Site-directed mutagenesis and PBAN activation of the Helicoverpa zea PBAN-receptor
Keywords: PBAN-receptor; GPCR; Point mutation; Extracellular domain; Pyrokinin;
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3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu5: Identification of easily prepared tool compounds with CNS exposure in rats
Keywords: mGlu5; GPCR; Allosteric modulator; CNS; GERD; Fragile X syndrome; Addiction; PD-LID;
Piperidinyl-nicotinamides as potent and selective somatostatin receptor subtype 5 antagonists
Keywords: GPCR; Somatostatin; Pancreas; Antagonists;
Mapping the CGRP receptor ligand binding domain: Tryptophan-84 of RAMP1 is critical for agonist and antagonist binding
Keywords: CGRP; Migraine; Telcagepant; GPCR;
Functional coupling of Cys-226 and Cys-296 in the glucagon-like peptide-1 (GLP-1) receptor indicates a disulfide bond that is close to the activation pocket
Keywords: GPCR; GLP-1; Mutagenesis; Agonist; Receptor
A novel enzyme immunoassay for the determination of phosphatidylserine-specific phospholipase A1 in human serum samples
Keywords: LPS; lysophosphatidylserine; LPA; lysophosphatidic acid; Sph-1-P; sphingosine 1-phosphate; PS; phosphatidylserine; RPMC; rat peritoneal mast cell; GPCR; G protein coupled receptor; PTX; pertussis toxin; sPLA2-IIA; secretory-type phospholipase A2; PS-PLA1;
Molecular basis of lysophosphatidic acid-induced NF-κB activation
Keywords: NF-κB; LPA; GPCR
Dynamic association of p300 with the promoter of the G protein-coupled rat delta opioid receptor gene during NGF-induced neuronal differentiation
Keywords: p300; NGF; GPCR; NF-κB; RNA polymerase II; Neuronal differentiation
Functional expression of 5-HT2A receptor in osteoblastic MC3T3-E1 cells
Keywords: 5-HT, 5-hydroxytryptamine; 5-HTT, 5-HT transporter; α-MEM, α-modification of minimum essential medium; DIC, days in culture; DOI, (±)-1-(2,5-di-methoxy-4-iodophenyl-2) aminopropane; ERK, extracellular signal-regulated-kinase; FBS, fetal bovine serum; GPCR
Discovery of substituted benzyl tetrazoles as histamine H3 receptor antagonists
Keywords: Histamine; H3R; Antagonists; CNS; GPCR; Drug discovery
Identification and hit-to-lead optimization of a novel class of CB1 antagonists
Keywords: Cannabinoid; CB1; Antagonist; GPCR; Obesity; Benzimidazole; Indole; Inverted indole
Pyrido pyrimidinones as selective agonists of the high affinity niacin receptor GPR109A: Optimization of in vitro activity
Keywords: Flushing; GPR109A; GPR109B; GPCR; Lead identification; Lipolysis; Niacin; Pyrido pyrimidinone
Synthesis of novel 7-imino-2-thioxo-3,7-dihydro-2H-thiazolo [4,5-d] pyrimidine derivatives as adenosine A2A receptor antagonists
Keywords: Adenosine; A2AR; Combinatorial chemistry; GPCR; Radioligand binding; Parkinson’s disease; Thiazolopyrimidines
Identification of a red-emitting fluorescent ligand for in vitro visualization of human serotonin 5-HT1A receptors
Keywords: 5-HT1A receptor; Fluorescence; SAR; 1-Arylpiperazine; Confocal laser scanning microscopy; 8-OH-DPAT; 8-hydroxy-N,N-dipropylaminotetraline; GPCR; G-protein coupled receptor;
Novel GPR119 agonist AS1535907 contributes to first-phase insulin secretion in rat perfused pancreas and diabetic db/db mice
Keywords: GPR119; G protein-coupled receptor 119; GSIS; glucose-stimulated insulin secretion; T2DM; type 2 diabetes mellitus; SU; sulfonylurea; GPCR; G protein-coupled receptor; GLP-1; glucagon-like peptide-1; HEK; human embryonic kidney; LPC; lysophosphatidylcholi
Modulation of μ-opioid receptor desensitization in peripheral sensory neurons by phosphoinositide 3-kinase γ
Keywords: MOR; PI3Kγ; DRG; VGCC; desensitization; opioid tolerance; DAMGO; D-Ala2,N-Me-Phe4,Gly5-ol-enkephalin; DRG; dorsal root ganglion; GPCR; G protein-coupled receptor; MOR; μ-opioid receptor; PI3K; phosphoinositide 3-kinase, class 1; TRPV1; transient recepto
VPAC1 receptor binding site: Contribution of photoaffinity labeling approach
Keywords: GPCR; Class B GPCR; VPAC1 receptor; VIP; Structure–activity relationship; Inflammation
A vHTS approach for the identification of β-adrenoceptor ligands
Keywords: Adrenoceptor; GPCR; Molecular modeling; Virtual high throughput screening;
Prokineticins in angiogenesis and cancer
Keywords: Prokineticins; Cancer; Angiogenesis; Chemokine; GPCR; Innate immunity
Ecdysteroids elicit a rapid Ca2+ flux leading to Akt activation and increased protein synthesis in skeletal muscle cells
Keywords: Ecdysteroid; Skeletal muscle; Akt; GPCR; Calcium; C2C12
γ-Lactams as glycinamide replacements in cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists
Keywords: CCR2; CCR2 Antagonist; Chemokine antagonist; γ-lactam; GPCR
Non-peptidic antagonists of the CGRP receptor, BIBN4096BS and MK-0974, interact with the calcitonin receptor-like receptor via methionine-42 and RAMP1 via tryptophan-74
Keywords: Antagonist; Receptor; GPCR; CGRP; Migraine; Pharmacology;
Involvement of aquaporin in thromboxane A2 receptor-mediated, G12/13/RhoA/NHE-sensitive cell swelling in 1321N1 human astrocytoma cells
Keywords: dbcAMP; dibutyryl adenosine 3â²,5â²-monophosphate; EIPA; 5-(N-Ethyl-N-isopropyl)amiloride; GF109203X; (R)-(+)-trans-N-(4-pyridyl)-4-(1-aminoethyl)-cyclohexanecarboxamide;3-[1-[3-(dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dion
Importance of lipid-exposed residues in transmembrane segment four for family B calcitonin receptor homo-dimerization
Keywords: BRET; bioluminescence resonance energy transfer; hCTR; human calcitonin receptor; rCTR; rabbit calcitonin receptor; DMEM; Dulbecco's modified Eagle's medium; GPCR; G protein-coupled receptor; KRH; Krebs-Ringers-HEPES; PBS; phosphate-buffered saline; Rlu
Decahydroisoquinoline derivatives as novel non-peptidic, potent and subtype-selective somatostatin sst3 receptor antagonists
Keywords: Somatostatin; GPCR; Somatostatin sst3 receptor; Non-peptidic somatostatin receptor ligands; Subtype-selective sst3 receptor antagonists
4-Substituted-7-N-alkyl-N-acetyl 2-aminobenzothiazole amides: Drug-like and non-xanthine based A2B adenosine receptor antagonists
Keywords: Adenosine; GPCR; Antagonist;
PAC1hop receptor activation facilitates catecholamine secretion selectively through 2-APB-sensitive Ca2+ channels in PC12 cells
Keywords: AC; Adenylate cyclase; BCCs; Bovine chromaffin cells; Ca2+; Calcium; [Ca2+]i; Cytosolic calcium concentration; cAMP; Cyclic adenosine monophosphate; DMEM; Dulbecco's Modification of Eagle's Medium; ER; Endoplasmic reticulum; GPCR; G-protein coupled recept
Identification and biological significance of G protein-coupled receptor associated sorting proteins (GASPs)
Keywords: ALEX; arm protein lost in epithelial cancers; ARM; armadillo repeat-containing protein, bHLH, basic helix-loop-helix; BAIP3; BARD1 associated interacting protein 3; BARD1; Breast cancer 1-associated ring domain protein 1; CNS; central nervous system;
The anionic amphiphile SDS is an antagonist for the human neutrophil formyl peptide receptor 1
Keywords: Pattern recognition; GPCR; FPR; Antagonist; NADPH-oxidase, Priming;
Mapping interaction sites within the N-terminus of the calcitonin gene-related peptide receptor; the role of residues 23-60 of the calcitonin receptor-like receptor
Keywords: CGRP; calcitonin gene-related peptide; CLR; calcitonin receptor-like receptor; ECD; extracellular domain; GPCR; G-protein coupled receptor; HA; hemagglutinin; pEC50; -log(EC50); PBS; phosphate buffered saline; RAMP; receptor activity modifying protein;
Thienopyrimidines as β3-adrenoceptor agonists: Hit-to-lead optimization
Keywords: Adrenoceptor; β3-Adrenergic receptor; GPCR; Molecular modeling; vHTS
Expression of the nuclear transport protein importin ß-1 and its association with the neurokinin 3 receptor in the rat hypothalamus following acute hyperosmotic challenge
Keywords: GPCR; epigenetics; vasopressin; nuclear trafficking; nuclear pore; brainDTT, dithiothreitol; GPCR, G-protein coupled receptor; imp ß-1, importin ß-1; NKB, neurokinin B; NK3R, neurokinin 3 receptor; NLS, nuclear localization sequence; NPC, nuclear pore com
The p1D4-hrGFP II expression vector: A tool for expressing and purifying visual pigments and other G protein-coupled receptors
Keywords: Visual pigment; Rhodopsin; GPCR; Expression vector
Functional analysis of a type 1 parathyroid hormone receptor intracellular tail mutant [KRK(484-6)AAA]: Effects on second messenger generation and cellular targeting
Keywords: PTHR1; GPCR; Intracellular signalling; Cellular localization; Green fluorescent protein;
Non-canonical functions of RGS proteins
Keywords: AC; adenylyl cyclase; CHO; Chinese hamster ovary; CNK1; connector enhancer of KSR1; CREB; cAMP-response element binding protein; DH; dbl-homology; DMAP1; Dnmt1-associated protein 1; EGF; epidermal growth factor; eIF; eukaryotic initiation factor; ERK; ext
Determining receptor–ligand interaction of human galanin receptor type 3
Keywords: Galanin; Galanin receptor type 3; hGalR3; GPCR; Docking
Cortical M1 receptor concentration increases without a concomitant change in function in Alzheimer's disease
Keywords: Bmax; GPCR; Functional activity; MCI; Muscarinic receptor
Allatostatin-C receptors in mosquitoes
Keywords: Mosquito; Allatostatin; Receptor; GPCR; Juvenile hormone; Aedes;
Importance of extracellular loop one of the neuropeptide S receptor for biogenesis and function
Keywords: Neuropeptide S; GPCR; Extracellular loop one; Biogenesis; Mutagenesis; Pharmacological chaperone;
Proteinase-activated receptor-2 mediated inhibition of TNFα-stimulated JNK activation - A novel paradigm for Gq/11 linked GPCRs
Keywords: PAR-2; proteinase-activated receptor-2; PAR-2 AP; PAR-2 activating peptide; 2f-LIGKV-OH; 2-furoyl-LIGKV-hydroxyl; JNK; c-jun N-terminal protein kinase; NFκB; nuclear factor kappa B; PKC; protein kinase C; MAP kinase; mitogen-activated protein kinase; PMA
EP2 receptor mediated cAMP release is augmented by PGF2α activation of the FP receptor via the calcium-calmodulin pathway
Keywords: COX; cyclooxygenase; DMEM; Dulbecco's modified eagle medium; DMSO; dimethylsulphoxide; EGFR; epidermal growth factor receptor; ERK; extracellular signal-regulated kinase; GPCR; G protein-coupled receptor; IBMX; 3-isobutyl-1-methyl xanthine; PBS; phosphate
Efecto diferencial de espironolactona frente a eplerenona sobre el papel protector in vitro de testosterona en la apoptosis de cardiocitos
Keywords: Apoptosis; Antagonistas de aldosterona; Testosterona; LÃnea celular cardiaca; Apoptosis; Aldosterone antagonists; Testosterone; Heart cell line; GPCR; receptor de membrana acoplado a proteÃna G; MAPK; proteincinasa activada por mitógenos;
C-terminal processing of GABARAP is not required for trafficking of the angiotensin II type 1A receptor
Keywords: Protein binding; Yeast two-hybrid; GPCR; cAMP signaling pathway; Autophagy
Identification of domains responsible for specific membrane transport and ligand specificity of the ACTH receptor (MC2R)
Keywords: GPCR; Rhodopsin; Melanocortin; ACTHR; Chimeric receptors; MRAP; GFP; Membrane transport
An Angiotensin II type 1 receptor activation switch patch revealed through Evolutionary Trace analysis
Keywords: 7TM receptor; GPCR; Evolutionary Trace; Constitutive activity; Angiotensin
Immunoactive effects of cannabinoids: Considerations for the therapeutic use of cannabinoid receptor agonists and antagonists
Keywords: Cannabinoids; Signaling; GPCR; Immunosuppression; Metabolic disorders; Neuroimmunology
Research ArticlePhosphatidylinositol-3-kinase p110γ contributes to bile salt-induced apoptosis in primary rat hepatocytes and human hepatoma cells
Keywords: CPT-2-Me-cAMP; 4-(4-chloro-phenylthio)-2'-O-methyladenosine-3â²-5â²-cyclic monophosphate; JNK; c-Jun N-terminal kinase; GCDC; glycochenodeoxycholate; GPCR; G protein-coupled receptors; PtIns; phosphatidylinositides; PI3K; phosphatidylinositol 3-kinase
γ2-Melanocyte stimulation hormone (γ2-MSH) truncation studies results in the cautionary note that γ2-MSH is not selective for the mouse MC3R over the mouse MC5R
Keywords: Melanotropin; Heart; Blood pressure; Obesity; Receptor brain expression; GPCR
Gαq allosterically activates and relieves autoinhibition of p63RhoGEF
Keywords: AF; Alexa Fluor 532; Dbs; Dbl's big sister; DH; Dbl homology; FCPIA; Flow cytometry protein interaction assay; FP; Fluorescence polarization; GFP; Green fluorescent protein; GRK; G protein-coupled receptor kinase; GPCR; G protein-coupled receptor; MFI; Me
A reporter assay for G-protein-coupled receptors using a B-cell line suitable for stable episomal expression
Keywords: GPCR; Reporter assay; Chimeric G protein; Estrogen-inducible expression; Namalwa KJM-1; Episomal vector; Constitutive activity; Inverse agonist