Keywords: AMP-PNP; adenosine 5â²- (β,γ-imido)triphosphate; BSA; bovine albumin; [Ca2+]i; cytosolic free Ca2+ concentration; cAMP; adenosine cyclic 3â²,5â²-monophosphate; CMP; cytidine 5â²-monophosphate; CREB; cAMP response element binding protein; DMEM; Dulbe
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Keywords: Opioids; Analgesia; Adverse effects; Mechanisms; Constipation; Nausea; Vomiting; Respiratory depression; 5-HT; 5-hydroxytryptamine; 7TMRs; 7-transmembrane spanning G-protein coupled receptors; AC; adenylyl cyclase; β-arr1; β-arrestin1; β-arr2; β-arres
Keywords: AC; adenylate cyclase; Actn4; α-Actinin-4; ARF6; ADP-ribosylation factor 6; ATD; amino terminal domain; CAIN; calcineurin inhibitor protein; CaM; calmodulin; CaMKII; Ca2+/calmodulin-dependent protein kinase II; Cbln1; cerebellin 1 precursor; CC; coiled-c
Keywords: Fog; Folded gastrulation; TF; transcription factor; GPCR; G-protein coupled receptor; Mist; mesoderm invagination signal transducer; Cta; Concertina; RhoGEF; Rho guanine nucleotide exchange factor; Rok; Rho kinase; PMG; posterior midgut; GBE; germ band ex
Keywords: AC; adenylate cyclase; β-AR; β-adrenergic receptor; CaM; calmoduline; cAMP; cyclic adenosine monophosphate; CHO; Chinese hamster ovary; EGFR; epidermal growth factor receptor; ERK; extracellular signal-regulated kinase; DAG; diacylglycerol; DR; dopamine
Keywords: IR; insulin receptor; IRS1; insulin receptor substrate-1; IGF-R; insulin growth factor receptor; EGF; epidermal growth factor; MMP; matrix metalloproteinase; RTK; receptor tyrosine kinase; NGF; nerve growth factor; Neu1; mammalian neuraminidase-1; 4-MUNAN
Keywords: λmax; absorption maximum wavelength; GRK; G protein-coupled receptor kinase; UV; ultraviolet; CHAPS; 3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonate; PC; l-α-phosphatidylcholine; Pi; inorganic phosphate; Cone visual pigment; Phosphorylation; G
Keywords: GPCR; G protein-coupled receptor; GRK; G protein-coupled receptor kinase; WT; wild type; Rh; dark unphosphorylated rhodopsin; Rh*; light-activated unphosphorylated rhodopsin; P-Rh; dark phosphorylated rhodopsin; P-Rh*; light-activated phosphorylated rhodo
Keywords: Abl; Abelson leukemia proto-oncogene; ADAP; adhesion and degranulation promoting adapter protein (Fyb, SLAP-130); Asc; apoptosis-associated speck-like protein containing a CARD; BCR; B-cell receptor; C3G; Crk SH3 domain-binding guanine nucleotide exchange
β3-adrenergic receptor activation induces TGFβ1 expression in cardiomyocytes via the PKG/JNK/c-Jun pathway
Keywords: β3-adrenergic receptor; Transforming growth factor β1; Protein kinase G; c-Jun N-Terminal kinase; c-Jun; Cardiomyocyte; AP-1; activator protein 1; β-AR; β-adrenergic receptor; cGMP; cyclic guanosine monophosphate; GRK; G protein-coupled receptor kinas
G protein-coupled receptor kinases: Past, present and future
Keywords: αN-helix; N-terminal α-helical domain; α2AAR; α2A-adrenergic receptor; AST; active site tether; βAR; β-adrenergic receptor; β2AR; β2-adrenergic receptor; βARK; β-adrenergic receptor kinase; CLBD; C-terminal lipid binding domain; EM; electron mic
Designer Approaches for G Protein-Coupled Receptor Modulation for Cardiovascular Disease
Keywords: biased ligands; G protein-coupled receptor kinases; G protein-coupled receptors; AR; adrenergic receptor; AT1R; angiotensin II type 1A receptor; CRF; corticotropin-releasing factor; EGFR; epidermal growth factor receptor; ERK1/2; extracellular signal-
Bifunctional ligands of the bradykinin B2 and B1 receptors: An exercise in peptide hormone plasticity
Keywords: ACE; angiotensin converting enzyme; ε-ACA; ε-aminocaprolyl; APEX2; engineered soya bean peroxidase; Arg-CP; arginine carboxypeptidase; B1R; B1 receptor; B2R; B2 receptor; B2R-GFP; rabbit B2 receptor fused to green fluorescent protein; BK; bradykinin; CF
β-Adrenergic Receptor Trafficking, Degradation, and Cell Surface Expression Are Altered in Dermal Fibroblasts from Hypertrophic Scars
Keywords: β-AR; adrenergic receptor; HSF; hypertrophic scar fibroblast; GRK; GPCR kinase; NSF; non-scar fibroblast; NF; normal fibroblast; PKA; protein kinase A;
Different mode of arrestin-3 binding at the human Y1 and Y2 receptor
Keywords: ANOVA; analysis of variance; arr; arrestin; BRET; bioluminescence resonance energy transfer; EYFP; enhanced yellow fluorescent protein; FLR; finger loop region; GPCR; G protein-coupled receptor; GRK; G protein-coupled receptor kinase; YxR; neuropeptide Yx
GPCR Kinase (GRK)-2 Is a Key Negative Regulator of Itch: l-Glutamine Attenuates Itch via a Rapid Induction of GRK2 in an ERK-Dependent Way
Keywords: Ad-GRK2; adenovirus expressing GPCR kinase-2; CD; contact dermatitis; CQ; chloroquine; DNCB; dinitrochlorobenzene; Gln; l-glutamine; GRK; GPCR kinase; MKP-1; MAPK phosphatase-1; siRNA; small interfering RNA;
Different phosphorylation patterns regulate α1D-adrenoceptor signaling and desensitization
Keywords: α1D-AR; α1D-adrenergic receptor; ERK; extracellular signal-regulated kinase; NA; noradrenaline; PMA; phorbol 12-myristate, 13-acetate; PKC; protein kinase C; GPCR; G protein-coupled receptor; GRK; GPCR kinase; IL3; intracellular loop 3; Ctail; carboxyl
β-arrestin-biased agonism of β-adrenergic receptor regulates Dicer-mediated microRNA maturation to promote cardioprotective signaling
Keywords: βARs; β-adrenergic receptors; β-blockers; β-adrenergic receptor antagonists; β-miRs; β-adrenergic receptor/β-arrestin-regulated miRs; Carv; carvedilol; GPCR; G protein-coupled receptor; GRK; G protein-coupled receptor kinase; KO; knockout; MiRNAs o
AGC kinases, mechanisms of regulation âand innovative drug development
Keywords: AGC kinase; group of kinases related to PKA PKG and PKC; PKA; protein kinase A; PKC; protein kinase C; PKG; protein kinase G; PRK; protein kinase C related kinase (also termed PKN protein kinase N); PDK1; 3-phosphoinositide-dependent protein kinase 1; PKB
Human melanocortin 1 receptor-mediated ubiquitination of nonvisual arrestins. Role of Mahogunin Ring Finger 1 E3 ligase
Keywords: ARRB; β-arrestin; β2AR; β2-adrenergic receptor; GRK; G protein-coupled receptor kinase; GPCR; G protein-coupled receptor; LOF; loss-of-function; αMSH; α melanocyte-stimulating hormone; MCR; melanocortin receptor; MC1R; melanocortin 1 receptor; MGRN1;
The G protein-coupled receptors deorphanization landscape
Keywords: GPCRs; G protein-coupled receptors; GRK; GPCR kinase; IUPHAR; International Union of Basic and Clinical Pharmacology; BPS; British Pharmacological Society; CTR; Calcitonin receptor; CLR; CT Receptor-like; RAMP; Receptor Activity-Modifying Proteins; β2AR;
Impact of paroxetine on proximal β-adrenergic receptor signaling
Keywords: βAR; β-adrenergic receptor; βarr; β-arrestin; EC50; half-maximal effective concentration; FRET; fluorescence resonance energy transfer; GRK; G protein-coupled receptor; IC50; half-maximal inhibitory concentration; ISO; isoproterenol; mCFP; monomeric c
C-terminal motif of human neuropeptide Y4 receptor determines internalization and arrestin recruitment
Keywords: ANOVA; analysis of variance; arr; arrestin; BRET; bioluminescence resonance energy transfer; EYFP; enhanced yellow fluorescent protein; GPCR; G protein-coupled receptor; GRK; G protein-coupled receptor kinase; hPP; human pancreatic polypeptide; hY1R; huma
Pathophysiological consequences of receptor mistraffic: Tales from the platelet P2Y12 receptor
Keywords: ADP; Adenosine diphosphate; CNM; centronuclear myopathy; CMT; Charcot-Marie- Tooth; CAMs; constitutively active mutants; GAPP; Genotyping and Phenotyping of Platelets consortium; GPCR; G protein-coupled receptor; GRK; G protein-coupled receptor kinase
Matrix Signaling Subsequent to a Myocardial Infarction
Keywords: βAR signaling; chronic ischemic cardiomyopathy; matrix signaling; myocardial infarction; tissue factor-bearing microparticles; Yucatan mini swine; ADRB1; β1-adrenergic receptor; ADRB2; β2-adrenergic receptor; AR; adrenergic receptor; ARRB1; β1-arresti
Purinergic P2Y receptors: Molecular diversity and implications for treatment of cardiovascular diseases
Keywords: ADP; adenosine 5â²-diphosphate; AgRP; agouti-related peptide; AMPK; 5â²-AMP-activated protein kinase; ApnA; diadenosine polyphosphate; ApoE; apolipoprotein E; AT1R; angiotensin II type 1 receptor; ATP; adenosine 5â²-triphosphate; BN-PAGE; blue native-p
G protein-coupled receptor kinase 4-induced cellular senescence and its senescence-associated gene expression profiling
Keywords: GPCR; G protein-coupled receptor; GRK; G protein-coupled receptor kinases; SA-β-Gal; senescence-associated-β-galactosidase; FACS; fluorescence-activated cell sorting; CCK-8; cell counting kit-8; CDK; cyclin-dependent kinase; CKI; cyclin-dependent kinase
Spatial encryption of G protein-coupled receptor signaling in endosomes; Mechanisms and applications
Keywords: AKT (PKB); protein kinase B; AP2; adaptor protein 2; APPL1; adaptor protein containing PH domain, PTB domain, and Leucine zipper motif; ARRDC; arresting domain containing; Î1AR; B2AR, beta-adrenergic receptor 1 or 2; CCP; clathrin coated pit; CXCR4; chem
MC1R signaling. Intracellular partners and pathophysiological implications
Keywords: AC; adenylyl cyclase; ACTH; adrenocorticotropic hormone; ARRB; β-arrestin; ASIP; agouti signal protein; CBD103; dog β-defensin-3; CREB; cAMP responsive-element binding protein; EDN1; endothelin 1; ER; endoplasmic reticulum; ERK; extracellular signal-reg
Roles of Mas-related G protein-coupled receptor X2 on mast cell-mediated host defense, pseudoallergic drug reactions, and chronic inflammatory diseases
Keywords: G protein-coupled receptor; MRGPRX2; mast cells; host defense peptides; neuropeptides; drug-induced pseudoallergy; chronic urticaria; asthma; C3aR; Anaphylatoxin C3a receptor; CGRP; Calcitonin gene-related peptide; CTMC; Connective tissue mast cell; C
CNS remyelination as a novel reparative approach to neurodegenerative diseases: The roles of purinergic signaling and the P2Y-like receptor GPR17
Keywords: Purinergic receptors; Oligodendrocytes; Remyelination; AD; Alzheimer's disease; ALS; amyotrophic lateral sclerosis; ATX; autotaxin; CNS; central nervous system; DRG; dorsal root ganglion; EAE; experimental autoimmune encephalomyelitis; GDNF; glial cell de
Feedback regulation of G protein-coupled receptor signaling by GRKs and arrestins
Keywords: GPCR; G protein; Arrestin; GRK; Signal transduction; Biased signaling;
Characterization of the interaction between the dopamine D4 receptor, KLHL12 and β-arrestins
Keywords: GPCR; β-arrestin; KLHL12; ubiquitination; dopamine D4 receptor; β2AR; β2-adrenergic receptor; ADHD; attention deficit hyperactivity disorder; BTB; bric à brac 1, tramtrack, and broad-complex; co-IP; co-immunoprecipitation; CXCR4; C-X-C chemokine recep
Systematic analysis of factors influencing observations of biased agonism at the mu-opioid receptor
Keywords: AC; adenylyl cyclase; α-neo; α-neoendorphin; β-arr1 and β-arr2; β-arrestin 1 and 2; BRET; bioluminescence resonance energy transfer; CHO; Chinese hamster ovary; DAMGO; d-Ala2-N-MePhe4-Gly-ol enkephalin; endo; endomorphin; pERK; extracellular signal r
Research ReportInvolvement of NFκB signaling in mediating the effects of GRK5 on neural stem cells
Keywords: AD; Alzheimer׳s disease; GPCR; G protein-coupled receptor; GRK; G-protein receptor kinase; IL-6; interleukin-6; IL-1β; interleukin-1β; NAC; N-acetyl cysteine; NFκB; nuclear factor κB; NPCs; neural progenitor cells; NSCs; neuron stem cells; PKA; prote
The carboxy-terminal tail or the intracellular loop 3 is required for β-arrestin-dependent internalization of a mammalian type II GnRH receptor
Keywords: GnRH receptor; Internalization; G protein-coupled receptor kinase; β-Arrestin; ERK; DMEM; Dulbecco's modified Eagle medium; EC50; concentration that stimulates half-maximal IP production; ERK; extracellular signal-regulated kinases; FSH; follicle-stimula
The dichotomy of the Insulin-like growth factor 1 receptor: RTK and GPCR: friend or foe for cancer treatment?
Keywords: IGF-1R; RTK; GPCR; beta-Arrestin; GRK; Biased signalling; Cancer; Ubiquitination;
Cannabinoid receptor interacting protein (CRIP1a) attenuates CB1R signaling in neuronal cells
Keywords: 2-AG; 2-arachidonoylglycerol; BSA; bovine serum albumin; CB1; cannabinoid receptor; CP55940; (â)-cis-3-[2-Hydroxy-4-(1,1-dimethylÂheptyl)phenyl]-trans-4-(3-hydroxypropyl)cyclohexanol; CRIP1a; Cannabinoid Receptor Interacting Protein 1a; DAGL; diacylgly
PDZK1/NHERF3 Differentially Regulates Corticotropin-releasing Factor Receptor 1 and Serotonin 2A Receptor Signaling and Endocytosis
Keywords: ANOVA; analysis of variance; β 1AR; β 1-adrenergic receptor; β2AR; β2-adrenergic receptor; CRF; corticotropin-releasing factor; CRFR1; CRF receptor 1; CRFR2; CRF receptor 2; ERK1/2; extracellular signal-regulated kinase; GKAP; guanylate kinase-associa
γ-Glutamyl cysteine and γ-glutamyl valine inhibit TNF-α signaling in intestinal epithelial cells and reduce inflammation in a mouse model of colitis via allosteric activation of the calcium-sensing receptor
Keywords: CaSR; calcium-sensing receptor; GPCR; G-protein-coupled receptor; IBD; inflammatory bowel disease; CD; Crohn's disease; UC; ulcerative colitis; γ-EC; γ-glutamyl cysteine; γ-EV; γ-glutamyl valine; GRK; GPCR kinase; TRAF; TNF-receptor-associated factor;
The CXC chemokine receptors of fish: Insights into CXCR evolution in the vertebrates
Keywords: ACKR; atypical chemokine receptor; AGTR; angiotensin II receptor; AP-2; activated protein 2; CCR; CC chemokine receptors; CD; cluster of differentiation; CXC; CXC chemokine; CXCR; CXC chemokine receptor; CX3CR; CX3C receptor; ERK; extracellular regulated
New paradigms in GPCR drug discovery
Keywords: cAMP; 3â²,5â²-cyclic adenosine monophosphate; ADP; adenosine 5â²- diphosphate; GPCR; G protein-coupled receptor; TM; transmembrane helix; ERK; extracellular signal-regulated kinase; T4L; T-4 lysozyme; BRIL; thermostabilized apocytochrome b562; StaRs; s
Cardioprotective potential of annexin-A1 mimetics in myocardial infarction
Keywords: Ac2-26; Cardioprotection; Cardiomyopathy; Formyl peptide receptors; Inflammation; Ischemia-reperfusion; Aβ42; 42-amino acid beta-amyloid peptide; ABC; ATP-binding cassette; Ac2-26; N-terminal-derived annexin-A1 peptide (acetyl-AMVSEFLKQAWIENEEQEYVVQTVK
Mechanisms that underlie the internalization and extracellular signal regulated kinase 1/2 activation by PKR2 receptor
Keywords: AT1AR; angiotensin type 1A receptor; ConA; Concanavalin A; DN-GRK; dominant-negative G-protein-coupled receptor kinase 2; EGFP; enhanced green fluorescent protein; ERK; extracellular signal regulated kinase; GPCR; G-protein-coupled receptors; GRK; GPCR ki
Phosphodiesterase 4 interacts with the 5-HT4(b) receptor to regulate cAMP signaling
Keywords: 5-HT; 5-hydroxytryptamine; AKAP; A-kinase anchoring protein; DMSO; dimethyl sulfoxide; GRK; G protein-coupled receptor kinase; HEK293; human embryonic kidney cell line; IBMX; isobutylmethylxanthine; IP; immunoprecipitation; PDE; phosphodiesterase; PKA; pr
Selective regulation of recombinantly expressed mGlu7 metabotropic glutamate receptors by G protein-coupled receptor kinases and arrestins
Keywords: mGlu7 receptors; GRK; Arrestins; MAP kinases; Jun kinases; Signaling regulation; GPCR; G protein-coupled receptor; mGlu; metabotropic glutamate receptor; GRK; G protein-coupled receptor kinase; FSK; forskolin; L-AP4; l-2-amino-4-phosphonobutanoate; MAPK;
In vivo modulation of polo-like kinases supports a key role for PLK2 in Ser129 α-synuclein phosphorylation in mouse brain
Keywords: ANOVA; analysis of variance; Ce; cerebellum; CEB; cell extraction buffer; CHAPS; 3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonate; Co; cerebral cortex; CSNK2a2; alpha prime subunit of casein kinase II; EDTA; ethylenediaminetetraacetic acid; EGTA;
Homologous desensitization of human histamine H3 receptors expressed in CHO-K1 cells
Keywords: Histamine; H3 receptor; Desensitization; GRK; CHO-K1 cells; Neuromodulation; H3R; histamine H3 receptor; GPCR; G protein-coupled receptor; GRK; GPCR kinase; RAMH; R-α-methylhistamine;
Activation of Bombyx neuropeptide G protein-coupled receptor A4 via a Gαi-dependent signaling pathway by direct interaction with neuropeptide F from silkworm, Bombyx mori
Keywords: Neuropeptide; GPCR; Signaling; Arrestin; MAP kinases; AKH; adipokinetic hormone; cAMP; cyclic AMP; CRE; cAMP-response element; EGFP; enhanced green fluorescent protein; ERK1/2; extracellular signal-regulated kinase1/2; Gi; inhibitory GTP-binding protein o
Sphingosine-1-phosphate (S1P) displays sustained S1P1 receptor agonism and signaling through S1P lyase-dependent receptor recycling
Keywords: BSA; bovine serum albumin; CHO; Chinese hamster ovary; CRC; concentration-response curve; EC50; half maximimal excitatory concentration; Emax; maximal efficacy versus a defined control; FBS; fetal bovine serum; GPCR; G protein coupled receptor; GRK; GPC