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Items: 1 to 20 of 91

1.

Differential effects of allosteric M(1) muscarinic acetylcholine receptor agonists on receptor activation, arrestin 3 recruitment, and receptor downregulation.

Davis AA, Heilman CJ, Brady AE, Miller NR, Fuerstenau-Sharp M, Hanson BJ, Lindsley CW, Conn PJ, Lah JJ, Levey AI.

ACS Chem Neurosci. 2010 Aug 18;1(8):542-551.

2.

Reverse engineering of the selective agonist TBPB unveils both orthosteric and allosteric modes of action at the M₁ muscarinic acetylcholine receptor.

Keov P, Valant C, Devine SM, Lane JR, Scammells PJ, Sexton PM, Christopoulos A.

Mol Pharmacol. 2013 Sep;84(3):425-37. doi: 10.1124/mol.113.087320. Epub 2013 Jun 24.

3.

Orthosteric and allosteric modes of interaction of novel selective agonists of the M1 muscarinic acetylcholine receptor.

Avlani VA, Langmead CJ, Guida E, Wood MD, Tehan BG, Herdon HJ, Watson JM, Sexton PM, Christopoulos A.

Mol Pharmacol. 2010 Jul;78(1):94-104. doi: 10.1124/mol.110.064345. Epub 2010 Apr 22.

4.

FRET-based detection of M1 muscarinic acetylcholine receptor activation by orthosteric and allosteric agonists.

Markovic D, Holdich J, Al-Sabah S, Mistry R, Krasel C, Mahaut-Smith MP, Challiss RA.

PLoS One. 2012;7(1):e29946. doi: 10.1371/journal.pone.0029946. Epub 2012 Jan 17.

5.

G protein coupling and signaling pathway activation by m1 muscarinic acetylcholine receptor orthosteric and allosteric agonists.

Thomas RL, Mistry R, Langmead CJ, Wood MD, Challiss RA.

J Pharmacol Exp Ther. 2008 Nov;327(2):365-74. doi: 10.1124/jpet.108.141788. Epub 2008 Jul 29.

6.

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.

J Biol Chem. 2010 Mar 5;285(10):7459-74. doi: 10.1074/jbc.M109.094011. Epub 2010 Jan 5.

7.

Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats.

Jones CK, Brady AE, Davis AA, Xiang Z, Bubser M, Tantawy MN, Kane AS, Bridges TM, Kennedy JP, Bradley SR, Peterson TE, Ansari MS, Baldwin RM, Kessler RM, Deutch AY, Lah JJ, Levey AI, Lindsley CW, Conn PJ.

J Neurosci. 2008 Oct 8;28(41):10422-33. doi: 10.1523/JNEUROSCI.1850-08.2008.

8.

Differential regulation of muscarinic M1 receptors by orthosteric and allosteric ligands.

Davis CN, Bradley SR, Schiffer HH, Friberg M, Koch K, Tolf BR, Bonhaus DW, Lameh J.

BMC Pharmacol. 2009 Dec 2;9:14. doi: 10.1186/1471-2210-9-14.

9.

Allosteric modulation of M1 muscarinic acetylcholine receptor internalization and subcellular trafficking.

Yeatman HR, Lane JR, Choy KH, Lambert NA, Sexton PM, Christopoulos A, Canals M.

J Biol Chem. 2014 May 30;289(22):15856-66. doi: 10.1074/jbc.M113.536672. Epub 2014 Apr 21.

10.

Contrasting effects of allosteric and orthosteric agonists on m1 muscarinic acetylcholine receptor internalization and down-regulation.

Thomas RL, Langmead CJ, Wood MD, Challiss RA.

J Pharmacol Exp Ther. 2009 Dec;331(3):1086-95. doi: 10.1124/jpet.109.160242. Epub 2009 Sep 18.

11.

Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.

Sheffler DJ, Sevel C, Le U, Lovell KM, Tarr JC, Carrington SJ, Cho HP, Digby GJ, Niswender CM, Conn PJ, Hopkins CR, Wood MR, Lindsley CW.

Bioorg Med Chem Lett. 2013 Jan 1;23(1):223-7. doi: 10.1016/j.bmcl.2012.10.132. Epub 2012 Nov 9.

12.

Development of a radioligand, [(3)H]LY2119620, to probe the human M(2) and M(4) muscarinic receptor allosteric binding sites.

Schober DA, Croy CH, Xiao H, Christopoulos A, Felder CC.

Mol Pharmacol. 2014 Jul;86(1):116-23. doi: 10.1124/mol.114.091785. Epub 2014 May 7.

13.

Regulation of muscarinic acetylcholine receptor signaling.

van Koppen CJ, Kaiser B.

Pharmacol Ther. 2003 May;98(2):197-220. Review.

PMID:
12725869
14.

Allosteric modulation of muscarinic acetylcholine receptors.

Gregory KJ, Sexton PM, Christopoulos A.

Curr Neuropharmacol. 2007 Sep;5(3):157-67. doi: 10.2174/157015907781695946.

15.

Structural determinants of allosteric agonism and modulation at the M4 muscarinic acetylcholine receptor: identification of ligand-specific and global activation mechanisms.

Nawaratne V, Leach K, Felder CC, Sexton PM, Christopoulos A.

J Biol Chem. 2010 Jun 18;285(25):19012-21. doi: 10.1074/jbc.M110.125096. Epub 2010 Apr 20.

16.

Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders.

Conn PJ, Jones CK, Lindsley CW.

Trends Pharmacol Sci. 2009 Mar;30(3):148-55. doi: 10.1016/j.tips.2008.12.002. Epub 2009 Feb 7. Review.

17.

The M1 muscarinic receptor allosteric agonists AC-42 and 1-[1'-(2-methylbenzyl)-1,4'-bipiperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one bind to a unique site distinct from the acetylcholine orthosteric site.

Jacobson MA, Kreatsoulas C, Pascarella DM, O'Brien JA, Sur C.

Mol Pharmacol. 2010 Oct;78(4):648-57. doi: 10.1124/mol.110.065771. Epub 2010 Jul 21.

18.

Pharmacological characterization of LY593093, an M1 muscarinic acetylcholine receptor-selective partial orthosteric agonist.

Watt ML, Schober DA, Hitchcock S, Liu B, Chesterfield AK, McKinzie D, Felder CC.

J Pharmacol Exp Ther. 2011 Aug;338(2):622-32. doi: 10.1124/jpet.111.182063. Epub 2011 May 10.

19.

Molecular mechanisms of bitopic ligand engagement with the M1 muscarinic acetylcholine receptor.

Keov P, López L, Devine SM, Valant C, Lane JR, Scammells PJ, Sexton PM, Christopoulos A.

J Biol Chem. 2014 Aug 22;289(34):23817-37. doi: 10.1074/jbc.M114.582874. Epub 2014 Jul 8.

20.

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, Christopoulos A.

J Biol Chem. 2008 Oct 24;283(43):29312-21. doi: 10.1074/jbc.M803801200. Epub 2008 Aug 22.

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