. (2005) New concepts in drug discovery: collateral efficacy and permissive antagonism. Nat. Rev. Drug Discov., 4, 919-927.
    • (2005) Nat. Rev. Drug Discov. , vol.4 , pp. 919-927
    • Kenakin, T.1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.