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Volumn 115, Issue , 2013, Pages 1-59

Approaches for probing allosteric interactions at 7 transmembrane spanning receptors

Author keywords

7TMR; Allosteric drug discovery; Allosteric modulator; GPCR; HTS; Keywords

Indexed keywords


EID: 84873886491     PISSN: 18771173     EISSN: None     Source Type: Book Series    
DOI: 10.1016/B978-0-12-394587-7.00001-4     Document Type: Chapter
Times cited : (17)

References (158)
  • 2
    • 58149193205 scopus 로고    scopus 로고
    • Allosteric modulators of GPCRs: A novel approach for the treatment of CNS disorders
    • P.J. Conn, A. Christopoulos, and C.W. Lindsley Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders Nat Rev Drug Discov 8 2009 41 54
    • (2009) Nat Rev Drug Discov , vol.8 , pp. 41-54
    • Conn, P.J.1    Christopoulos, A.2    Lindsley, C.W.3
  • 3
    • 53449093828 scopus 로고    scopus 로고
    • G-protein-coupled receptors: From classical modes of modulation to allosteric mechanisms
    • T.M. Bridges, and C.W. Lindsley G-protein-coupled receptors: from classical modes of modulation to allosteric mechanisms ACS Chem Biol 3 2008 530 541
    • (2008) ACS Chem Biol , vol.3 , pp. 530-541
    • Bridges, T.M.1    Lindsley, C.W.2
  • 4
    • 0036258990 scopus 로고    scopus 로고
    • G protein-coupled receptor allosterism and complexing
    • A. Christopoulos, and T. Kenakin G protein-coupled receptor allosterism and complexing Pharmacol Rev 54 2002 323 374
    • (2002) Pharmacol Rev , vol.54 , pp. 323-374
    • Christopoulos, A.1    Kenakin, T.2
  • 6
    • 34147137118 scopus 로고    scopus 로고
    • Seven transmembrane receptors: Something old, something new
    • R.J. Lefkowitz Seven transmembrane receptors: something old, something new Acta Physiol (Oxf) 190 2007 9 19
    • (2007) Acta Physiol (Oxf) , vol.190 , pp. 9-19
    • Lefkowitz, R.J.1
  • 7
    • 0028338534 scopus 로고
    • GCRDb: A G-protein-coupled receptor database
    • L.F. Kolakowski Jr. GCRDb: a G-protein-coupled receptor database Receptors Channels 2 1994 1 7
    • (1994) Receptors Channels , vol.2 , pp. 1-7
    • Kolakowski, Jr.L.F.1
  • 8
    • 0035716295 scopus 로고    scopus 로고
    • Family-B G-protein-coupled receptors
    • REVIEWS3013
    • A.J. Harmar Family-B G-protein-coupled receptors Genome Biol 2 2001 REVIEWS3013
    • (2001) Genome Biol , vol.2
    • Harmar, A.J.1
  • 9
    • 77949516412 scopus 로고    scopus 로고
    • Metabotropic glutamate receptors: Physiology, pharmacology, and disease
    • C.M. Niswender, and P.J. Conn Metabotropic glutamate receptors: physiology, pharmacology, and disease Annu Rev Pharmacol Toxicol 50 2010 295 322
    • (2010) Annu Rev Pharmacol Toxicol , vol.50 , pp. 295-322
    • Niswender, C.M.1    Conn, P.J.2
  • 10
    • 77952354490 scopus 로고    scopus 로고
    • Seven transmembrane receptors as shapeshifting proteins: The impact of allosteric modulation and functional selectivity on new drug discovery
    • T. Kenakin, and L.J. Miller Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery Pharmacol Rev 62 2010 265 304
    • (2010) Pharmacol Rev , vol.62 , pp. 265-304
    • Kenakin, T.1    Miller, L.J.2
  • 11
    • 84857375139 scopus 로고    scopus 로고
    • Allosteric modulation of seven transmembrane spanning receptors: Theory, practice, and opportunities for central nervous system drug discovery
    • B.J. Melancon, C.R. Hopkins, M.R. Wood, K.A. Emmitte, C.M. Niswender, and A. Christopoulos Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery J Med Chem 55 2012 1445 1464
    • (2012) J Med Chem , vol.55 , pp. 1445-1464
    • Melancon, B.J.1    Hopkins, C.R.2    Wood, M.R.3    Emmitte, K.A.4    Niswender, C.M.5    Christopoulos, A.6
  • 13
    • 34447632041 scopus 로고    scopus 로고
    • Allosteric GPCR modulators: Taking advantage of permissive receptor pharmacology
    • K. Leach, P.M. Sexton, and A. Christopoulos Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology Trends Pharmacol Sci 28 2007 382 389
    • (2007) Trends Pharmacol Sci , vol.28 , pp. 382-389
    • Leach, K.1    Sexton, P.M.2    Christopoulos, A.3
  • 14
    • 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
    • K. Leach, R.E. Loiacono, C.C. Felder, D.L. McKinzie, A. Mogg, and D.B. Shaw Molecular mechanisms of action and in vivo validation of an M4 muscarinic acetylcholine receptor allosteric modulator with potential antipsychotic properties Neuropsychopharmacology 35 2010 855 869
    • (2010) Neuropsychopharmacology , vol.35 , pp. 855-869
    • Leach, K.1    Loiacono, R.E.2    Felder, C.C.3    McKinzie, D.L.4    Mogg, A.5    Shaw, D.B.6
  • 15
    • 84455173446 scopus 로고    scopus 로고
    • Probe dependence in the allosteric modulation of a G protein-coupled receptor: Implications for detection and validation of allosteric ligand effects
    • C. Valant, C.C. Felder, P.M. Sexton, and A. Christopoulos Probe dependence in the allosteric modulation of a G protein-coupled receptor: implications for detection and validation of allosteric ligand effects Mol Pharmacol 81 2012 41 52
    • (2012) Mol Pharmacol , vol.81 , pp. 41-52
    • Valant, C.1    Felder, C.C.2    Sexton, P.M.3    Christopoulos, A.4
  • 16
    • 79952396557 scopus 로고    scopus 로고
    • Impact of species variability and 'probe-dependence' on the detection and in vivo validation of allosteric modulation at the M4 muscarinic acetylcholine receptor
    • S. Suratman, K. Leach, P. Sexton, C. Felder, R. Loiacono, and A. Christopoulos Impact of species variability and 'probe-dependence' on the detection and in vivo validation of allosteric modulation at the M4 muscarinic acetylcholine receptor Br J Pharmacol 162 2011 1659 1670
    • (2011) Br J Pharmacol , vol.162 , pp. 1659-1670
    • Suratman, S.1    Leach, K.2    Sexton, P.3    Felder, C.4    Loiacono, R.5    Christopoulos, A.6
  • 17
    • 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
    • C. Koole, D. Wootten, J. Simms, C. Valant, R. Sridhar, and O.L. Woodman 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 78 2010 456 465
    • (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
  • 18
    • 78751529194 scopus 로고    scopus 로고
    • Modulation of the glucagon-like peptide-1 receptor signaling by naturally occurring and synthetic flavonoids
    • D. Wootten, J. Simms, C. Koole, O.L. Woodman, R.J. Summers, and A. Christopoulos Modulation of the glucagon-like peptide-1 receptor signaling by naturally occurring and synthetic flavonoids J Pharmacol Exp Ther 336 2011 540 550
    • (2011) J Pharmacol Exp Ther , vol.336 , pp. 540-550
    • Wootten, D.1    Simms, J.2    Koole, C.3    Woodman, O.L.4    Summers, R.J.5    Christopoulos, A.6
  • 19
    • 33645106023 scopus 로고    scopus 로고
    • On the mechanism of interaction of potent surmountable and insurmountable antagonists with the prostaglandin D2 receptor CRTH2
    • J.M. Mathiesen, A. Christopoulos, T. Ulven, J.F. Royer, M. Campillo, and A. Heinemann On the mechanism of interaction of potent surmountable and insurmountable antagonists with the prostaglandin D2 receptor CRTH2 Mol Pharmacol 69 2006 1441 1453
    • (2006) Mol Pharmacol , vol.69 , pp. 1441-1453
    • Mathiesen, J.M.1    Christopoulos, A.2    Ulven, T.3    Royer, J.F.4    Campillo, M.5    Heinemann, A.6
  • 21
    • 77956398267 scopus 로고    scopus 로고
    • Orthosteric- and allosteric-induced ligand-directed trafficking at GPCRs
    • G.J. Digby, P.J. Conn, and C.W. Lindsley Orthosteric- and allosteric-induced ligand-directed trafficking at GPCRs Curr Opin Drug Discov Dev 13 2010 587 594
    • (2010) Curr Opin Drug Discov Dev , vol.13 , pp. 587-594
    • Digby, G.J.1    Conn, P.J.2    Lindsley, C.W.3
  • 22
    • 34447649922 scopus 로고    scopus 로고
    • Beta-Arrestin-biased ligands at seven-transmembrane receptors
    • J.D. Violin, and R.J. Lefkowitz Beta-Arrestin-biased ligands at seven-transmembrane receptors Trends Pharmacol Sci 28 2007 416 422
    • (2007) Trends Pharmacol Sci , vol.28 , pp. 416-422
    • Violin, J.D.1    Lefkowitz, R.J.2
  • 23
    • 84857497773 scopus 로고    scopus 로고
    • Biased signalling and allosteric machines: New vistas and challenges for drug discovery
    • T.P. Kenakin Biased signalling and allosteric machines: new vistas and challenges for drug discovery Br J Pharmacol 165 2012 1659 1669
    • (2012) Br J Pharmacol , vol.165 , pp. 1659-1669
    • Kenakin, T.P.1
  • 24
    • 77956677462 scopus 로고    scopus 로고
    • A holistic view of GPCR signaling
    • T. Kenakin A holistic view of GPCR signaling Nat Biotechnol 28 2010 928 929
    • (2010) Nat Biotechnol , vol.28 , pp. 928-929
    • Kenakin, T.1
  • 25
  • 26
    • 62149135311 scopus 로고    scopus 로고
    • Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity
    • J.E. Marlo, C.M. Niswender, E.L. Days, T.M. Bridges, Y. Xiang, and A.L. Rodriguez Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity Mol Pharmacol 75 2009 577 588
    • (2009) Mol Pharmacol , vol.75 , pp. 577-588
    • Marlo, J.E.1    Niswender, C.M.2    Days, E.L.3    Bridges, T.M.4    Xiang, Y.5    Rodriguez, A.L.6
  • 27
    • 77957063745 scopus 로고    scopus 로고
    • G protein coupled receptors as allosteric proteins and the role of allosteric modulators
    • T. Kenakin G protein coupled receptors as allosteric proteins and the role of allosteric modulators J Recept Signal Transduct Res 30 2010 313 321
    • (2010) J Recept Signal Transduct Res , vol.30 , pp. 313-321
    • Kenakin, T.1
  • 28
    • 77149174796 scopus 로고    scopus 로고
    • Context-dependent pharmacology exhibited by negative allosteric modulators of metabotropic glutamate receptor 7
    • C.M. Niswender, K.A. Johnson, N.R. Miller, J.E. Ayala, Q. Luo, and R. Williams Context-dependent pharmacology exhibited by negative allosteric modulators of metabotropic glutamate receptor 7 Mol Pharmacol 77 2010 459 468
    • (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
  • 29
    • 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
    • M.J. Noetzel, J.M. Rook, P.N. Vinson, H.P. Cho, E. Days, and Y. Zhou 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 81 2012 120 133
    • (2012) Mol Pharmacol , vol.81 , pp. 120-133
    • Noetzel, M.J.1    Rook, J.M.2    Vinson, P.N.3    Cho, H.P.4    Days, E.5    Zhou, Y.6
  • 30
    • 84894898038 scopus 로고    scopus 로고
    • Triple-Addition assay protocols for detecting and characterizing modulators of seven-transmembrane receptors
    • C.D. Weaver Triple-Addition assay protocols for detecting and characterizing modulators of seven-transmembrane receptors Current Protocols in Chemical Biology 3 2011 119 140
    • (2011) Current Protocols in Chemical Biology , vol.3 , pp. 119-140
    • Weaver, C.D.1
  • 31
    • 0033003760 scopus 로고    scopus 로고
    • A simple statistical parameter for use in evaluation and validation of high throughput screening assays
    • J.-H. Zhang, T.D.Y. Chung, and K.R. Oldenburg A simple statistical parameter for use in evaluation and validation of high throughput screening assays J Biomol Screen 4 1999 67 73
    • (1999) J Biomol Screen , vol.4 , pp. 67-73
    • Zhang, J.-H.1    Chung, T.D.Y.2    Oldenburg, K.R.3
  • 32
    • 0041353568 scopus 로고    scopus 로고
    • A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5
    • J.A. O'Brien, W. Lemaire, T.B. Chen, R.S. Chang, M.A. Jacobson, and S.N. Ha A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5 Mol Pharmacol 64 2003 731 740
    • (2003) Mol Pharmacol , vol.64 , pp. 731-740
    • O'Brien, J.A.1    Lemaire, W.2    Chen, T.B.3    Chang, R.S.4    Jacobson, M.A.5    Ha, S.N.6
  • 33
    • 47149106805 scopus 로고    scopus 로고
    • Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: Unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold
    • S. Sharma, A.L. Rodriguez, P.J. Conn, and C.W. Lindsley Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl) pyrimidine scaffold Bioorg Med Chem Lett 18 2008 4098 4101
    • (2008) Bioorg Med Chem Lett , vol.18 , pp. 4098-4101
    • Sharma, S.1    Rodriguez, A.L.2    Conn, P.J.3    Lindsley, C.W.4
  • 34
    • 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
    • A.L. Rodriguez, Y. Nong, N.K. Sekaran, D. Alagille, G.D. Tamagnan, and P.J. Conn 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 68 2005 1793 1802
    • (2005) Mol Pharmacol , vol.68 , 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
  • 36
    • 0033151694 scopus 로고    scopus 로고
    • Chimeric G proteins allow a high-throughput signaling assay of Gi-coupled receptors
    • P. Coward, S.D.H. Chan, H.G. Wada, G.M. Humphries, and B.R. Conklin Chimeric G proteins allow a high-throughput signaling assay of Gi-coupled receptors Anal Biochem 270 1999 242 248
    • (1999) Anal Biochem , vol.270 , pp. 242-248
    • Coward, P.1    Chan, S.D.H.2    Wada, H.G.3    Humphries, G.M.4    Conklin, B.R.5
  • 37
    • 27144434813 scopus 로고    scopus 로고
    • Techniques: Promiscuous Gα proteins in basic research and drug discovery
    • E. Kostenis, M. Waelbroeck, and G. Milligan Techniques: promiscuous Gα proteins in basic research and drug discovery Trends Pharmacol Sci 26 2005 595 602
    • (2005) Trends Pharmacol Sci , vol.26 , pp. 595-602
    • Kostenis, E.1    Waelbroeck, M.2    Milligan, G.3
  • 38
    • 0038697483 scopus 로고    scopus 로고
    • Development of a high-throughput bioassay to screen melatonin receptor agonists using human melatonin receptor expressing CHO cells
    • T. Yokoyama, N. Kato, and N. Yamada Development of a high-throughput bioassay to screen melatonin receptor agonists using human melatonin receptor expressing CHO cells Neurosci Lett 344 2003 45 48
    • (2003) Neurosci Lett , vol.344 , pp. 45-48
    • Yokoyama, T.1    Kato, N.2    Yamada, N.3
  • 39
    • 84862895073 scopus 로고    scopus 로고
    • A biased ligand for OXE-R uncouples Galpha and Gbetagamma signaling within a heterotrimer
    • S. Blattermann, L. Peters, P.A. Ottersbach, A. Bock, V. Konya, and C.D. Weaver A biased ligand for OXE-R uncouples Galpha and Gbetagamma signaling within a heterotrimer Nat Chem Biol 8 2012 631 638
    • (2012) Nat Chem Biol , vol.8 , pp. 631-638
    • Blattermann, S.1    Peters, L.2    Ottersbach, P.A.3    Bock, A.4    Konya, V.5    Weaver, C.D.6
  • 40
    • 16844367241 scopus 로고    scopus 로고
    • A thallium-sensitive, fluorescence-based assay for detecting and characterizing potassium channel modulators in mammalian cells
    • C.D. Weaver, D. Harden, S.I. Dworetzky, B. Robertson, and R.J. Knox A thallium-sensitive, fluorescence-based assay for detecting and characterizing potassium channel modulators in mammalian cells J Biomol Screen 9 2004 671 677
    • (2004) J Biomol Screen , vol.9 , pp. 671-677
    • Weaver, C.D.1    Harden, D.2    Dworetzky, S.I.3    Robertson, B.4    Knox, R.J.5
  • 41
    • 78651340650 scopus 로고    scopus 로고
    • Development of a selective small-molecule inhibitor of Kir1.1, the renal outer medullary potassium channel
    • G. Bhave, B.A. Chauder, W. Liu, E.S. Dawson, R. Kadakia, and T.T. Nguyen Development of a selective small-molecule inhibitor of Kir1.1, the renal outer medullary potassium channel Mol Pharmacol 79 2011 42 50
    • (2011) Mol Pharmacol , vol.79 , pp. 42-50
    • Bhave, G.1    Chauder, B.A.2    Liu, W.3    Dawson, E.S.4    Kadakia, R.5    Nguyen, T.T.6
  • 42
    • 70350434090 scopus 로고    scopus 로고
    • High-throughput screening reveals a small-molecule inhibitor of the renal outer medullary potassium channel and Kir7.1
    • L.M. Lewis, G. Bhave, B.A. Chauder, S. Banerjee, K.A. Lornsen, and R. Redha High-throughput screening reveals a small-molecule inhibitor of the renal outer medullary potassium channel and Kir7.1 Mol Pharmacol 76 2009 1094 1103
    • (2009) Mol Pharmacol , vol.76 , pp. 1094-1103
    • Lewis, L.M.1    Bhave, G.2    Chauder, B.A.3    Banerjee, S.4    Lornsen, K.A.5    Redha, R.6
  • 43
    • 41149111966 scopus 로고    scopus 로고
    • A novel assay of Gi/o-linked G protein coupled receptor coupling to potassium channels provides new insights into the pharmacology of the group III metabotropic glutamate receptors
    • C.M. Niswender, K.A. Johnson, Q. Luo, J.E. Ayala, C. Kim, and P.J. Conn A novel assay of Gi/o-linked G protein coupled receptor coupling to potassium channels provides new insights into the pharmacology of the group III metabotropic glutamate receptors Mol Pharmacol 73 2008 1213 1224
    • (2008) Mol Pharmacol , vol.73 , pp. 1213-1224
    • Niswender, C.M.1    Johnson, K.A.2    Luo, Q.3    Ayala, J.E.4    Kim, C.5    Conn, P.J.6
  • 44
    • 52049100343 scopus 로고    scopus 로고
    • Initial SAR studies on apamin-displacing 2-Aminothiazole blockers of calcium-Activated small conductance potassium channels
    • R.G. Gentles, K. Grant-Young, S. Hu, Y. Huang, M.A. Poss, and C. Andres Initial SAR studies on apamin-displacing 2-Aminothiazole blockers of calcium-Activated small conductance potassium channels Bioorg Med Chem Lett 18 2008 5316 5319
    • (2008) Bioorg Med Chem Lett , vol.18 , pp. 5316-5319
    • Gentles, R.G.1    Grant-Young, K.2    Hu, S.3    Huang, Y.4    Poss, M.A.5    Andres, C.6
  • 45
    • 53349162200 scopus 로고    scopus 로고
    • Preliminary SAR studies on non-Apamin-displacing 4-(aminomethylaryl) pyrrazolopyrimidine K(Ca) channel blockers
    • R.G. Gentles, S. Hu, Y. Huang, K. Grant-Young, M.A. Poss, and C. Andres Preliminary SAR studies on non-Apamin-displacing 4-(aminomethylaryl) pyrrazolopyrimidine K(Ca) channel blockers Bioorg Med Chem Lett 18 2008 5694 5697
    • (2008) Bioorg Med Chem Lett , vol.18 , pp. 5694-5697
    • Gentles, R.G.1    Hu, S.2    Huang, Y.3    Grant-Young, K.4    Poss, M.A.5    Andres, C.6
  • 46
    • 78650441804 scopus 로고    scopus 로고
    • Identification of human Ether-A-go-go related gene modulators by three screening platforms in an academic drug-discovery setting
    • X.P. Huang, T. Mangano, S. Hufeisen, V. Setola, and B.L. Roth Identification of human Ether-A-go-go related gene modulators by three screening platforms in an academic drug-discovery setting Assay Drug Dev Technol 8 2010 727 742
    • (2010) Assay Drug Dev Technol , vol.8 , pp. 727-742
    • Huang, X.P.1    Mangano, T.2    Hufeisen, S.3    Setola, V.4    Roth, B.L.5
  • 47
    • 81155161027 scopus 로고    scopus 로고
    • Identification of novel KCNQ4 openers by a high-throughput fluorescence-based thallium flux assay
    • Q. Li, M. Rottlander, M. Xu, C.T. Christoffersen, K. Frederiksen, and M.W. Wang Identification of novel KCNQ4 openers by a high-throughput fluorescence-based thallium flux assay Anal Biochem 418 2011 66 72
    • (2011) Anal Biochem , vol.418 , pp. 66-72
    • Li, Q.1    Rottlander, M.2    Xu, M.3    Christoffersen, C.T.4    Frederiksen, K.5    Wang, M.W.6
  • 48
    • 78650496072 scopus 로고    scopus 로고
    • A pharmacologically validated, high-capacity, functional thallium flux assay for the human Ether-A-go-go related gene potassium channel
    • W.A. Schmalhofer, A.M. Swensen, B.S. Thomas, J.P. Felix, R.J. Haedo, and K. Solly A pharmacologically validated, high-capacity, functional thallium flux assay for the human Ether-A-go-go related gene potassium channel Assay Drug Dev Technol 8 2010 714 726
    • (2010) Assay Drug Dev Technol , vol.8 , pp. 714-726
    • Schmalhofer, W.A.1    Swensen, A.M.2    Thomas, B.S.3    Felix, J.P.4    Haedo, R.J.5    Solly, K.6
  • 49
    • 69249213919 scopus 로고    scopus 로고
    • A new homogeneous high-throughput screening assay for profiling compound activity on the human ether-A-go-go-related gene channel
    • S.A. Titus, D. Beacham, S.A. Shahane, N. Southall, M. Xia, and R. Huang A new homogeneous high-throughput screening assay for profiling compound activity on the human ether-A-go-go-related gene channel Anal Biochem 394 2009 30 38
    • (2009) Anal Biochem , vol.394 , pp. 30-38
    • Titus, S.A.1    Beacham, D.2    Shahane, S.A.3    Southall, N.4    Xia, M.5    Huang, R.6
  • 51
    • 78650503264 scopus 로고    scopus 로고
    • Profiling diverse compounds by flux- and electrophysiology-based primary screens for inhibition of human ether-A-go-go related gene potassium channels
    • B. Zou, H. Yu, J.J. Babcock, P. Chanda, J.S. Bader, and O.B. McManus Profiling diverse compounds by flux- and electrophysiology-based primary screens for inhibition of human ether-A-go-go related gene potassium channels Assay Drug Dev Technol 8 2010 743 754
    • (2010) Assay Drug Dev Technol , vol.8 , pp. 743-754
    • Zou, B.1    Yu, H.2    Babcock, J.J.3    Chanda, P.4    Bader, J.S.5    McManus, O.B.6
  • 52
    • 70349325819 scopus 로고    scopus 로고
    • Screening G protein-coupled receptors: Measurement of intracellular calcium using the fluorometric imaging plate reader
    • R. Emkey, and N.B. Rankl Screening G protein-coupled receptors: measurement of intracellular calcium using the fluorometric imaging plate reader Methods Mol Biol 565 2009 145 158
    • (2009) Methods Mol Biol , vol.565 , pp. 145-158
    • Emkey, R.1    Rankl, N.B.2
  • 53
    • 78649919580 scopus 로고    scopus 로고
    • Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity
    • A.L. Rodriguez, M.D. Grier, C.K. Jones, E.J. Herman, A.S. Kane, and R.L. Smith Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity Mol Pharmacol 78 2010 1105 1123
    • (2010) Mol Pharmacol , vol.78 , pp. 1105-1123
    • Rodriguez, A.L.1    Grier, M.D.2    Jones, C.K.3    Herman, E.J.4    Kane, A.S.5    Smith, R.L.6
  • 54
    • 30044435787 scopus 로고    scopus 로고
    • Probing the molecular mechanism of interaction between 4-n-butyl-1-[4-(2-methylphenyl)-4-oxo-1-butyl]-piperidine (AC-42) and the muscarinic M(1) receptor: Direct pharmacological evidence that AC-42 is an allosteric agonist
    • C.J. Langmead, V.A. Fry, I.T. Forbes, C.L. Branch, A. Christopoulos, and M.D. Wood Probing the molecular mechanism of interaction between 4-n-butyl-1-[4-(2-methylphenyl)-4-oxo-1-butyl]-piperidine (AC-42) and the muscarinic M(1) receptor: direct pharmacological evidence that AC-42 is an allosteric agonist Mol Pharmacol 69 2006 236 246
    • (2006) Mol Pharmacol , vol.69 , pp. 236-246
    • Langmead, C.J.1    Fry, V.A.2    Forbes, I.T.3    Branch, C.L.4    Christopoulos, A.5    Wood, M.D.6
  • 55
    • 33644847375 scopus 로고    scopus 로고
    • Microdomains of intracellular Ca2 +: Molecular determinants and functional consequences
    • R. Rizzuto, and T. Pozzan Microdomains of intracellular Ca2 +: molecular determinants and functional consequences Physiol Rev 86 2006 369 408
    • (2006) Physiol Rev , vol.86 , pp. 369-408
    • Rizzuto, R.1    Pozzan, T.2
  • 56
    • 0031260472 scopus 로고    scopus 로고
    • A bioluminescent assay for agonist activity at potentially any G-protein-coupled receptor
    • J. Stables, A. Green, F. Marshall, N. Fraser, E. Knight, and M. Sautel A bioluminescent assay for agonist activity at potentially any G-protein-coupled receptor Anal Biochem 252 1997 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
  • 58
    • 46149110286 scopus 로고    scopus 로고
    • Characterization of the 5-HT2b receptor in evaluation of aequorin detection of calcium mobilization for miniaturized GPCR high-throughput screening
    • M.A. Gilchrist, A. Cacace, and D.G. Harden Characterization of the 5-HT2b receptor in evaluation of aequorin detection of calcium mobilization for miniaturized GPCR high-throughput screening J Biomol Screen 13 2008 486 493
    • (2008) J Biomol Screen , vol.13 , pp. 486-493
    • Gilchrist, M.A.1    Cacace, A.2    Harden, D.G.3
  • 59
    • 77950691434 scopus 로고    scopus 로고
    • Aequorin functional assay for characterization of G-protein-coupled receptors: Implementation with cryopreserved transiently transfected cells
    • B. Jones, B. Holskin, S. Meyer, T. Ung, V. Dupriez, and S.Y. Flores Aequorin functional assay for characterization of G-protein-coupled receptors: implementation with cryopreserved transiently transfected cells Anal Biochem 400 2010 184 189
    • (2010) Anal Biochem , vol.400 , pp. 184-189
    • Jones, B.1    Holskin, B.2    Meyer, S.3    Ung, T.4    Dupriez, V.5    Flores, S.Y.6
  • 60
    • 77958134183 scopus 로고    scopus 로고
    • The tetrahydroisoquinoline derivative SB269,652 is an allosteric antagonist at dopamine D3 and D2 receptors
    • E. Silvano, M.J. Millan, C.M. la Cour, Y. Han, L. Duan, and S.A. Griffin The tetrahydroisoquinoline derivative SB269,652 is an allosteric antagonist at dopamine D3 and D2 receptors Mol Pharmacol 78 2010 925 934
    • (2010) Mol Pharmacol , vol.78 , pp. 925-934
    • Silvano, E.1    Millan, M.J.2    La Cour, C.M.3    Han, Y.4    Duan, L.5    Griffin, S.A.6
  • 61
    • 34047183687 scopus 로고    scopus 로고
    • Evaluation of cellular dielectric spectroscopy, a whole-cell, label-free technology for drug discovery on Gi-coupled GPCRs
    • M.F. Peters, K.S. Knappenberger, D. Wilkins, L.A. Sygowski, L.A. Lazor, and J. Liu Evaluation of cellular dielectric spectroscopy, a whole-cell, label-free technology for drug discovery on Gi-coupled GPCRs J Biomol Screen 12 2007 312 319
    • (2007) J Biomol Screen , vol.12 , pp. 312-319
    • Peters, M.F.1    Knappenberger, K.S.2    Wilkins, D.3    Sygowski, L.A.4    Lazor, L.A.5    Liu, J.6
  • 62
    • 77952067930 scopus 로고    scopus 로고
    • Comparing label-free biosensors for pharmacological screening with cell-based functional assays
    • M.F. Peters, F. Vaillancourt, M. Heroux, M. Valiquette, and C.W. Scott Comparing label-free biosensors for pharmacological screening with cell-based functional assays Assay Drug Dev Technol 8 2010 219 227
    • (2010) Assay Drug Dev Technol , vol.8 , pp. 219-227
    • Peters, M.F.1    Vaillancourt, F.2    Heroux, M.3    Valiquette, M.4    Scott, C.W.5
  • 64
    • 33845876624 scopus 로고    scopus 로고
    • Cellular dielectric spectroscopy: A label-free comprehensive platform for functional evaluation of endogenous receptors
    • E. Verdonk, K. Johnson, R. McGuinness, G. Leung, Y.W. Chen, and H.R. Tang Cellular dielectric spectroscopy: a label-free comprehensive platform for functional evaluation of endogenous receptors Assay Drug Dev Technol 4 2006 609 619
    • (2006) Assay Drug Dev Technol , vol.4 , pp. 609-619
    • Verdonk, E.1    Johnson, K.2    McGuinness, R.3    Leung, G.4    Chen, Y.W.5    Tang, H.R.6
  • 65
    • 41649109866 scopus 로고    scopus 로고
    • Back to basics: Label-free technologies for small molecule screening
    • A.K. Shiau, M.E. Massari, and C.C. Ozbal Back to basics: label-free technologies for small molecule screening Comb Chem High Throughput Screen 11 2008 231 237
    • (2008) Comb Chem High Throughput Screen , vol.11 , pp. 231-237
    • Shiau, A.K.1    Massari, M.E.2    Ozbal, C.C.3
  • 67
    • 70349758970 scopus 로고    scopus 로고
    • A 100K well screen for a muscarinic receptor using the Epic label-free system - A reflection on the benefits of the label-free approach to screening seven-transmembrane receptors
    • K. Dodgson, L. Gedge, D.C. Murray, and M. Coldwell A 100K well screen for a muscarinic receptor using the Epic label-free system - a reflection on the benefits of the label-free approach to screening seven-transmembrane receptors J Recept Signal Transduct Res 29 2009 163 172
    • (2009) J Recept Signal Transduct Res , vol.29 , pp. 163-172
    • Dodgson, K.1    Gedge, L.2    Murray, D.C.3    Coldwell, M.4
  • 68
    • 84864762542 scopus 로고    scopus 로고
    • Modulating cell-cell communication with a high-throughput label-free cell assay
    • G. Li, F. Lai, and Y. Fang Modulating cell-cell communication with a high-throughput label-free cell assay J Lab Autom 17 2012 6 15
    • (2012) J Lab Autom , vol.17 , pp. 6-15
    • Li, G.1    Lai, F.2    Fang, Y.3
  • 69
    • 79953309698 scopus 로고    scopus 로고
    • Conjugated linoleic acids mediate insulin release through islet G protein-coupled receptor FFA1/GPR40
    • J. Schmidt, K. Liebscher, N. Merten, M. Grundmann, M. Mielenz, and H. Sauerwein Conjugated linoleic acids mediate insulin release through islet G protein-coupled receptor FFA1/GPR40 J Biol Chem 286 2011 11890 11894
    • (2011) J Biol Chem , vol.286 , pp. 11890-11894
    • Schmidt, J.1    Liebscher, K.2    Merten, N.3    Grundmann, M.4    Mielenz, M.5    Sauerwein, H.6
  • 70
    • 40749084402 scopus 로고    scopus 로고
    • Evaluation of dynamic mass redistribution technology for pharmacological studies of recombinant and endogenously expressed g protein-coupled receptors
    • P.H. Lee, A. Gao, C. van Staden, J. Ly, J. Salon, and A. Xu Evaluation of dynamic mass redistribution technology for pharmacological studies of recombinant and endogenously expressed g protein-coupled receptors Drug Dev Technol 6 2008 83 94
    • (2008) Drug Dev Technol , vol.6 , pp. 83-94
    • Lee, P.H.1    Gao, A.2    Van Staden, C.3    Ly, J.4    Salon, J.5    Xu, A.6
  • 71
    • 33846933305 scopus 로고    scopus 로고
    • Optical biosensors for monitoring dynamic mass redistribution in living cells mediated by epidermal growth factor receptor activation
    • Y. Fang, A. Ferrie, N. Fontaine, and P. Ki Yuen Optical biosensors for monitoring dynamic mass redistribution in living cells mediated by epidermal growth factor receptor activation Conf Proc IEEE Eng Med Biol Soc 1 2005 666 669
    • (2005) Conf Proc IEEE Eng Med Biol Soc , vol.1 , pp. 666-669
    • Fang, Y.1    Ferrie, A.2    Fontaine, N.3    Ki Yuen, P.4
  • 72
    • 34547430160 scopus 로고    scopus 로고
    • Optical biosensor differentiates signaling of endogenous PAR1 and PAR2 in A431 cells
    • Y. Fang, and A.M. Ferrie Optical biosensor differentiates signaling of endogenous PAR1 and PAR2 in A431 cells BMC Cell Biol 8 2007 24
    • (2007) BMC Cell Biol , vol.8 , pp. 24
    • Fang, Y.1    Ferrie, A.M.2
  • 73
    • 39649108870 scopus 로고    scopus 로고
    • Label-free optical biosensor for ligand-directed functional selectivity acting on beta(2) adrenoceptor in living cells
    • Y. Fang, and A.M. Ferrie Label-free optical biosensor for ligand-directed functional selectivity acting on beta(2) adrenoceptor in living cells FEBS Lett 582 2008 558 564
    • (2008) FEBS Lett , vol.582 , pp. 558-564
    • Fang, Y.1    Ferrie, A.M.2
  • 75
    • 67650373898 scopus 로고    scopus 로고
    • Resonant waveguide grating biosensor for whole-cell GPCR assays
    • Y. Fang, A.M. Ferrie, and E. Tran Resonant waveguide grating biosensor for whole-cell GPCR assays Methods Mol Biol 552 2009 239 252
    • (2009) Methods Mol Biol , vol.552 , pp. 239-252
    • Fang, Y.1    Ferrie, A.M.2    Tran, E.3
  • 76
    • 33947217218 scopus 로고    scopus 로고
    • Non-invasive optical biosensor for assaying endogenous G protein-coupled receptors in adherent cells
    • Y. Fang, G. Li, and A.M. Ferrie Non-invasive optical biosensor for assaying endogenous G protein-coupled receptors in adherent cells J Pharmacol Toxicol Methods 55 2007 314 322
    • (2007) J Pharmacol Toxicol Methods , vol.55 , pp. 314-322
    • Fang, Y.1    Li, G.2    Ferrie, A.M.3
  • 77
    • 81355148507 scopus 로고    scopus 로고
    • GPCRs regulate the assembly of a multienzyme complex for purine biosynthesis
    • F. Verrier, S. An, A.M. Ferrie, H. Sun, M. Kyoung, and H. Deng GPCRs regulate the assembly of a multienzyme complex for purine biosynthesis Nat Chem Biol 7 2011 909 915
    • (2011) Nat Chem Biol , vol.7 , pp. 909-915
    • Verrier, F.1    An, S.2    Ferrie, A.M.3    Sun, H.4    Kyoung, M.5    Deng, H.6
  • 78
    • 80054935789 scopus 로고    scopus 로고
    • Discovery of 2-(4-methylfuran-2(5H)-ylidene)malononitrile and thieno[3,2-b]thiophene-2-carboxylic acid derivatives as G protein-coupled receptor 35 (GPR35) agonists
    • H. Deng, H. Hu, M. He, J. Hu, W. Niu, and A.M. Ferrie Discovery of 2-(4-methylfuran-2(5H)-ylidene)malononitrile and thieno[3,2-b]thiophene-2- carboxylic acid derivatives as G protein-coupled receptor 35 (GPR35) agonists J Med Chem 54 2011 7385 7396
    • (2011) J Med Chem , vol.54 , pp. 7385-7396
    • Deng, H.1    Hu, H.2    He, M.3    Hu, J.4    Niu, W.5    Ferrie, A.M.6
  • 79
    • 79955631465 scopus 로고    scopus 로고
    • Agonist-directed desensitization of the beta2-Adrenergic receptor
    • V. Goral, Y. Jin, H. Sun, A.M. Ferrie, Q. Wu, and Y. Fang Agonist-directed desensitization of the beta2-Adrenergic receptor PLoS One 6 2011 e19282
    • (2011) PLoS One , vol.6 , pp. 19282
    • Goral, V.1    Jin, Y.2    Sun, H.3    Ferrie, A.M.4    Wu, Q.5    Fang, Y.6
  • 80
    • 80053899050 scopus 로고    scopus 로고
    • Label-free integrative pharmacology on-target of drugs at the beta(2)-Adrenergic receptor
    • A.M. Ferrie, H. Sun, and Y. Fang Label-free integrative pharmacology on-target of drugs at the beta(2)-Adrenergic receptor Sci Rep 1 2011 33
    • (2011) Sci Rep , vol.1 , pp. 33
    • Ferrie, A.M.1    Sun, H.2    Fang, Y.3
  • 81
    • 78650667671 scopus 로고    scopus 로고
    • Resonant waveguide grating imager for live cell sensing
    • A.M. Ferrie, Q. Wu, and Y. Fang Resonant waveguide grating imager for live cell sensing Appl Phys Lett 97 2010 223704
    • (2010) Appl Phys Lett , vol.97 , pp. 223704
    • Ferrie, A.M.1    Wu, Q.2    Fang, Y.3
  • 82
    • 84860389995 scopus 로고    scopus 로고
    • Dynamic mass redistribution as a means to measure and differentiate signaling via opioid and cannabinoid receptors
    • E.E. Codd, J.R. Mabus, B.S. Murray, S.P. Zhang, and C.M. Flores Dynamic mass redistribution as a means to measure and differentiate signaling via opioid and cannabinoid receptors Assay Drug Dev Technol 9 2011 362 372
    • (2011) Assay Drug Dev Technol , vol.9 , pp. 362-372
    • Codd, E.E.1    Mabus, J.R.2    Murray, B.S.3    Zhang, S.P.4    Flores, C.M.5
  • 83
    • 0142090782 scopus 로고    scopus 로고
    • (-)-PHCCC, a positive allosteric modulator of mGluR4: Characterization, mechanism of action, and neuroprotection
    • M. Maj, V. Bruno, Z. Dragic, R. Yamamoto, G. Battaglia, and W. Inderbitzin (-)-PHCCC, a positive allosteric modulator of mGluR4: characterization, mechanism of action, and neuroprotection Neuropharmacology 45 2003 895 906
    • (2003) Neuropharmacology , vol.45 , pp. 895-906
    • Maj, M.1    Bruno, V.2    Dragic, Z.3    Yamamoto, R.4    Battaglia, G.5    Inderbitzin, W.6
  • 84
    • 0345686620 scopus 로고    scopus 로고
    • Allosteric modulation of group III metabotropic glutamate receptor 4: A potential approach to Parkinson's disease treatment
    • M.J. Marino, D.L. Williams Jr., J.A. O'Brien, O. Valenti, T.P. McDonald, and M.K. Clements Allosteric modulation of group III metabotropic glutamate receptor 4: a potential approach to Parkinson's disease treatment Proc Natl Acad Sci USA 100 2003 13668 13673
    • (2003) Proc Natl Acad Sci USA , vol.100 , pp. 13668-13673
    • Marino, M.J.1    Williams, Jr.D.L.2    O'Brien, J.A.3    Valenti, O.4    McDonald, T.P.5    Clements, M.K.6
  • 85
    • 54349110319 scopus 로고    scopus 로고
    • Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4
    • C.M. Niswender, K.A. Johnson, C.D. Weaver, C.K. Jones, Z. Xiang, and Q. Luo Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4 Mol Pharmacol 74 2008 1345 1358
    • (2008) Mol Pharmacol , vol.74 , pp. 1345-1358
    • Niswender, C.M.1    Johnson, K.A.2    Weaver, C.D.3    Jones, C.K.4    Xiang, Z.5    Luo, Q.6
  • 86
    • 84858121231 scopus 로고    scopus 로고
    • Tools for GPCR drug discovery
    • R. Zhang, and X. Xie Tools for GPCR drug discovery Acta Pharmacol Sin 33 2012 372 384
    • (2012) Acta Pharmacol Sin , vol.33 , pp. 372-384
    • Zhang, R.1    Xie, X.2
  • 87
    • 49449091293 scopus 로고    scopus 로고
    • Profiling of multiple signal pathway activities by multiplexing antibody and GFP-based translocation assays
    • U. Henriksen, J. Fog, F. Loechel, and M. Praestegaard Profiling of multiple signal pathway activities by multiplexing antibody and GFP-based translocation assays Comb Chem High Throughput Screen 11 2008 537 544
    • (2008) Comb Chem High Throughput Screen , vol.11 , pp. 537-544
    • Henriksen, U.1    Fog, J.2    Loechel, F.3    Praestegaard, M.4
  • 88
    • 0016374975 scopus 로고
    • A highly sensitive adenylate cyclase assay
    • Y. Salomon, C. Londos, and M. Rodbell A highly sensitive adenylate cyclase assay Anal Biochem 58 1974 541 548
    • (1974) Anal Biochem , vol.58 , pp. 541-548
    • Salomon, Y.1    Londos, C.2    Rodbell, M.3
  • 89
    • 0020580023 scopus 로고
    • Thrombin-induced phosphodiesteratic cleavage of phosphatidylinositol bisphosphate in human platelets
    • B.W. Agranoff, P. Murthy, and E.B. Seguin Thrombin-induced phosphodiesteratic cleavage of phosphatidylinositol bisphosphate in human platelets J Biol Chem 258 1983 2076 2078
    • (1983) J Biol Chem , vol.258 , pp. 2076-2078
    • Agranoff, B.W.1    Murthy, P.2    Seguin, E.B.3
  • 91
    • 0021334519 scopus 로고
    • Guanine nucleotide-binding regulatory proteins and dual control of adenylate cyclase
    • A.G. Gilman Guanine nucleotide-binding regulatory proteins and dual control of adenylate cyclase J Clin Invest 73 1984 1 4
    • (1984) J Clin Invest , vol.73 , pp. 1-4
    • Gilman, A.G.1
  • 92
    • 0034711397 scopus 로고    scopus 로고
    • Beta-Arrestin 2: A receptor-regulated MAPK scaffold for the activation of JNK3
    • P.H. McDonald, C.W. Chow, W.E. Miller, S.A. Laporte, M.E. Field, and F.T. Lin Beta-Arrestin 2: a receptor-regulated MAPK scaffold for the activation of JNK3 Science 290 2000 1574 1577
    • (2000) Science , vol.290 , pp. 1574-1577
    • McDonald, P.H.1    Chow, C.W.2    Miller, W.E.3    Laporte, S.A.4    Field, M.E.5    Lin, F.T.6
  • 93
    • 77953181018 scopus 로고    scopus 로고
    • An emerging role for kinase screening in GPCR drug discovery
    • R.I. Osmond, M.F. Crouch, and V.J. Dupriez An emerging role for kinase screening in GPCR drug discovery Curr Opin Mol Ther 12 2010 305 315
    • (2010) Curr Opin Mol Ther , vol.12 , pp. 305-315
    • Osmond, R.I.1    Crouch, M.F.2    Dupriez, V.J.3
  • 94
    • 33646516019 scopus 로고    scopus 로고
    • Mechanisms of ERK1/2 regulation by seven-transmembrane-domain receptors
    • T.D. Werry, A. Christopoulos, and P.M. Sexton Mechanisms of ERK1/2 regulation by seven-transmembrane-domain receptors Curr Pharm Des 12 2006 1683 1702
    • (2006) Curr Pharm des , vol.12 , pp. 1683-1702
    • Werry, T.D.1    Christopoulos, A.2    Sexton, P.M.3
  • 95
    • 17644402459 scopus 로고    scopus 로고
    • Transduction of receptor signals by beta-Arrestins
    • R.J. Lefkowitz, and S.K. Shenoy Transduction of receptor signals by beta-Arrestins Science 308 2005 512 517
    • (2005) Science , vol.308 , pp. 512-517
    • Lefkowitz, R.J.1    Shenoy, S.K.2
  • 97
    • 0035487327 scopus 로고    scopus 로고
    • Classical and new roles of beta-Arrestins in the regulation of G-protein-coupled receptors
    • K.L. Pierce, and R.J. Lefkowitz Classical and new roles of beta-Arrestins in the regulation of G-protein-coupled receptors Nat Rev Neurosci 2 2001 727 733
    • (2001) Nat Rev Neurosci , vol.2 , pp. 727-733
    • Pierce, K.L.1    Lefkowitz, R.J.2
  • 98
    • 0014854395 scopus 로고
    • A protein binding assay for adenosine 3′:5′-cyclic monophosphate
    • A.G. Gilman A protein binding assay for adenosine 3′:5′- cyclic monophosphate Proc Natl Acad Sci USA 67 1970 305 312
    • (1970) Proc Natl Acad Sci USA , vol.67 , pp. 305-312
    • Gilman, A.G.1
  • 99
    • 78751501237 scopus 로고    scopus 로고
    • Risperidone-induced inactivation and clozapine-induced reactivation of rat cortical astrocyte 5-hydroxytryptamine(7) receptors: Evidence for in situ G protein-coupled receptor homodimer protomer cross-talk
    • C. Smith, N. Toohey, J.A. Knight, M.T. Klein, and M. Teitler Risperidone-induced inactivation and clozapine-induced reactivation of rat cortical astrocyte 5-hydroxytryptamine(7) receptors: evidence for in situ G protein-coupled receptor homodimer protomer cross-talk Mol Pharmacol 79 2011 318 325
    • (2011) Mol Pharmacol , vol.79 , pp. 318-325
    • Smith, C.1    Toohey, N.2    Knight, J.A.3    Klein, M.T.4    Teitler, M.5
  • 100
    • 84862864622 scopus 로고    scopus 로고
    • Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models
    • G.J. Digby, M.J. Noetzel, M. Bubser, T.J. Utley, A.G. Walker, and N.E. Byun Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models J Neurosci 32 2012 8532 8544
    • (2012) J Neurosci , vol.32 , pp. 8532-8544
    • Digby, G.J.1    Noetzel, M.J.2    Bubser, M.3    Utley, T.J.4    Walker, A.G.5    Byun, N.E.6
  • 101
    • 84861307152 scopus 로고    scopus 로고
    • Distribution of 5-ht(1E) receptors in the mammalian brain and cerebral vasculature: An immunohistochemical and pharmacological study
    • M. Klein, and M. Teitler Distribution of 5-ht(1E) receptors in the mammalian brain and cerebral vasculature: an immunohistochemical and pharmacological study Br J Pharmacol 166 2012 1290 1302
    • (2012) Br J Pharmacol , vol.166 , pp. 1290-1302
    • Klein, M.1    Teitler, M.2
  • 102
    • 0016231591 scopus 로고
    • Biosynthesis of myo-inositol in rat mammary gland. Isolation and properties of the enzymes
    • W.F. Naccarato, R.E. Ray, and W.W. Wells Biosynthesis of myo-inositol in rat mammary gland. Isolation and properties of the enzymes Arch Biochem Biophys 164 1974 194 201
    • (1974) Arch Biochem Biophys , vol.164 , pp. 194-201
    • Naccarato, W.F.1    Ray, R.E.2    Wells, W.W.3
  • 103
    • 0346279807 scopus 로고    scopus 로고
    • Evaluation of fluorescent compound interference in 4 fluorescence polarization assays: 2 kinases, 1 protease, and 1 phosphatase
    • T.C. Turek-Etienne, E.C. Small, S.C. Soh, T.A. Xin, P.V. Gaitonde, and E.B. Barrabee Evaluation of fluorescent compound interference in 4 fluorescence polarization assays: 2 kinases, 1 protease, and 1 phosphatase J Biomol Screen 8 2003 176 184
    • (2003) J Biomol Screen , vol.8 , pp. 176-184
    • Turek-Etienne, T.C.1    Small, E.C.2    Soh, S.C.3    Xin, T.A.4    Gaitonde, P.V.5    Barrabee, E.B.6
  • 104
    • 0030798464 scopus 로고    scopus 로고
    • Time-resolved fluorometry: An overview of the labels and core technologies for drug screening applications
    • I. Hemmilä, and S. Webb Time-resolved fluorometry: an overview of the labels and core technologies for drug screening applications Drug Discov Today 2 1997 373 381
    • (1997) Drug Discov Today , vol.2 , pp. 373-381
    • Hemmilä, I.1    Webb, S.2
  • 105
    • 0028982948 scopus 로고
    • Distinct pathways of Gi- and Gq-mediated mitogen-Activated protein kinase activation
    • B.E. Hawes, T. van Biesen, W.J. Koch, L.M. Luttrell, and R.J. Lefkowitz Distinct pathways of Gi- and Gq-mediated mitogen-Activated protein kinase activation J Biol Chem 270 1995 17148 17153
    • (1995) J Biol Chem , vol.270 , pp. 17148-17153
    • Hawes, B.E.1    Van Biesen, T.2    Koch, W.J.3    Luttrell, L.M.4    Lefkowitz, R.J.5
  • 106
    • 0034647517 scopus 로고    scopus 로고
    • Signaling from G protein-coupled receptors to ERK5/Big MAPK 1 involves Galpha q and Galpha 12/13 families of heterotrimeric G proteins. Evidence for the existence of a novel Ras and Rho-independent pathway
    • S. Fukuhara, M.J. Marinissen, M. Chiariello, and J.S. Gutkind Signaling from G protein-coupled receptors to ERK5/Big MAPK 1 involves Galpha q and Galpha 12/13 families of heterotrimeric G proteins. Evidence for the existence of a novel Ras AND Rho-independent pathway J Biol Chem 275 2000 21730 21736
    • (2000) J Biol Chem , vol.275 , pp. 21730-21736
    • Fukuhara, S.1    Marinissen, M.J.2    Chiariello, M.3    Gutkind, J.S.4
  • 107
    • 0029036494 scopus 로고
    • Differential activation of cytosolic phospholipase A2 (cPLA2) by thrombin and thrombin receptor agonist peptide in human platelets. Evidence for activation of cPLA2 independent of the mitogen-Activated protein kinases ERK1/2
    • R.M. Kramer, E.F. Roberts, P.A. Hyslop, B.G. Utterback, K.Y. Hui, and J.A. Jakubowski Differential activation of cytosolic phospholipase A2 (cPLA2) by thrombin and thrombin receptor agonist peptide in human platelets. Evidence for activation of cPLA2 independent of the mitogen-Activated protein kinases ERK1/2 J Biol Chem 270 1995 14816 14823
    • (1995) J Biol Chem , vol.270 , pp. 14816-14823
    • Kramer, R.M.1    Roberts, E.F.2    Hyslop, P.A.3    Utterback, B.G.4    Hui, K.Y.5    Jakubowski, J.A.6
  • 108
    • 9544244753 scopus 로고    scopus 로고
    • Luminescent oxygen channeling assay (LOCI): Sensitive, broadly applicable homogeneous immunoassay method
    • E.F. Ullman, H. Kirakossian, A.C. Switchenko, J. Ishkanian, M. Ericson, and C.A. Wartchow Luminescent oxygen channeling assay (LOCI): sensitive, broadly applicable homogeneous immunoassay method Clin Chem 42 1996 1518 1526
    • (1996) Clin Chem , vol.42 , pp. 1518-1526
    • Ullman, E.F.1    Kirakossian, H.2    Switchenko, A.C.3    Ishkanian, J.4    Ericson, M.5    Wartchow, C.A.6
  • 109
    • 0028276006 scopus 로고
    • Luminescent oxygen channeling immunoassay: Measurement of particle binding kinetics by chemiluminescence
    • E.F. Ullman, H. Kirakossian, S. Singh, Z.P. Wu, B.R. Irvin, and J.S. Pease Luminescent oxygen channeling immunoassay: measurement of particle binding kinetics by chemiluminescence Proc Natl Acad Sci USA 91 1994 5426 5430
    • (1994) Proc Natl Acad Sci USA , vol.91 , pp. 5426-5430
    • Ullman, E.F.1    Kirakossian, H.2    Singh, S.3    Wu, Z.P.4    Irvin, B.R.5    Pease, J.S.6
  • 110
    • 2142829476 scopus 로고    scopus 로고
    • Development of a high-throughput screening assay for inhibitors of aggrecan cleavage using luminescent oxygen channeling (AlphaScreen)
    • J. Peppard, F. Glickman, Y. He, S.I. Hu, J. Doughty, and R. Goldberg Development of a high-throughput screening assay for inhibitors of aggrecan cleavage using luminescent oxygen channeling (AlphaScreen) J Biomol Screen 8 2003 149 156
    • (2003) J Biomol Screen , vol.8 , pp. 149-156
    • Peppard, J.1    Glickman, F.2    He, Y.3    Hu, S.I.4    Doughty, J.5    Goldberg, R.6
  • 111
    • 26944466076 scopus 로고    scopus 로고
    • GPCR screening via ERK 1/2: A novel platform for screening G protein-coupled receptors
    • R.I. Osmond, A. Sheehan, R. Borowicz, E. Barnett, G. Harvey, and C. Turner GPCR screening via ERK 1/2: a novel platform for screening G protein-coupled receptors J Biomol Screen 10 2005 730 737
    • (2005) J Biomol Screen , vol.10 , pp. 730-737
    • Osmond, R.I.1    Sheehan, A.2    Borowicz, R.3    Barnett, E.4    Harvey, G.5    Turner, C.6
  • 112
    • 84855966123 scopus 로고    scopus 로고
    • NMDA-induced ERK signalling is mediated by NR2B subunit in rat cortical neurons and switches from positive to negative depending on stage of development
    • A. Sava, E. Formaggio, C. Carignani, F. Andreetta, E. Bettini, and C. Griffante NMDA-induced ERK signalling is mediated by NR2B subunit in rat cortical neurons and switches from positive to negative depending on stage of development Neuropharmacology 62 2012 925 932
    • (2012) Neuropharmacology , vol.62 , pp. 925-932
    • Sava, A.1    Formaggio, E.2    Carignani, C.3    Andreetta, F.4    Bettini, E.5    Griffante, C.6
  • 113
    • 0000025689 scopus 로고
    • Phosphodiesterase activation by photoexcited rhodopsin is quenched when rhodopsin is phosphorylated and binds the intrinsic 48-kDa protein of rod outer segments
    • U. Wilden, S.W. Hall, and H. Kuhn Phosphodiesterase activation by photoexcited rhodopsin is quenched when rhodopsin is phosphorylated and binds the intrinsic 48-kDa protein of rod outer segments Proc Natl Acad Sci USA 83 1986 1174 1178
    • (1986) Proc Natl Acad Sci USA , vol.83 , pp. 1174-1178
    • Wilden, U.1    Hall, S.W.2    Kuhn, H.3
  • 114
    • 0023515309 scopus 로고
    • Functional desensitization of the isolated beta-Adrenergic receptor by the beta-Adrenergic receptor kinase: Potential role of an analog of the retinal protein arrestin (48-kDa protein)
    • J.L. Benovic, H. Kuhn, I. Weyand, J. Codina, M.G. Caron, and R.J. Lefkowitz Functional desensitization of the isolated beta-Adrenergic receptor by the beta-Adrenergic receptor kinase: potential role of an analog of the retinal protein arrestin (48-kDa protein) Proc Natl Acad Sci USA 84 1987 8879 8882
    • (1987) Proc Natl Acad Sci USA , vol.84 , pp. 8879-8882
    • Benovic, J.L.1    Kuhn, H.2    Weyand, I.3    Codina, J.4    Caron, M.G.5    Lefkowitz, R.J.6
  • 115
    • 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
    • R.H. Oakley, C.C. Hudson, R.D. Cruickshank, D.M. Meyers, R.E. Payne Jr., and S.M. Rhem The cellular distribution of fluorescently labeled arrestins provides a robust, sensitive, and universal assay for screening G protein-coupled receptors Assay Drug Dev Technol 1 2002 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
  • 116
    • 67649321841 scopus 로고    scopus 로고
    • G protein-coupled receptor kinase-mediated phosphorylation regulates post-endocytic trafficking of the D2 dopamine receptor
    • Y. Namkung, C. Dipace, J.A. Javitch, and D.R. Sibley G protein-coupled receptor kinase-mediated phosphorylation regulates post-endocytic trafficking of the D2 dopamine receptor J Biol Chem 284 2009 15038 15051
    • (2009) J Biol Chem , vol.284 , pp. 15038-15051
    • Namkung, Y.1    Dipace, C.2    Javitch, J.A.3    Sibley, D.R.4
  • 117
    • 0027284218 scopus 로고
    • Binding of wild type and chimeric arrestins to the m2 muscarinic cholinergic receptor
    • V.V. Gurevich, R.M. Richardson, C.M. Kim, M.M. Hosey, and J.L. Benovic Binding of wild type and chimeric arrestins to the m2 muscarinic cholinergic receptor J Biol Chem 268 1993 16879 16882
    • (1993) J Biol Chem , vol.268 , pp. 16879-16882
    • Gurevich, V.V.1    Richardson, R.M.2    Kim, C.M.3    Hosey, M.M.4    Benovic, J.L.5
  • 118
    • 69549121564 scopus 로고    scopus 로고
    • A homogeneous fluorescent live-cell assay for measuring 7-transmembrane receptor activity and agonist functional selectivity through beta-Arrestin recruitment
    • B.J. Hanson, J. Wetter, M.R. Bercher, L. Kopp, M. Fuerstenau-Sharp, and K.L. Vedvik A homogeneous fluorescent live-cell assay for measuring 7-transmembrane receptor activity and agonist functional selectivity through beta-Arrestin recruitment J Biomol Screen 14 2009 798 810
    • (2009) J Biomol Screen , vol.14 , pp. 798-810
    • Hanson, B.J.1    Wetter, J.2    Bercher, M.R.3    Kopp, L.4    Fuerstenau-Sharp, M.5    Vedvik, K.L.6
  • 119
    • 12344252237 scopus 로고    scopus 로고
    • AP-1 subunits: Quarrel and harmony among siblings
    • J. Hess, P. Angel, and M. Schorpp-Kistner AP-1 subunits: quarrel and harmony among siblings J Cell Sci 117 2004 5965 5973
    • (2004) J Cell Sci , vol.117 , pp. 5965-5973
    • Hess, J.1    Angel, P.2    Schorpp-Kistner, M.3
  • 120
    • 59449085290 scopus 로고    scopus 로고
    • Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: Design, synthesis, and effects on behavior
    • S. Butini, S. Gemma, G. Campiani, S. Franceschini, F. Trotta, and M. Borriello Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior J Med Chem 52 2009 151 169
    • (2009) J Med Chem , vol.52 , pp. 151-169
    • Butini, S.1    Gemma, S.2    Campiani, G.3    Franceschini, S.4    Trotta, F.5    Borriello, M.6
  • 121
    • 79951962147 scopus 로고    scopus 로고
    • CREB and the CRTC co-Activators: Sensors for hormonal and metabolic signals
    • J.Y. Altarejos, and M. Montminy CREB and the CRTC co-Activators: sensors for hormonal and metabolic signals Nat Rev Mol Cell Biol 12 2011 141 151
    • (2011) Nat Rev Mol Cell Biol , vol.12 , pp. 141-151
    • Altarejos, J.Y.1    Montminy, M.2
  • 122
    • 79954573504 scopus 로고    scopus 로고
    • The role of CREB signaling in Alzheimer's disease and other cognitive disorders
    • C.A. Saura, and J. Valero The role of CREB signaling in Alzheimer's disease and other cognitive disorders Rev Neurosci 22 2011 153 169
    • (2011) Rev Neurosci , vol.22 , pp. 153-169
    • Saura, C.A.1    Valero, J.2
  • 127
    • 0029812311 scopus 로고    scopus 로고
    • The classification of seven transmembrane receptors in recombinant expression systems
    • T. Kenakin The classification of seven transmembrane receptors in recombinant expression systems Pharmacol Rev 48 1996 413 463
    • (1996) Pharmacol Rev , vol.48 , pp. 413-463
    • Kenakin, T.1
  • 128
    • 84864408766 scopus 로고    scopus 로고
    • Synthesis and application of the first radioligand targeting the allosteric binding pocket of chemokine receptor CXCR3
    • V. Bernat, M.R. Heinrich, P. Baumeister, A. Buschauer, and N. Tschammer Synthesis and application of the first radioligand targeting the allosteric binding pocket of chemokine receptor CXCR3 ChemMedChem 7 2012 1481 1489
    • (2012) ChemMedChem , vol.7 , pp. 1481-1489
    • Bernat, V.1    Heinrich, M.R.2    Baumeister, P.3    Buschauer, A.4    Tschammer, N.5
  • 129
    • 0037330358 scopus 로고    scopus 로고
    • [H-3]-methoxymethyl-MTEP and [H-3]-methoxy-PEPy: Potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor
    • N.D.P. Cosford, J. Roppe, L. Tehrani, E.J. Schweiger, T.J. Seiders, and A. Chaudary [H-3]-methoxymethyl-MTEP and [H-3]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor Bioorg Med Chem Lett 13 2003 351 354
    • (2003) Bioorg Med Chem Lett , vol.13 , pp. 351-354
    • Cosford, N.D.P.1    Roppe, J.2    Tehrani, L.3    Schweiger, E.J.4    Seiders, T.J.5    Chaudary, A.6
  • 130
    • 38549139769 scopus 로고    scopus 로고
    • [3H]Org 43553, the first low-molecular-weight agonistic and allosteric radioligand for the human luteinizing hormone receptor
    • L.H. Heitman, J. Oosterom, K.M. Bonger, C.M. Timmers, P.H.G. Wiegerinck, and A.P. IJzerman [3H]Org 43553, the first low-molecular-weight agonistic and allosteric radioligand for the human luteinizing hormone receptor Mol Pharmacol 73 2008 518 524
    • (2008) Mol Pharmacol , vol.73 , pp. 518-524
    • Heitman, L.H.1    Oosterom, J.2    Bonger, K.M.3    Timmers, C.M.4    Wiegerinck, P.H.G.5    Ijzerman, A.P.6
  • 131
    • 79959508604 scopus 로고    scopus 로고
    • Identification and characterization of INCB9471, an allosteric noncompetitive small-molecule antagonist of C-C chemokine receptor 5 with potent inhibitory activity against monocyte migration and HIV-1 infection
    • N. Shin, K. Solomon, N. Zhou, K.H. Wang, V. Garlapati, and B. Thomas Identification and characterization of INCB9471, an allosteric noncompetitive small-molecule antagonist of C-C chemokine receptor 5 with potent inhibitory activity against monocyte migration and HIV-1 infection J Pharmacol Exp Ther 338 2011 228 239
    • (2011) J Pharmacol Exp Ther , vol.338 , pp. 228-239
    • Shin, N.1    Solomon, K.2    Zhou, N.3    Wang, K.H.4    Garlapati, V.5    Thomas, B.6
  • 132
    • 0031595749 scopus 로고    scopus 로고
    • Identification of a [3H]ligand for the common allosteric site of muscarinic acetylcholine M2 receptors
    • C. Tränkle, E. Mies-Klomfass, M.H.B. Cid, U. Holzgrabe, and K. Mohr Identification of a [3H]ligand for the common allosteric site of muscarinic acetylcholine M2 receptors Mol Pharmacol 54 1998 139 145
    • (1998) Mol Pharmacol , vol.54 , pp. 139-145
    • Tränkle, C.1    Mies-Klomfass, E.2    Cid, M.H.B.3    Holzgrabe, U.4    Mohr, K.5
  • 133
    • 58149193205 scopus 로고    scopus 로고
    • Allosteric modulators of GPCRs: A novel approach for the treatment of CNS disorders
    • P. Jeffrey Conn, A. Christopoulos, and C.W. Lindsley Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders Nat Rev Drug Discov 8 2009 41 54
    • (2009) Nat Rev Drug Discov , vol.8 , pp. 41-54
    • Jeffrey Conn, P.1    Christopoulos, A.2    Lindsley, C.W.3
  • 134
    • 37249089038 scopus 로고    scopus 로고
    • Synthesis and preliminary biological evaluation of 3-[(18)F]fluoro-5-(2- pyridinylethynyl)benzonitrile as a PET radiotracer for imaging metabotropic glutamate receptor subtype 5
    • J.Q. Wang, W. Tueckmantel, A. Zhu, D. Pellegrino, and A.L. Brownell Synthesis and preliminary biological evaluation of 3-[(18)F]fluoro-5-(2- pyridinylethynyl)benzonitrile as a PET radiotracer for imaging metabotropic glutamate receptor subtype 5 Synapse 61 2007 951 961
    • (2007) Synapse , vol.61 , pp. 951-961
    • Wang, J.Q.1    Tueckmantel, W.2    Zhu, A.3    Pellegrino, D.4    Brownell, A.L.5
  • 135
    • 1342323325 scopus 로고    scopus 로고
    • Application of a kinetic model to the apparently complex behavior of negative and positive allosteric modulators of muscarinic acetylcholine receptors
    • V. Avlani, L.T. May, P.M. Sexton, and A. Christopoulos Application of a kinetic model to the apparently complex behavior of negative and positive allosteric modulators of muscarinic acetylcholine receptors J Pharmacol Exp Ther 308 2004 1062 1072
    • (2004) J Pharmacol Exp Ther , vol.308 , pp. 1062-1072
    • Avlani, V.1    May, L.T.2    Sexton, P.M.3    Christopoulos, A.4
  • 136
    • 84856697011 scopus 로고    scopus 로고
    • Quantification of allosteric interactions at G protein-coupled receptors using radioligand binding assays
    • Chapter 1, Unit 1.22
    • K. Leach, P.M. Sexton, and A. Christopoulos Quantification of allosteric interactions at G protein-coupled receptors using radioligand binding assays Curr Protoc Pharmacol 2011 Chapter 1, Unit 1.22
    • (2011) Curr Protoc Pharmacol
    • Leach, K.1    Sexton, P.M.2    Christopoulos, A.3
  • 137
    • 81555222803 scopus 로고    scopus 로고
    • Identification of a novel allosteric binding site in the CXCR2 chemokine receptor
    • P. de Kruijf, H.D. Lim, L. Roumen, V.A. Renjaän, J. Zhao, and M.L. Webb Identification of a novel allosteric binding site in the CXCR2 chemokine receptor Mol Pharmacol 80 2011 1108 1118
    • (2011) Mol Pharmacol , vol.80 , pp. 1108-1118
    • De Kruijf, P.1    Lim, H.D.2    Roumen, L.3    Renjaän, V.A.4    Zhao, J.5    Webb, M.L.6
  • 138
    • 78149495647 scopus 로고    scopus 로고
    • Allosteric modulation of metabotropic glutamate receptors: Structural insights and therapeutic potential
    • K.J. Gregory, E.N. Dong, J. Meiler, and P.J. Conn Allosteric modulation of metabotropic glutamate receptors: structural insights and therapeutic potential Neuropharmacology 60 2011 66 81
    • (2011) Neuropharmacology , vol.60 , pp. 66-81
    • Gregory, K.J.1    Dong, E.N.2    Meiler, J.3    Conn, P.J.4
  • 139
    • 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
    • C. Valant, K.J. Gregory, N.E. Hall, P.J. Scammells, M.J. Lew, and P.M. Sexton 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 283 2008 29312 29321
    • (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
  • 140
    • 67849119253 scopus 로고    scopus 로고
    • An allosteric binding site at the human serotonin transporter mediates the inhibition of escitalopram by R-citalopram: Kinetic binding studies with the ALI/VFL-SI/TT mutant
    • H. Zhong, K.B. Hansen, N.J. Boyle, K. Han, G. Muske, and X. Huang An allosteric binding site at the human serotonin transporter mediates the inhibition of escitalopram by R-citalopram: kinetic binding studies with the ALI/VFL-SI/TT mutant Neurosci Lett 462 2009 207 212
    • (2009) Neurosci Lett , vol.462 , pp. 207-212
    • Zhong, H.1    Hansen, K.B.2    Boyle, N.J.3    Han, K.4    Muske, G.5    Huang, X.6
  • 141
  • 142
    • 77951223981 scopus 로고    scopus 로고
    • Identification of orthosteric and allosteric site mutations in M2 muscarinic acetylcholine receptors that contribute to ligand-selective signaling bias
    • K.J. Gregory, N.E. Hall, A.B. Tobin, P.M. Sexton, and A. Christopoulos Identification of orthosteric and allosteric site mutations in M2 muscarinic acetylcholine receptors that contribute to ligand-selective signaling bias J Biol Chem 285 2010 7459 7474
    • (2010) J Biol Chem , vol.285 , pp. 7459-7474
    • Gregory, K.J.1    Hall, N.E.2    Tobin, A.B.3    Sexton, P.M.4    Christopoulos, A.5
  • 143
    • 84856693524 scopus 로고    scopus 로고
    • Second extracellular loop of human glucagon-like peptide-1 receptor (GLP-1R) differentially regulates orthosteric but not allosteric agonist binding and function
    • C. Koole, D. Wootten, J. Simms, E.E. Savage, L.J. Miller, and A. Christopoulos Second extracellular loop of human glucagon-like peptide-1 receptor (GLP-1R) differentially regulates orthosteric but not allosteric agonist binding and function J Biol Chem 287 2012 3659 3673
    • (2012) J Biol Chem , vol.287 , pp. 3659-3673
    • Koole, C.1    Wootten, D.2    Simms, J.3    Savage, E.E.4    Miller, L.J.5    Christopoulos, A.6
  • 145
    • 80052817143 scopus 로고    scopus 로고
    • Determining allosteric modulator mechanism of action: Integration of radioligand binding and functional assay data
    • C.J. Langmead Determining allosteric modulator mechanism of action: integration of radioligand binding and functional assay data Methods Mol Biol 746 2011 195 209
    • (2011) Methods Mol Biol , vol.746 , pp. 195-209
    • Langmead, C.J.1
  • 146
    • 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
    • V. Nawaratne, K. Leach, C.C. Felder, P.M. Sexton, and A. Christopoulos Structural determinants of allosteric agonism and modulation at the M4 muscarinic acetylcholine receptor: identification of ligand-specific and global activation mechanisms J Biol Chem 285 2010 19012 19021
    • (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
  • 147
    • 0030944020 scopus 로고    scopus 로고
    • Kinetic studies of co-operativity at atrial muscarinic M2 receptors with an "infinite dilution" procedure
    • A. Christopoulos, A. Lanzafame, A. Ziegler, and F. Mitchelson Kinetic studies of co-operativity at atrial muscarinic M2 receptors with an "infinite dilution" procedure Biochem Pharmacol 53 1997 795 800
    • (1997) Biochem Pharmacol , vol.53 , pp. 795-800
    • Christopoulos, A.1    Lanzafame, A.2    Ziegler, A.3    Mitchelson, F.4
  • 148
    • 80053906571 scopus 로고    scopus 로고
    • Allosteric interactions across native adenosine-A3 receptor homodimers: Quantification using single-cell ligand-binding kinetics
    • L.T. May, L.J. Bridge, L.A. Stoddart, S.J. Briddon, and S.J. Hill Allosteric interactions across native adenosine-A3 receptor homodimers: quantification using single-cell ligand-binding kinetics FASEB J 25 2011 3465 3476
    • (2011) FASEB J , vol.25 , pp. 3465-3476
    • May, L.T.1    Bridge, L.J.2    Stoddart, L.A.3    Briddon, S.J.4    Hill, S.J.5
  • 149
    • 79956317677 scopus 로고    scopus 로고
    • G protein-coupled receptor heteromerization: A role in allosteric modulation of ligand binding
    • I. Gomes, A.P. IJzerman, K. Ye, E.L. Maillet, and L.A. Devi G protein-coupled receptor heteromerization: a role in allosteric modulation of ligand binding Mol Pharmacol 79 2011 1044 1052
    • (2011) Mol Pharmacol , vol.79 , pp. 1044-1052
    • Gomes, I.1    Ijzerman, A.P.2    Ye, K.3    Maillet, E.L.4    Devi, L.A.5
  • 150
    • 84860755958 scopus 로고    scopus 로고
    • Development of [(18)F]-PSS223 as a PET tracer for imaging of metabotropic glutamate receptor subtype 5 (mGluR5)
    • S.M. Sephton, P. Dennler, D.S. Leutwiler, L. Mu, R. Schibli, and S.D. Kramer Development of [(18)F]-PSS223 as a PET tracer for imaging of metabotropic glutamate receptor subtype 5 (mGluR5) Chimia (Aarau) 66 2012 201 204
    • (2012) Chimia (Aarau) , vol.66 , pp. 201-204
    • Sephton, S.M.1    Dennler, P.2    Leutwiler, D.S.3    Mu, L.4    Schibli, R.5    Kramer, S.D.6
  • 151
    • 79955471361 scopus 로고    scopus 로고
    • In vitro and in vivo evaluation of [18F]-FDEGPECO as a PET tracer for imaging the metabotropic glutamate receptor subtype 5 (mGluR5)
    • C.A. Wanger-Baumann, L. Mu, M. Honer, S. Belli, M.F. Alf, and P.A. Schubiger In vitro and in vivo evaluation of [18F]-FDEGPECO as a PET tracer for imaging the metabotropic glutamate receptor subtype 5 (mGluR5) Neuroimage 56 2011 984 991
    • (2011) Neuroimage , vol.56 , pp. 984-991
    • Wanger-Baumann, C.A.1    Mu, L.2    Honer, M.3    Belli, S.4    Alf, M.F.5    Schubiger, P.A.6
  • 152
    • 77955472961 scopus 로고    scopus 로고
    • Syntheses and pharmacological characterization of novel thiazole derivatives as potential mGluR5 PET ligands
    • C.A. Baumann, L. Mu, N. Wertli, S.D. Kramer, M. Honer, and P.A. Schubiger Syntheses and pharmacological characterization of novel thiazole derivatives as potential mGluR5 PET ligands Bioorg Med Chem 18 2010 6044 6054
    • (2010) Bioorg Med Chem , vol.18 , pp. 6044-6054
    • Baumann, C.A.1    Mu, L.2    Wertli, N.3    Kramer, S.D.4    Honer, M.5    Schubiger, P.A.6
  • 153
    • 77952723100 scopus 로고    scopus 로고
    • Structure-Activity relationships of fluorinated (E)-3-((6-methylpyridin- 2-yl)ethynyl)cyclohex-2-enone-O-methyloxime (ABP688) derivatives and the discovery of a high affinity analogue as a potential candidate for imaging metabotropic glutamate recepors subtype 5 (mGluR5) with positron emission tomography (PET)
    • C.A. Baumann, L. Mu, S. Johannsen, M. Honer, P.A. Schubiger, and S.M. Ametamey Structure-Activity relationships of fluorinated (E)-3-((6- methylpyridin-2-yl)ethynyl)cyclohex-2-enone-O-methyloxime (ABP688) derivatives and the discovery of a high affinity analogue as a potential candidate for imaging metabotropic glutamate recepors subtype 5 (mGluR5) with positron emission tomography (PET) J Med Chem 53 2010 4009 4017
    • (2010) J Med Chem , vol.53 , pp. 4009-4017
    • Baumann, C.A.1    Mu, L.2    Johannsen, S.3    Honer, M.4    Schubiger, P.A.5    Ametamey, S.M.6
  • 154
  • 156
    • 34447343093 scopus 로고    scopus 로고
    • Evaluation of the metabotropic glutamate receptor subtype 5 using PET and 11C-ABP688: Assessment of methods
    • V. Treyer, J. Streffer, M.T. Wyss, A. Bettio, S.M. Ametamey, and U. Fischer Evaluation of the metabotropic glutamate receptor subtype 5 using PET and 11C-ABP688: assessment of methods J Nucl Med 48 2007 1207 1215
    • (2007) J Nucl Med , vol.48 , pp. 1207-1215
    • Treyer, V.1    Streffer, J.2    Wyss, M.T.3    Bettio, A.4    Ametamey, S.M.5    Fischer, U.6
  • 157
    • 46649093145 scopus 로고    scopus 로고
    • Metabotropic glutamate receptor modulation, translational methods, and biomarkers: Relationships with anxiety
    • R.E. Nordquist, T. Steckler, J.G. Wettstein, C. Mackie, and W. Spooren Metabotropic glutamate receptor modulation, translational methods, and biomarkers: relationships with anxiety Psychopharmacology (Berl) 199 2008 389 402
    • (2008) Psychopharmacology (Berl) , vol.199 , pp. 389-402
    • Nordquist, R.E.1    Steckler, T.2    Wettstein, J.G.3    MacKie, C.4    Spooren, W.5
  • 158
    • 78649996218 scopus 로고    scopus 로고
    • Synthesis, characterization, and monkey PET studies of [(1)(8)F]MK-1312, a PET tracer for quantification of mGluR1 receptor occupancy by MK-5435
    • E.D. Hostetler, W. Eng, A.D. Joshi, S. Sanabria-Bohorquez, H. Kawamoto, and S. Ito Synthesis, characterization, and monkey PET studies of [(1)(8)F]MK-1312, a PET tracer for quantification of mGluR1 receptor occupancy by MK-5435 Synapse 65 2011 125 135
    • (2011) Synapse , vol.65 , pp. 125-135
    • Hostetler, E.D.1    Eng, W.2    Joshi, A.D.3    Sanabria-Bohorquez, S.4    Kawamoto, H.5    Ito, S.6


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