Published in Cell Signal on April 01, 2003
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Maternal imprinting at the H19-Igf2 locus maintains adult haematopoietic stem cell quiescence. Nature (2013) 2.22
Lipid G protein-coupled receptor ligand identification using beta-arrestin PathHunter assay. J Biol Chem (2009) 1.91
Cardiovascular effects of sphingosine-1-phosphate and other sphingomyelin metabolites. Br J Pharmacol (2004) 1.48
GPCR activation: protonation and membrane potential. Protein Cell (2013) 0.89
Deep sequencing of the murine olfactory receptor neuron transcriptome. PLoS One (2015) 0.87
Genome-wide sequencing for the identification of rearrangements associated with Tourette syndrome and obsessive-compulsive disorder. BMC Med Genet (2012) 0.82
Sphingosine-1-phosphate signaling in vasculogenesis and angiogenesis. World J Biol Chem (2010) 0.82
Analysis of the goldfish Carassius auratus olfactory epithelium transcriptome reveals the presence of numerous non-olfactory GPCR and putative receptors for progestin pheromones. BMC Genomics (2008) 0.81
Discrete influx events refill depleted Ca2+ stores in a chick retinal neuron. J Physiol (2007) 0.80
Intercellular Lipid Mediators and GPCR Drug Discovery. Biomol Ther (Seoul) (2013) 0.77
Differential expression of pancreatic protein and chemosensing receptor mRNAs in NKCC1-null intestine. World J Gastrointest Pathophysiol (2016) 0.76
Molecular mechanisms of target recognition by lipid GPCRs: relevance for cancer. Oncogene (2015) 0.75
Neuro-psychopharmacological perspective of Orphan receptors of Rhodopsin (class A) family of G protein-coupled receptors. Psychopharmacology (Berl) (2017) 0.75
PUMA-G and HM74 are receptors for nicotinic acid and mediate its anti-lipolytic effect. Nat Med (2003) 2.97
A heterodimer-selective agonist shows in vivo relevance of G protein-coupled receptor dimers. Proc Natl Acad Sci U S A (2005) 2.31
Matuzumab binding to EGFR prevents the conformational rearrangement required for dimerization. Cancer Cell (2008) 2.21
Deconvolution of complex G protein-coupled receptor signaling in live cells using dynamic mass redistribution measurements. Nat Biotechnol (2010) 2.11
An autocrine lactate loop mediates insulin-dependent inhibition of lipolysis through GPR81. Cell Metab (2010) 1.81
Heterotrimeric G-proteins: a short history. Br J Pharmacol (2006) 1.79
Decoding signaling and function of the orphan G protein-coupled receptor GPR17 with a small-molecule agonist. Sci Signal (2013) 1.71
Targeting the prostaglandin D2 receptors DP and CRTH2 for treatment of inflammation. Curr Top Med Chem (2006) 1.70
Nicotinic acid- and monomethyl fumarate-induced flushing involves GPR109A expressed by keratinocytes and COX-2-dependent prostanoid formation in mice. J Clin Invest (2010) 1.64
Identification of indole derivatives exclusively interfering with a G protein-independent signaling pathway of the prostaglandin D2 receptor CRTH2. Mol Pharmacol (2005) 1.54
GPR55 ligands promote receptor coupling to multiple signalling pathways. Br J Pharmacol (2010) 1.39
Phosphorylation by casein kinase 2 induces PACS-1 binding of nephrocystin and targeting to cilia. EMBO J (2005) 1.35
Phosphorylation and regulation of a G protein-coupled receptor by protein kinase CK2. J Cell Biol (2007) 1.31
GPR109A, GPR109B and GPR81, a family of hydroxy-carboxylic acid receptors. Trends Pharmacol Sci (2009) 1.28
Applying label-free dynamic mass redistribution technology to frame signaling of G protein-coupled receptors noninvasively in living cells. Nat Protoc (2011) 1.26
Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes. J Med Chem (2008) 1.25
Sphingosine 1-phosphate is a ligand of the human gpr3, gpr6 and gpr12 family of constitutively active G protein-coupled receptors. Cell Signal (2002) 1.22
GPR55 regulates cannabinoid 2 receptor-mediated responses in human neutrophils. Cell Res (2011) 1.21
Dualsteric GPCR targeting: a novel route to binding and signaling pathway selectivity. FASEB J (2008) 1.17
Antagonism of the prostaglandin D2 receptor CRTH2 attenuates asthma pathology in mouse eosinophilic airway inflammation. Respir Res (2007) 1.15
Thyrocyte-specific Gq/G11 deficiency impairs thyroid function and prevents goiter development. J Clin Invest (2007) 1.15
Effects of human urotensin II in isolated vessels of various species; comparison with other vasoactive agents. Naunyn Schmiedebergs Arch Pharmacol (2001) 1.14
Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist. J Med Chem (2005) 1.12
Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3. J Biol Chem (2011) 1.09
Characterization of c-kit expression in small cell lung cancer: prognostic and therapeutic implications. Clin Cancer Res (2003) 1.09
Rational design of dualsteric GPCR ligands: quests and promise. Br J Pharmacol (2010) 1.07
A physicogenetic method to assign ligand-binding relationships between 7TM receptors. Bioorg Med Chem Lett (2005) 1.06
The novel cellular mechanism of human 5-HT6 receptor through an interaction with Fyn. J Biol Chem (2006) 1.06
Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties. J Med Chem (2012) 1.06
Conserved MIP receptor-ligand pair regulates Platynereis larval settlement. Proc Natl Acad Sci U S A (2013) 1.05
The allosteric vestibule of a seven transmembrane helical receptor controls G-protein coupling. Nat Commun (2012) 1.05
Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties. J Med Chem (2011) 1.03
The C-terminal tail of CRTH2 is a key molecular determinant that constrains Galphai and downstream signaling cascade activation. J Biol Chem (2008) 1.01
Mutation of tyrosine in the conserved NPXXY sequence leads to constitutive phosphorylation and internalization, but not signaling, of the human B2 bradykinin receptor. J Biol Chem (2004) 1.01
Extracellular loop 2 of the free fatty acid receptor 2 mediates allosterism of a phenylacetamide ago-allosteric modulator. Mol Pharmacol (2011) 0.99
The tyrosine kinase Pyk2 regulates Arf1 activity by phosphorylation and inhibition of the Arf-GTPase-activating protein ASAP1. J Biol Chem (2003) 0.98
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling. J Med Chem (2009) 0.98
The role of the prostaglandin D2 receptor, DP, in eosinophil trafficking. J Immunol (2007) 0.98
Prediction of the 3D structure and dynamics of human DP G-protein coupled receptor bound to an agonist and an antagonist. J Am Chem Soc (2007) 0.96
Lack of evidence for AT1R/B2R heterodimerization in COS-7, HEK293, and NIH3T3 cells: how common is the AT1R/B2R heterodimer? J Biol Chem (2008) 0.95
A new ligand for the urotensin II receptor. Br J Pharmacol (2002) 0.95
Pharmacological profile of NOP receptors coupled with calcium signaling via the chimeric protein G alpha qi5. Naunyn Schmiedebergs Arch Pharmacol (2009) 0.95
Deorphanization of GPR109B as a receptor for the beta-oxidation intermediate 3-OH-octanoic acid and its role in the regulation of lipolysis. J Biol Chem (2009) 0.95
Protective autophagy is involved in resistance towards MET inhibitors in human gastric adenocarcinoma cells. Biochem Biophys Res Commun (2013) 0.95
Nicotinic acid (niacin): new lipid-independent mechanisms of action and therapeutic potentials. Trends Pharmacol Sci (2011) 0.94
Conjugated linoleic acids mediate insulin release through islet G protein-coupled receptor FFA1/GPR40. J Biol Chem (2011) 0.93
Identification of a novel site within G protein alpha subunits important for specificity of receptor-G protein interaction. Mol Pharmacol (2004) 0.93
A biased ligand for OXE-R uncouples Gα and Gβγ signaling within a heterotrimer. Nat Chem Biol (2012) 0.92
EMD 1214063 and EMD 1204831 constitute a new class of potent and highly selective c-Met inhibitors. Clin Cancer Res (2013) 0.89
Mechanisms for 2-methoxyestradiol-induced apoptosis of prostate cancer cells. FEBS Lett (2002) 0.88
Chemically engineering ligand selectivity at the free fatty acid receptor 2 based on pharmacological variation between species orthologs. FASEB J (2012) 0.88
Novel CRTH2 antagonists: a review of patents from 2006 to 2009. Expert Opin Ther Pat (2010) 0.88
Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes. ACS Med Chem Lett (2013) 0.87
An optical dynamic mass redistribution assay reveals biased signaling of dualsteric GPCR activators. J Recept Signal Transduct Res (2009) 0.87
Nephrocystin-4 regulates Pyk2-induced tyrosine phosphorylation of nephrocystin-1 to control targeting to monocilia. J Biol Chem (2011) 0.87
Reevaluation of fatty acid receptor 1 as a drug target for the stimulation of insulin secretion in humans. Diabetes (2013) 0.87
Regulated and constitutive activation of specific signalling pathways by the human S1P5 receptor. Br J Pharmacol (2003) 0.85
Functional and binding characterizations of urotensin II-related peptides in human and rat urotensin II-receptor assay. J Pharmacol Exp Ther (2003) 0.84
Discovery of a potent and selective free fatty acid receptor 1 agonist with low lipophilicity and high oral bioavailability. J Med Chem (2013) 0.83
Fluid shear stress differentially regulates gpr3, gpr6, and gpr12 expression in human umbilical vein endothelial cells. Cell Physiol Biochem (2003) 0.82
On the mechanism of interaction of potent surmountable and insurmountable antagonists with the prostaglandin D2 receptor CRTH2. Mol Pharmacol (2006) 0.82
Urotensin II causes fatal circulatory collapse in anesthesized monkeys in vivo: a "vasoconstrictor" with a unique hemodynamic profile. Am J Physiol Heart Circ Physiol (2003) 0.82
D-type prostanoid receptor enhances the signaling of chemoattractant receptor-homologous molecule expressed on T(H)2 cells. J Allergy Clin Immunol (2011) 0.82
Comparative analysis of functional assays for characterization of agonist ligands at G protein-coupled receptors. J Biomol Screen (2003) 0.80
Muscarinic allosteric modulators: atypical structure-activity-relationships in bispyridinium-type compounds. Arch Pharm (Weinheim) (2006) 0.80
Functional human 5-HT6 receptor assay for high throughput screening of chemical ligands and binding proteins. Comb Chem High Throughput Screen (2008) 0.79
A biased non-Gαi OXE-R antagonist demonstrates that Gαi protein subunit is not directly involved in neutrophil, eosinophil, and monocyte activation by 5-oxo-ETE. J Immunol (2014) 0.79
Comparative analysis of human and rat S1P(5) (edg8): differential expression profiles and sensitivities to antagonists. Biochem Pharmacol (2002) 0.79
PGH1, the precursor for the anti-inflammatory prostaglandins of the 1-series, is a potent activator of the pro-inflammatory receptor CRTH2/DP2. PLoS One (2012) 0.78
Mining the potential of label-free biosensors for seven-transmembrane receptor drug discovery. Prog Mol Biol Transl Sci (2013) 0.78
Understanding DP receptor antagonism using a CoMSIA approach. Bioorg Med Chem Lett (2010) 0.78
Modulation of myocardial contractility by lysophosphatidic acid (LPA). J Mol Cell Cardiol (2003) 0.78
Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits. J Med Chem (2006) 0.77
Dualsteric muscarinic antagonists--orthosteric binding pose controls allosteric subtype selectivity. J Med Chem (2014) 0.77
The novel ATP-competitive inhibitor of the MET hepatocyte growth factor receptor EMD1214063 displays inhibitory activity against selected MET-mutated variants. Mol Cancer Ther (2013) 0.77
Label-free biosensor assays in GPCR screening. Methods Mol Biol (2015) 0.76
Signaling pathways: Purinosomes under GPCR control. Nat Chem Biol (2011) 0.76
Mice Lacking Free Fatty Acid Receptor 1 (GPR40/FFAR1) are Protected Against Conjugated Linoleic Acid-Induced Fatty Liver but Develop Inflammation and Insulin Resistance in the Brain. Cell Physiol Biochem (2015) 0.76
Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D2 receptor CRTH2. Bioorg Med Chem Lett (2007) 0.75
Assay and functional properties of the tyrosine kinase Pyk2 in regulation of Arf1 through ASAP1 phosphorylation. Methods Enzymol (2005) 0.75
Detection of free fatty acid receptor 1 expression: the critical role of negative and positive controls. Diabetologia (2014) 0.75
Novel insights into appropriate encapsulation methods for bioactive compounds into polymers: a study with peptides and HDAC inhibitors. Macromol Biosci (2013) 0.75
Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2. Bioorg Med Chem Lett (2009) 0.75
Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1. Bioorg Med Chem Lett (2009) 0.75