Published in Br J Pharmacol on August 13, 2007
Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery. Pharmacol Rev (2010) 3.27
The effect of ligand efficacy on the formation and stability of a GPCR-G protein complex. Proc Natl Acad Sci U S A (2009) 2.86
Ligand-specific interactions modulate kinetic, energetic, and mechanical properties of the human β2 adrenergic receptor. Structure (2012) 1.85
Morphine-like opiates selectively antagonize receptor-arrestin interactions. J Biol Chem (2010) 1.45
New concepts in pharmacological efficacy at 7TM receptors: IUPHAR review 2. Br J Pharmacol (2013) 1.43
Discovery and characterization of a G protein-biased agonist that inhibits β-arrestin recruitment to the D2 dopamine receptor. Mol Pharmacol (2014) 0.96
Biased agonism. F1000 Biol Rep (2009) 0.88
Ensemble of G protein-coupled receptor active states. Curr Med Chem (2012) 0.88
An innovative method to classify SERMs based on the dynamics of estrogen receptor transcriptional activity in living animals. Mol Endocrinol (2010) 0.85
Identification of G protein-biased agonists that fail to recruit β-arrestin or promote internalization of the D1 dopamine receptor. ACS Chem Neurosci (2015) 0.80
Being mindful of seven-transmembrane receptor 'guests' when assessing agonist selectivity. Br J Pharmacol (2010) 0.78
A modification of receptor theory. Br J Pharmacol Chemother (1956) 14.20
The fluorescent toolbox for assessing protein location and function. Science (2006) 14.02
Transduction of receptor signals by beta-arrestins. Science (2005) 9.87
Functional selectivity and classical concepts of quantitative pharmacology. J Pharmacol Exp Ther (2006) 7.03
Beta-arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G protein-coupled receptors. Proc Natl Acad Sci U S A (2003) 3.75
Functionally different agonists induce distinct conformations in the G protein coupling domain of the beta 2 adrenergic receptor. J Biol Chem (2001) 3.41
Oligomerization of G-protein-coupled transmitter receptors. Nat Rev Neurosci (2001) 3.30
Agonist-receptor efficacy. II. Agonist trafficking of receptor signals. Trends Pharmacol Sci (1995) 3.25
Illuminating insights into protein-protein interactions using bioluminescence resonance energy transfer (BRET). Nat Methods (2006) 3.17
New roles for beta-arrestins in cell signaling: not just for seven-transmembrane receptors. Mol Cell (2006) 3.11
Distinct beta-arrestin- and G protein-dependent pathways for parathyroid hormone receptor-stimulated ERK1/2 activation. J Biol Chem (2006) 3.00
Distinct signaling profiles of beta1 and beta2 adrenergic receptor ligands toward adenylyl cyclase and mitogen-activated protein kinase reveals the pluridimensionality of efficacy. Mol Pharmacol (2006) 2.69
Sequential binding of agonists to the beta2 adrenoceptor. Kinetic evidence for intermediate conformational states. J Biol Chem (2003) 2.68
Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins. Proc Natl Acad Sci U S A (1989) 2.51
Inverse, protean, and ligand-selective agonism: matters of receptor conformation. FASEB J (2001) 2.51
Drug efficacy at G protein-coupled receptors. Annu Rev Pharmacol Toxicol (2002) 2.22
Historical review: a brief history and personal retrospective of seven-transmembrane receptors. Trends Pharmacol Sci (2004) 2.22
The CCR5 receptor-based mechanism of action of 873140, a potent allosteric noncompetitive HIV entry inhibitor. Mol Pharmacol (2005) 2.16
An opioid agonist that does not induce mu-opioid receptor--arrestin interactions or receptor internalization. Mol Pharmacol (2006) 2.06
Chemically distinct ligands promote differential CB1 cannabinoid receptor-Gi protein interactions. Mol Pharmacol (2005) 1.86
What's next in translational medicine? Clin Sci (Lond) (2007) 1.85
The ligand paradox between affinity and efficacy: can you be there and not make a difference? Trends Pharmacol Sci (2002) 1.78
Agonist and inverse agonist actions of beta-blockers at the human beta 2-adrenoceptor provide evidence for agonist-directed signaling. Mol Pharmacol (2003) 1.67
Pharmacological proteus? Trends Pharmacol Sci (1995) 1.67
Receptor activity-independent recruitment of betaarrestin2 reveals specific signalling modes. EMBO J (2004) 1.55
Paradoxical trafficking and regulation of 5-HT(2A) receptors by agonists and antagonists. Brain Res Bull (2001) 1.53
Fluorescent labeling of purified beta 2 adrenergic receptor. Evidence for ligand-specific conformational changes. J Biol Chem (1995) 1.52
Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors. Mol Pharmacol (1997) 1.38
Composition and function of g protein-coupled receptor signalsomes controlling mitogen-activated protein kinase activity. J Mol Neurosci (2005) 1.36
Efficacy as a vector: the relative prevalence and paucity of inverse agonism. Mol Pharmacol (2004) 1.35
Inverse agonism of histamine H2 antagonist accounts for upregulation of spontaneously active histamine H2 receptors. Proc Natl Acad Sci U S A (1996) 1.25
Chemokine blockers--therapeutics in the making? Trends Pharmacol Sci (2005) 1.21
Inverse agonism and the regulation of receptor number. Trends Pharmacol Sci (1997) 1.21
Identification of allosteric peptide agonists of CXCR4. J Biol Chem (2002) 1.19
The use of stimulus-biased assay systems to detect agonist-specific receptor active states: implications for the trafficking of receptor stimulus by agonists. Mol Pharmacol (2000) 1.18
Protein biosensors based on the principle of fluorescence resonance energy transfer for monitoring cellular dynamics. Biotechnol Lett (2006) 1.18
The neurokinin A receptor activates calcium and cAMP responses through distinct conformational states. J Biol Chem (2001) 1.11
The dynamin-dependent, arrestin-independent internalization of 5-hydroxytryptamine 2A (5-HT2A) serotonin receptors reveals differential sorting of arrestins and 5-HT2A receptors during endocytosis. J Biol Chem (2000) 1.10
Ago-antagonist muscle spindle inputs contribute together to joint movement coding in man. Brain Res (1998) 1.08
Clozapine and other 5-hydroxytryptamine-2A receptor antagonists alter the subcellular distribution of 5-hydroxytryptamine-2A receptors in vitro and in vivo. Neuroscience (1999) 1.08
Agonist-induced modulation of inverse agonist efficacy at the beta 2-adrenergic receptor. Mol Pharmacol (1996) 1.08
Achieving signalling selectivity of ligands for the corticotropin-releasing factor type 1 receptor by modifying the agonist's signalling domain. Br J Pharmacol (2007) 0.99
Bombesin and substance P analogues differentially regulate G-protein coupling to the bombesin receptor. Direct evidence for biased agonism. J Biol Chem (2001) 0.96
Agonist efficacy and allosteric models of receptor action. Ann N Y Acad Sci (1997) 0.96
Ago-allosteric modulation and other types of allostery in dimeric 7TM receptors. J Recept Signal Transduct Res (2006) 0.95
Tracking the opioid receptors on the way of desensitization. Cell Signal (2006) 0.93
Inhibitory effect of oxytocin on corticotrope function in humans: are vasopressin and oxytocin ying-yang neurohormones? Psychoneuroendocrinology (2001) 0.92
Opioid receptors are coupled tightly to G proteins but loosely to adenylate cyclase in NG108-15 cell membranes. Mol Pharmacol (1988) 0.91
Collateral efficacy as a pharmacological problem applied to new drug discovery. Expert Opin Drug Discov (2006) 0.87
Technology Insight: modern methods to monitor protein-protein interactions reveal functional TSH receptor oligomerization. Nat Clin Pract Endocrinol Metab (2007) 0.84
The new generation of antipsychotic drugs: how atypical are they? Int J Neuropsychopharmacol (2000) 0.84
Selective and divergent regulation of cortical 5-HT(2A) receptors in rabbit. J Pharmacol Exp Ther (2001) 0.81