Complex steroid–peptide–receptor cascade controls insect ecdysis
Keywords: Manduca; Drosophila; Ecdysis; ETH; Receptors; GPCR; Hormones; Neuropeptides
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Agonist versus antagonist induce distinct thermodynamic modes of co-factor binding to the glucocorticoid receptor
Keywords: AP-1; activating protein 1; CD; circular dichroism; CHAPS; 3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonate; DEX; Dexamethasone; DTT; dithiothreitol; EDTA; ethylenediaminetetraacetic acid; FP; fluorescence polarization; GPCR; G-protein coupled re
Click chemistry based solid phase supported synthesis of dopaminergic phenylacetylenes
Keywords: Click resins; Click chemistry; Copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC); BAL strategy; Microwave assisted Sonogashira coupling; GPCR; Dopamine D3 receptor binding; Dopamine D4 receptor binding; Partial agonist activity
Cloning and activation of the bullfrog apelin receptor: Gi/o coupling and high affinity for [Pro1]apelin-13
Keywords: APJ; Apelin; Bullfrog; Gi/o; GPCR
Affinity purification and characterization of a G-protein coupled receptor, Saccharomyces cerevisiae Ste2p
Keywords: G-protein coupled receptor; GPCR; Yeast; Ste2p; Purification; Mass spectrometry
mGluR7 undergoes rapid internalization in response to activation by the allosteric agonist AMN082
Keywords: mGluR7; Endocytosis; Internalization; Allosteric; GPCR; pHluorin
The G protein-coupled receptor kinase (GRK) interactome: Role of GRKs in GPCR regulation and signaling
Keywords: GRKs; GPCR; Arrestin; G protein; Kinase
Regulatory mechanisms underlying GKR2 levels in U937 cells: Evidence for GRK3 involvement
Keywords: GRK2; GRK3; Inositol phosphate; GPCR; Receptor desensitizationGPCR, G protein-coupled receptor; GRK, G protein-coupled receptor kinase; G-418, geneticin; IBMX, isobutylmethylxanthine; BSA, bovine serum albumin; PBS, phosphate-buffered saline; InsP, inosit
Dynorphin peptides differentially regulate the human κ opioid receptor
Keywords: Endogenous opioid peptides; Ligand-dependent; GPCR; Down-regulation; Internalization;
Protein kinase Cα mediates feedback inhibition of EGF receptor transactivation induced by Gq-coupled receptor agonists
Keywords: DAG; diacylglycerol; EGF; epidermal growth factor; EGFR; epidermal growth factor receptor; ERK; extracellular signal-regulated kinase; GPCR; G-protein-coupled receptor; HB-EGF; heparin-bound EGF-like growth factor; MMP; matrix metalloprotease; PDB; phorbo
Role of extracellular charged amino acids in the yeast α-factor receptor
Keywords: GPCR; G protein coupled receptor; [Orn7(NBD), Nle12] α-factor; (Ornithine7 (7-nitrobenz-2-oxa-1,3-diazol-4-yl), norleucine12 α-factor); [Orn7(NBD), E10, Nle12]; α-factor; (Ornithine7 (7-nitrobenz-2-oxa-1,3-diazol-4-yl); Glu10, norleucine12 α-factor);
Modeling of human ghrelin receptor (hGHS-R1a) in its close state and validation by molecular docking
Keywords: Ghrelin; Human grelin receptor hGHS-R1a; Growth hormone secretagogues; GPCR; Homology modeling; Molecular docking
Fish calcitonin receptor has novel features
Keywords: GPCR; CGRP; Amylin; CTR; RAMP; Hormone-binding domain
Mechanical stress-initiated signal transduction in vascular smooth muscle cells in vitro and in vivo
Keywords: AgIIR; angiotensin II receptor; cAMP; cyclic adenosine monophosphate; EC; endothelial cells; eNOS; endothelial nitric oxide synthase; ERK; extracellular signal-regulated kinase; GPCR; G protein-coupled receptor; IGFR; insulin-like growth factor receptor;
Finding ligands for G protein-coupled receptors based on the protein–compound affinity matrix
Keywords: Receptor–ligand docking; GPCR; Protein–compound interaction matrix; Principal component analysis; Database enrichment
Role of extracellular domains in PBAN/pyrokinin GPCRs from insects using chimera receptors
Keywords: PBAN receptor; PBAN; GPCR; Neuromedin U; Pheromone; Pyrokinin
A functional transmembrane complex: The luteinizing hormone receptor with bound ligand and G protein
Keywords: LH; luteinizing hormone; LHR; LH receptor; CG; chorionic gonadotropin; GPCR; G protein-coupled receptor; GPHR; glycoprotein hormone receptor; FSH; follicle stimulating hormone; FSHR; FSH receptor; TSH; thyroid stimulating hormone; TSHR; TSH receptor; LRR;
Differential effects of RGS proteins on Gαq and Gα11 activity
Keywords: GPCR; Human Gα subunits; Signalling; RGS-Gα specificity; Sz. pombe
The truncated ghrelin receptor polypeptide (GHS-R1b) acts as a dominant-negative mutant of the ghrelin receptor
Keywords: ANOVA; Analysis of variance; BRET; Bioluminescence resonance energy transfer; ERK1/2; Extracellular signal-regulated kinases 1/2; GFP2; Green fluorescent protein2; GHS; Growth hormone secretagogue; GPCR; G-protein-coupled receptor; GRLN-R; Ghrelin recepto
Generation and functional characterization of fluorescent, N-terminally tagged CB1 receptor chimeras for live-cell imaging
Keywords: Endocytosis; Cannabinoid; GPCR; pHluorin; GFP; Imaging
The cell biology of Smo signalling and its relationships with GPCRs
Keywords: Hh signalling; Smoothened; GPCR; GRKs; β-arrestin
Structure of the human 5-HT7 receptor gene and characterization of its promoter region
Keywords: 5-HT; 5-hydroxytryptamine; CNS; central nervous system; EMSA; Electrophoresis Mobility Shift Assay; GPCR; G-protein-coupled receptor; KLF; Krüppel-like factor; MAZ; Myc-Associated Zinc finger protein; NCBI; National Center for Biotechnology Information;
Heterooligomerization of human dopamine receptor 2 and somatostatin receptor 2
Keywords: C-tail; carboxy-terminal tail; DA; dopamine; DR; dopamine receptor; hD2R; human dopamine receptor 2; FSK; forskolin; GPCR; G-protein-coupled receptor; HA; hemoagglutinin; ICL; intracellular loop; pbFRET; photobleaching fluorescence resonance energy transf
Delayed transactivation of the receptor for nerve growth factor is required for sustained signaling and differentiation by α2-adrenergic receptors in transfected PC12 cells
Keywords: GPCR; G-protein-coupled receptor; MAPK; mitogen-activated protein kinase; PI3-K; phosphatidylinositol 3-kinase; RTK; receptor tyrosine kinase; Trk; tropomyosin related kinase; PACAP; pituitary adenylate cyclase-activating polypeptide; α2-AR; α2-adrenerg
The last 59 amino acids of Smoothened cytoplasmic tail directly bind the protein kinase Fused and negatively regulate the Hedgehog pathway
Keywords: Hedgehog; Smoothened; GPCR; Fused; Signaling; Imaginal disc; Clone 8 cells; Drosophila development; Two hybrid; Fluorescent imaging
On the role of receptor-receptor interactions and volume transmission in learning and memory
Keywords: BN; Boolean network; CNS; central nervous system; DA; dopamine; ECM; extracellular matrix; ECS; extracellular space; EEG; electroencephalogram; GPCR; G-protein-coupled receptor; LTD; long-term depression; LTF; long-term facilitation; LTP; long-term potent
Palmitoylation of the TPβ isoform of the human thromboxane A2 receptor.
Keywords: AR; adrenergic receptor; C-tail; carboxyl-terminal tail; [Ca2+]i; intracellular calcium; eNOS; endothelial nitric oxide synthase; GFP; green fluorescent protein; GPCR; G protein-coupled receptor; HA; hemagglutinin; HEK; human embryonic kidney; 5-hydroxytr
A GPCR involved in post aggregation events in Dictyostelium discoideum
Keywords: GPCR; GrlA; Live dynamics of a GPCR; Dictyostelium; Spore formation; Microarray
Melatonin receptors in the eye: Location, second messengers and role in ocular physiology
Keywords: AANAT; arylalkylamine N-acetyltransferase; GPCR; seven-transmembrane G protein-coupled receptor family; HIOMT; hydroxyindole-O-methyltransferase; IOP; intraocular pressure; QR2; quinone reductase 2.Melatonin; Melatonin receptors; Eye
G-protein coupled receptor structure
Keywords: GPCR; Structure; Membrane protein
Formation of new genes explains lower intron density in mammalian Rhodopsin G protein-coupled receptors
Keywords: GPCR; Evolution; Introns; Rhodopsin
Neuropeptidergic signaling in the nematode Caenorhabditis elegans
Keywords: cGMP; 3â²,5â²-cyclic guanosine monophosphate; 5-HT; serotonin; AC; adenylyl cyclase; ACE; angiotensin-converting enzyme; ACh; acetylcholine; CAPS; Ca2+-dependent activator protein for secretion; CELPC2; C. elegans proprotein convertase 2; CHO; Chinese h
PI3K pathway is involved in ERK signaling cascade activation by histamine H2R agonist in HEK293T cells
Keywords: HR; histamine receptor; GPCR; G-protein coupled-receptor; ERK1/2; extracellular signal-regulated kinases; PI3K; phosphoinositide 3-kinase; DMEM; Dulbecco's modified Eagle's medium; PBS; phosphate-buffered saline; DMEM/F12; Dulbecco's modified Eagle's medi
Hypothesis: VPAC G protein-coupled receptors for vasoactive intestinal peptide constitute a dynamic system for signaling T cells from plasma membrane and nuclear membrane complexes
Keywords: VIP; vasoactive intestinal peptide; GPCR; G protein-coupled receptor; VPAC1; type 1 VIP receptor; VPAC2; type 2 VIP receptor; T cell; T lymphocyte; LPA; lysophosphatidic acid; S1P; sphingosine 1-phosphate; LPA1; type 1 LPA receptor; iNOS; inducible nitric
The CART receptors: Background and recent advances
Keywords: CART signaling; GPCR; AtT20; ERK
Identification and initial evaluation of 4-N-aryl-[1,4]diazepane ureas as potent CXCR3 antagonists
Keywords: CXCR3; Chemokine; GPCR; Antagonist; Diazepane; Urea
Privileged structure based ligands for melanocortin receptors—4,4-Disubstituted piperidine derivatives
Keywords: Melanocortin; MC4; Privileged structure; G-protein coupled receptors; GPCR
Synthesis and SAR of substituted tetrahydrocarbazole derivatives as new NPY-1 antagonists
Keywords: NPY-1; Antagonists; GPCR
Optimization of 2-aminothiazole derivatives as CCR4 antagonists
Keywords: CCR4; Chemokine; Chemokine receptor; TARC; CCL17; MDC; CCL22; GPCR
The human cytomegalovirus-encoded receptor US28 increases the activity of the major immediate-early promoter/enhancer
Keywords: NF-κB; GPCR; Viral gene expression; Chemokine receptor; MIEP
2-Aminoquinoline melanin-concentrating hormone (MCH)1R antagonists
Keywords: GPCR; Antagonist; Obesity; Quinoline; Melanin-concentrating hormone
The design and synthesis of a tricyclic single-nitrogen scaffold that serves as a 5-HT2C receptor agonist
Keywords: Obesity; 5-HT2C; GPCR
Discovery of 3,5-bis(trifluoromethyl)benzyl l-arylglycinamide based potent CCR2 antagonists
Keywords: CCR2; CCR2b; MCP-1; CCL2; Antagonist; Chemokine; Chemotaxis; GPCR
Obestatin does not activate orphan G protein-coupled receptor GPR39 &z.star
Keywords: Obestatin; GPR39; GPCR
Dimethylsulphoxide as a tool to increase functional expression of heterologously produced GPCRs in mammalian cells
Keywords: GPCR; BHK cells; Overexpression; DMSO; LocalizationGPCR, G protein-coupled receptor; DMSO, dimethylsulphoxide; BHK cells, baby hamster kidney cells
Cloning and characterization of the adipokinetic hormone receptor from the cockroach Periplaneta americana
Keywords: GPCR; Neuropeptide; Neurohormone; Endocrinology; Insect; Drosophila; Honey bee; Mosquito; Beetle; Silkworm
Substituted chromones and quinolones as potent melanin-concentrating hormone receptor 1 antagonists
Keywords: MCH; Obesity; Anorectic; Anxiety; Depression; GPCR
Molecular identification of the first SIFamide receptor
Keywords: G protein-coupled receptor; GPCR; Neuropeptide; Neurohormone; Peptide hormone; Endocrinology; Insects; Crustaceans; Drosophila; Honey bee; Mosquito; Malaria
Relationship between the G protein signaling and homologous desensitization of G protein-coupled receptors
Keywords: Signaling; Desensitization; GPCR; GRK; β-Arrestin; Dopamine D3 receptor; β2-Adrenergic receptor; Ste2p