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Volumn 169, Issue 2, 2013, Pages 357-370

Agonists with supraphysiological efficacy at the muscarinic M2 ACh receptor

Author keywords

biased agonism; cell signalling; dynamic mass redistribution; efficacy; GPCRs; iperoxo; label free technologies; muscarinic ACh receptors; Superagonism

Indexed keywords

ACETYLCHOLINE; GUANINE NUCLEOTIDE BINDING PROTEIN; IPEROXO; MUSCARINIC M2 RECEPTOR; MUSCARINIC M2 RECEPTOR AGONIST; UNCLASSIFIED DRUG;

EID: 84875696642     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/bph.12003     Document Type: Article
Times cited : (60)

References (37)
  • 1
    • 81355156238 scopus 로고    scopus 로고
    • Guide to Receptors and Channels (GRAC), 5th edition
    • Alexander SPH, Mathie A, Peters JA, (2011). Guide to Receptors and Channels (GRAC), 5th edition. Br J Pharmacol 164 (Suppl. 1): 1-324.
    • (2011) Br J Pharmacol , vol.164 , Issue.SUPPL. 1 , pp. 1-324
    • Alexander, S.P.H.1    Mathie, A.2    Peters, J.A.3
  • 2
    • 59649112659 scopus 로고    scopus 로고
    • Dualsteric GPCR targeting: A novel route to binding and signaling pathway selectivity
    • Antony J, Kellersohn K, Mohr-Andrae M, Kebig K, Prilla S, Muth M, et al. (2009). Dualsteric GPCR targeting: a novel route to binding and signaling pathway selectivity. FASEB J 23: 442-450.
    • (2009) FASEB J , vol.23 , pp. 442-450
    • Antony, J.1    Kellersohn, K.2    Mohr-Andrae, M.3    Kebig, K.4    Prilla, S.5    Muth, M.6
  • 3
    • 0021058380 scopus 로고
    • Operational models of pharmacological agonism
    • Black JW, Leff P, (1983). Operational models of pharmacological agonism. Proc R Soc Lond B 220: 141-162.
    • (1983) Proc R Soc Lond B , vol.220 , pp. 141-162
    • Black, J.W.1    Leff, P.2
  • 4
    • 84867010308 scopus 로고    scopus 로고
    • The allosteric vestibule of a seven transmembrane helical receptor controls G-protein coupling
    • doi: 10.1038/ncomms2028
    • Bock A, Merten N, Schrage R, Dallanoce C, Bätz J, Klöckner J, et al. (2012). The allosteric vestibule of a seven transmembrane helical receptor controls G-protein coupling. Nat Commun 3: 1044. doi: 10.1038/ncomms2028.
    • (2012) Nat Commun , vol.3 , pp. 1044
    • Bock, A.1    Merten, N.2    Schrage, R.3    Dallanoce, C.4    Bätz, J.5    Klöckner, J.6
  • 5
    • 0032790339 scopus 로고    scopus 로고
    • Synthesis and functional characterization of novel derivatives related to oxotremorine and oxotremorine-M
    • Dallanoce C, Conti P, De Amici M, De Micheli C, Barocelli E, Chiavarini M, et al. (1999). Synthesis and functional characterization of novel derivatives related to oxotremorine and oxotremorine-M. Bioorg Med Chem 7: 1539-1547.
    • (1999) Bioorg Med Chem , vol.7 , pp. 1539-1547
    • Dallanoce, C.1    Conti, P.2    De Amici, M.3    De Micheli, C.4    Barocelli, E.5    Chiavarini, M.6
  • 6
    • 0000564694 scopus 로고
    • An analysis of the direct and indirect actions of drugs on the isolated guinea-pig ileum
    • Day M, Vane JR, (1963). An analysis of the direct and indirect actions of drugs on the isolated guinea-pig ileum. Br J Pharmacol Chemother 20: 150-170.
    • (1963) Br J Pharmacol Chemother , vol.20 , pp. 150-170
    • Day, M.1    Vane, J.R.2
  • 7
    • 0024332759 scopus 로고
    • Calculating receptor number from binding experiments using same compound as radioligand and competitor
    • DeBlasi A, O'Reilly K, Motulsky HJ, (1989). Calculating receptor number from binding experiments using same compound as radioligand and competitor. Trends Pharmacol Sci 10: 227-229.
    • (1989) Trends Pharmacol Sci , vol.10 , pp. 227-229
    • Deblasi, A.1    O'Reilly, K.2    Motulsky, H.J.3
  • 8
    • 77958039571 scopus 로고    scopus 로고
    • Energy landscapes as a tool to integrate GPCR structure, dynamics, and function
    • Deupi X, Kobilka BK, (2010). Energy landscapes as a tool to integrate GPCR structure, dynamics, and function. Physiology (Bethesda) 25: 293-303.
    • (2010) Physiology (Bethesda) , vol.25 , pp. 293-303
    • Deupi, X.1    Kobilka, B.K.2
  • 10
    • 30444436744 scopus 로고    scopus 로고
    • Design, synthesis, and action of oxotremorine-related hybrid-type allosteric modulators of muscarinic acetylcholine receptors
    • Disingrini T, Muth M, Dallanoce C, Barocelli E, Bertoni S, Kellershohn K, et al. (2006). Design, synthesis, and action of oxotremorine-related hybrid-type allosteric modulators of muscarinic acetylcholine receptors. J Med Chem 49: 366-372.
    • (2006) J Med Chem , vol.49 , pp. 366-372
    • Disingrini, T.1    Muth, M.2    Dallanoce, C.3    Barocelli, E.4    Bertoni, S.5    Kellershohn, K.6
  • 12
    • 77951223981 scopus 로고    scopus 로고
    • Identification of orthosteric and allosteric site mutations in M2 muscarinic acetylcholine receptors that contribute to ligand-selective signaling bias
    • Gregory KJ, Hall NE, Tobin AB, Sexton PM, Christopoulos A, (2010). Identification of orthosteric and allosteric site mutations in M2 muscarinic acetylcholine receptors that contribute to ligand-selective signaling bias. J Biol Chem 285: 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
  • 13
    • 0022367080 scopus 로고
    • Functional reconstitution of purified muscarinic receptors and inhibitory guanine nucleotide regulatory protein
    • Haga K, Haga T, Ichiyama A, Katada T, Kurose H, Ui M, (1985). Functional reconstitution of purified muscarinic receptors and inhibitory guanine nucleotide regulatory protein. Nature 316: 731-733.
    • (1985) Nature , vol.316 , pp. 731-733
    • Haga, K.1    Haga, T.2    Ichiyama, A.3    Katada, T.4    Kurose, H.5    Ui, M.6
  • 14
    • 78049363852 scopus 로고    scopus 로고
    • Insight into GPCR pharmacology from the measurement of changes in intracellular cyclic AMP; Advantages and pitfalls of differing methodologies
    • Hill SJ, Williams C, May LT, (2010). Insight into GPCR pharmacology from the measurement of changes in intracellular cyclic AMP; advantages and pitfalls of differing methodologies. Br J Pharmacol 161: 1266-1275.
    • (2010) Br J Pharmacol , vol.161 , pp. 1266-1275
    • Hill, S.J.1    Williams, C.2    May, L.T.3
  • 15
    • 0014510095 scopus 로고
    • The actions of some cholinomimetic drugs on the isolated taenia of the guinea-pig caecum
    • Hobbiger F, Mitchelson F, Rand MJ, (1969). The actions of some cholinomimetic drugs on the isolated taenia of the guinea-pig caecum. Br J Pharmacol 36: 53-69.
    • (1969) Br J Pharmacol , vol.36 , pp. 53-69
    • Hobbiger, F.1    Mitchelson, F.2    Rand, M.J.3
  • 16
    • 36849071252 scopus 로고    scopus 로고
    • Allosteric small molecules unveil a role of an extracellular E2/transmembrane helix 7 junction for G protein-coupled receptor activation
    • Jäger D, Schmalenbach C, Prilla S, Schrobang J, Kebig A, Sennwitz M, et al. (2007). Allosteric small molecules unveil a role of an extracellular E2/transmembrane helix 7 junction for G protein-coupled receptor activation. J Biol Chem 282: 34968-34976.
    • (2007) J Biol Chem , vol.282 , pp. 34968-34976
    • Jäger, D.1    Schmalenbach, C.2    Prilla, S.3    Schrobang, J.4    Kebig, A.5    Sennwitz, M.6
  • 17
    • 77952354490 scopus 로고    scopus 로고
    • Seven transmembrane receptors as shapeshifting proteins: The impact of allosteric modulation and functional selectivity on new drug discovery
    • Kenakin T, Miller LJ, (2010). Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery. Pharmacol Rev 62: 265-304.
    • (2010) Pharmacol Rev , vol.62 , pp. 265-304
    • Kenakin, T.1    Miller, L.J.2
  • 19
    • 77954243052 scopus 로고    scopus 로고
    • Convergent, short synthesis of the muscarinic superagonist iperoxo
    • Klöckner J, Schmitz J, Holzgrabe U, (2010). Convergent, short synthesis of the muscarinic superagonist iperoxo. Tetrahedron Lett 51: 3470-3472.
    • (2010) Tetrahedron Lett , vol.51 , pp. 3470-3472
    • Klöckner, J.1    Schmitz, J.2    Holzgrabe, U.3
  • 20
    • 0028117967 scopus 로고
    • Endogenous butyrylcholinesterase in SV40 transformed cell lines: COS-l, COS-7, MRC°5 SV40, and WI-38 VA13
    • Kris M, Jbilo O, Bartels CF, Masson P, Rhode S, Lockridge O, (1994). Endogenous butyrylcholinesterase in SV40 transformed cell lines: COS-l, COS-7, MRC°5 SV40, and WI-38 VA13. In Vitro Cell Dev Biol 30A: 680-689.
    • (1994) Vitro Cell Dev Biol , vol.30 A , pp. 680-689
    • Kris, M.1    Jbilo, O.2    Bartels, C.F.3    Masson, P.4    Rhode, S.5    Lockridge, O.6
  • 21
    • 42149181885 scopus 로고    scopus 로고
    • Structural diversity of G protein-coupled receptors and significance for drug discovery
    • Lagerström MC, Schiöth HB, (2008). Structural diversity of G protein-coupled receptors and significance for drug discovery. Nat Rev Drug Discov 7: 339-357.
    • (2008) Nat Rev Drug Discov , vol.7 , pp. 339-357
    • Lagerström, M.C.1    Schiöth, H.B.2
  • 22
    • 79961173346 scopus 로고    scopus 로고
    • The β2-subtype of adrenoceptors mediates inhibition of pro-fibrotic events in human lung fibroblasts Naunyn Schmiedebergs Arch
    • Lamyel F, Warnken-Uhlich M, Seemann WK, Mohr K, Kostenis E, Ahmedat AS, et al. (2011). The β2-subtype of adrenoceptors mediates inhibition of pro-fibrotic events in human lung fibroblasts Naunyn Schmiedebergs Arch. Pharmacol 384: 133-145.
    • (2011) Pharmacol , vol.384 , pp. 133-145
    • Lamyel, F.1    Warnken-Uhlich, M.2    Seemann, W.K.3    Mohr, K.4    Kostenis, E.5    Ahmedat, A.S.6
  • 23
  • 24
    • 0028055257 scopus 로고
    • Agonist induced muscarinic cholinergic receptor internalization, recycling and degradation in cultured neuronal cells
    • Maloteaux JM, Hermans E, (1994). Agonist induced muscarinic cholinergic receptor internalization, recycling and degradation in cultured neuronal cells. Biochem Pharmacol 47: 77-88.
    • (1994) Biochem Pharmacol , vol.47 , pp. 77-88
    • Maloteaux, J.M.1    Hermans, E.2
  • 26
    • 0035079910 scopus 로고    scopus 로고
    • 2 acetylcholine receptors on the synthesis of cyclic AMP in CHO cells: Dependence on time, receptor density and receptor agonists
    • 2 acetylcholine receptors on the synthesis of cyclic AMP in CHO cells: dependence on time, receptor density and receptor agonists. Br J Pharmacol 132: 1217-1228.
    • (2001) Br J Pharmacol , vol.132 , pp. 1217-1228
    • Michal, P.1    Lysíková, M.2    Tuček, S.3
  • 27
    • 0037305047 scopus 로고    scopus 로고
    • Principles: Extending the utility of [35S]GTPγS binding assays
    • Milligan G, (2003). Principles: extending the utility of [35S]GTPγS binding assays. Trends Pharmacol Sci 24: 87-90.
    • (2003) Trends Pharmacol Sci , vol.24 , pp. 87-90
    • Milligan, G.1
  • 28
    • 14844283796 scopus 로고    scopus 로고
    • An investigation of whether agonist-selective receptor conformations occur with respect to M2 and M4 muscarinic acetylcholine receptor signalling via Gi/o and Gs proteins
    • Mistry R, Dowling MR, Challiss RAJ, (2005). An investigation of whether agonist-selective receptor conformations occur with respect to M2 and M4 muscarinic acetylcholine receptor signalling via Gi/o and Gs proteins. Br J Pharmacol 144: 566-575.
    • (2005) Br J Pharmacol , vol.144 , pp. 566-575
    • Mistry, R.1    Dowling, M.R.2    Challiss, R.A.J.3
  • 31
    • 77956657852 scopus 로고    scopus 로고
    • Deconvolution of complex G protein-coupled receptor signaling in live cells using dynamic mass redistribution measurements
    • Schröder R, Janssen N, Schmidt J, Kebig A, Merten N, Hennen S, et al. (2010). Deconvolution of complex G protein-coupled receptor signaling in live cells using dynamic mass redistribution measurements. Nat Biotechnol 28: 943-949.
    • (2010) Nat Biotechnol , vol.28 , pp. 943-949
    • Schröder, R.1    Janssen, N.2    Schmidt, J.3    Kebig, A.4    Merten, N.5    Hennen, S.6
  • 32
    • 80054807491 scopus 로고    scopus 로고
    • Applying label-free dynamic mass redistribution technology to frame signaling of G protein-coupled receptors noninvasively in living cells
    • Schröder R, Schmidt J, Blättermann S, Peters L, Janssen N, Grundmann M, et al. (2011). Applying label-free dynamic mass redistribution technology to frame signaling of G protein-coupled receptors noninvasively in living cells. Nat Protocols 6: 1748-1760.
    • (2011) Nat Protocols , vol.6 , pp. 1748-1760
    • Schröder, R.1    Schmidt, J.2    Blättermann, S.3    Peters, L.4    Janssen, N.5    Grundmann, M.6
  • 33
    • 78650301416 scopus 로고    scopus 로고
    • When simple agonism is not enough: Emerging modalities of GPCR ligands
    • Smith NJ, Bennett KA, Milligan G, (2011). When simple agonism is not enough: emerging modalities of GPCR ligands. Mol Cell Endocrinol 331: 241-247.
    • (2011) Mol Cell Endocrinol , vol.331 , pp. 241-247
    • Smith, N.J.1    Bennett, K.A.2    Milligan, G.3
  • 34
    • 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
    • Suratman S, Leach K, Sexton PM, Felder CC, Loiacono LE, Christopoulos A, (2011). 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: 1659-1670.
    • (2011) Br J Pharmacol , vol.162 , pp. 1659-1670
    • Suratman, S.1    Leach, K.2    Sexton, P.M.3    Felder, C.C.4    Loiacono, L.E.5    Christopoulos, A.6
  • 35
    • 0030433044 scopus 로고    scopus 로고
    • Search for lead structures to develop new allosteric modulators of muscarinic receptors
    • Tränkle C, Kostenis E, Burgmer U, Mohr K, (1996). Search for lead structures to develop new allosteric modulators of muscarinic receptors. J Pharmacol Exp Ther 279: 926-933.
    • (1996) J Pharmacol Exp Ther , vol.279 , pp. 926-933
    • Tränkle, C.1    Kostenis, E.2    Burgmer, U.3    Mohr, K.4
  • 36
    • 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
    • Valant C, Gregory KJ, Hall NE, Scammells PJ, Lew MJ, Sexton PM, et al. (2008). 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: 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
  • 37
    • 84855879360 scopus 로고    scopus 로고
    • The best of both worlds? Bitopic orthosteric/allosteric ligands of G protein-coupled receptors
    • Valant C, Lane RJ, Sexton PM, Christopoulos A, (2012). The best of both worlds? Bitopic orthosteric/allosteric ligands of G protein-coupled receptors. Annu Rev Pharmacol Toxicol 52: 153-178.
    • (2012) Annu Rev Pharmacol Toxicol , vol.52 , pp. 153-178
    • Valant, C.1    Lane, R.J.2    Sexton, P.M.3    Christopoulos, A.4


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