Published in Mol Pharmacol on October 15, 2008
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Identification of orthosteric and allosteric site mutations in M2 muscarinic acetylcholine receptors that contribute to ligand-selective signaling bias. J Biol Chem (2010) 1.46
Allosteric modulation of metabotropic glutamate receptors: structural insights and therapeutic potential. Neuropharmacology (2010) 1.30
A conserved aromatic lock for the tryptophan rotameric switch in TM-VI of seven-transmembrane receptors. J Biol Chem (2009) 1.25
Functionally biased signalling properties of 7TM receptors - opportunities for drug development for the ghrelin receptor. Br J Pharmacol (2013) 0.92
Growth hormone secretagogues and growth hormone releasing peptides act as orthosteric super-agonists but not allosteric regulators for activation of the G protein Galpha(o1) by the Ghrelin receptor. Mol Pharmacol (2009) 0.89
Molecular characterization of oxysterol binding to the Epstein-Barr virus-induced gene 2 (GPR183). J Biol Chem (2012) 0.88
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Heterodimerization with Its splice variant blocks the ghrelin receptor 1a in a non-signaling conformation: a study with a purified heterodimer assembled into lipid discs. J Biol Chem (2013) 0.84
Structural and functional roles of small group-conserved amino acids present on helix-H7 in the β(2)-adrenergic receptor. Biochim Biophys Acta (2011) 0.82
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Molecular mechanism of 7TM receptor activation--a global toggle switch model. Annu Rev Pharmacol Toxicol (2006) 3.33
Ligand binding and micro-switches in 7TM receptor structures. Trends Pharmacol Sci (2009) 2.33
High constitutive signaling of the ghrelin receptor--identification of a potent inverse agonist. Mol Endocrinol (2003) 1.97
GPR41/FFAR3 and GPR43/FFAR2 as cosensors for short-chain fatty acids in enteroendocrine cells vs FFAR3 in enteric neurons and FFAR2 in enteric leukocytes. Endocrinology (2013) 1.89
High constitutive activity of a virus-encoded seven transmembrane receptor in the absence of the conserved DRY motif (Asp-Arg-Tyr) in transmembrane helix 3. Mol Pharmacol (2005) 1.86
The chemokine system -- a major regulator of angiogenesis in health and disease. APMIS (2004) 1.72
Localization of HCMV UL33 and US27 in endocytic compartments and viral membranes. Traffic (2002) 1.65
GPR39 signaling is stimulated by zinc ions but not by obestatin. Endocrinology (2006) 1.60
Murine cytomegalovirus (CMV) M33 and human CMV US28 receptors exhibit similar constitutive signaling activities. J Virol (2002) 1.56
Molecular mechanism of AMD3100 antagonism in the CXCR4 receptor: transfer of binding site to the CXCR3 receptor. J Biol Chem (2003) 1.50
Common structural basis for constitutive activity of the ghrelin receptor family. J Biol Chem (2004) 1.49
Metal ion enhanced binding of AMD3100 to Asp262 in the CXCR4 receptor. Biochemistry (2003) 1.40
The human herpes virus 8-encoded chemokine receptor is required for angioproliferation in a murine model of Kaposi's sarcoma. J Immunol (2005) 1.35
Metal ion site engineering indicates a global toggle switch model for seven-transmembrane receptor activation. J Biol Chem (2006) 1.35
The minor binding pocket: a major player in 7TM receptor activation. Trends Pharmacol Sci (2010) 1.35
A gut feeling for obesity: 7TM sensors on enteroendocrine cells. Cell Metab (2008) 1.35
Molecular pharmacological phenotyping of EBI2. An orphan seven-transmembrane receptor with constitutive activity. J Biol Chem (2006) 1.32
A major lineage of enteroendocrine cells coexpress CCK, secretin, GIP, GLP-1, PYY, and neurotensin but not somatostatin. Endocrinology (2012) 1.31
A conserved aromatic lock for the tryptophan rotameric switch in TM-VI of seven-transmembrane receptors. J Biol Chem (2009) 1.25
Oxyntomodulin differentially affects glucagon-like peptide-1 receptor beta-arrestin recruitment and signaling through Galpha(s). J Pharmacol Exp Ther (2007) 1.22
Structural biology: A moving story of receptors. Nature (2008) 1.22
The carboxyl terminus of human cytomegalovirus-encoded 7 transmembrane receptor US28 camouflages agonism by mediating constitutive endocytosis. J Biol Chem (2003) 1.20
GPR119 as a fat sensor. Trends Pharmacol Sci (2012) 1.20
Constitutive ghrelin receptor activity as a signaling set-point in appetite regulation. Trends Pharmacol Sci (2004) 1.15
Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells. Mol Metab (2013) 1.14
Molecular mechanism of action of monocyclam versus bicyclam non-peptide antagonists in the CXCR4 chemokine receptor. J Biol Chem (2007) 1.13
AMD3465, a monomacrocyclic CXCR4 antagonist and potent HIV entry inhibitor. Biochem Pharmacol (2005) 1.11
NK1 receptor fused to beta-arrestin displays a single-component, high-affinity molecular phenotype. Mol Pharmacol (2002) 1.08
Importance of constitutive activity and arrestin-independent mechanisms for intracellular trafficking of the ghrelin receptor. Mol Endocrinol (2007) 1.07
Nonpeptide and peptide growth hormone secretagogues act both as ghrelin receptor agonist and as positive or negative allosteric modulators of ghrelin signaling. Mol Endocrinol (2005) 1.07
Similar activation of signal transduction pathways by the herpesvirus-encoded chemokine receptors US28 and ORF74. Virology (2004) 1.06
The imprinted gene neuronatin is regulated by metabolic status and associated with obesity. Obesity (Silver Spring) (2009) 1.02
CC and CX3C chemokines differentially interact with the N terminus of the human cytomegalovirus-encoded US28 receptor. J Biol Chem (2004) 1.01
Enteroendocrine cell types revisited. Curr Opin Pharmacol (2013) 1.00
Positive versus negative modulation of different endogenous chemokines for CC-chemokine receptor 1 by small molecule agonists through allosteric versus orthosteric binding. J Biol Chem (2008) 0.99
Conserved water-mediated hydrogen bond network between TM-I, -II, -VI, and -VII in 7TM receptor activation. J Biol Chem (2010) 0.99
Allosteric and orthosteric sites in CC chemokine receptor (CCR5), a chimeric receptor approach. J Biol Chem (2011) 0.98
Characterization of glucagon-like peptide-1 receptor beta-arrestin 2 interaction: a high-affinity receptor phenotype. Mol Endocrinol (2004) 0.97
Identification of an efficacy switch region in the ghrelin receptor responsible for interchange between agonism and inverse agonism. J Biol Chem (2007) 0.96
G protein-coupled receptor 39 deficiency is associated with pancreatic islet dysfunction. Endocrinology (2009) 0.96
Ghrelin receptor mutations--too little height and too much hunger. J Clin Invest (2006) 0.95
Biased and constitutive signaling in the CC-chemokine receptor CCR5 by manipulating the interface between transmembrane helices 6 and 7. J Biol Chem (2013) 0.95
Long-acting lipidated analogue of human pancreatic polypeptide is slowly released into circulation. J Med Chem (2011) 0.94
Metal ion-mediated agonism and agonist enhancement in melanocortin MC1 and MC4 receptors. J Biol Chem (2002) 0.94
Identification of a novel site within G protein alpha subunits important for specificity of receptor-G protein interaction. Mol Pharmacol (2004) 0.93
Molecular mechanism of agonism and inverse agonism in the melanocortin receptors: Zn(2+) as a structural and functional probe. Ann N Y Acad Sci (2003) 0.93
Ligand modulation of the Epstein-Barr virus-induced seven-transmembrane receptor EBI2: identification of a potent and efficacious inverse agonist. J Biol Chem (2011) 0.92
GluVII:06--a highly conserved and selective anchor point for non-peptide ligands in chemokine receptors. Curr Top Med Chem (2006) 0.91
Mutations at the CXCR4 interaction sites for AMD3100 influence anti-CXCR4 antibody binding and HIV-1 entry. FEBS Lett (2003) 0.90
Molecular mechanism of Zn2+ agonism in the extracellular domain of GPR39. FEBS Lett (2008) 0.90
Design and optimization of quinazoline derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists. Bioorg Med Chem Lett (2012) 0.90
Kaposi sarcoma-associated herpes virus targets the lymphotactin receptor with both a broad spectrum antagonist vCCL2 and a highly selective and potent agonist vCCL3. J Biol Chem (2007) 0.89
GPR39 splice variants versus antisense gene LYPD1: expression and regulation in gastrointestinal tract, endocrine pancreas, liver, and white adipose tissue. Mol Endocrinol (2007) 0.89
Activation of the CXCR3 chemokine receptor through anchoring of a small molecule chelator ligand between TM-III, -IV, and -VI. Mol Pharmacol (2006) 0.88
Molecular interaction of a potent nonpeptide agonist with the chemokine receptor CCR8. Mol Pharmacol (2007) 0.88
Bioorthogonal fluorescent labeling of functional G-protein-coupled receptors. Chembiochem (2014) 0.87
Characterization of G-protein coupled receptor kinase interaction with the neurokinin-1 receptor using bioluminescence resonance energy transfer. Mol Pharmacol (2007) 0.87
The virus-encoded chemokine vMIP-II inhibits virus-induced Tc1-driven inflammation. J Virol (2003) 0.87
Distinct in vitro interaction pattern of dopamine receptor subtypes with adaptor proteins involved in post-endocytotic receptor targeting. FEBS Lett (2004) 0.87
MTNR1B G24E variant associates With BMI and fasting plasma glucose in the general population in studies of 22,142 Europeans. Diabetes (2010) 0.86
PheVI:09 (Phe6.44) as a sliding microswitch in seven-transmembrane (7TM) G protein-coupled receptor activation. J Biol Chem (2012) 0.85
Virally encoded chemokines and chemokine receptors in the role of viral infections. Contrib Microbiol (2003) 0.84
Assessment and challenges of ligand docking into comparative models of G-protein coupled receptors. PLoS One (2013) 0.84
The CXC chemokine receptor encoded by herpesvirus saimiri, ECRF3, shows ligand-regulated signaling through Gi, Gq, and G12/13 proteins but constitutive signaling only through Gi and G12/13 proteins. J Biol Chem (2004) 0.84
Ghrelin receptor inverse agonists: identification of an active peptide core and its interaction epitopes on the receptor. Mol Pharmacol (2006) 0.84
β-Cell Specific Overexpression of GPR39 Protects against Streptozotocin-Induced Hyperglycemia. Int J Endocrinol (2011) 0.84
A second disulfide bridge from the N-terminal domain to extracellular loop 2 dampens receptor activity in GPR39. Biochemistry (2008) 0.84
A highly selective CCR2 chemokine agonist encoded by human herpesvirus 6. J Biol Chem (2003) 0.83
Modulation of constitutive activity and signaling bias of the ghrelin receptor by conformational constraint in the second extracellular loop. J Biol Chem (2012) 0.83
The PP-fold solution structure of human polypeptide YY and human PYY3-36 as determined by NMR. Biochemistry (2006) 0.83
Dissecting signaling and functions of adhesion G protein-coupled receptors. Ann N Y Acad Sci (2012) 0.83
Single-chain vascular endothelial growth factor variant with antagonist activity. J Biol Chem (2002) 0.83
Inhibition of human immunodeficiency virus replication by a dual CCR5/CXCR4 antagonist. J Virol (2004) 0.83
G protein-coupled receptor modulation with pepducins: moving closer to the clinic. Ann N Y Acad Sci (2011) 0.82
Modulation in selectivity and allosteric properties of small-molecule ligands for CC-chemokine receptors. J Med Chem (2012) 0.82
An aromatic region to induce a switch between agonism and inverse agonism at the ghrelin receptor. J Med Chem (2012) 0.81
The arginine of the DRY motif in transmembrane segment III functions as a balancing micro-switch in the activation of the β2-adrenergic receptor. J Biol Chem (2012) 0.81
Unique interaction pattern for a functionally biased ghrelin receptor agonist. J Biol Chem (2011) 0.81
PDZ domain-mediated interactions of G protein-coupled receptors with postsynaptic density protein 95: quantitative characterization of interactions. PLoS One (2013) 0.80
Design and optimization of quinazoline derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists: part 2. Bioorg Med Chem Lett (2012) 0.80