Structural insight into receptor-selectivity for lurasidone
Keywords: Lurasidone; Schizophrenia; GPCR; Selectivity; In silico; Molecular modeling;
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Determination of different putative allosteric binding pockets at the lutropin receptor by using diverse drug-like low molecular weight ligands
Keywords: 7-TM; seven transmembrane; A2AR; adenosine A2A receptor; A3R; adenosine A3 receptor; BSA; bovine serum albumin; cAMP; cyclic adenosine-5â²-monophosphate; CHO; Chinese Hamster Ovary; CHOhLHr_luc; human LH receptor and luciferase reporter gene transfected
Role of phospholipase Cε in physiological phosphoinositide signaling networks
Keywords: PLC; phosphoinositide-specific phospholipase C; PKC; protein kinase C; LPA; lysophosphatidic acid; S1P; sphingosine-1 phosphate; Epac; Exchange protein directly activated by cAMP; GPCR; G protein-coupled receptor; GEF; guanine nucleotide exchange factor;
Extracellular cysteine (Cys)/cystine (CySS) redox regulates metabotropic glutamate receptor 5 activity
Keywords: Extracellular cysteine (Cys)/cystine (CySS); Metabotropic glutamate receptor 5; Parkinson's disease; AMS; 4-Acetamide-4â²-maleimidylstilbene-2,2â²-disulfonic acid, disodium salt; BCA; Bradford Protein Assay; CRD; cysteine-rich domain; Cys; cysteine; C
Lysophosphatidylinositol signalling: New wine from an old bottle
Keywords: Lysophospolipid; Lysophosphatidylinositol; GPCR; GPR55;
Combined deep microRNA and mRNA sequencing identifies protective transcriptomal signature of enhanced PI3Kα signaling in cardiac hypertrophy
Keywords: ANF; atrial natriuretic factor; caPI3Kα; constitutively active phosphoinositide-3-kinase p110α; FDR; false discovery rate; GAPDH; glyceraldehydes 3-phosphate dehydrogenase; GO; gene ontology; GPCR; G-protein coupled receptor; LV; Left ventricle; LVH; Le
MMP-2 expression by fibroblasts is suppressed by the myofibroblast phenotype
Keywords: DMEM; Dulbecco's Modified Eagle's Medium; ECM; extracellular matrix; ET-1; endothelin; GAPDH; glyceraldehyde 3-phosphate dehydrogenase; GPCR; G-protein-coupled receptor; IGF-I; insulin-like growth factor-I; Lat B; Latrunculin B; MMP; matrix metalloprotein
Zinc and the modulation of redox homeostasis
Keywords: Akt; protein kinase B; BDNF; brain-derived neurotrophic factor; ERK; extracellular signal-regulated kinases; GCL; glutamate-cysteine ligase; GSH; glutathione; GPCR; G-protein-coupled receptor; Keap1; Kelch-like ECH-associated protein; JNK; Jun N-termina
Bivalent molecular probes for dopamine D2-like receptors
Keywords: GPCR; Subtype selectivity; Dopamine; Bivalent ligand; D3 receptor;
Chemotography for multi-target SAR analysis in the context of biological pathways
Keywords: GPCR; G-protein coupled receptor; LGIC; ligand-gated ion channel; SAR; structure-activity relationship; Chemical space; Color; Visualization; Molecular fingerprints; Chemogenomics; Systems pharmacology; Molecular pathways;
Experimental and computational study of inter- and intra- species specificity of gonadotropins for various gonadotropin receptors
Keywords: 7TMD; seven-transmembrane domain; b; bovine; CG; chorionic gonadotropin; e; Japanese eel (Anguilla japonica); ECD; extracellular domain; FSH; follicle-stimulating hormone; FSHR; FSH receptor; GPCR; G-protein-coupled receptor; GTH; gonadotropins; GTHR; gon
Membrane structure and interactions of peptide hormones with model lipid bilayers
Keywords: Adg; (S)-2-(1-adamantyl)glycine; AVP; arginine vasopressin; cis-Apc; cis-1-amino-4-phenylcyclohexane-1-carboxylic acid; D-Igl; D-α-2-indanylglycine; DPC; dodecylphosphocholine; DPPC; 1,2-dipalmitoyl-sn-glycero-3-phosphocholine; DPPG; 1,2-dipalmitoyl-sn-g
A new approach for studying GPCR dimers: Drug-induced inactivation and reactivation to reveal GPCR dimer function in vitro, in primary culture, and in vivo
Keywords: GPCR; Homodimer; Heterodimers; 5-HT7; 5-HT2A; Allosterism
Characterization of dual agonists for kinin B1 and B2 receptors and their biased activation of B2 receptors
Keywords: CP; carboxypeptidase; kB1R; kinin B1 receptor; kB2R; bradykinin B2 receptor; [Ca2Â +]i; intracellular calcium concentration; PBS; phosphate buffered saline; DMEM; Dulbecco's Modified Eagle's Medium; GPCR; G protein-coupled receptor; BK; bradykinin; KD; ka
Increased interaction of connexin43 with zonula occludens-1 during inhibition of gap junctions by G protein-coupled receptor agonists
Keywords: BSA; bovine serum albumin; C; carboxyl; Cx; connexin; Cx43; connexin43; DG; deoxyglucose; ET; endothelin; ERK; extracellular signal-regulated kinase; G; GTP-binding protein; GJ; gap junction; GJIC; gap junctional intercellular communication; GPCR; GTP-bin
The third intracellular loop of D1 and D5 dopaminergic receptors dictates their subtype-specific PKC-induced sensitization and desensitization in a receptor conformation-dependent manner
Keywords: AC; adenylyl cyclase; Bmax; maximal binding capacity; BSA; bovine serum albumin; β2-AR; β2-adrenergic receptor; CA; [3H]-cAMP formed; CT; cytoplasmic tail; DA; dopamine; DMSO; dimethyl sulfoxide; EL3; third extracellular loop; EC50; effective concentrat
Selective interactions of spinophilin with the C-terminal domains of the δ- and μ-opioid receptors and G proteins differentially modulate opioid receptor signaling
Keywords: GPCR; G protein-coupled receptors; RGS; Regulators of G protein Signaling; ÎÎRGS4; RGS4 lacking its N-terminal domain; 6xHis; hexahistidine; aa; amino acids; GEFs; Guanine nucleotide exchange factors; AC; adenylyl cyclase; DAMGO; [D-Ala2,N-MePhe4,Gly5-o
A role for the vesicle-associated tubulin binding protein ARL6 (BBS3) in flagellum extension in Trypanosoma brucei
Keywords: Arf; ADP-ribosylation factor; Arl; ADP-ribosylation factor-like; Arl6ip; Arl6 interacting protein; BBS; Bardet-Biedl syndrome; BBS1; Bardet-Biedl syndrome 1 protein; BSF; bloodstream form; ConA; Concanavalin A; GEF; guanine nucleotide exchange factor;
Fluorescence correlation spectroscopy, combined with bimolecular fluorescence complementation, reveals the effects of β-arrestin complexes and endocytic targeting on the membrane mobility of neuropeptide Y receptors
Keywords: BiFC; bimolecular fluorescence complementation; BIBO3304; (R)-N2-(diphenylacetyl)-N-[(4-(aminocarbonylaminomethyl-)phenyl)methyl]-argininamide; BSA; bovine serum albumin; DMEM; Dulbecco's modified Eagle's medium; FCS; fluorescence correlation spectroscopy
Interaction of the human prostacyclin receptor and the NHERF4 family member intestinal and kidney enriched PDZ protein (IKEPP)
Keywords: DDO; double drop-out; FTI; farnesyl transferase inhibitor; GPCR; G protein-coupled receptor; HA; hemagglutinin; hIP; human prostacyclin receptor; HUVEC; human umbilical vein endothelial cell; IKEPP; intestinal and kidney enriched PDZ protein; IP; prostacy
D-type prostanoid receptor enhances the signaling of chemoattractant receptor-homologous molecule expressed on TH2 cells
Keywords: Chemoattractant receptor-homologous molecule expressed on TH2 cells; eosinophils; prostaglandin D2; Ca2+ flux; GÂ protein-coupled receptor; D-type prostanoid receptor; CRTH2; Chemoattractant receptor-homologous molecule expressed on TH2 cells; DK-PG
Stress and visceral pain: From animal models to clinical therapies
Keywords: ASICs; acid-sensing ion channels; BDNF; brain-derived neutrophic factor; ATP; adenosine triphosphate; CB; cannabinoid; CeA; central amygdala; CNS; central nervous system; CRD; colorectal distension; CRF; corticotropin releasing factor; CRF1; CRF receptor
Cannabinoid receptor trafficking in peripheral cells is dynamically regulated by a binary biochemical switch
Keywords: ATTC; American type culture collection; AMAM; anilino-monoindolylmaleimide; CB1; cannabinoid receptor type-1; CB2; cannabinoid receptor type-2; CDx; cluster of differentiation x; CHO; Chinese hamster ovary-K1; CM; cell membrane; CNR1; CB1 receptor gene; C
Structure-activity relationships of 2-arylamido-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxamide derivatives as cannabinoid receptor agonists and their analgesic action
Keywords: GPCR; CB2 agonists; HTS; SAR; Inflammatory pain models;
Design and evaluation of a novel fluorescent CB2 ligand as probe for receptor visualization in immune cells
Keywords: Cannabinoid receptor 2; CB2; Fluorescent probe; GPCR
Prostaglandin E2 modulation of blood pressure homeostasis: Studies in rodent models
Keywords: Prostaglandin E2; Hypertension; GPCR; Mouse; Rat; EP receptors; Blood pressure; Kidney
Resolution of controversies in drug/receptor interactions by protein structure. Limitations and pharmacological solutions
Keywords: GPCR; Drug interaction
Cholesterol depletion enhances adrenergic signaling in cardiac myocytes
Keywords: GPCR; G-protein coupled receptor; MβCD; methyl-β-cyclodextrin; NE; norepinephrine; Adrenergic receptors; Adrenergic signaling; Cholesterol depletion; Cholesterol replenishment; H9c2 cardiac myocytes; MβCD;
Design of potent and selective GPR119 agonists for type II diabetes
Keywords: GPR119 agonist; GPCR; Diabetes; GDIS
Oxidative stress increases angiotensin receptor type I responsiveness by increasing receptor degree of aggregation using image correlation spectroscopy
Keywords: AT1R; angiotensin II receptor type I; AT2R; angiotensin II receptor type II; Ang II; angiotensin II; BMP; bone morphogenetic protein; CD; cluster density; DA; degree of aggregation; EGFP; enhanced green fluorescent protein; GPCR; G - protein coupled recep
Identification of the endogenous cysteine-rich peptide trissin, a ligand for an orphan G protein-coupled receptor in Drosophila
Keywords: GPCRs; G protein-coupled receptors; CHO; Chinese hamster ovary; CM; carboxymethyl; ACN; acetonitrile; TFA; trifluoroacetic acid; PTH; phenyl thiohydantoin; GPCR; Cysteine-rich peptide; Drosophila;
Novel and highly potent histamine H3 receptor ligands. Part 2: Exploring the cyclohexylamine-based series
Keywords: Histamine; Histamine H3 receptor; GPCR; hERG;
WNT-5A stimulates the GDP/GTP exchange at pertussis toxin-sensitive heterotrimeric G proteins
Keywords: FZD; Frizzled; GPCR; G protein-coupled receptor; [γS]GTP; Guanosine 5â²-[γ-thio]triphosphate; SDS-PAGE; sodiumdodecylsulfate-polyacrylamide gelelectrophoresis; RT-PCR; reverse transcriptase polymerase chain reaction; QPCR; quantitative PCR; Frizzled; G
The angiotensin II type 1 receptor antagonist Losartan binds and activates bradykinin B2 receptor signaling
Keywords: 7TM receptor; GPCR; Losartan; Bradykinin; Cardiac protection; Angiotensin;
Cloning of the TSH receptor: The story from a Brussels perspective
Keywords: TSH; Thyréotropine; GPCR; Clonage; Hyperthyroïdie; Hypothyroïdie; RécepteurTSH; Thyrotropin; GPCR; Cloning; Hyperthyroidism; Hypothyroidism; Receptor
III. Identification of novel CXCR3 chemokine receptor antagonists with a pyrazinyl–piperazinyl–piperidine scaffold
Keywords: CXCR3; Chemokine; GPCR
GPCR production in a novel yeast strain that makes cholesterol-like sterols
Keywords: SI, C8-C7 sterol isomerase; C24SR, C24 sterol reductase; C7SR, C7 sterol reductase; GPCR, G-protein coupled receptor; ORF, open reading frame; MW, molecular weightYeast; Cholesterol; Membrane protein; GPCR; Overexpression; Genetic modification
Design, synthesis and structure–activity relationships of (indo-3-yl) heterocyclic derivatives as agonists of the CB1 receptor. Discovery of a clinical candidate
Keywords: Cannabinoid; CB1 receptor agonist; GPCR; Clinical candidate
3-Oxo-2-piperazinyl acetamides as potent bradykinin B1 receptor antagonists for the treatment of pain and inflammation
Keywords: Bradykinin B1; Antagonist; Pain; Inflammation; GPCR; Oxopiperazine; Tetralin
Production of the stable human histamine H1 receptor in Pichia pastoris for structural determination
Keywords: GPCR; Expression; Pichia pastoris; Yeast; Structure; Membrane protein
Expression and purification of human FROUNT, a common cytosolic regulator of CCR2 and CCR5
Keywords: GPCR; Chemokine receptor; FROUNT; pCold; Trigger factor
Large-scale production of a disulfide-stabilized constitutively active mutant opsin
Keywords: GPCR; Receptor; G protein; Constitutive activation; Signaling;
Amplification of agonist stimulation of human G-protein-coupled receptor signaling in yeast
Keywords: Yeast; GPCR; G-protein signaling; Gβ subunit; Feedback signal activation
Multi-Tox: Application of the ToxR-transcriptional reporter assay to the study of multi-pass protein transmembrane domain oligomerization
Keywords: DAGK; diacylglycerol kinase; DN; dominant-negative; EBV; Epstein-Barr Virus; GpA; Glycophorin A; GPCR; G protein-coupled receptors; LMP-1; latent membrane protein-1; MBP; maltose binding protein; ONPG; ortho-nitrophenyl β-galactoside; SDS-PAGE; sodium do
Taking the heart failure battle inside the cell: Small molecule targeting of Gβγ subunits
Keywords: GPCR; Heart failure; Beta-adrenergic receptor; Gβγ signaling; Gβγ inhibitory compounds
Identification of the novel bioactive peptides dRYamide-1 and dRYamide-2, ligands for a neuropeptide Y-like receptor in Drosophila
Keywords: GPCR; Novel bioactive peptide; Drosophila; Neuropeptide Y;
Uniform assessment and ranking of opioid Mu receptor binding constants for selected opioid drugs
Keywords: MOR; Mu opioid receptor; DOR; delta opioid receptor; KOR; kappa opioid receptor; DAMGO; (d-Ala2, N-MePhe4, Gly-ol)-enkephalin; GPCR; G-protein coupled receptors; FDA; Food and Drug Administration; Ki; equilibrium dissociation constant for the test compoun
Multifaceted cardiac signal transduction mediated by G protein-coupled receptors: Potential target sites where an unambiguous attention is needed for exploring new drugs for cardiovascular disorders
Keywords: GPCR; G proteins; CaM kinase II; RGS2; β-arrestin; EGFR; β-arrestin-biased ligands
Structure, function and regulation of the melanocortin receptors
Keywords: Orthosteric binding; Allosteric binding; Melanocortin receptor; GPCR
Transmembrane signaling by GPCRs: Insight from rhodopsin and opsin structures
Keywords: GPCR; 7TM receptor; Signal transduction