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Therapeutic potential of β-arrestin- and G protein-biased agonists.

Whalen EJ, Rajagopal S, Lefkowitz RJ.

Trends Mol Med. 2011 Mar;17(3):126-39. doi: 10.1016/j.molmed.2010.11.004. Epub 2010 Dec 21. Review.


Quantification of functional selectivity at the human α(1A)-adrenoceptor.

Evans BA, Broxton N, Merlin J, Sato M, Hutchinson DS, Christopoulos A, Summers RJ.

Mol Pharmacol. 2011 Feb;79(2):298-307. doi: 10.1124/mol.110.067454. Epub 2010 Oct 26. Erratum in: Mol Pharmacol. 2011 Mar;79(3):627.


Differential signaling of the endogenous agonists at the beta2-adrenergic receptor.

Reiner S, Ambrosio M, Hoffmann C, Lohse MJ.

J Biol Chem. 2010 Nov 12;285(46):36188-98. doi: 10.1074/jbc.M110.175604. Epub 2010 Sep 13.


Selectively engaging β-arrestins at the angiotensin II type 1 receptor reduces blood pressure and increases cardiac performance.

Violin JD, DeWire SM, Yamashita D, Rominger DH, Nguyen L, Schiller K, Whalen EJ, Gowen M, Lark MW.

J Pharmacol Exp Ther. 2010 Dec;335(3):572-9. doi: 10.1124/jpet.110.173005. Epub 2010 Aug 26.


μ-opioid receptors: correlation of agonist efficacy for signalling with ability to activate internalization.

McPherson J, Rivero G, Baptist M, Llorente J, Al-Sabah S, Krasel C, Dewey WL, Bailey CP, Rosethorne EM, Charlton SJ, Henderson G, Kelly E.

Mol Pharmacol. 2010 Oct;78(4):756-66. doi: 10.1124/mol.110.066613. Epub 2010 Jul 20.


Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner: implications for drug screening.

Koole C, Wootten D, Simms J, Valant C, Sridhar R, Woodman OL, Miller LJ, Summers RJ, Christopoulos A, Sexton PM.

Mol Pharmacol. 2010 Sep;78(3):456-65. doi: 10.1124/mol.110.065664. Epub 2010 Jun 14.


Teaching old receptors new tricks: biasing seven-transmembrane receptors.

Rajagopal S, Rajagopal K, Lefkowitz RJ.

Nat Rev Drug Discov. 2010 May;9(5):373-86. doi: 10.1038/nrd3024. Review.


Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery.

Kenakin T, Miller LJ.

Pharmacol Rev. 2010 Jun;62(2):265-304. doi: 10.1124/pr.108.000992. Epub 2010 Apr 14. Review.


A beta-arrestin-biased agonist of the parathyroid hormone receptor (PTH1R) promotes bone formation independent of G protein activation.

Gesty-Palmer D, Flannery P, Yuan L, Corsino L, Spurney R, Lefkowitz RJ, Luttrell LM.

Sci Transl Med. 2009 Oct 7;1(1):1ra1. doi: 10.1126/scitranslmed.3000071.


Morphine-like opiates selectively antagonize receptor-arrestin interactions.

Molinari P, Vezzi V, Sbraccia M, Grò C, Riitano D, Ambrosio C, Casella I, Costa T.

J Biol Chem. 2010 Apr 23;285(17):12522-35. doi: 10.1074/jbc.M109.059410. Epub 2010 Feb 26.


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.


Selectivity of agonists for the active state of M1 to M4 muscarinic receptor subtypes.

Figueroa KW, Griffin MT, Ehlert FJ.

J Pharmacol Exp Ther. 2009 Jan;328(1):331-42. doi: 10.1124/jpet.108.145219. Epub 2008 Sep 29.


Novel genetically encoded biosensors using firefly luciferase.

Fan F, Binkowski BF, Butler BL, Stecha PF, Lewis MK, Wood KV.

ACS Chem Biol. 2008 Jun 20;3(6):346-51. doi: 10.1021/cb8000414.


On the analysis of ligand-directed signaling at G protein-coupled receptors.

Ehlert FJ.

Naunyn Schmiedebergs Arch Pharmacol. 2008 Jun;377(4-6):549-77. doi: 10.1007/s00210-008-0260-4. Epub 2008 Feb 6. Review.


The genetic design of signaling cascades to record receptor activation.

Barnea G, Strapps W, Herrada G, Berman Y, Ong J, Kloss B, Axel R, Lee KJ.

Proc Natl Acad Sci U S A. 2008 Jan 8;105(1):64-9. doi: 10.1073/pnas.0710487105. Epub 2007 Dec 28.


beta-arrestin-biased agonism at the beta2-adrenergic receptor.

Drake MT, Violin JD, Whalen EJ, Wisler JW, Shenoy SK, Lefkowitz RJ.

J Biol Chem. 2008 Feb 29;283(9):5669-76. Epub 2007 Dec 17.


A unique mechanism of beta-blocker action: carvedilol stimulates beta-arrestin signaling.

Wisler JW, DeWire SM, Whalen EJ, Violin JD, Drake MT, Ahn S, Shenoy SK, Lefkowitz RJ.

Proc Natl Acad Sci U S A. 2007 Oct 16;104(42):16657-62. Epub 2007 Oct 9.


Functional selectivity through protean and biased agonism: who steers the ship?

Kenakin T.

Mol Pharmacol. 2007 Dec;72(6):1393-401. Epub 2007 Sep 27. Review.


Beta-arrestins and cell signaling.

DeWire SM, Ahn S, Lefkowitz RJ, Shenoy SK.

Annu Rev Physiol. 2007;69:483-510. Review.

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