메뉴 건너뛰기




Volumn 113, Issue , 2016, Pages 747-753

Dynamics of ligand binding to GPCR: Residence time of melanocortins and its modulation

Author keywords

Binding model; Budded baculoviruses; Fluorescence anisotropy; G protein coupled receptors; Melanocortin 4 receptor; Residence time

Indexed keywords

FLUORESCENT DYE; G PROTEIN COUPLED RECEPTOR; IODINE NDP I 125; IODINE THIQ I 125; MELANOCORTIN; MELANOCORTIN 4 RECEPTOR; RADIOLIGAND; RADIOPHARMACEUTICAL AGENT; UNCLASSIFIED DRUG; LIGAND; PROTEIN BINDING;

EID: 84997417707     PISSN: 10436618     EISSN: 10961186     Source Type: Journal    
DOI: 10.1016/j.phrs.2016.05.030     Document Type: Review
Times cited : (8)

References (47)
  • 1
    • 84891751622 scopus 로고    scopus 로고
    • The druggable genome: evaluation of drug targets in clinical trials suggests major shifts in molecular class and indication
    • [1] Rask-Andersen, M., Masuram, S., Schiöth, H.B., The druggable genome: evaluation of drug targets in clinical trials suggests major shifts in molecular class and indication. Annu. Rev. Pharmacol. Toxicol. 54 (2014), 9–26.
    • (2014) Annu. Rev. Pharmacol. Toxicol. , vol.54 , pp. 9-26
    • Rask-Andersen, M.1    Masuram, S.2    Schiöth, H.B.3
  • 2
    • 33748325882 scopus 로고    scopus 로고
    • Drug-target residence time and its implications for lead optimization
    • [2] Copeland, R.A., Pompliano, D.L., Meek, T.D., Drug-target residence time and its implications for lead optimization. Nat. Rev. Drug Discov. 5 (2006), 730–739.
    • (2006) Nat. Rev. Drug Discov. , vol.5 , pp. 730-739
    • Copeland, R.A.1    Pompliano, D.L.2    Meek, T.D.3
  • 3
    • 78651175536 scopus 로고
    • The uptake of atropine and related drugs by intestinal smooth muscle of the guinea-pig in relation to acetylcholine receptors
    • [3] Paton, W.D., Rang, H.P., The uptake of atropine and related drugs by intestinal smooth muscle of the guinea-pig in relation to acetylcholine receptors. Proc. R. Soc. Lond. [Biol.] 163 (1965), 1–44.
    • (1965) Proc. R. Soc. Lond. [Biol.] , vol.163 , pp. 1-44
    • Paton, W.D.1    Rang, H.P.2
  • 4
    • 84901827515 scopus 로고    scopus 로고
    • Drug-target residence time – a case for G protein-coupled receptors
    • [4] Guo, D., Hillger, J.M., Ijzerman, A.P., Heitman, L.H., Drug-target residence time – a case for G protein-coupled receptors. Med. Res. Rev. 34 (2014), 856–892.
    • (2014) Med. Res. Rev. , vol.34 , pp. 856-892
    • Guo, D.1    Hillger, J.M.2    Ijzerman, A.P.3    Heitman, L.H.4
  • 5
    • 0023099807 scopus 로고
    • Scintillation proximity assay: a sensitive and continuous isotopic method for monitoring ligand/receptor and antigen/antibody interactions
    • [5] Udenfriend, S., Gerber, L., Nelson, N., Scintillation proximity assay: a sensitive and continuous isotopic method for monitoring ligand/receptor and antigen/antibody interactions. Anal. Biochem. 161 (1987), 494–500.
    • (1987) Anal. Biochem. , vol.161 , pp. 494-500
    • Udenfriend, S.1    Gerber, L.2    Nelson, N.3
  • 6
    • 84919346511 scopus 로고    scopus 로고
    • 1 orexin (hypocretin) receptor responses by modifying both orexin binding and the signal transduction machinery
    • 1 orexin (hypocretin) receptor responses by modifying both orexin binding and the signal transduction machinery. Br. J. Pharmacol. 171 (2014), 5816–5828.
    • (2014) Br. J. Pharmacol. , vol.171 , pp. 5816-5828
    • Putula, J.1    Pihlajamaa, T.2    Kukkonen, J.P.3
  • 7
    • 51149107449 scopus 로고    scopus 로고
    • Scintillation proximity assays in high-throughput screening
    • [7] Glickman, J.F., Schmid, A., Ferrand, S., Scintillation proximity assays in high-throughput screening. Assay Drug Devel. Technol. 6 (2008), 433–455.
    • (2008) Assay Drug Devel. Technol. , vol.6 , pp. 433-455
    • Glickman, J.F.1    Schmid, A.2    Ferrand, S.3
  • 9
    • 33847667536 scopus 로고    scopus 로고
    • Scintillation proximity assay as a high-throughput method to identify slowly dissociating nonpeptide ligand binding to the GnRH receptor
    • [9] Heise, C.E., Sullivan, S.K., Crowe, P.D., Scintillation proximity assay as a high-throughput method to identify slowly dissociating nonpeptide ligand binding to the GnRH receptor. J. Biomol. Screen. 12 (2007), 235–239.
    • (2007) J. Biomol. Screen. , vol.12 , pp. 235-239
    • Heise, C.E.1    Sullivan, S.K.2    Crowe, P.D.3
  • 10
    • 0017116267 scopus 로고
    • Direct localisation of beta-adrenoceptor sites in rat cerebellum by a new fluorescent analogue of propranolol
    • [10] Melamed, E., Lahav, M., Atlas, D., Direct localisation of beta-adrenoceptor sites in rat cerebellum by a new fluorescent analogue of propranolol. Nature 261 (1976), 420–422.
    • (1976) Nature , vol.261 , pp. 420-422
    • Melamed, E.1    Lahav, M.2    Atlas, D.3
  • 12
    • 84865518493 scopus 로고    scopus 로고
    • An update of novel screening methods for GPCR in drug discovery
    • [12] Chen, L., Jin, L., Zhou, N., An update of novel screening methods for GPCR in drug discovery. Exp. Opin. Drug Discov. 7 (2012), 791–806.
    • (2012) Exp. Opin. Drug Discov. , vol.7 , pp. 791-806
    • Chen, L.1    Jin, L.2    Zhou, N.3
  • 13
    • 84858203893 scopus 로고    scopus 로고
    • Fluorescence/bioluminescence resonance energy transfer techniques to study G-protein-coupled receptor activation and signaling
    • [13] Lohse, M.J., Nuber, S., Hoffmann, C., Fluorescence/bioluminescence resonance energy transfer techniques to study G-protein-coupled receptor activation and signaling. Pharmacol. Rev. 64 (2012), 299–336.
    • (2012) Pharmacol. Rev. , vol.64 , pp. 299-336
    • Lohse, M.J.1    Nuber, S.2    Hoffmann, C.3
  • 15
    • 84890258726 scopus 로고    scopus 로고
    • Biarsenical ligands bind to endogenous G-protein alpha-subunits and enable allosteric sensing of nucleotide binding
    • [15] Tõntson, L., Kopanchuk, S., Rinken, A., Biarsenical ligands bind to endogenous G-protein alpha-subunits and enable allosteric sensing of nucleotide binding. BMC Biochem., 14, 2013, 37.
    • (2013) BMC Biochem. , vol.14 , pp. 37
    • Tõntson, L.1    Kopanchuk, S.2    Rinken, A.3
  • 17
    • 84940556538 scopus 로고    scopus 로고
    • Characterization of the biological activities of human luteinizing hormone and chorionic gonadotropin by a Förster resonance energy transfer-based biosensor assay
    • [17] Mazina, O., Luik, T., Kopanchuk, S., Salumets, A., Rinken, A., Characterization of the biological activities of human luteinizing hormone and chorionic gonadotropin by a Förster resonance energy transfer-based biosensor assay. Anal. Lett. 48 (2015), 2799–2809.
    • (2015) Anal. Lett. , vol.48 , pp. 2799-2809
    • Mazina, O.1    Luik, T.2    Kopanchuk, S.3    Salumets, A.4    Rinken, A.5
  • 19
    • 36448965981 scopus 로고    scopus 로고
    • Pharmacology under the microscope: the use of fluorescence correlation spectroscopy to determine the properties of ligand-receptor complexes
    • [19] Briddon, S.J., Hill, S.J., Pharmacology under the microscope: the use of fluorescence correlation spectroscopy to determine the properties of ligand-receptor complexes. Trends Pharmacol. Sci. 28 (2007), 637–645.
    • (2007) Trends Pharmacol. Sci. , vol.28 , pp. 637-645
    • Briddon, S.J.1    Hill, S.J.2
  • 20
    • 84907692805 scopus 로고    scopus 로고
    • Kinetic analysis of antagonist-occupied adenosine-A3 receptors within membrane microdomains of individual cells provides evidence of receptor dimerization and allosterism
    • [20] Corriden, R., Kilpatrick, L.E., Kellam, B., Briddon, S.J., Hill, S.J., Kinetic analysis of antagonist-occupied adenosine-A3 receptors within membrane microdomains of individual cells provides evidence of receptor dimerization and allosterism. FASEB J. 28 (2014), 4211–4222.
    • (2014) FASEB J. , vol.28 , pp. 4211-4222
    • Corriden, R.1    Kilpatrick, L.E.2    Kellam, B.3    Briddon, S.J.4    Hill, S.J.5
  • 21
    • 84857467320 scopus 로고    scopus 로고
    • A novel fluorescent histamine H(1) receptor antagonist demonstrates the advantage of using fluorescence correlation spectroscopy to study the binding of lipophilic ligands
    • [21] Rose, R.H., Briddon, S.J., Hill, S.J., A novel fluorescent histamine H(1) receptor antagonist demonstrates the advantage of using fluorescence correlation spectroscopy to study the binding of lipophilic ligands. Br. J. Pharmacol. 165 (2012), 1789–1800.
    • (2012) Br. J. Pharmacol. , vol.165 , pp. 1789-1800
    • Rose, R.H.1    Briddon, S.J.2    Hill, S.J.3
  • 22
    • 84884683292 scopus 로고    scopus 로고
    • Fluorescence correlation spectroscopy analysis of serotonin, adrenergic, muscarinic, and dopamine receptor dimerization: the oligomer number puzzle
    • [22] Herrick-Davis, K., Grinde, E., Cowan, A., Mazurkiewicz, J.E., Fluorescence correlation spectroscopy analysis of serotonin, adrenergic, muscarinic, and dopamine receptor dimerization: the oligomer number puzzle. Mol. Pharmacol. 84 (2013), 630–642.
    • (2013) Mol. Pharmacol. , vol.84 , pp. 630-642
    • Herrick-Davis, K.1    Grinde, E.2    Cowan, A.3    Mazurkiewicz, J.E.4
  • 23
    • 44849096225 scopus 로고    scopus 로고
    • Cell-free assay of G-protein-coupled receptors using fluorescence polarization
    • [23] Jones, J.W., Greene, T.A., Grygon, C.A., Doranz, B.J., Brown, M.P., Cell-free assay of G-protein-coupled receptors using fluorescence polarization. J. Biomol. Screen. 13 (2008), 424–429.
    • (2008) J. Biomol. Screen. , vol.13 , pp. 424-429
    • Jones, J.W.1    Greene, T.A.2    Grygon, C.A.3    Doranz, B.J.4    Brown, M.P.5
  • 24
    • 77952744237 scopus 로고    scopus 로고
    • Fluorescence anisotropy assay for pharmacological characterization of ligand binding dynamics to melanocortin 4 receptors
    • [24] Veiksina, S., Kopanchuk, S., Rinken, A., Fluorescence anisotropy assay for pharmacological characterization of ligand binding dynamics to melanocortin 4 receptors. Anal. Biochem. 402 (2010), 32–39.
    • (2010) Anal. Biochem. , vol.402 , pp. 32-39
    • Veiksina, S.1    Kopanchuk, S.2    Rinken, A.3
  • 25
    • 77954499978 scopus 로고    scopus 로고
    • A fluorescence anisotropy assay for the muscarinic M1 G-protein-coupled receptor
    • [25] Huwiler, K.G., De Rosier, T., Hanson, B., Vogel, K.W., A fluorescence anisotropy assay for the muscarinic M1 G-protein-coupled receptor. Assay Drug Dev. Technol. 8 (2010), 356–366.
    • (2010) Assay Drug Dev. Technol. , vol.8 , pp. 356-366
    • Huwiler, K.G.1    De Rosier, T.2    Hanson, B.3    Vogel, K.W.4
  • 26
    • 84894475279 scopus 로고    scopus 로고
    • 1A receptors and their complexes with G-proteins in budded baculovirus particles using fluorescence anisotropy of Bodipy-FL-NAN-190
    • 1A receptors and their complexes with G-proteins in budded baculovirus particles using fluorescence anisotropy of Bodipy-FL-NAN-190. Neurochem. Int. 67 (2014), 32–38.
    • (2014) Neurochem. Int. , vol.67 , pp. 32-38
    • Tõntson, L.1    Kopanchuk, S.2    Rinken, A.3
  • 28
  • 30
    • 44049103958 scopus 로고    scopus 로고
    • Residence time of receptor-ligand complexes and its effect on biological function
    • [30] Tummino, P.J., Copeland, R.A., Residence time of receptor-ligand complexes and its effect on biological function. Biochemistry 47 (2008), 5481–5492.
    • (2008) Biochemistry , vol.47 , pp. 5481-5492
    • Tummino, P.J.1    Copeland, R.A.2
  • 31
    • 84881171375 scopus 로고    scopus 로고
    • Pharmacokinetics and the drug-target residence time concept
    • [31] Dahl, G., Akerud, T., Pharmacokinetics and the drug-target residence time concept. Drug Discov. Today 18 (2013), 697–707.
    • (2013) Drug Discov. Today , vol.18 , pp. 697-707
    • Dahl, G.1    Akerud, T.2
  • 32
    • 84939780109 scopus 로고    scopus 로고
    • Ligand residence time at G-protein-coupled receptors – why we should take our time to study it
    • [32] Hoffmann, C., Castro, M., Rinken, A., Leurs, R., Hill, S.J., Vischer, H.F., Ligand residence time at G-protein-coupled receptors – why we should take our time to study it. Mol. Pharmacol. 88 (2015), 552–560.
    • (2015) Mol. Pharmacol. , vol.88 , pp. 552-560
    • Hoffmann, C.1    Castro, M.2    Rinken, A.3    Leurs, R.4    Hill, S.J.5    Vischer, H.F.6
  • 33
    • 42149124403 scopus 로고    scopus 로고
    • Targeting melanocortin receptors: an approach to treat weight disorders and sexual dysfunction
    • [33] Wikberg, J.E.S., Mutulis, F., Targeting melanocortin receptors: an approach to treat weight disorders and sexual dysfunction. Nat. Rev. Drug Discov. 7 (2008), 307–323.
    • (2008) Nat. Rev. Drug Discov. , vol.7 , pp. 307-323
    • Wikberg, J.E.S.1    Mutulis, F.2
  • 35
    • 0029961314 scopus 로고    scopus 로고
    • Characterisation of the melanocortin 4 receptor by radioligand binding
    • [35] Schiöth, H.B., Muceniece, R., Wikberg, J.E.S., Characterisation of the melanocortin 4 receptor by radioligand binding. Pharmacol. Toxicol. 79 (1996), 161–165.
    • (1996) Pharmacol. Toxicol. , vol.79 , pp. 161-165
    • Schiöth, H.B.1    Muceniece, R.2    Wikberg, J.E.S.3
  • 38
    • 17444407862 scopus 로고    scopus 로고
    • Co-operative regulation of ligand binding to melanocortin receptor subtypes: evidence for interacting binding sites
    • [38] Kopanchuk, S., Veiksina, S., Petrovska, R., Mutule, I., Szardenings, M., Rinken, A., Wikberg, J.E.S., Co-operative regulation of ligand binding to melanocortin receptor subtypes: evidence for interacting binding sites. Eur. J. Pharmacol. 512 (2005), 85–95.
    • (2005) Eur. J. Pharmacol. , vol.512 , pp. 85-95
    • Kopanchuk, S.1    Veiksina, S.2    Petrovska, R.3    Mutule, I.4    Szardenings, M.5    Rinken, A.6    Wikberg, J.E.S.7
  • 40
    • 0016749447 scopus 로고
    • Determination of dissociation constants and specific rate constants of enzyme-substrate (or protein-ligand) interactions from rapid reaction kinetic data
    • [40] Strickland, S., Palmer, G., Massey, V., Determination of dissociation constants and specific rate constants of enzyme-substrate (or protein-ligand) interactions from rapid reaction kinetic data. J. Biol. Chem. 250 (1975), 4048–4052.
    • (1975) J. Biol. Chem. , vol.250 , pp. 4048-4052
    • Strickland, S.1    Palmer, G.2    Massey, V.3
  • 41
    • 0029905350 scopus 로고    scopus 로고
    • Kinetic evidence for isomerization of the dopamine receptor-raclopride complex
    • [41] Lepiku, M., Rinken, A., Järv, J., Fuxe, K., Kinetic evidence for isomerization of the dopamine receptor-raclopride complex. Neurochem. Int. 28 (1996), 591–595.
    • (1996) Neurochem. Int. , vol.28 , pp. 591-595
    • Lepiku, M.1    Rinken, A.2    Järv, J.3    Fuxe, K.4
  • 43
    • 0021336303 scopus 로고
    • The kinetics of competitive radioligand binding predicted by the law of mass action
    • [43] Motulsky, H.J., Mahan, L.C., The kinetics of competitive radioligand binding predicted by the law of mass action. Mol. Pharmacol. 25 (1984), 1–9.
    • (1984) Mol. Pharmacol. , vol.25 , pp. 1-9
    • Motulsky, H.J.1    Mahan, L.C.2
  • 44
    • 85012229912 scopus 로고    scopus 로고
    • Application of baculovirus technology for studies of G protein-coupled receptor signaling
    • O. Fesenko L. Yatsenko M. Brodin Springer
    • [44] Mazina, O., Tõntson, L., Kopanchuk, S., Rinken, A., Application of baculovirus technology for studies of G protein-coupled receptor signaling. Fesenko, O., Yatsenko, L., Brodin, M., (eds.) Nanomaterials Imaging Techniques, Surface Studies and Applications, 2013, Springer, 339–348.
    • (2013) Nanomaterials Imaging Techniques, Surface Studies and Applications , pp. 339-348
    • Mazina, O.1    Tõntson, L.2    Kopanchuk, S.3    Rinken, A.4
  • 45
    • 84887862575 scopus 로고    scopus 로고
    • Budded baculoviruses as a tool for a homogeneous fluorescence anisotropy-based assay of ligand binding to G protein-coupled receptors: the case of melanocortin 4 receptors
    • [45] Veiksina, S., Kopanchuk, S., Rinken, A., Budded baculoviruses as a tool for a homogeneous fluorescence anisotropy-based assay of ligand binding to G protein-coupled receptors: the case of melanocortin 4 receptors. Biochim. Biophys. Acta 1838 (2014), 372–381.
    • (2014) Biochim. Biophys. Acta , vol.1838 , pp. 372-381
    • Veiksina, S.1    Kopanchuk, S.2    Rinken, A.3
  • 46
    • 65349148442 scopus 로고    scopus 로고
    • G-protein coupled receptor array technologies: site directed immobilisation of liposomes containing the H1-histamine or M2-muscarinic receptors
    • [46] Bailey, K., Bally, M., Leifert, W., Voros, J., McMurchie, T., G-protein coupled receptor array technologies: site directed immobilisation of liposomes containing the H1-histamine or M2-muscarinic receptors. Proteomics 9 (2009), 2052–2063.
    • (2009) Proteomics , vol.9 , pp. 2052-2063
    • Bailey, K.1    Bally, M.2    Leifert, W.3    Voros, J.4    McMurchie, T.5
  • 47
    • 40449084755 scopus 로고    scopus 로고
    • The baculovirus display technology–an evolving instrument for molecular screening and drug delivery
    • [47] Makela, A.R., Oker-Blom, C., The baculovirus display technology–an evolving instrument for molecular screening and drug delivery. Comb. Chem. High Throughput Screen. 11 (2008), 86–98.
    • (2008) Comb. Chem. High Throughput Screen. , vol.11 , pp. 86-98
    • Makela, A.R.1    Oker-Blom, C.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.