메뉴 건너뛰기




Volumn 60, Issue 1, 2011, Pages 36-44

The properties of thermostabilised G protein-coupled receptors (StaRs) and their use in drug discovery

Author keywords

Drug discovery; G protein coupled receptor; Receptor kinetics; Thermostability

Indexed keywords

ADENOSINE A2 RECEPTOR; G PROTEIN COUPLED RECEPTOR; MUSCARINIC M1 RECEPTOR;

EID: 78149501282     PISSN: 00283908     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.neuropharm.2010.07.001     Document Type: Article
Times cited : (138)

References (37)
  • 3
    • 0032199006 scopus 로고    scopus 로고
    • Binding, gating, affinity and efficacy: the interpretation of structure-activity relationships for agonists and of the effects of mutating receptors
    • Colquhoun D. Binding, gating, affinity and efficacy: the interpretation of structure-activity relationships for agonists and of the effects of mutating receptors. Br. J. Pharmacol. 1998, 125:924-947.
    • (1998) Br. J. Pharmacol. , vol.125 , pp. 924-947
    • Colquhoun, D.1
  • 4
    • 4644259071 scopus 로고    scopus 로고
    • Affinity-based screening techniques for enhancing lead discovery
    • Comess K.M., Schurdak M.E. Affinity-based screening techniques for enhancing lead discovery. Curr. Opin. Drug Discov. Devel. 2004, 7:411-416.
    • (2004) Curr. Opin. Drug Discov. Devel. , vol.7 , pp. 411-416
    • Comess, K.M.1    Schurdak, M.E.2
  • 6
    • 77949370572 scopus 로고    scopus 로고
    • The impact of GPCR structures on pharmacology and structure-based drug design
    • Congreve M., Marshall F. The impact of GPCR structures on pharmacology and structure-based drug design. Br. J. Pharmacol. 2010, 159:986-996.
    • (2010) Br. J. Pharmacol. , vol.159 , pp. 986-996
    • Congreve, M.1    Marshall, F.2
  • 7
    • 58149193205 scopus 로고    scopus 로고
    • Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders
    • Conn P.J., Christopoulos A., Lindsley C.W. Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders. Nat. Rev. Drug Discov. 2009, 8:41-54.
    • (2009) Nat. Rev. Drug Discov. , vol.8 , pp. 41-54
    • Conn, P.J.1    Christopoulos, A.2    Lindsley, C.W.3
  • 8
    • 33748325882 scopus 로고    scopus 로고
    • Drug-target residence time and its implications for lead optimization
    • Copeland R.A., Pompliano D.L., Meek T.D. Drug-target residence time and its implications for lead optimization. Nat. Rev. Drug Discov. 2006, 5:730-739.
    • (2006) Nat. Rev. Drug Discov. , vol.5 , pp. 730-739
    • Copeland, R.A.1    Pompliano, D.L.2    Meek, T.D.3
  • 9
    • 0033534194 scopus 로고    scopus 로고
    • Tiotropium (Spiriva): mechanistical considerations and clinical profile in obstructive lung disease
    • Disse B., Speck G.A., Rominger K.L., Witek T.J., Hammer R. Tiotropium (Spiriva): mechanistical considerations and clinical profile in obstructive lung disease. Life Sci. 1999, 64:457-464.
    • (1999) Life Sci. , vol.64 , pp. 457-464
    • Disse, B.1    Speck, G.A.2    Rominger, K.L.3    Witek, T.J.4    Hammer, R.5
  • 10
    • 0031018485 scopus 로고    scopus 로고
    • Structural instability of a constitutively active G protein-coupled receptor. Agonist-independent activation due to conformational flexibility
    • Gether U., Ballesteros J.A., Seifert R., Sanders-Bush E., Weinstein H., Kobilka B.K. Structural instability of a constitutively active G protein-coupled receptor. Agonist-independent activation due to conformational flexibility. J. Biol. Chem. 1997, 272:2587-2590.
    • (1997) J. Biol. Chem. , vol.272 , pp. 2587-2590
    • Gether, U.1    Ballesteros, J.A.2    Seifert, R.3    Sanders-Bush, E.4    Weinstein, H.5    Kobilka, B.K.6
  • 11
    • 35748984700 scopus 로고    scopus 로고
    • To market, to market - 2006
    • Academic Press, London, J.E. Macor (Ed.)
    • Hegde S., Schmidt M. To market, to market - 2006. Annual Reports in Medicinal Chemistry 2007, vol. 42:505-554. Academic Press, London. J.E. Macor (Ed.).
    • (2007) Annual Reports in Medicinal Chemistry , vol.42 , pp. 505-554
    • Hegde, S.1    Schmidt, M.2
  • 12
    • 77949321753 scopus 로고    scopus 로고
    • Light activation of rhodopsin: insights from molecular dynamics simulations guided by solid-state NMR distance restraints
    • Hornak V., Ahuja S., Eilers M., Goncalves J.A., Sheves M., Reeves P.J., Smith S.O. Light activation of rhodopsin: insights from molecular dynamics simulations guided by solid-state NMR distance restraints. J. Mol. Biol. 2010, 396:510-527.
    • (2010) J. Mol. Biol. , vol.396 , pp. 510-527
    • Hornak, V.1    Ahuja, S.2    Eilers, M.3    Goncalves, J.A.4    Sheves, M.5    Reeves, P.J.6    Smith, S.O.7
  • 13
    • 0035094264 scopus 로고    scopus 로고
    • Does fast dissociation from the dopamine d(2) receptor explain the action of atypical antipsychotics?: a new hypothesis
    • Kapur S., Seeman P. Does fast dissociation from the dopamine d(2) receptor explain the action of atypical antipsychotics?: a new hypothesis. Am. J. Psychiatry 2001, 158:360-369.
    • (2001) Am. J. Psychiatry , vol.158 , pp. 360-369
    • Kapur, S.1    Seeman, P.2
  • 14
    • 61649109015 scopus 로고    scopus 로고
    • The influence of lead discovery strategies on the properties of drug candidates
    • Keseru G.M., Makara G.M. The influence of lead discovery strategies on the properties of drug candidates. Nat. Rev. Drug Discov. 2009, 8:203-212.
    • (2009) Nat. Rev. Drug Discov. , vol.8 , pp. 203-212
    • Keseru, G.M.1    Makara, G.M.2
  • 15
    • 34447633368 scopus 로고    scopus 로고
    • Conformational complexity of G-protein-coupled receptors
    • Kobilka B.K., Deupi X. Conformational complexity of G-protein-coupled receptors. Trends Pharmacol. Sci. 2007, 28:397-406.
    • (2007) Trends Pharmacol. Sci. , vol.28 , pp. 397-406
    • Kobilka, B.K.1    Deupi, X.2
  • 16
    • 38349193123 scopus 로고    scopus 로고
    • Muscarinic acetylcholine receptors as CNS drug targets
    • Langmead C.J., Watson J., Reavill C. Muscarinic acetylcholine receptors as CNS drug targets. Pharmacol. Ther. 2008, 117:232-243.
    • (2008) Pharmacol. Ther. , vol.117 , pp. 232-243
    • Langmead, C.J.1    Watson, J.2    Reavill, C.3
  • 17
    • 0017303494 scopus 로고
    • Regulation of beta-adrenergic receptors by guanyl-5'-yl imidodiphosphate and other purine nucleotides
    • Lefkowitz R.J., Mullikin D., Caron M.G. Regulation of beta-adrenergic receptors by guanyl-5'-yl imidodiphosphate and other purine nucleotides. J. Biol. Chem. 1976, 251:4686-4692.
    • (1976) J. Biol. Chem. , vol.251 , pp. 4686-4692
    • Lefkowitz, R.J.1    Mullikin, D.2    Caron, M.G.3
  • 18
    • 0019124032 scopus 로고
    • Relationship of octanol/water partition coefficient and molecular weight to rat brain capillary permeability
    • Levin V.A. Relationship of octanol/water partition coefficient and molecular weight to rat brain capillary permeability. J. Med. Chem. 1980, 23:682-684.
    • (1980) J. Med. Chem. , vol.23 , pp. 682-684
    • Levin, V.A.1
  • 21
    • 0021336303 scopus 로고
    • The kinetics of competitive radioligand binding predicted by the law of mass action
    • Motulsky H.J., Mahan L.C. The kinetics of competitive radioligand binding predicted by the law of mass action. Mol. Pharmacol. 1984, 25:1-9.
    • (1984) Mol. Pharmacol. , vol.25 , pp. 1-9
    • Motulsky, H.J.1    Mahan, L.C.2
  • 22
    • 0034282271 scopus 로고    scopus 로고
    • Implementing surface plasmon resonance biosensors in drug discovery
    • Myszka D.G., Rich R.L. Implementing surface plasmon resonance biosensors in drug discovery. Pharm. Sci. Technol. Today 2000, 3:310-317.
    • (2000) Pharm. Sci. Technol. Today , vol.3 , pp. 310-317
    • Myszka, D.G.1    Rich, R.L.2
  • 23
    • 33745902222 scopus 로고    scopus 로고
    • Analyzing ligand and small molecule binding activity of solubilized GPCRs using biosensor technology
    • Navratilova I., Dioszegi M., Myszka D.G. Analyzing ligand and small molecule binding activity of solubilized GPCRs using biosensor technology. Anal. Biochem. 2006, 355:132-139.
    • (2006) Anal. Biochem. , vol.355 , pp. 132-139
    • Navratilova, I.1    Dioszegi, M.2    Myszka, D.G.3
  • 25
    • 33947172767 scopus 로고    scopus 로고
    • Detergents for the stabilization and crystallization of membrane proteins
    • Prive G.G. Detergents for the stabilization and crystallization of membrane proteins. Methods 2007, 41:388-397.
    • (2007) Methods , vol.41 , pp. 388-397
    • Prive, G.G.1
  • 26
    • 18744362461 scopus 로고    scopus 로고
    • Mechanisms of inverse agonist action at D2 dopamine receptors
    • Roberts D.J., Strange P.G. Mechanisms of inverse agonist action at D2 dopamine receptors. Br. J. Pharmacol. 2005, 145:34-42.
    • (2005) Br. J. Pharmacol. , vol.145 , pp. 34-42
    • Roberts, D.J.1    Strange, P.G.2
  • 27
    • 40549098400 scopus 로고    scopus 로고
    • Population pharmacokinetic/pharmacodynamic analysis of CCR5 receptor occupancy by maraviroc in healthy subjects and HIV-positive patients
    • Rosario M.C., Jacqmin P., Dorr P., James I., Jenkins T.M., Abel S., van der Ryst E. Population pharmacokinetic/pharmacodynamic analysis of CCR5 receptor occupancy by maraviroc in healthy subjects and HIV-positive patients. Br. J. Clin. Pharmacol. 2008, 65(Suppl. 1):86-94.
    • (2008) Br. J. Clin. Pharmacol. , vol.65 , Issue.SUPPL. 1 , pp. 86-94
    • Rosario, M.C.1    Jacqmin, P.2    Dorr, P.3    James, I.4    Jenkins, T.M.5    Abel, S.6    van der Ryst, E.7
  • 28
    • 70350749580 scopus 로고    scopus 로고
    • Transferability of thermostabilizing mutations between beta-adrenergic receptors
    • Serrano-Vega M.J., Tate C.G. Transferability of thermostabilizing mutations between beta-adrenergic receptors. Mol. Membr. Biol. 2009, 26:385-396.
    • (2009) Mol. Membr. Biol. , vol.26 , pp. 385-396
    • Serrano-Vega, M.J.1    Tate, C.G.2
  • 29
    • 38949158505 scopus 로고    scopus 로고
    • Conformational thermostabilization of the b1-adrenergic receptor in a detergent-resistant form
    • Serrano-Vega M.J., Magnani F., Shibata Y., Tate C.G. Conformational thermostabilization of the b1-adrenergic receptor in a detergent-resistant form. Proc. Natl. Acad. Sci. U S A 2008, 105:877-882.
    • (2008) Proc. Natl. Acad. Sci. U S A , vol.105 , pp. 877-882
    • Serrano-Vega, M.J.1    Magnani, F.2    Shibata, Y.3    Tate, C.G.4
  • 31
    • 68049093203 scopus 로고    scopus 로고
    • G-protein-coupled-receptor-mediated presynaptic inhibition in the cerebellum
    • Stephens G.J. G-protein-coupled-receptor-mediated presynaptic inhibition in the cerebellum. Trends Pharmacol. Sci. 2009, 30:421-430.
    • (2009) Trends Pharmacol. Sci. , vol.30 , pp. 421-430
    • Stephens, G.J.1
  • 33
    • 69249146075 scopus 로고    scopus 로고
    • Engineering G protein-coupled receptors to facilitate their structure determination
    • Tate C.G., Schertler G.F. Engineering G protein-coupled receptors to facilitate their structure determination. Curr. Opin. Struct. Biol. 2009, 19:386-395.
    • (2009) Curr. Opin. Struct. Biol. , vol.19 , pp. 386-395
    • Tate, C.G.1    Schertler, G.F.2
  • 34
    • 78149499602 scopus 로고    scopus 로고
    • Practical considerations of membrane protein instability for purification and crystallisation.
    • Tate, C.G., 2009. Practical considerations of membrane protein instability for purification and crystallisation.
    • (2009)
    • Tate, C.G.1
  • 35
    • 0034567073 scopus 로고    scopus 로고
    • Differences among angiotensin II type 1 receptor blockers: characteristics of candesartan cilexetil
    • Unger T. Differences among angiotensin II type 1 receptor blockers: characteristics of candesartan cilexetil. Blood Press. 2000, (Suppl. 1):14-18.
    • (2000) Blood Press. , Issue.SUPPL. 1 , pp. 14-18
    • Unger, T.1
  • 37
    • 61849145185 scopus 로고    scopus 로고
    • Development and crystallization of a minimal thermostabilised G protein-coupled receptor
    • Warne T., Serrano-Vega M.J., Tate C.G., Schertler G.F. Development and crystallization of a minimal thermostabilised G protein-coupled receptor. Protein Expr. Purif. 2009, 65:204-213.
    • (2009) Protein Expr. Purif. , vol.65 , pp. 204-213
    • Warne, T.1    Serrano-Vega, M.J.2    Tate, C.G.3    Schertler, G.F.4


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.