Regulation of GPCR signal networks via membrane trafficking
Keywords: GPCR; Trafficking; Signaling; Endocytosis; Recycling; Degradation;
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Chemokine triggered integrin activation and actin remodeling events guiding lymphocyte migration across vascular barriers
Keywords: Cdc42; cell division cycle 42; GEF; Guanine nucleotide exchange factor; GPCR; G-protein coupled receptor; LFA-1; Leukocyte function-associated antigen-1; LTB4; leukotriene B4; PAF; platelet activating factor; PI3K; Phosphatidylinositol 3-kinase; PIP2; pho
Research ReportSubstance P induces the reversible formation of varicosities in the dendrites of rat brainstem neurons
Keywords: ACSF; Artificial cerebrospinal fluid; DV; Dendritic varicosity; GPCR; G protein coupled receptor; NK-1R; Neurokinin-1 receptor; PBS; Phosphate buffered saline; RVM; Rostral ventromedial medulla; Sub P; Substance P; Rostral ventromedial medulla; Dendritic
Synthetic biosensing systems
Keywords: RBS; ribosome binding site; GPCR; G protein coupled receptor; RTK; receptor tyrosine kinase; MAPK; mitogen-activated protein kinase; GDP; guanosine diphosphate; GTP; guanosine triphosphate; GEF; guanine nucleotide exchange factor; GAP; GTPase activating p
Adrenocorticotropin hormone (ACTH) effects on MAPK phosphorylation in human fasciculata cells and in embryonic kidney 293 cells expressing human melanocortin 2 receptor (MC2R) and MC2R accessory protein (MRAP)β
Keywords: DAPI; 4â²,6â²-diamino-2-phenylindole dihydrochloride; ACTH; adrenocorticotropin hormone; Rp-cAMPS; adenosine-3-5-cyclic monophosphorothioate, Rp isomer; BFA; brefeldin A; Epac; exchange protein directly activated by cAMP; ERK; extracellular regulated re
In cardiac myoblasts, cellular redox regulates FosB and Fra-1 through multiple cis-regulatory modules
Keywords: CEBP; CCAAT enhancer binding protein; GPCR; G-protein-coupled receptor; NE; norepinephrine; ROS; reactive oxygen species; SP-1; specificity protein 1; H9c2 cardiac myoblast; Hypertrophy; Apoptosis; FosB; Fra-1; Norepinephrine; ROS; SP-1; Free radicals;
Understanding DP receptor antagonism using a CoMSIA approach
Keywords: CoMSIA; QSAR; DP; DP1; Prostaglandin; PGD2; GPCR;
The lipid language of plant–fungal interactions
Keywords: Aspergillus spp.; Oxylipins; Signaling cross-talk; Jasmonic acid; GPCR; Fusarium verticillioides
Functionally biased modulation of A3 adenosine receptor agonist efficacy and potency by imidazoquinolinamine allosteric enhancers
Keywords: CCPA; 2-chloro-N6-cyclopentyladenosine; Cl-IB-MECA; 2-chloro-N6-(3-iodobenzyl)-adenosine-5â²-N-methyluronamide; ERK; extracellular signal-regulated kinase; GPCR; G protein-coupled receptor; LUF5833; 2-aminophenyl-6-(1H-imidazol-2-ylmethylsulfanyl)-pyridi
Fluorescence spectroscopy studies of HEK293 cells expressing DOR-Gi1α fusion protein; the effect of cholesterol depletion
Keywords: β-CDX; β-cyclodextrin; DADLE; D-Ala2-D-Leu5 enkephalin; DMEM; Dulbecco's modified Eagle's medium; DOR; δ-opioid receptor; DOR-Gi1α cells; HEK293 cells stably expressing DOR-Gi1α (Cys351-Ile351) fusion protein; DPH; 1,6-diphenyl-1,3,5-hexatriene; DR
G protein-coupled receptors involved in GnRH regulation: Molecular insights from human disease
Keywords: GPCR; Hypogonadotropic hypogonadism; Mutation
Contribution of a tyrosine-based motif to cellular trafficking of wild-type and truncated NPY Y1 receptors
Keywords: NPY; neuropeptide Y; EGFP; enhanced green fluorescent protein; GPCR; G protein-coupled receptor; Gi/o; inhibitory GTP binding protein of adenylyl cyclase; HEK; human embryonic kidney; SP; signal peptide; LIC; ligation independent cloning; PBS; phosphate b
Comparative NMR analysis of an 80-residue G protein-coupled receptor fragment in two membrane mimetic environments
Keywords: GPCR; Membrane protein structure; Fragment; Transmembrane;
Cleavage-resistant fusion proteins of the M2 muscarinic receptor and Gαi1. Homotropic and heterotropic effects in the binding of ligands
Keywords: CHO; Chinese hamster ovary; DEAE; diethylaminoethyl; DTT; dithiothreitol; GMP-PNP; guanylylimidodiphosphate; GPCR; G protein-coupled receptor; HA; influenza hemagglutinin; IB; immunoblot; IP; immunoprecipitate; MOI; multiplicity of infection; NMS; N-methy
Induction of LYVE-1/stabilin-2-positive liver sinusoidal endothelial-like cells from embryoid bodies by modulation of adrenomedullin-RAMP2 signaling
Keywords: ESCs; Embryonic stem cells; EBs; Embryoid bodies; Ac-LDL; Acetylated low-density lipoprotein; AM; Adrenomedullin; RAMP; Receptor activity-modifying protein; CRLR; Calcitonin receptor-like receptor; GPCR; G protein-coupled receptor; TGFβ; Transforming gro
Epidermal growth factor receptor reactivation induced by E-prostanoid-3 receptor- and tumor necrosis factor-alpha-converting enzyme-dependent feedback exaggerates interleukin-8 production in airway cancer (NCI-H292) cells
Keywords: COX; cyclooxygenase; EGFR; epidermal growth factor receptor; EGFR-P; EGFR phosphorylation; EP; E-prostanoid; ERK; extracellular signal-regulated kinase; GPCR; G-protein-coupled receptor; IL; interleukin; NHBE; normal human bronchial epithelial; PG; prosta
2-(2-Fluorobenzamido)benzoate ethyl ester (EFB-1) inhibits superoxide production by human neutrophils and attenuates hemorrhagic shock-induced organ dysfunction in rats
Keywords: AC; adenylate cyclase; AKT; protein kinase B; cAMP; cyclic adenosine 3â²,5â²-monophosphate; CB; cytochalasin B; EFB-1; 2-(2-fluorobenzamido)benzoic acid ethyl ester; FMLP; formyl-l-methionyl-l-leucyl-l-phenylalanine; GPCR; G-protein-coupled receptor; IB
PKCθ activation in pancreatic acinar cells by gastrointestinal hormones/neurotransmitters and growth factors is needed for stimulation of numerous important cellular signaling cascades
Keywords: CCK; COOH-terminal octapeptide of cholecystokinin; TPA; 12-O-tetradecanoylphorbol-13-acetate; GI; gastrointestinal; CCK-JMV; CCK-JMV-180; IP; immunoprecipitation; Co-IP; co-immunoprecipitation; PKD; protein kinase D; GPCR; G protein-coupled receptor; PYK2
Cigarette smoking, cyclooxygenase-2 pathway and cancer
Keywords: AA; arachidonic acid; PLA2; phospholipase A2; COX; cyclooxygenase; PGE2; prostaglandin E2; TxA2; thromboxane A2; TxB2; thromboxane B2; PGI2; prostacyclin; PGES; prostaglandin E synthase; TxAS; thromboxane synthase; PGIS; prostacyclin synthase; GPCR; G-pro
Targeting PI3K Signaling as a Therapeutic Approach for Colorectal Cancer
Keywords: Colon Cancer; Neoplasm; Signal Transduction; Genetics; Tumor; CRC; colorectal cancer; EGF; epidermal growth factor; EGFR; epidermal growth factor receptor; GPCR; G-protein-coupled receptor; IRS1; insulin receptor substrate 1; MEF; murine embryonic fibro
Angiotensin II causes endothelial dysfunction via the GRK2/Akt/eNOS pathway in aortas from a murine type 2 diabetic model
Keywords: α-AR; α-adrenergi receptor; ACh; acetylcholine; AngII; angiotensin II; DM; diabetic mice; eNOS; endothelial oxide synthase; GPCR; G-protein-coupled receptor; GRK; G-protein-coupled receptor kinase; IGTT; intravenous glucose tolerance test; IRS-1; insuli
Strategies for the identification of allosteric modulators of G-protein-coupled receptors
Keywords: GPCR; G-protein-coupled receptor; PAM; positive allosteric modulator; NAM; negative allosteric modulator; SAM; silent allosteric modulator; NAL; neutral allosteric ligand; HTS; high-throughput screening; cAMP; 3â²-5â²-cyclic adenosine monophosphate; mGl
Resistance of a human immunodeficiency virus type 1 isolate to a small molecule CCR5 inhibitor can involve sequence changes in both gp120 and gp41
Keywords: HIV-1; Entry inhibitors; Vicriviroc; Escape mutants; Fusion peptide; GPCR
The multiple roles of amphiregulin in human cancer
Keywords: AREG; amphiregulin; TACE; tumor-necrosis factor-alpha converting enzyme; ADAM; a disintegrin and metalloproteinase; CTF; carboxy-terminal fragment; EGF; epidermal growth factor; EGFR; epidermal growth factor receptor; EGFR-TKI; epidermal growth factor rec
Molecular Dynamics Simulations of the Effect of the G-Protein and Diffusible Ligands on the β2-Adrenergic Receptor
Keywords: GPCR; β2-adrenergic receptor; molecular dynamics simulations; protein–receptor interactions; 7TM receptor activationGPCR, G-protein-coupled receptor; β2AR, β2-adrenergic receptor; GαCT, C-terminal end of the Gα subunit; TM, transmembrane helix; IL, intrac
NMR evidence of GM1-induced conformational change of Substance P using isotropic bicelles
Keywords: SP; Substance P; NK1R; Neurokinin-1 receptor; GPCR; G-protein coupled receptor; GM1; Ganglioside Monosialo 1; DMPC; Dimyristoyl-sn-glycero-3-phosphorylcholine; CHAPS; 3-[(3-Cholamidopropyl) dimethylammonio]-1-propanesulfonate; GT1; Ganglioside Trisialo 1;
The CCK(-like) receptor in the animal kingdom: Functions, evolution and structures
Keywords: Cholecystokinin (CCK)-like receptors; GPCR; Evolution; Physiological functions; Satiety; Structures; Ligand–receptor interactions; Agonist/antagonist
Role of the endocannabinoid system in food intake, energy homeostasis and regulation of the endocrine pancreas
Keywords: Cannabinoids; Cannabinoid receptors; Food intake; Obesity; Insulin secretion; Islets of Langerhans; β-cells; AC; adenylate cyclase; ACEA; N-(2-chloroethyl)5,8,11,14-eicosaetraenamide; AEA; N-arachidonoyl ethanolamine; 2-AG; 2-arachidonoyl glycerol; AM251
The increasing challenge of discovering asthma drugs
Keywords: ACQ; asthma control questionnaire; AHR; airway hyper-responsiveness; AQLQ; asthma quality-of-life questionnaire; BALF; bronchoalveolar lavage fluid; bn; billion; cysLT; cysteinyl leukotrienes; DZ; dizygotic; EAR; early airway response; FDA; Food and Drug
Resolvins: Natural agonists for resolution of pulmonary inflammation
Keywords: Catabasis; Lipid mediators; Lung; Neutrophils; Omega-3; Polyunsaturated fatty acids; AA; arachidonic acid; ALI; acid lung injury; ALX/FPR2; lipoxin A4 receptor/formyl peptide receptor 2; ARDS; acute respiratory distress syndrome; ATL; aspirin-triggered li
Long and short distance movements of β2-adrenoceptor in cell membrane assessed by photoconvertible fluorescent protein dendra2-β2-adrenoceptor fusion
Keywords: β2AR; β2-adrenoceptor; FRAP; fluorescence recovery after photobleaching; GFP; green fluorescent protein; GPCR; G protein-coupled receptor; FCS; fluorescence correlation spectroscopy; SPT; single particle (or fluorescent molecule) tracking; β-adrenocept
Solution- and solid-state NMR studies of GPCRs and their ligands
Keywords: β2AR; β2 adrenergic receptor; CP; cross polarisation; CXCR1; chemokine receptor; DAGK; diacylglycerol kinase; GPCR; G protein-coupled receptor; MAS; magic angle spinning; MBP; maltose binding protein; NOE; nuclear overhauser effect; NTS1; neurotensin re
Primary immunodeficiency diseases associated with increased susceptibility to viral infections and malignancies
Keywords: Immunodeficiency; viral infection; malignancies; X-linked lymphoproliferative syndrome; AR-HIES; Autosomal recessive hyper-IgE syndrome; CVID; Common variable immunodeficiency; DDR; DNA damage response; DOCK8; Dedicator of cytokinesis 8; EV; Epidermodyspl
Analysis of expression and structure of the rat GH-secretagogue/ghrelin receptor (Ghsr) gene: Roles of epigenetic modifications in transcriptional regulation
Keywords: 5-aza-dC; 5-aza-2-deoxycytidine; ChIP; chromatin immunoprecipitation; ERK1/2; extracellular signal-regulated kinase 1/2; DMEM; Dulbecco's modified Eagle's medium; DNMT; DNA methyltransferase; EST; expressed sequence tag; FBS; fetal bovine serum; GH; g
Redox signaling in cardiac myocytes
Keywords: AIF; apoptosis-inducing factor; ARC; apoptosis repressor with caspase recruitment domain; CamKII; calmodulin kinase II; CTGF; connective tissue growth factor; EB; embryoid body; ECC; excitation-contraction coupling; ER; endoplasmic reticulum; ES; embryo
Old and new generation lipid mediators in acute inflammation and resolution
Keywords: 5-HT; 5-hydroxytryptamine; HETEs; hydroxyeicosatetraenoic acids; 5-HEDH; 5-hydroxyeicosanoid dehydrogenase; 5(S)-HPETE; hydroperoxyeicosatetranoic acid; 15R-HETE; 15-R-hydroxyeicosatetraenoic acid; 17R-HDHA; 17R-hydroxydocosahexaenoic acid; AA; arachidoni
Associate Editor: V.J. WattsRegulation of stem cell pluripotency and differentiation by G protein coupled receptors
Keywords: G protein coupled receptor; GPCR; Pluripotency; Stem cell; Differentiation; EB; Embryoid body; ES cells; Embyronic stem cells; FZD; Frizzled; GPCRs; G protein coupled receptors; GSK3; Glycogen synthase kinase 3; hATSCs; Human adipose tissue-derived mesenc
Interaction of angio-associated migratory cell protein with the TPα and TPβ isoforms of the human thromboxane A2 receptor
Keywords: AAMP; angio-associated migratory cell protein; AoSMC; aortic smooth muscle cell; CoASMC; coronary artery smooth muscle cell; C-tail; carboxyl-terminal tail; FBS; foetal bovine serum; GPCR; G protein-coupled receptor; GST; glutathione-S-transferase; HA; ha
The RasGrf family of mammalian guanine nucleotide exchange factors
Keywords: GEFs; guanine nucleotide exchange factors; NMDA; N-methyl-d-aspartate; AMPA; α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid; CNS; Central Nervous System; DMD; differentially methylated domain; CTCF; CCCTC-binding protein; CDB; cyclin destruction b
Evolution of neuronal signalling: Transmitters and receptors
Keywords: Evolution; GPCR; Neuropeptides; Neurotransmitters; Receptors; Neuropeptides; Cannabinoids; ATP
Mimicking nature's noses: From receptor deorphaning to olfactory biosensing
Keywords: BAW; bulk acoustic wave; BRET; bioluminescence resonance energy transfer; cVA; 11-cis-vaccenyl acetate; cAMP; cyclic adenosine monophosphate; cGMP; cyclic guanosine monophosphate; CNG; cyclic nucleotide gated; EAG; electroantennagram; EOG; electroolfactog
Synthesis and biological evaluation of piperazinyl heterocyclic antagonists of the gonadotropin releasing hormone (GnRH) receptor
Keywords: GnRH; GnRH antagonist; Gonadotropin releasing hormone; Gonadotropin releasing hormone antagonist; GPCR
The discovery and SAR of indoline-3-carboxamides-A new series of 5-HT6 antagonists
Keywords: 5-HT6; GPCR; Antagonist;
The identification of novel orally active mGluR5 antagonist GSK2210875
Keywords: mGluR; mGluR5; Brain free fraction; Negative allosteric modulator; Allosteric modulator; GPCR; Family C GPCR; Metabotropic glutamate receptor
Azole derivatives as histamine H3 receptor antagonists, Part I: Thiazol-2-yl ethers
Keywords: GPCR; Histamine; H3; Pharmacophore
N-Heterocyclic derived M1 positive allosteric modulators
Keywords: M1; Muscarinic; Allosteric; Modulator; GPCR; Alzheimer’s; Quinolone
Acidic elements in histamine H3 receptor antagonists
Keywords: GPCR; Histamine; Antagonists; Pharmacophore; PPAR; Metabolic diseases; Ligands
Discovery of a class of calcium sensing receptor positive allosteric modulators; 1-(benzothiazol-2-yl)-1-phenylethanols
Keywords: SAR; GPCR; CaSR; PAM; Allosteric; Modulators; Structure-activity relationship; Calciumsensing receptor; Cinacalcet; Calindol; Hyperparathyroidism; Fendiline; In vivo; Parathyroid hormone; 1-(benzothiazol-2-yl)-1-phenylethanols;
Azole derivatives as histamine H3 receptor antagonists, Part 2: C–C and C–S coupled heterocycles
Keywords: GPCR; Histamine; H3; Pharmacophore; Medicinal chemistry; Bioisosteric replacement
Synthesis and structure–activity relationships of a series of 3-aryl-4-isoxazolecarboxamides as a new class of TGR5 agonists
Keywords: SAR; TGR5; TGR5 agonists; GPCR; Solution-phase synthesis