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Volumn 12, Issue 14, 2006, Pages 1717-1729

Integrative functional assays, chemical genomics and high throughput screening: Harnessing signal transduction pathways to a common HTS readout

Author keywords

Fluorescence polarization (FP); G protein coupled receptor (GPCR); GPCR assay; Histone acetylase transfer activity (HAT); Receptor Selection and Amplification Technology

Indexed keywords

CELL RECEPTOR; DRUG;

EID: 33646497262     PISSN: 13816128     EISSN: None     Source Type: Journal    
DOI: 10.2174/138161206776873662     Document Type: Review
Times cited : (33)

References (127)
  • 1
    • 0034677966 scopus 로고    scopus 로고
    • Drug Discovery: A Historical Perspective
    • Drews J. Drug Discovery: A Historical Perspective 2000; Science 287: 1960-1964.
    • (2000) Science , vol.287 , pp. 1960-1964
    • Drews, J.1
  • 2
    • 0031736497 scopus 로고    scopus 로고
    • Monoaminergic synapses and schizophrenia: 45 years of neuroleptics
    • Bennett MR. Monoaminergic synapses and schizophrenia: 45 years of neuroleptics. J Psychopharmacol 1998; 12: 289-304.
    • (1998) J Psychopharmacol , vol.12 , pp. 289-304
    • Bennett, M.R.1
  • 3
    • 0036446865 scopus 로고    scopus 로고
    • Historical development of the dopamine hypothesis of schizophrenia
    • Baumeister AA, Francis JL. Historical development of the dopamine hypothesis of schizophrenia. J Hist Neurosci 2002; 11: 265-77.
    • (2002) J Hist Neurosci , vol.11 , pp. 265-277
    • Baumeister, A.A.1    Francis, J.L.2
  • 4
    • 1242284561 scopus 로고    scopus 로고
    • New antipsychotics and schizophrenia: A review on efficacy and side effects
    • Serretti A, De Ronchi D, Lorenzi C, Berardi D. New antipsychotics and schizophrenia: a review on efficacy and side effects. Curr Med Chem 2004; 11: 343-58.
    • (2004) Curr Med Chem , vol.11 , pp. 343-358
    • Serretti, A.1    De Ronchi, D.2    Lorenzi, C.3    Berardi, D.4
  • 5
    • 0025163692 scopus 로고
    • The neuroleptics: A historical survey
    • Deniker P. The neuroleptics: a historical survey. Acta Psychiatr Scand Suppl 1990; 358: 83-7.
    • (1990) Acta Psychiatr Scand Suppl , vol.358 , pp. 83-87
    • Deniker, P.1
  • 8
    • 0034793718 scopus 로고    scopus 로고
    • Chemical-genomics: Functional analysis of orphan nuclear receptors in the regulation of bile acid metabolism
    • Willson TM, Jones SA, Moore JT, Kliewer SA. Chemical-genomics: Functional analysis of orphan nuclear receptors in the regulation of bile acid metabolism. Med Res Rev 2001; 21: 513-522
    • (2001) Med Res Rev , vol.21 , pp. 513-522
    • Willson, T.M.1    Jones, S.A.2    Moore, J.T.3    Kliewer, S.A.4
  • 11
  • 12
    • 0036498752 scopus 로고    scopus 로고
    • Functional and Cell-Based uHTS in Chemical Genomic Drug Discovery
    • Croston GE. Functional and Cell-Based uHTS in Chemical Genomic Drug Discovery. Trends Biotech 2001; 20: 110-115.
    • (2001) Trends Biotech , vol.20 , pp. 110-115
    • Croston, G.E.1
  • 13
    • 0036418653 scopus 로고    scopus 로고
    • Chemical Genomics: Massively Parallel Technologies for Rapid Lead Identification and Target Validation
    • Hacksell U, Nash N, Burstein ES, Piu F, Croston G, Brann MR. Chemical Genomics: Massively Parallel Technologies for Rapid Lead Identification and Target Validation. Cytotechnology 2002; 28: 3-10.
    • (2002) Cytotechnology , vol.28 , pp. 3-10
    • Hacksell, U.1    Nash, N.2    Burstein, E.S.3    Piu, F.4    Croston, G.5    Brann, M.R.6
  • 14
    • 1442284465 scopus 로고    scopus 로고
    • Allosteric modulation of G-protein coupled receptors
    • Jensen AA, Spalding TA. Allosteric modulation of G-protein coupled receptors. Eur J Pharm Sci 2004; 21: 407-20.
    • (2004) Eur J Pharm Sci , vol.21 , pp. 407-420
    • Jensen, A.A.1    Spalding, T.A.2
  • 16
    • 0028986883 scopus 로고
    • High throughput assays of cloned adrenergic, muscarinic, neurokinin, and neurotrophin receptors in living mammalian cells
    • Messier TL, Dorman CM, Brauner-Osborne H, Eubanks D, Brann MR. High throughput assays of cloned adrenergic, muscarinic, neurokinin, and neurotrophin receptors in living mammalian cells. Pharmacol Toxicol 1995; 76: 308-11
    • (1995) Pharmacol Toxicol , vol.76 , pp. 308-311
    • Messier, T.L.1    Dorman, C.M.2    Brauner-Osborne, H.3    Eubanks, D.4    Brann, M.R.5
  • 17
    • 0032563937 scopus 로고    scopus 로고
    • The ras-related GTPase rac1 regulates a proliferative pathway selectively utilized by G-protein coupled receptors
    • Burstein ES, Hesterberg DJ, Gutkind JS, Brann MR, Currier EA, Messier TL. The ras-related GTPase rac1 regulates a proliferative pathway selectively utilized by G-protein coupled receptors. Oncogene 1998; 24: 1617-23.
    • (1998) Oncogene , vol.24 , pp. 1617-1623
    • Burstein, E.S.1    Hesterberg, D.J.2    Gutkind, J.S.3    Brann, M.R.4    Currier, E.A.5    Messier, T.L.6
  • 18
    • 0037118581 scopus 로고    scopus 로고
    • Dissection of the cytoplasmic domains of cytokine receptors involved in STAT and Ras dependent proliferation
    • Piu F, Magnani M, Ader ME. Dissection of the cytoplasmic domains of cytokine receptors involved in STAT and Ras dependent proliferation. Oncogene 2002 21: 3579-91.
    • (2002) Oncogene , vol.21 , pp. 3579-3591
    • Piu, F.1    Magnani, M.2    Ader, M.E.3
  • 19
    • 0028814543 scopus 로고
    • Structure-function of muscarinic receptor coupling to G proteins. Random saturation mutagenesis identifies a critical determinant of receptor affinity for G proteins
    • Burstein ES, Spalding TA, Hill-Eubanks D, Brann MR. Structure-function of muscarinic receptor coupling to G proteins. Random saturation mutagenesis identifies a critical determinant of receptor affinity for G proteins. J Biol Chem 1995; 270: 3141-6.
    • (1995) J Biol Chem , vol.270 , pp. 3141-3146
    • Burstein, E.S.1    Spalding, T.A.2    Hill-Eubanks, D.3    Brann, M.R.4
  • 20
    • 0032544633 scopus 로고    scopus 로고
    • The second intracellular loop of the M5 muscarinic receptor is the switch which enables G-protein coupling
    • Burstein ES, Spalding TA, Brann MR. The second intracellular loop of the M5 muscarinic receptor is the switch which enables G-protein coupling. J Biol Chem 1998 273: 24322-7.
    • (1998) J Biol Chem , vol.273 , pp. 24322-24327
    • Burstein, E.S.1    Spalding, T.A.2    Brann, M.R.3
  • 23
    • 1842336902 scopus 로고    scopus 로고
    • Interactions of muscarinic receptors with the heterotrimeric G proteins Gq and G12: Transduction of proliferative signals
    • Burstein ES, Brauner-Osborne H, Spalding TA, Conklin BR, Brann MR. Interactions of muscarinic receptors with the heterotrimeric G proteins Gq and G12: transduction of proliferative signals. J Neurochem 1997; 68: 525-33.
    • (1997) J Neurochem , vol.68 , pp. 525-533
    • Burstein, E.S.1    Brauner-Osborne, H.2    Spalding, T.A.3    Conklin, B.R.4    Brann, M.R.5
  • 24
    • 0942279490 scopus 로고    scopus 로고
    • G-protein-coupled receptor-mediated activation of rap GTPases: Characterization of a novel Galphai regulated pathway
    • Weissman JT, Ma JN, Essex A, Gao Y, Burstein ES. G-protein-coupled receptor-mediated activation of rap GTPases: characterization of a novel Galphai regulated pathway. Oncogene 2004 23: 241-9.
    • (2004) Oncogene , vol.23 , pp. 241-249
    • Weissman, J.T.1    Ma, J.N.2    Essex, A.3    Gao, Y.4    Burstein, E.S.5
  • 25
    • 1542375435 scopus 로고    scopus 로고
    • Discovery of novel peptide/receptor interactions: Identification of PHM-27 as a potent agonist of the human calcitonin receptor
    • Ma JN, Currier EA, Essex A, Feddock M, Spalding TA, Nash NR, et al. Burstein ES. Discovery of novel peptide/receptor interactions: identification of PHM-27 as a potent agonist of the human calcitonin receptor. Biochem Pharmacol 2004 67: 1279-84.
    • (2004) Biochem Pharmacol , vol.67 , pp. 1279-1284
    • Ma, J.N.1    Currier, E.A.2    Essex, A.3    Feddock, M.4    Spalding, T.A.5    Nash, N.R.6    Burstein, E.S.7
  • 26
    • 0037020329 scopus 로고    scopus 로고
    • Drug design strategies for targeting G-protein-coupled receptors
    • Klabunde T, Hessler G. Drug design strategies for targeting G-protein-coupled receptors. Chembiochem 2002; 3: 928-44.
    • (2002) Chembiochem , vol.3 , pp. 928-944
    • Klabunde, T.1    Hessler, G.2
  • 27
    • 0033932181 scopus 로고    scopus 로고
    • Cell-based, high-content screen for receptor internalization, recycling and intracellular trafficking
    • Ghosh RN, Chen YT, DeBiasio R, DeBiasio RL, Conway BR, Minor LK, et al. Cell-based, high-content screen for receptor internalization, recycling and intracellular trafficking. Biotechniques 2000; 29: 170-5.
    • (2000) Biotechniques , vol.29 , pp. 170-175
    • Ghosh, R.N.1    Chen, Y.T.2    DeBiasio, R.3    DeBiasio, R.L.4    Conway, B.R.5    Minor, L.K.6
  • 28
    • 0012132962 scopus 로고    scopus 로고
    • The cellular distribution of fluorescently labeled arrestins provides a robust, sensitive, and universal assay for screening G protein-coupled receptors
    • Oakley RH, Hudson CC, Cruickshank RD, Meyers DM, Payne RE Jr, Rhem SM, et al. The cellular distribution of fluorescently labeled arrestins provides a robust, sensitive, and universal assay for screening G protein-coupled receptors. Assay Drug Dev Technol 2002; 1: 21-30.
    • (2002) Assay Drug Dev Technol , vol.1 , pp. 21-30
    • Oakley, R.H.1    Hudson, C.C.2    Cruickshank, R.D.3    Meyers, D.M.4    Payne Jr., R.E.5    Rhem, S.M.6
  • 29
    • 0036973242 scopus 로고    scopus 로고
    • The BRET2/arrestin assay in stable recombinant cells: A platform to screen for compounds that interact with G protein-coupled receptors GPCRS
    • Bertrand L, Parent S, Caron M, Legault M, Joly E, Angers S, et al. The BRET2/arrestin assay in stable recombinant cells: a platform to screen for compounds that interact with G protein-coupled receptors GPCRS. J Recept Signal Transduct Res 2002; 22: 533-41
    • (2002) J Recept Signal Transduct Res , vol.22 , pp. 533-541
    • Bertrand, L.1    Parent, S.2    Caron, M.3    Legault, M.4    Joly, E.5    Angers, S.6
  • 30
    • 0028198301 scopus 로고
    • Tools for investigating functional interactions between ligands and G-protein-coupled receptors
    • Lerner MR. Tools for investigating functional interactions between ligands and G-protein-coupled receptors. Trends Neurosci 1994; 17: 142-146.
    • (1994) Trends Neurosci , vol.17 , pp. 142-146
    • Lerner, M.R.1
  • 31
    • 0032722628 scopus 로고    scopus 로고
    • Amphibian melanophore technology as a functional screen for antagonists of G-protein coupled 7-transmembrane receptors
    • Nuttall ME, Lee JC, Murdock PR, Badger AM, Wang FL, Laydon JT, et al. Amphibian melanophore technology as a functional screen for antagonists of G-protein coupled 7-transmembrane receptors. J Biomol Screening 1999; 4: 269-278.
    • (1999) J Biomol Screening , vol.4 , pp. 269-278
    • Nuttall, M.E.1    Lee, J.C.2    Murdock, P.R.3    Badger, A.M.4    Wang, F.L.5    Laydon, J.T.6
  • 33
    • 0032603524 scopus 로고    scopus 로고
    • Measurement of [Ca2+] using the Fluorometric Imaging Plate Reader FLIPR
    • Sullivan E, Tucker EM, Dale IL. Measurement of [Ca2+] using the Fluorometric Imaging Plate Reader FLIPR. Methods Mol. Biol 1999; 114: 125-133.
    • (1999) Methods Mol. Biol , vol.114 , pp. 125-133
    • Sullivan, E.1    Tucker, E.M.2    Dale, I.L.3
  • 34
    • 0032858740 scopus 로고    scopus 로고
    • Functional characterization of agonists at recombinant human 5-HT2A, 5-HT2B and 5-HT2C receptors in CHO-K1 cells
    • Porter RH, Benwell KR, Lamb H, Malcolm CS, Allen NH, Revell DF, et al., Functional characterization of agonists at recombinant human 5-HT2A, 5-HT2B and 5-HT2C receptors in CHO-K1 cells. Br. J. Pharmacol 1999; 128: 13-20.
    • (1999) Br. J. Pharmacol , vol.128 , pp. 13-20
    • Porter, R.H.1    Benwell, K.R.2    Lamb, H.3    Malcolm, C.S.4    Allen, N.H.5    Revell, D.F.6
  • 35
    • 0031260472 scopus 로고    scopus 로고
    • A bioluminescent assay for agonist activity at potentially any G-protein-coupled receptor
    • Stables J, Green A, Marshall F, Fraser N, Knight E, Sautel M, et al., A bioluminescent assay for agonist activity at potentially any G-protein-coupled receptor. Anal. Biochem 1997; 252: 115-126.
    • (1997) Anal. Biochem , vol.252 , pp. 115-126
    • Stables, J.1    Green, A.2    Marshall, F.3    Fraser, N.4    Knight, E.5    Sautel, M.6
  • 36
    • 0032472195 scopus 로고    scopus 로고
    • Quantitation of transcription and clonal selection of single living cells with beta-lactamase as reporter
    • Zlokarnik G, Negulescu PA, Knapp TE, Mere L, Burres N, Feng L, et al., Quantitation of transcription and clonal selection of single living cells with beta-lactamase as reporter. Science 1998; 279: 84-88.
    • (1998) Science , vol.279 , pp. 84-88
    • Zlokarnik, G.1    Negulescu, P.A.2    Knapp, T.E.3    Mere, L.4    Burres, N.5    Feng, L.6
  • 37
    • 0032949754 scopus 로고    scopus 로고
    • High throughput quantitation of cAMP production mediated by activation of seven transmembrane domain receptors
    • Kariv I I, Stevens ME, Behrens DL, Oldenburg KR. High throughput quantitation of cAMP production mediated by activation of seven transmembrane domain receptors. J Biomol Screening 1999; 4: 27-32.
    • (1999) J Biomol Screening , vol.4 , pp. 27-32
    • Kariv, I.I.1    Stevens, M.E.2    Behrens, D.L.3    Oldenburg, K.R.4
  • 38
    • 0033812847 scopus 로고    scopus 로고
    • Development of a functional reporter gene HTS assay for the identification of mGluR7 modulators
    • Terstappen GC, Giacometti A, Ballini E, Aldegheri L. Development of a functional reporter gene HTS assay for the identification of mGluR7 modulators. J Biomol Screening 2000; 5: 255-262.
    • (2000) J Biomol Screening , vol.5 , pp. 255-262
    • Terstappen, G.C.1    Giacometti, A.2    Ballini, E.3    Aldegheri, L.4
  • 39
    • 0033812568 scopus 로고    scopus 로고
    • A novel high throughput chemiluminescent assay for the measurement of cellular cyclic adenosine monophosphate levels
    • Chiulli AC, Trompeter K, Palmer M. A novel high throughput chemiluminescent assay for the measurement of cellular cyclic adenosine monophosphate levels. J. Biomol Screening 2000; 5: 239-248.
    • (2000) J. Biomol Screening , vol.5 , pp. 239-248
    • Chiulli, A.C.1    Trompeter, K.2    Palmer, M.3
  • 40
    • 0030610646 scopus 로고    scopus 로고
    • Fluorescent indicators for Ca2+ based on green fluorescent proteins and calmodulin
    • Miyawaki A, Llopis J, Heim R, McCaffery JM, Adams JA, Ikura M, et al., Fluorescent indicators for Ca2+ based on green fluorescent proteins and calmodulin. Nature 1997; 388: 882-887.
    • (1997) Nature , vol.388 , pp. 882-887
    • Miyawaki, A.1    Llopis, J.2    Heim, R.3    McCaffery, J.M.4    Adams, J.A.5    Ikura, M.6
  • 42
    • 1942487845 scopus 로고    scopus 로고
    • Recent advances in drug action and therapeutics: Relevance of novel concepts in G-protein-coupled receptor and signal transduction pharmacology
    • Brink CB, Harvey BH, Bodenstein J, Venter DP, Oliver DW. Recent advances in drug action and therapeutics: relevance of novel concepts in G-protein-coupled receptor and signal transduction pharmacology. Br J Clin Pharmacol 2004 57: 373-87.
    • (2004) Br J Clin Pharmacol , vol.57 , pp. 373-387
    • Brink, C.B.1    Harvey, B.H.2    Bodenstein, J.3    Venter, D.P.4    Oliver, D.W.5
  • 43
    • 0038540318 scopus 로고    scopus 로고
    • Biochemical and pharmacological control of the multiplicity of coupling at G-protein-coupled receptors
    • Hermans E. Biochemical and pharmacological control of the multiplicity of coupling at G-protein-coupled receptors. Pharmacol Ther 2003 99: 25-44.
    • (2003) Pharmacol Ther , vol.99 , pp. 25-44
    • Hermans, E.1
  • 44
    • 0036534741 scopus 로고    scopus 로고
    • Modelling the consequences of receptor-G-protein promiscuity
    • Tucek S, Michal P, Vlachova V. Modelling the consequences of receptor-G-protein promiscuity. Trends Pharmacol Sci 2002 23: 171-6.
    • (2002) Trends Pharmacol Sci , vol.23 , pp. 171-176
    • Tucek, S.1    Michal, P.2    Vlachova, V.3
  • 45
    • 0033620487 scopus 로고    scopus 로고
    • Heptahelical receptor signaling: Beyond the G protein paradigm
    • Hall RA, Premont RT, Lefkowitz RJ. Heptahelical receptor signaling: beyond the G protein paradigm. J Cell Biol 1999; 145: 927-32.
    • (1999) J Cell Biol , vol.145 , pp. 927-932
    • Hall, R.A.1    Premont, R.T.2    Lefkowitz, R.J.3
  • 46
    • 0034307486 scopus 로고    scopus 로고
    • G-protein-independent signaling by G-protein-coupled receptors
    • Heuss C, Gerber U. G-protein-independent signaling by G-protein-coupled receptors. Trends Neurosci 2000; 23: 469-75.
    • (2000) Trends Neurosci , vol.23 , pp. 469-475
    • Heuss, C.1    Gerber, U.2
  • 47
    • 0035336844 scopus 로고    scopus 로고
    • Signaling at zero G: G-protein-independent functions for 7-TM receptors
    • Brzostowski JA, Kimmel AR. Signaling at zero G: G-protein-independent functions for 7-TM receptors. Trends Biochem Sci 2001; 26: 291-7.
    • (2001) Trends Biochem Sci , vol.26 , pp. 291-297
    • Brzostowski, J.A.1    Kimmel, A.R.2
  • 48
    • 0036174898 scopus 로고    scopus 로고
    • G protein-coupled receptor interacting proteins: Emerging roles in localization and signal transduction
    • Brady AE, Limbird LE. G protein-coupled receptor interacting proteins: emerging roles in localization and signal transduction. Cell Signal 2002; 14: 297-309.
    • (2002) Cell Signal , vol.14 , pp. 297-309
    • Brady, A.E.1    Limbird, L.E.2
  • 49
    • 8144222927 scopus 로고    scopus 로고
    • Receptor activity-independent recruitment of betaarrestin2 reveals specific signaling modes
    • Terrillon S, Bouvier M. Receptor activity-independent recruitment of betaarrestin2 reveals specific signaling modes. EMBO J 2004; 23: 3950-3961.
    • (2004) EMBO J , vol.23 , pp. 3950-3961
    • Terrillon, S.1    Bouvier, M.2
  • 50
  • 51
    • 0032603524 scopus 로고    scopus 로고
    • Measurement of [Ca2+] using the Fluorometric Imaging Plate Reader FLIPR
    • Sullivan E, Tucker EM, Dale IL. Measurement of [Ca2+] using the Fluorometric Imaging Plate Reader FLIPR;. Methods Mol Biol 1999; 114: 125-33.
    • (1999) Methods Mol Biol , vol.114 , pp. 125-133
    • Sullivan, E.1    Tucker, E.M.2    Dale, I.L.3
  • 52
    • 0032858740 scopus 로고    scopus 로고
    • Functional characterization of agonists at recombinant human 5-HT2A, 5-HT2B and 5-HT2C receptors in CHO-K1 cells
    • Porter RH, Benwell KR, Lamb H, Malcolm CS, Allen NH, Revell DF, et al. Functional characterization of agonists at recombinant human 5-HT2A, 5-HT2B and 5-HT2C receptors in CHO-K1 cells. Br J Pharmacol 1999; 128: 13-20.
    • (1999) Br J Pharmacol , vol.128 , pp. 13-20
    • Porter, R.H.1    Benwell, K.R.2    Lamb, H.3    Malcolm, C.S.4    Allen, N.H.5    Revell, D.F.6
  • 53
    • 0025801402 scopus 로고
    • Cellular responsiveness to hormones and neurotransmitters: Conversion of [3H]adenine to [3H]cAMP in cell monolayers, cell suspensions, and tissue slices
    • Salomon Y. Cellular responsiveness to hormones and neurotransmitters: conversion of [3H]adenine to [3H]cAMP in cell monolayers, cell suspensions, and tissue slices. Methods Enzymol 1991; 195: 22-28.
    • (1991) Methods Enzymol , vol.195 , pp. 22-28
    • Salomon, Y.1
  • 54
    • 0028947365 scopus 로고
    • A colorimetric assay for measuring activation of Gs- and Gq-coupled signaling pathways
    • Chen W, Shields TS, Stork PJS, Cone RD. A colorimetric assay for measuring activation of Gs- and Gq-coupled signaling pathways. Anal Biochem 1995; 226: 349-54.
    • (1995) Anal Biochem , vol.226 , pp. 349-354
    • Chen, W.1    Shields, T.S.2    Stork, P.J.S.3    Cone, R.D.4
  • 55
    • 0026485548 scopus 로고
    • A method for evaluating the effects of ligands upon Gs protein-coupled receptors using a recombinant melanophore-based bioassay
    • Potenza MN, Graminski GF, Lerner MR. A method for evaluating the effects of ligands upon Gs protein-coupled receptors using a recombinant melanophore-based bioassay. Anal Biochem 1992; 206: 315-22.
    • (1992) Anal Biochem , vol.206 , pp. 315-322
    • Potenza, M.N.1    Graminski, G.F.2    Lerner, M.R.3
  • 56
    • 0027245830 scopus 로고
    • Substitution of three amino acids switches receptor specificity of Gq alpha to that of Gi alpha
    • Conklin BR, Farfel Z, Lustig KD, Julius D, Bourne HR. Substitution of three amino acids switches receptor specificity of Gq alpha to that of Gi alpha. Nature 1993; 363: 274-6
    • (1993) Nature , vol.363 , pp. 274-276
    • Conklin, B.R.1    Farfel, Z.2    Lustig, K.D.3    Julius, D.4    Bourne, H.R.5
  • 57
    • 0029957669 scopus 로고    scopus 로고
    • Carboxyl-terminal mutations of Gq alpha and Gs alpha that alter the fidelity of receptor activation
    • Conklin BR, Herzmark P, Ishida S, Voyno-Yasenetskaya TA, Sun Y, Farfel Z, et al. Carboxyl-terminal mutations of Gq alpha and Gs alpha that alter the fidelity of receptor activation. Mol Pharmacol 1996; 50: 885-90.
    • (1996) Mol Pharmacol , vol.50 , pp. 885-890
    • Conklin, B.R.1    Herzmark, P.2    Ishida, S.3    Voyno-Yasenetskaya, T.A.4    Sun, Y.5    Farfel, Z.6
  • 58
    • 0026053016 scopus 로고
    • G alpha 16, a G protein alpha subunit specifically expressed in hematopoietic cells
    • Amatruda TT 3rd, Steele DA, Slepak VZ, Simon MI. G alpha 16, a G protein alpha subunit specifically expressed in hematopoietic cells. Proc Natl Acad Sci USA 1991; 88: 5587-91.
    • (1991) Proc Natl Acad Sci USA , vol.88 , pp. 5587-5591
    • Amatruda III, T.T.1    Steele, D.A.2    Slepak, V.Z.3    Simon, M.I.4
  • 59
    • 0028981057 scopus 로고
    • G alpha 15 and G alpha 16 couple a wide variety of receptors to phospholipase C
    • Offermanns S, Simon MI. G alpha 15 and G alpha 16 couple a wide variety of receptors to phospholipase C. J Biol Chem 1995; 270: 15175-80.
    • (1995) J Biol Chem , vol.270 , pp. 15175-15180
    • Offermanns, S.1    Simon, M.I.2
  • 60
    • 0025834532 scopus 로고
    • Diversity of G proteins in signal transduction
    • Simon MI, Strathmann MP, Gautam N. Diversity of G proteins in signal transduction. Science 1991; 252: 802-8.
    • (1991) Science , vol.252 , pp. 802-808
    • Simon, M.I.1    Strathmann, M.P.2    Gautam, N.3
  • 61
    • 0026003089 scopus 로고
    • G alpha 12 and G alpha 13 subunits define a fourth class of G protein alpha subunits
    • Strathmann MP, Simon MI. G alpha 12 and G alpha 13 subunits define a fourth class of G protein alpha subunits. Proc Natl Acad Sci USA 1991; 88: 5582-6.
    • (1991) Proc Natl Acad Sci USA , vol.88 , pp. 5582-5586
    • Strathmann, M.P.1    Simon, M.I.2
  • 62
    • 0029908501 scopus 로고    scopus 로고
    • Coupling of metabotropic glutamate receptors 2 and 4 to G alpha 15, G alpha 16, and chimeric G alpha q/i proteins: Characterization of new antagonists
    • Gomeza J, Mary S, Brabet I, Parmentier ML, Restituito S, Bockaert J, et al. Coupling of metabotropic glutamate receptors 2 and 4 to G alpha 15, G alpha 16, and chimeric G alpha q/i proteins: characterization of new antagonists. Mol Pharmacol 1996; 50: 923-30.
    • (1996) Mol Pharmacol , vol.50 , pp. 923-930
    • Gomeza, J.1    Mary, S.2    Brabet, I.3    Parmentier, M.L.4    Restituito, S.5    Bockaert, J.6
  • 63
    • 0031969805 scopus 로고    scopus 로고
    • Differential coupling of mu-, delta-, and kappa-opioid receptors to G alpha16-mediated stimulation of phospholipase C
    • Lee JW, Joshi S, Chan JS, Wong YH Differential coupling of mu-, delta-, and kappa-opioid receptors to G alpha16-mediated stimulation of phospholipase C. J Neurochem 1998; 70: 2203-11.
    • (1998) J Neurochem , vol.70 , pp. 2203-2211
    • Lee, J.W.1    Joshi, S.2    Chan, J.S.3    Wong, Y.H.4
  • 64
    • 0035497743 scopus 로고    scopus 로고
    • Is Galpha16 the optimal tool for fishing ligands of orphan G-protein-coupled receptors?
    • Kostenis E. Is Galpha16 the optimal tool for fishing ligands of orphan G-protein-coupled receptors? Trends Pharmacol Sci 2001; 22: 560-4.
    • (2001) Trends Pharmacol Sci , vol.22 , pp. 560-564
    • Kostenis, E.1
  • 65
    • 0038380750 scopus 로고    scopus 로고
    • High-content assays for ligand regulation of G-protein-coupled receptors
    • Milligan G. High-content assays for ligand regulation of G-protein-coupled receptors. Drug Discov Today 2003 8: 579-85.
    • (2003) Drug Discov Today , vol.8 , pp. 579-585
    • Milligan, G.1
  • 66
    • 0029815128 scopus 로고    scopus 로고
    • Interplay between Ras-related and heterotrimeric GTP binding proteins: Lifestyles of the BIG and little
    • Bokoch GM. Interplay between Ras-related and heterotrimeric GTP binding proteins: lifestyles of the BIG and little. FASEB J 1996; 10: 1290-5.
    • (1996) FASEB J , vol.10 , pp. 1290-1295
    • Bokoch, G.M.1
  • 67
    • 0033520427 scopus 로고    scopus 로고
    • Activation of mitogen-activated protein kinase by the A2A;-adenosine receptor via a rap1-dependent and via a p21ras;-dependent pathway
    • Seidel MG, Klinger M, Freissmuth M, Holler C. Activation of mitogen-activated protein kinase by the A2A;-adenosine receptor via a rap1-dependent and via a p21ras;-dependent pathway. J Biol Chem 1999; 274: 25833-41.
    • (1999) J Biol Chem , vol.274 , pp. 25833-25841
    • Seidel, M.G.1    Klinger, M.2    Freissmuth, M.3    Holler, C.4
  • 68
    • 0034682836 scopus 로고    scopus 로고
    • Beta-adrenergic receptor activates extracellular regulated kinases ERKs; via the small G protein Rap1 and the serine/threonine kinase B-Raf
    • Schmitt JM, Stork PJS 2000. Beta-adrenergic receptor activates extracellular regulated kinases ERKs; via the small G protein Rap1 and the serine/threonine kinase B-Raf. J Biol Chem 275: 25342-25350.
    • (2000) J Biol Chem , vol.275 , pp. 25342-25350
    • Schmitt, J.M.1    Stork, P.J.S.2
  • 69
    • 0037023134 scopus 로고    scopus 로고
    • A Gi-dependent pathway is required for activation of the small GTPase Rap1B in human platelets
    • Lova P, Paganini S, Sinigaglia F, Balduini C, Torti M. A Gi-dependent pathway is required for activation of the small GTPase Rap1B in human platelets. J Biol Chem 2002; 277: 12009-15.
    • (2002) J Biol Chem , vol.277 , pp. 12009-12015
    • Lova, P.1    Paganini, S.2    Sinigaglia, F.3    Balduini, C.4    Torti, M.5
  • 71
    • 0035816623 scopus 로고    scopus 로고
    • A CalDAG-GEFI/Rap1/B-Raf cassette couples M1; muscarinic acetylcholine receptors to the activation of ERK1/2
    • Guo FF, Kumahara E, Saffen D. A CalDAG-GEFI/Rap1/B-Raf cassette couples M1; muscarinic acetylcholine receptors to the activation of ERK1/2. J Biol Chem 2001; 276: 25568-25581.
    • (2001) J Biol Chem , vol.276 , pp. 25568-25581
    • Guo, F.F.1    Kumahara, E.2    Saffen, D.3
  • 72
    • 0036364408 scopus 로고    scopus 로고
    • A growing family of guanine nucleotide exchange factors is responsible for activation of Ras-family GTPases
    • Quilliam LA, Rebhun JF, Castro AF. A growing family of guanine nucleotide exchange factors is responsible for activation of Ras-family GTPases. Prog Nucleic Acid Res Mol Biol 2002; 71: 391-444.
    • (2002) Prog Nucleic Acid Res Mol Biol , vol.71 , pp. 391-444
    • Quilliam, L.A.1    Rebhun, J.F.2    Castro, A.F.3
  • 73
    • 0033179296 scopus 로고    scopus 로고
    • GEFs: Structural basis for their activation of small GTP-binding proteins
    • Cherfils J, Chardin P. GEFs: structural basis for their activation of small GTP-binding proteins. Trends Biochem Sci 1999; 24: 306-11.
    • (1999) Trends Biochem Sci , vol.24 , pp. 306-311
    • Cherfils, J.1    Chardin, P.2
  • 76
    • 0024600222 scopus 로고
    • A ras-related gene with transformation suppressor activity
    • Kitayama H, Sugimoto Y, Matsuzaki T, Ikawa Y, Noda M. A ras-related gene with transformation suppressor activity. Cell 1989; 56: 77-84
    • (1989) Cell , vol.56 , pp. 77-84
    • Kitayama, H.1    Sugimoto, Y.2    Matsuzaki, T.3    Ikawa, Y.4    Noda, M.5
  • 77
    • 0025335812 scopus 로고
    • Identification of small clusters of divergent amino acids that mediate the opposing effects of ras and Krev-1
    • Zhang K, Noda M, Vass WC, Papageorge AG, Lowy DR. Identification of small clusters of divergent amino acids that mediate the opposing effects of ras and Krev-1. Science 1990; 249: 162-5.
    • (1990) Science , vol.249 , pp. 162-165
    • Zhang, K.1    Noda, M.2    Vass, W.C.3    Papageorge, A.G.4    Lowy, D.R.5
  • 78
    • 0033574435 scopus 로고    scopus 로고
    • Discriminatory residues in Ras and Rap for guanine nucleotide exchange factor recognition
    • Van den Berghe N, Cool RH, Wittinghofer A. Discriminatory residues in Ras and Rap for guanine nucleotide exchange factor recognition. J Biol Chem 1999; 274: 11078-85.
    • (1999) J Biol Chem , vol.274 , pp. 11078-11085
    • Van den Berghe, N.1    Cool, R.H.2    Wittinghofer, A.3
  • 79
    • 0035040818 scopus 로고    scopus 로고
    • Regulation and role of adenylyl cyclase isoforms
    • Hanoune J, Defer N. Regulation and role of adenylyl cyclase isoforms. Annu Rev Pharmacol Toxicol 2001; 41: 145-74.
    • (2001) Annu Rev Pharmacol Toxicol , vol.41 , pp. 145-174
    • Hanoune, J.1    Defer, N.2
  • 80
    • 0036089264 scopus 로고    scopus 로고
    • Molecular mechanisms for heterologous sensitization of adenylate cyclase
    • Watts VJ. Molecular mechanisms for heterologous sensitization of adenylate cyclase. J Pharmacol Exp Ther 2002; 302: 1-7.
    • (2002) J Pharmacol Exp Ther , vol.302 , pp. 1-7
    • Watts, V.J.1
  • 81
    • 0027168708 scopus 로고
    • Type II adenylylcyclase integrates coincident signals from Gs, Gi, and Gq
    • Lustig KD, Conklin BR, Herzmark P, Taussig R, Bourne HR. Type II adenylylcyclase integrates coincident signals from Gs, Gi, and Gq. J Biol Chem 1993; 268: 13900-5
    • (1993) J Biol Chem , vol.268 , pp. 13900-13905
    • Lustig, K.D.1    Conklin, B.R.2    Herzmark, P.3    Taussig, R.4    Bourne, H.R.5
  • 82
    • 0036463901 scopus 로고    scopus 로고
    • Efficacy at G-protein-coupled receptors
    • Kenakin T. Efficacy at G-protein-coupled receptors Nat Rev Drug Discov 2002; 1: 103-10.
    • (2002) Nat Rev Drug Discov , vol.1 , pp. 103-110
    • Kenakin, T.1
  • 83
    • 0032544061 scopus 로고    scopus 로고
    • Morphine-activated opioid receptors elude desensitization by beta-arrestin
    • Whistler JL, von Zastrow M. Morphine-activated opioid receptors elude desensitization by beta-arrestin. Proc Natl Acad Sci USA 1998; 95: 9914-9.
    • (1998) Proc Natl Acad Sci USA , vol.95 , pp. 9914-9919
    • Whistler, J.L.1    von Zastrow, M.2
  • 84
    • 0033179904 scopus 로고    scopus 로고
    • Functional dissociation of mu opioid receptor signaling and endocytosis: Implications for the biology of opiate tolerance and addiction
    • Whistler JL, Chuang HH, Chu P, Jan LY, von Zastrow M. Functional dissociation of mu opioid receptor signaling and endocytosis: implications for the biology of opiate tolerance and addiction. Neuron 1999; 23: 737-46.
    • (1999) Neuron , vol.23 , pp. 737-746
    • Whistler, J.L.1    Chuang, H.H.2    Chu, P.3    Jan, L.Y.4    von Zastrow, M.5
  • 85
    • 0037169345 scopus 로고    scopus 로고
    • Regulation of opioid receptor trafficking and morphine tolerance by receptor oligomerization
    • He L, Fong J, von Zastrow M, Whistler JL. Regulation of opioid receptor trafficking and morphine tolerance by receptor oligomerization. Cell 2002; 108: 271-82.
    • (2002) Cell , vol.108 , pp. 271-282
    • He, L.1    Fong, J.2    von Zastrow, M.3    Whistler, J.L.4
  • 86
    • 0037794320 scopus 로고    scopus 로고
    • Predicting therapeutic value in the lead optimization phase of drug discovery
    • Kenakin T. Predicting therapeutic value in the lead optimization phase of drug discovery. Nat Rev Drug Discov 2003; 2: 429-38.
    • (2003) Nat Rev Drug Discov , vol.2 , pp. 429-438
    • Kenakin, T.1
  • 87
    • 0030613761 scopus 로고    scopus 로고
    • Switching of the coupling of the beta2-adrenergic receptor to different G proteins by protein kinase A
    • Daaka Y, Luttrell LM, Lefkowitz RJ. Switching of the coupling of the beta2-adrenergic receptor to different G proteins by protein kinase A. Nature 1997; 390: 88-91.
    • (1997) Nature , vol.390 , pp. 88-91
    • Daaka, Y.1    Luttrell, L.M.2    Lefkowitz, R.J.3
  • 88
    • 0035079910 scopus 로고    scopus 로고
    • Dual effects of muscarinic M2; acetylcholine receptors on the synthesis of cyclic AMP in CHO cells: Dependence on time, receptor density and receptor agonists
    • Michal P, Lysikova M, Tucek S. Dual effects of muscarinic M2; acetylcholine receptors on the synthesis of cyclic AMP in CHO cells: dependence on time, receptor density and receptor agonists. Br J Pharmacol 2001; 132: 1217-28.
    • (2001) Br J Pharmacol , vol.132 , pp. 1217-1228
    • Michal, P.1    Lysikova, M.2    Tucek, S.3
  • 89
    • 0029417130 scopus 로고
    • Constitutive activity of the M1-M4 subtypes of muscarinic receptors in transfected CHO cells and of muscarinic receptors in the heart cells revealed by negative antagonists
    • Jakubik J, Bacakova L, el-Fakahany EE, Tucek S. Constitutive activity of the M1-M4 subtypes of muscarinic receptors in transfected CHO cells and of muscarinic receptors in the heart cells revealed by negative antagonists. FEBS Lett 1995 377: 275-9.
    • (1995) FEBS Lett , vol.377 , pp. 275-279
    • Jakubik, J.1    Bacakova, L.2    el-Fakahany, E.E.3    Tucek, S.4
  • 90
    • 0142210286 scopus 로고    scopus 로고
    • Protease-activated receptors: New concepts in regulation of G protein-coupled receptor signaling and trafficking
    • Trejo J. Protease-activated receptors: new concepts in regulation of G protein-coupled receptor signaling and trafficking. J Pharmacol Exp Ther 2003; 307: 437-42.
    • (2003) J Pharmacol Exp Ther , vol.307 , pp. 437-442
    • Trejo, J.1
  • 91
    • 11244328357 scopus 로고    scopus 로고
    • Multiple Independent Functions of Arrestins in the Regulation of Protease-activated Receptor-2 Signaling and Trafficking
    • Stalheim L, Ding Y, Gullapalli A, Paing MM, Wolfe BL, Morris DR, et al. Multiple Independent Functions of Arrestins in the Regulation of Protease-activated Receptor-2 Signaling and Trafficking. Mol Pharmacol 2005; 67: 78-87.
    • (2005) Mol Pharmacol , vol.67 , pp. 78-87
    • Stalheim, L.1    Ding, Y.2    Gullapalli, A.3    Paing, M.M.4    Wolfe, B.L.5    Morris, D.R.6
  • 92
    • 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: 1271-6.
    • (2003) Mol Pharmacol , vol.64 , pp. 1271-1276
    • Milligan, G.1
  • 93
    • 0026509982 scopus 로고
    • Agonist-independent inhibition of G protein activation by muscarinic acetylcholine receptor antagonists in cardiac membranes
    • Hilf G, Jakobs KH. Agonist-independent inhibition of G protein activation by muscarinic acetylcholine receptor antagonists in cardiac membranes. Eur J Pharmacol 1992; 225: 245-52
    • (1992) Eur J Pharmacol , vol.225 , pp. 245-252
    • Hilf, G.1    Jakobs, K.H.2
  • 94
    • 0035130843 scopus 로고    scopus 로고
    • AgRP(83-132) acts as an inverse agonist on the human-melanocortin-4 receptor
    • Nijenhuis WA, Oosterom J, Adan RA. AgRP(83-132) acts as an inverse agonist on the human-melanocortin-4 receptor. Mol Endocrinol 2001; 15: 164-71
    • (2001) Mol Endocrinol , vol.15 , pp. 164-171
    • Nijenhuis, W.A.1    Oosterom, J.2    Adan, R.A.3
  • 95
    • 0242330291 scopus 로고    scopus 로고
    • High constitutive signaling of the ghrelin receptor - Identification of a potent inverse agonist
    • Holst B, Cygankiewicz A, Jensen TH, Ankersen M, Schwartz TW. High constitutive signaling of the ghrelin receptor - identification of a potent inverse agonist. Mol Endocrinol 2003; 17: 2201-10
    • (2003) Mol Endocrinol , vol.17 , pp. 2201-2210
    • Holst, B.1    Cygankiewicz, A.2    Jensen, T.H.3    Ankersen, M.4    Schwartz, T.W.5
  • 96
    • 0031032769 scopus 로고    scopus 로고
    • Human herpesvirus KSHV encodes a constitutively active G-protein-coupled receptor linked to cell proliferation
    • Arvanitakis L, Geras-Raaka E, Varma A, Gershengorn MC, Cesarman E. Human herpesvirus KSHV encodes a constitutively active G-protein-coupled receptor linked to cell proliferation. Nature 1997; 385: 347-50
    • (1997) Nature , vol.385 , pp. 347-350
    • Arvanitakis, L.1    Geras-Raaka, E.2    Varma, A.3    Gershengorn, M.C.4    Cesarman, E.5
  • 97
    • 0035846939 scopus 로고    scopus 로고
    • Constitutive signaling of the human cytomegalovirus-encoded chemokine receptor US28
    • Casarosa P, Bakker RA, Verzijl D, Navis M, Timmerman H, Leurs R, et al. Constitutive signaling of the human cytomegalovirus-encoded chemokine receptor US28. J Biol Chem 2001; 276: 1133-7.
    • (2001) J Biol Chem , vol.276 , pp. 1133-1137
    • Casarosa, P.1    Bakker, R.A.2    Verzijl, D.3    Navis, M.4    Timmerman, H.5    Leurs, R.6
  • 98
    • 0027203808 scopus 로고
    • Haloperidol increases prolactin release and cyclic AMP formation in vitro: Inverse agonism at dopamine D2 receptors?
    • Nilsson CL, Eriksson E. Haloperidol increases prolactin release and cyclic AMP formation in vitro: inverse agonism at dopamine D2 receptors? J Neural Transm Gen Sect 1993; 92: 213-20.
    • (1993) J Neural Transm Gen Sect , vol.92 , pp. 213-220
    • Nilsson, C.L.1    Eriksson, E.2
  • 99
    • 1642495639 scopus 로고    scopus 로고
    • Efficacy as a vector: The relative prevalence and paucity of inverse agonism
    • Kenakin T. Efficacy as a vector: the relative prevalence and paucity of inverse agonism. Mol Pharmacol 2004; 65: 2-11.
    • (2004) Mol Pharmacol , vol.65 , pp. 2-11
    • Kenakin, T.1
  • 100
    • 0034752736 scopus 로고    scopus 로고
    • Histamine H(1)-receptor activation of nuclear factor-kappa B: Roles for G beta gamma- and G alpha(q/11)-subunits in constitutive and agonist-mediated signaling
    • Bakker RA, Schoonus SB, Smit MJ, Timmerman H, Leurs R. Histamine H(1)-receptor activation of nuclear factor-kappa B: roles for G beta gamma- and G alpha(q/11)-subunits in constitutive and agonist-mediated signaling. Mol Pharmacol 2001; 60: 1133-42.
    • (2001) Mol Pharmacol , vol.60 , pp. 1133-1142
    • Bakker, R.A.1    Schoonus, S.B.2    Smit, M.J.3    Timmerman, H.4    Leurs, R.5
  • 101
    • 1242294511 scopus 로고    scopus 로고
    • Constitutively active Gq/11-coupled receptors enable signaling by coexpressed G(i/o)-coupled receptors
    • Bakker RA, Casarosa P, Timmerman H, Smit MJ, Leurs R. Constitutively active Gq/11-coupled receptors enable signaling by coexpressed G(i/ o)-coupled receptors. J Biol Chem 2004; 279: 5152-61.
    • (2004) J Biol Chem , vol.279 , pp. 5152-5161
    • Bakker, R.A.1    Casarosa, P.2    Timmerman, H.3    Smit, M.J.4    Leurs, R.5
  • 103
    • 0031037633 scopus 로고    scopus 로고
    • Pharmacology of muscarinic receptor subtypes constitutively activated by G proteins
    • Burstein ES, Spalding TA, Brann MR. Pharmacology of muscarinic receptor subtypes constitutively activated by G proteins. Mol Pharmacol 1997; 51: 312-9
    • (1997) Mol Pharmacol , vol.51 , pp. 312-319
    • Burstein, E.S.1    Spalding, T.A.2    Brann, M.R.3
  • 105
    • 0030790777 scopus 로고    scopus 로고
    • Constitutive activation of the M5 muscarinic receptor by a series of mutations at the extracellular end of transmembrane 6
    • Spalding TA, Burstein ES, Wells JW, Brann MR. Constitutive activation of the M5 muscarinic receptor by a series of mutations at the extracellular end of transmembrane 6. Biochemistry 1997; 36: 10109-16.
    • (1997) Biochemistry , vol.36 , pp. 10109-10116
    • Spalding, T.A.1    Burstein, E.S.2    Wells, J.W.3    Brann, M.R.4
  • 106
    • 0035957579 scopus 로고    scopus 로고
    • Constitutively active muscarinic receptors
    • Spalding TA, Burstein ES. Constitutively active muscarinic receptors. Life Sci 2001; 68: 2511-6
    • (2001) Life Sci , vol.68 , pp. 2511-2516
    • Spalding, T.A.1    Burstein, E.S.2
  • 107
    • 0037192858 scopus 로고    scopus 로고
    • Related Evidence for a model of agonist-induced activation of 5-hydroxytryptamine 2A serotonin receptors that involves the disruption of a strong ionic interaction between helices 3 and 6
    • Mar 29
    • Shapiro DA, Kristiansen K, Weiner DM, Kroeze WK, Roth BL. Related Evidence for a model of agonist-induced activation of 5-hydroxytryptamine 2A serotonin receptors that involves the disruption of a strong ionic interaction between helices 3 and 6. J Biol Chem 2002 Mar 29;277(13): 11441-9.
    • (2002) J Biol Chem , vol.277 , Issue.13 , pp. 11441-11449
    • Shapiro, D.A.1    Kristiansen, K.2    Weiner, D.M.3    Kroeze, W.K.4    Roth, B.L.5
  • 109
    • 8844262660 scopus 로고    scopus 로고
    • Principles for modulation of the nuclear receptor superfamily
    • Gronemeyer H, Gustafsson JA, Laudet V. Principles for modulation of the nuclear receptor superfamily. Nat Rev Drug Discov 2004 3: 950-64.
    • (2004) Nat Rev Drug Discov , vol.3 , pp. 950-964
    • Gronemeyer, H.1    Gustafsson, J.A.2    Laudet, V.3
  • 110
    • 77957168579 scopus 로고    scopus 로고
    • Orphan nuclear receptors: An emerging family of metabolic regulators
    • Sladek R, Giguere V. Orphan nuclear receptors: an emerging family of metabolic regulators. Adv Pharmacol 2000; 47: 23-87.
    • (2000) Adv Pharmacol , vol.47 , pp. 23-87
    • Sladek, R.1    Giguere, V.2
  • 111
    • 1342344034 scopus 로고    scopus 로고
    • Nuclear hormone and orphan receptors: Their role in neuronal differentiation and cytoprotection and in the pathogenesis of Parkinson's disease
    • Malaspina A, Pearce RK, Graeber MB. Nuclear hormone and orphan receptors: their role in neuronal differentiation and cytoprotection and in the pathogenesis of Parkinson's disease. Dev Neurosci 2003 6: 375-83.
    • (2003) Dev Neurosci , vol.6 , pp. 375-383
    • Malaspina, A.1    Pearce, R.K.2    Graeber, M.B.3
  • 112
    • 0036195383 scopus 로고    scopus 로고
    • A comparison of ALPHAScreen, TR-FRET, and TRF as assay methods for FXR nuclear receptors
    • Glickman JF, Wu X, Mercuri R, Illy C, Bowen BR, He Y, et al. A comparison of ALPHAScreen, TR-FRET, and TRF as assay methods for FXR nuclear receptors. J Biomol Screen 2002 7: 3-10.
    • (2002) J Biomol Screen , vol.7 , pp. 3-10
    • Glickman, J.F.1    Wu, X.2    Mercuri, R.3    Illy, C.4    Bowen, B.R.5    He, Y.6
  • 113
    • 0242483911 scopus 로고    scopus 로고
    • Comparison of assay technologies for a nuclear receptor assay screen reveals differences in the sets of identified functional antagonists
    • Wu X, Glickman JF, Bowen BR, Sills MA. Comparison of assay technologies for a nuclear receptor assay screen reveals differences in the sets of identified functional antagonists. J Biomol Screen 2003 8: 381-92.
    • (2003) J Biomol Screen , vol.8 , pp. 381-392
    • Wu, X.1    Glickman, J.F.2    Bowen, B.R.3    Sills, M.A.4
  • 114
    • 0008190079 scopus 로고    scopus 로고
    • Development of high throughput screening assays using fluorescence polarization: Nuclear receptor-ligand-binding and kinase/phosphatase assays
    • Parker GJ, Law TL, Lenoch FJ, Bolger RE. Development of high throughput screening assays using fluorescence polarization: nuclear receptor-ligand-binding and kinase/phosphatase assays. J Biomol Screen 2000 5: 77-88.
    • (2000) J Biomol Screen , vol.5 , pp. 77-88
    • Parker, G.J.1    Law, T.L.2    Lenoch, F.J.3    Bolger, R.E.4
  • 115
    • 0035813186 scopus 로고    scopus 로고
    • Nuclear receptor minireview
    • Olefsky JM. Nuclear receptor minireview. J Biol Chem 2001 276: 36863-4.
    • (2001) J Biol Chem , vol.276 , pp. 36863-36864
    • Olefsky, J.M.1
  • 118
    • 0033621396 scopus 로고    scopus 로고
    • Serine 157, a retinoic acid receptor alpha residue phosphorylated by protein kinase C in vitro, is involved in RXR.RARalpha heterodimerization and transcriptional activity
    • Delmotte MH, Tahayato A, Formstecher P, Lefebvre P. Serine 157, a retinoic acid receptor alpha residue phosphorylated by protein kinase C in vitro, is involved in RXR.RARalpha heterodimerization and transcriptional activity. J Biol Chem 1999 274: 38225-31.
    • (1999) J Biol Chem , vol.274 , pp. 38225-38231
    • Delmotte, M.H.1    Tahayato, A.2    Formstecher, P.3    Lefebvre, P.4
  • 120
    • 14844353662 scopus 로고    scopus 로고
    • Rapid actions of steroid receptors in cellular signaling pathways
    • Print 2002 Jun 25
    • Cato AC, Nestl A, Mink S. Rapid actions of steroid receptors in cellular signaling pathways. Sci STKE 2002(138): RE9. Print 2002 Jun 25.
    • (2002) Sci STKE , Issue.138
    • Cato, A.C.1    Nestl, A.2    Mink, S.3
  • 121
    • 0035902557 scopus 로고    scopus 로고
    • 4-Hydroxytamoxifen binds to and deactivates the estrogen-related receptor gamma
    • Coward P, Lee D, Hull MV, Lehmann JM. 4-Hydroxytamoxifen binds to and deactivates the estrogen-related receptor gamma. Proc Natl Acad Sci USA 2001 98: 8880-4.
    • (2001) Proc Natl Acad Sci USA , vol.98 , pp. 8880-8884
    • Coward, P.1    Lee, D.2    Hull, M.V.3    Lehmann, J.M.4
  • 122
    • 0034812571 scopus 로고    scopus 로고
    • 4-Hydroxytamoxifen is an isoform-specific inhibitor of orphan estrogen-receptor-related (ERR) nuclear receptors beta and gamma
    • Tremblay GB, Bergeron D, Giguere V. 4-Hydroxytamoxifen is an isoform-specific inhibitor of orphan estrogen-receptor-related (ERR) nuclear receptors beta and gamma. Endocrinology 2001 142: 4572-5.
    • (2001) Endocrinology , vol.142 , pp. 4572-4575
    • Tremblay, G.B.1    Bergeron, D.2    Giguere, V.3
  • 123
    • 0036246250 scopus 로고    scopus 로고
    • Characterization of the retinoid orphan-related receptor-alpha coactivator binding interface: A structural basis for ligand-independent transcription
    • Harris JM, Lau P, Chen SL, Muscat GE. Characterization of the retinoid orphan-related receptor-alpha coactivator binding interface: a structural basis for ligand-independent transcription. Mol Endocrinol 2002 16: 998-1012.
    • (2002) Mol Endocrinol , vol.16 , pp. 998-1012
    • Harris, J.M.1    Lau, P.2    Chen, S.L.3    Muscat, G.E.4
  • 124
    • 0028264812 scopus 로고
    • C3G, a guanine nucleotide-releasing protein expressed ubiquitously, binds to the Src homology 3 domains of CRK and GRB2/ASH proteins
    • Tanaka S, Morishita T, Hashimoto Y, Hattori S, Nakamura S, Shibuya M, et al. C3G, a guanine nucleotide-releasing protein expressed ubiquitously, binds to the Src homology 3 domains of CRK and GRB2/ASH proteins. Proc Natl Acad Sci USA 1994; 91, 3443-3447.
    • (1994) Proc Natl Acad Sci USA , vol.91 , pp. 3443-3447
    • Tanaka, S.1    Morishita, T.2    Hashimoto, Y.3    Hattori, S.4    Nakamura, S.5    Shibuya, M.6
  • 125
    • 2342439577 scopus 로고    scopus 로고
    • Indolactam and benzolactam compounds as new medicinal leads with binding selectivity for C1 domains of protein kinase C isozymes
    • Irie K, Nakagawa Y, Ohigashi H. Indolactam and benzolactam compounds as new medicinal leads with binding selectivity for C1 domains of protein kinase C isozymes. Curr Pharm Des 2004; 10(12): 1371-85.
    • (2004) Curr Pharm Des , vol.10 , Issue.12 , pp. 1371-1385
    • Irie, K.1    Nakagawa, Y.2    Ohigashi, H.3
  • 126
    • 2442511737 scopus 로고    scopus 로고
    • High throughput screening and characterization of HIV-1 entry inhibitors targeting gp41: Theories and techniques
    • Liu S, Jiang S. High throughput screening and characterization of HIV-1 entry inhibitors targeting gp41: theories and techniques. Curr Pharm Des 2004; 10(15): 1827-43.
    • (2004) Curr Pharm Des , vol.10 , Issue.15 , pp. 1827-1843
    • Liu, S.1    Jiang, S.2
  • 127
    • 22944438393 scopus 로고    scopus 로고
    • Application of MALDI-TOF mass spectrometry in screening and diagnostic research
    • Pusch W, Kostrzewa M. Application of MALDI-TOF mass spectrometry in screening and diagnostic research. Curr Pharm Des 2005; 11(20): 2577-91.
    • (2005) Curr Pharm Des , vol.11 , Issue.20 , pp. 2577-2591
    • Pusch, W.1    Kostrzewa, M.2


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