메뉴 건너뛰기




Volumn 289, Issue 36, 2014, Pages 24911-24921

Structural and functional studies of the modulator NS9283 reveal agonist-like mechanism of action at α4β2 nicotinic acetylcholine receptors

Author keywords

[No Author keywords available]

Indexed keywords

AMINO ACIDS; BINDING ENERGY; CHEMICAL ACTIVATION; MODULATION; QUANTUM THEORY;

EID: 84906984055     PISSN: 00219258     EISSN: 1083351X     Source Type: Journal    
DOI: 10.1074/jbc.M114.568097     Document Type: Article
Times cited : (34)

References (42)
  • 2
    • 77950494200 scopus 로고    scopus 로고
    • Binding, activation and modulation of Cys loop receptors
    • Miller, P. S., and Smart, T. G. (2010) Binding, activation and modulation of Cys loop receptors. Trends Pharmacol. Sci. 31, 161-174
    • (2010) Trends Pharmacol. Sci. , vol.31 , pp. 161-174
    • Miller, P.S.1    Smart, T.G.2
  • 3
    • 69949159308 scopus 로고    scopus 로고
    • Nicotinic receptors: Allosteric transitions and therapeutic targets in the nervous system
    • Taly, A., Corringer, P. J., Guedin, D., Lestage, P., and Changeux, J. P. (2009) Nicotinic receptors: allosteric transitions and therapeutic targets in the nervous system. Nat. Rev. Drug Discov. 8, 733-750
    • (2009) Nat. Rev. Drug Discov. , vol.8 , pp. 733-750
    • Taly, A.1    Corringer, P.J.2    Guedin, D.3    Lestage, P.4    Changeux, J.P.5
  • 5
    • 33747422892 scopus 로고    scopus 로고
    • Brain nicotinic acetylcholine receptors: Native subtypes and their relevance
    • Gotti, C., Zoli, M., and Clementi, F. (2006) Brain nicotinic acetylcholine receptors: native subtypes and their relevance. Trends Pharmacol. Sci. 27, 482-491
    • (2006) Trends Pharmacol. Sci. , vol.27 , pp. 482-491
    • Gotti, C.1    Zoli, M.2    Clementi, F.3
  • 7
    • 34548677767 scopus 로고    scopus 로고
    • Allosteric modulation of nicotinic acetylcholine receptors
    • Bertrand, D., and Gopalakrishnan, M. (2007) Allosteric modulation of nicotinic acetylcholine receptors. Biochem. Pharmacol. 74, 1155-1163
    • (2007) Biochem. Pharmacol. , vol.74 , pp. 1155-1163
    • Bertrand, D.1    Gopalakrishnan, M.2
  • 8
    • 80052026910 scopus 로고    scopus 로고
    • Positive allosteric modulators as an approach to nicotinic acetylcholine receptor-targeted therapeutics: Advantages and limitations
    • Williams, D. K., Wang, J., and Papke, R. L. (2011) Positive allosteric modulators as an approach to nicotinic acetylcholine receptor-targeted therapeutics: advantages and limitations. Biochem. Pharmacol. 82, 915-930
    • (2011) Biochem. Pharmacol. , vol.82 , pp. 915-930
    • Williams, D.K.1    Wang, J.2    Papke, R.L.3
  • 10
    • 84890318414 scopus 로고    scopus 로고
    • Two distinct allosteric binding sites at α4β2 nicotinic acetylcholine receptors revealed by NS206 and NS9283 give unique insights to binding activity-associated linkage at Cys loop receptors
    • Olsen, J. A., Kastrup, J. S., Peters, D., Gajhede, M., Balle, T., and Ahring, P. K. (2013) Two distinct allosteric binding sites at α4β2 nicotinic acetylcholine receptors revealed by NS206 and NS9283 give unique insights to binding activity-associated linkage at Cys loop receptors. J. Biol. Chem. 288, 35997-36006
    • (2013) J. Biol. Chem. , vol.288 , pp. 35997-36006
    • Olsen, J.A.1    Kastrup, J.S.2    Peters, D.3    Gajhede, M.4    Balle, T.5    Ahring, P.K.6
  • 11
    • 0024549518 scopus 로고
    • Differential regulation of γ-aminobutyric acid receptor channels by diazepam and phenobarbital
    • Twyman, R. E., Rogers, C. J., and Macdonald, R. L. (1989) Differential regulation of γ-aminobutyric acid receptor channels by diazepam and phenobarbital. Ann. Neurol. 25, 213-220
    • (1989) Ann. Neurol. , vol.25 , pp. 213-220
    • Twyman, R.E.1    Rogers, C.J.2    Macdonald, R.L.3
  • 12
    • 33751119897 scopus 로고    scopus 로고
    • Identification of a GABAA receptor anesthetic binding site at subunit interfaces by photolabeling with an etomidate analog
    • Li, G. D., Chiara, D. C., Sawyer, G. W., Husain, S. S., Olsen, R. W., and Cohen, J. B. (2006) Identification of a GABAA receptor anesthetic binding site at subunit interfaces by photolabeling with an etomidate analog. J. Neurosci. 26, 11599-11605
    • (2006) J. Neurosci. , vol.26 , pp. 11599-11605
    • Li, G.D.1    Chiara, D.C.2    Sawyer, G.W.3    Husain, S.S.4    Olsen, R.W.5    Cohen, J.B.6
  • 13
    • 84873157538 scopus 로고    scopus 로고
    • How theories evolved concerning the mechanism of action of barbiturates
    • Loscher, W., and Rogawski, M. A. (2012) How theories evolved concerning the mechanism of action of barbiturates. Epilepsia 53, 12-25
    • (2012) Epilepsia , vol.53 , pp. 12-25
    • Loscher, W.1    Rogawski, M.A.2
  • 14
    • 80052027395 scopus 로고    scopus 로고
    • α4β2 neuronal nicotinic receptor-positive allosteric modulation: An approach for improving the therapeutic index of α4β2 nAChR agonists in pain
    • Lee, C. H., Zhu, C., Malysz, J., Campbell, T., Shaughnessy, T., Honore, P., Polakowski, J., and Gopalakrishnan, M. (2011) α4β2 neuronal nicotinic receptor-positive allosteric modulation: an approach for improving the therapeutic index of α4β2 nAChR agonists in pain. Biochem. Pharmacol. 82, 959-966
    • (2011) Biochem. Pharmacol. , vol.82 , pp. 959-966
    • Lee, C.H.1    Zhu, C.2    Malysz, J.3    Campbell, T.4    Shaughnessy, T.5    Honore, P.6    Polakowski, J.7    Gopalakrishnan, M.8
  • 16
    • 80052032018 scopus 로고    scopus 로고
    • Allosteric modulators of the α4β2 subtype of neuronal nicotinic acetylcholine receptors
    • Pandya, A., and Yakel, J. L. (2011) Allosteric modulators of the α4β2 subtype of neuronal nicotinic acetylcholine receptors. Biochem. Pharmacol. 82, 952-958
    • (2011) Biochem. Pharmacol. , vol.82 , pp. 952-958
    • Pandya, A.1    Yakel, J.L.2
  • 17
    • 67649240389 scopus 로고    scopus 로고
    • Nicotinic acetylcholine receptors: An overview on drug discovery
    • D'hoedt, D., and Bertrand, D. (2009) Nicotinic acetylcholine receptors: an overview on drug discovery. Expert Opin. Ther. Targets 13, 395-411
    • (2009) Expert Opin. Ther. Targets , vol.13 , pp. 395-411
    • D'Hoedt, D.1    Bertrand, D.2
  • 18
    • 84875466730 scopus 로고    scopus 로고
    • Unravelling the mechanism of action of NS9283, a positive allosteric modulator of (α4)3(β2)2 nicotinic ACh receptors
    • Grupe, M., Jensen, A. A., Ahring, P. K., Christensen, J. K., and Grunnet, M. (2013) Unravelling the mechanism of action of NS9283, a positive allosteric modulator of (α4)3(β2)2 nicotinic ACh receptors. Br. J. Pharmacol. 168, 2000-2010
    • (2013) Br. J. Pharmacol. , vol.168 , pp. 2000-2010
    • Grupe, M.1    Jensen, A.A.2    Ahring, P.K.3    Christensen, J.K.4    Grunnet, M.5
  • 20
    • 79960953776 scopus 로고    scopus 로고
    • Unraveling the high- and low-sensitivity agonist responses of nicotinic acetylcholine receptors
    • Harpsøe, K., Ahring, P. K., Christensen, J. K., Jensen, M. L., Peters, D., and Balle, T. (2011) Unraveling the high- and low-sensitivity agonist responses of nicotinic acetylcholine receptors. J. Neurosci. 31, 10759-10766
    • (2011) J. Neurosci. , vol.31 , pp. 10759-10766
    • Harpsøe, K.1    Ahring, P.K.2    Christensen, J.K.3    Jensen, M.L.4    Peters, D.5    Balle, T.6
  • 21
    • 0034213308 scopus 로고    scopus 로고
    • Novel potent ligands for the central nicotinic acetylcholine receptor: Synthesis, receptor binding, and 3D-QSAR analysis
    • Nielsen, S. F., Nielsen, E. O., Olsen, G. M., Liljefors, T., and Peters, D. (2000) Novel potent ligands for the central nicotinic acetylcholine receptor: synthesis, receptor binding, and 3D-QSAR analysis. J. Med. Chem. 43, 2217-2226
    • (2000) J. Med. Chem. , vol.43 , pp. 2217-2226
    • Nielsen, S.F.1    Nielsen, E.O.2    Olsen, G.M.3    Liljefors, T.4    Peters, D.5
  • 23
    • 57349185677 scopus 로고    scopus 로고
    • NS11394 [3′-[5-(1-hydroxy-1-methyl-ethyl)-benzoimidazol-1-yl]-biphenyl-2-carbonitrile], a unique subtype-selective GABAA receptor positive allosteric modulator: In vitro actions, pharmacokinetic properties and in vivo anxiolytic efficacy
    • Mirza, N. R., Larsen, J. S., Mathiasen, C., Jacobsen, T. A., Munro, G., Erichsen, H. K., Nielsen, A. N., Troelsen, K. B., Nielsen, E. Ø., and Ahring, P. K. (2008) NS11394 [3′-[5-(1-hydroxy-1-methyl-ethyl)-benzoimidazol-1-yl]-biphenyl-2-carbonitrile], a unique subtype-selective GABAA receptor positive allosteric modulator: in vitro actions, pharmacokinetic properties and in vivo anxiolytic efficacy. J. Pharmacol. Exp. Ther. 327, 954-968
    • (2008) J. Pharmacol. Exp. Ther. , vol.327 , pp. 954-968
    • Mirza, N.R.1    Larsen, J.S.2    Mathiasen, C.3    Jacobsen, T.A.4    Munro, G.5    Erichsen, H.K.6    Nielsen, A.N.7    Troelsen, K.B.8    Nielsen E.Ø.9    Ahring, P.K.10
  • 24
    • 1842475289 scopus 로고    scopus 로고
    • Nicotine and carbamylcholine binding to nicotinic acetylcholine receptors as studied in AChBP crystal structures
    • Celie, P. H., van Rossum-Fikkert, S. E., van Dijk, W. J., Brejc, K., Smit, A. B., and Sixma, T. K. (2004) Nicotine and carbamylcholine binding to nicotinic acetylcholine receptors as studied in AChBP crystal structures. Neuron 41, 907-914
    • (2004) Neuron , vol.41 , pp. 907-914
    • Celie, P.H.1    Van Rossum-Fikkert, S.E.2    Van Dijk, W.J.3    Brejc, K.4    Smit, A.B.5    Sixma, T.K.6
  • 28
    • 13244281317 scopus 로고    scopus 로고
    • Coot: Model-building tools for molecular graphics
    • Emsley, P., and Cowtan, K. (2004) Coot: model-building tools for molecular graphics. Acta Crystallogr. D Biol Crystallogr. 60, 2126-2132
    • (2004) Acta Crystallogr. D Biol Crystallogr. , vol.60 , pp. 2126-2132
    • Emsley, P.1    Cowtan, K.2
  • 29
    • 0027136282 scopus 로고
    • Comparative protein modelling by satisfaction of spatial restraints
    • Sali, A., and Blundell, T. L. (1993) Comparative protein modelling by satisfaction of spatial restraints. J. Mol. Biol. 234, 779-815
    • (1993) J. Mol. Biol. , vol.234 , pp. 779-815
    • Sali, A.1    Blundell, T.L.2
  • 30
    • 33749578940 scopus 로고    scopus 로고
    • Statistical potential for assessment and prediction of protein structures
    • Shen, M. Y., and Sali, A. (2006) Statistical potential for assessment and prediction of protein structures. Protein Sci. 15, 2507-2524
    • (2006) Protein Sci. , vol.15 , pp. 2507-2524
    • Shen, M.Y.1    Sali, A.2
  • 31
    • 0036310711 scopus 로고    scopus 로고
    • On the role of the crystal environment in determining protein side-chain conformations
    • Jacobson, M. P., Friesner, R. A., Xiang, Z., and Honig, B. (2002) On the role of the crystal environment in determining protein side-chain conformations. J. Mol. Biol. 320, 597-608
    • (2002) J. Mol. Biol. , vol.320 , pp. 597-608
    • Jacobson, M.P.1    Friesner, R.A.2    Xiang, Z.3    Honig, B.4
  • 32
    • 0035902009 scopus 로고    scopus 로고
    • Crystal structure of an ACh-binding protein reveals the ligand-binding domain of nicotinic receptors
    • Brejc, K., van Dijk, W. J., Klaassen, R. V., Schuurmans, M., van Der Oost, J., Smit, A. B., and Sixma, T. K. (2001) Crystal structure of an ACh-binding protein reveals the ligand-binding domain of nicotinic receptors. Nature 411, 269-276
    • (2001) Nature , vol.411 , pp. 269-276
    • Brejc, K.1    Van Dijk, W.J.2    Klaassen, R.V.3    Schuurmans, M.4    Van Der Oost, J.5    Smit, A.B.6    Sixma, T.K.7
  • 33
    • 34248598024 scopus 로고    scopus 로고
    • Galanthamine and noncompetitive inhibitor binding to ACh-binding protein: Evidence for a binding site on non-α-subunit interfaces of heteromeric neuronal nicotinic receptors
    • Hansen, S. B., and Taylor, P. (2007) Galanthamine and noncompetitive inhibitor binding to ACh-binding protein: evidence for a binding site on non-α-subunit interfaces of heteromeric neuronal nicotinic receptors. J. Mol. Biol. 369, 895-901
    • (2007) J. Mol. Biol. , vol.369 , pp. 895-901
    • Hansen, S.B.1    Taylor, P.2
  • 34
    • 84865176531 scopus 로고    scopus 로고
    • Crystal structure of Lymnaea stagnalis AChBP complexed with the potent nAChR antagonist DHßE suggests a unique mode of antagonism
    • Shahsavar, A., Kastrup, J. S., Nielsen, E. Ø., Kristensen, J. L., Gajhede, M., and Balle, T. (2012) Crystal structure of Lymnaea stagnalis AChBP complexed with the potent nAChR antagonist DHßE suggests a unique mode of antagonism. PLoS One 7, e40757
    • (2012) PLoS One , vol.7 , pp. e40757
    • Shahsavar, A.1    Kastrup, J.S.2    Nielsen E.Ø.3    Kristensen, J.L.4    Gajhede, M.5    Balle, T.6
  • 35
    • 44949241532 scopus 로고    scopus 로고
    • Atomic interactions of neonicotinoid agonists with AChBP: Molecular recognition of the distinctive electronegative pharmacophore
    • Talley, T. T., Harel, M., Hibbs, R. E., Radic, Z., Tomizawa, M., Casida, J. E., and Taylor, P. (2008) Atomic interactions of neonicotinoid agonists with AChBP: molecular recognition of the distinctive electronegative pharmacophore. Proc. Natl. Acad. Sci. U.S.A. 105, 7606-7611
    • (2008) Proc. Natl. Acad. Sci. U.S.A. , vol.105 , pp. 7606-7611
    • Talley, T.T.1    Harel, M.2    Hibbs, R.E.3    Radic, Z.4    Tomizawa, M.5    Casida, J.E.6    Taylor, P.7
  • 36
    • 84898657848 scopus 로고    scopus 로고
    • Molecular recognition of the neurotransmitter acetylcholine by an acetylcholine binding protein reveals determinants of binding to nicotinic acetylcholine receptors
    • Olsen, J. A., Balle, T., Gajhede, M., Ahring, P. K., and Kastrup, J. S. (2014) Molecular recognition of the neurotransmitter acetylcholine by an acetylcholine binding protein reveals determinants of binding to nicotinic acetylcholine receptors. PLoS One 9, e91232
    • (2014) PLoS One , vol.9 , pp. e91232
    • Olsen, J.A.1    Balle, T.2    Gajhede, M.3    Ahring, P.K.4    Kastrup, J.S.5
  • 37
    • 63649149427 scopus 로고    scopus 로고
    • Nicotine binding to brain receptors requires a strong cation-π interaction
    • Xiu, X., Puskar, N. L., Shanata, J. A., Lester, H. A., and Dougherty, D. A. (2009) Nicotine binding to brain receptors requires a strong cation-π interaction. Nature 458, 534-537
    • (2009) Nature , vol.458 , pp. 534-537
    • Xiu, X.1    Puskar, N.L.2    Shanata, J.A.3    Lester, H.A.4    Dougherty, D.A.5
  • 38
    • 0033565007 scopus 로고    scopus 로고
    • Can lone pairs bind to a π system? The water·hexafluorobenzene interaction
    • Gallivan, J. P., and Dougherty, D. A. (1999) Can lone pairs bind to a π system? The water·hexafluorobenzene interaction. Org. Lett. 1, 103-105
    • (1999) Org. Lett. , vol.1 , pp. 103-105
    • Gallivan, J.P.1    Dougherty, D.A.2
  • 39
    • 65949085351 scopus 로고    scopus 로고
    • Number and locations of agonist binding sites required to activate homomeric Cys loop receptors
    • Rayes, D., De Rosa, M. J., Sine, S. M., and Bouzat, C. (2009) Number and locations of agonist binding sites required to activate homomeric Cys loop receptors. J. Neurosci. 29, 6022-6032
    • (2009) J. Neurosci. , vol.29 , pp. 6022-6032
    • Rayes, D.1    De Rosa, M.J.2    Sine, S.M.3    Bouzat, C.4
  • 40
    • 0345490945 scopus 로고    scopus 로고
    • International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification. XXXVIII. Update on terms and symbols in quantitative pharmacology
    • Neubig, R. R., Spedding, M., Kenakin, T., and Christopoulos, A. (2003) International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification. XXXVIII. Update on terms and symbols in quantitative pharmacology. Pharmacol. Rev. 55, 597-606
    • (2003) Pharmacol. Rev. , vol.55 , pp. 597-606
    • Neubig, R.R.1    Spedding, M.2    Kenakin, T.3    Christopoulos, A.4
  • 41
    • 67650473173 scopus 로고    scopus 로고
    • The positive allosteric modulator morantel binds at noncanonical subunit interfaces of neuronal nicotinic acetylcholine receptors
    • Seo, S., Henry, J. T., Lewis, A. H., Wang, N., and Levandoski, M. M. (2009) The positive allosteric modulator morantel binds at noncanonical subunit interfaces of neuronal nicotinic acetylcholine receptors. J. Neurosci. 29, 8734-8742
    • (2009) J. Neurosci. , vol.29 , pp. 8734-8742
    • Seo, S.1    Henry, J.T.2    Lewis, A.H.3    Wang, N.4    Levandoski, M.M.5
  • 42
    • 84872033261 scopus 로고    scopus 로고
    • A unified model of the GABA(A) receptor comprising agonist and benzodiazepine binding sites
    • Bergmann, R., Kongsbak, K., Sørensen, P. L., Sander, T., and Balle, T. (2013) A unified model of the GABA(A) receptor comprising agonist and benzodiazepine binding sites. PLoS One 8, e52323
    • (2013) PLoS One , vol.8 , pp. e52323
    • Bergmann, R.1    Kongsbak, K.2    Sørensen, P.L.3    Sander, T.4    Balle, T.5


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.