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Results: 1 to 20 of 110

1.

Determining allosteric modulator mechanism of action: integration of radioligand binding and functional assay data.

Langmead CJ.

Methods Mol Biol. 2011;746:195-209. doi: 10.1007/978-1-61779-126-0_10.

PMID:
21607858
[PubMed - indexed for MEDLINE]
2.

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.

PMID:
18723515
[PubMed - indexed for MEDLINE]
Free PMC Article
3.

Allosteric interactions at muscarinic cholinoceptors.

Christopoulos A, Lanzafame A, Mitchelson F.

Clin Exp Pharmacol Physiol. 1998 Mar-Apr;25(3-4):185-94. Review.

PMID:
9590567
[PubMed - indexed for MEDLINE]
4.

Interactions of orthosteric and allosteric ligands with [3H]dimethyl-W84 at the common allosteric site of muscarinic M2 receptors.

Tränkle C, Weyand O, Voigtländer U, Mynett A, Lazareno S, Birdsall NJ, Mohr K.

Mol Pharmacol. 2003 Jul;64(1):180-90.

PMID:
12815174
[PubMed - indexed for MEDLINE]
Free Article
5.

Quantification of allosteric interactions at G protein-coupled receptors using radioligand binding assays.

Leach K, Sexton PM, Christopoulos A.

Curr Protoc Pharmacol. 2011 Mar;Chapter 1:Unit 1.22. doi: 10.1002/0471141755.ph0122s52.

PMID:
21935902
[PubMed - indexed for MEDLINE]
6.

The impact of orthosteric radioligand depletion on the quantification of allosteric modulator interactions.

Avlani VA, McLoughlin DJ, Sexton PM, Christopoulos A.

J Pharmacol Exp Ther. 2008 Jun;325(3):927-34. doi: 10.1124/jpet.108.136978. Epub 2008 Mar 5.

PMID:
18322151
[PubMed - indexed for MEDLINE]
Free Article
7.

Allosteric modulators of G-protein-coupled receptors.

May LT, Christopoulos A.

Curr Opin Pharmacol. 2003 Oct;3(5):551-6. Review.

PMID:
14559102
[PubMed - indexed for MEDLINE]
8.

Allosteric modulation of G protein-coupled receptors.

May LT, Avlani VA, Sexton PM, Christopoulos A.

Curr Pharm Des. 2004;10(17):2003-13. Review.

PMID:
15279541
[PubMed - indexed for MEDLINE]
9.

Discovery and characterization of orthosteric and allosteric muscarinic M2 acetylcholine receptor ligands by affinity selection-mass spectrometry.

Whitehurst CE, Nazef N, Annis DA, Hou Y, Murphy DM, Spacciapoli P, Yao Z, Ziebell MR, Cheng CC, Shipps GW Jr, Felsch JS, Lau D, Nash HM.

J Biomol Screen. 2006 Mar;11(2):194-207. Epub 2006 Feb 20.

PMID:
16490772
[PubMed - indexed for MEDLINE]
11.

Towards a high-affinity allosteric enhancer at muscarinic M1 receptors.

Lazareno S, Popham A, Birdsall NJ.

J Mol Neurosci. 2002 Aug-Oct;19(1-2):123-7.

PMID:
12212769
[PubMed - indexed for MEDLINE]
12.

Allosteric properties of G protein-coupled receptor oligomers.

Springael JY, Urizar E, Costagliola S, Vassart G, Parmentier M.

Pharmacol Ther. 2007 Sep;115(3):410-8. Epub 2007 Jun 27. Review.

PMID:
17655934
[PubMed - indexed for MEDLINE]
13.

G protein-coupled receptor allosterism and complexing.

Christopoulos A, Kenakin T.

Pharmacol Rev. 2002 Jun;54(2):323-74. Review.

PMID:
12037145
[PubMed - indexed for MEDLINE]
Free Article
14.

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.

PMID:
19767446
[PubMed - indexed for MEDLINE]
Free PMC Article
15.

Application of a kinetic model to the apparently complex behavior of negative and positive allosteric modulators of muscarinic acetylcholine receptors.

Avlani V, May LT, Sexton PM, Christopoulos A.

J Pharmacol Exp Ther. 2004 Mar;308(3):1062-72. Epub 2004 Jan 7.

PMID:
14711931
[PubMed - indexed for MEDLINE]
Free Article
16.

Identification of a [3H]Ligand for the common allosteric site of muscarinic acetylcholine M2 receptors.

Tränkle C, Mies-Klomfass E, Cid MH, Holzgrabe U, Mohr K.

Mol Pharmacol. 1998 Jul;54(1):139-45.

PMID:
9658199
[PubMed - indexed for MEDLINE]
Free Article
17.

Screening for positive allosteric modulators: assessment of modulator concentration-response curves as a screening paradigm.

Langmead CJ.

J Biomol Screen. 2007 Aug;12(5):668-76. Epub 2007 May 3.

PMID:
17478477
[PubMed - indexed for MEDLINE]
18.
19.

The role of transmembrane domain 3 in the actions of orthosteric, allosteric, and atypical agonists of the M4 muscarinic acetylcholine receptor.

Leach K, Davey AE, Felder CC, Sexton PM, Christopoulos A.

Mol Pharmacol. 2011 May;79(5):855-65. doi: 10.1124/mol.111.070938. Epub 2011 Feb 7.

PMID:
21300722
[PubMed - indexed for MEDLINE]
Free Article
20.

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.

PMID:
20406819
[PubMed - indexed for MEDLINE]
Free PMC Article
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