2022
Insights into distinct signaling profiles of the µOR activated by diverse agonists
Qu Q, Huang W, Aydin D, Paggi J, Seven A, Wang H, Chakraborty S, Che T, DiBerto J, Robertson M, Inoue A, Suomivuori C, Roth B, Majumdar S, Dror R, Kobilka B, Skiniotis G. Insights into distinct signaling profiles of the µOR activated by diverse agonists. Nature Chemical Biology 2022, 19: 423-430. PMID: 36411392, PMCID: PMC11098091, DOI: 10.1038/s41589-022-01208-y.Peer-Reviewed Original ResearchMeSH KeywordsAnalgesics, OpioidAnimalsbeta-ArrestinsBinding SitesGTP-Binding ProteinsSignal TransductionConceptsRespiratory depressionCryo-EM structureMitragynine pseudoindoxylM-opioid receptorSignaling outcomesB-arrestinMolecular dynamics simulationsFatal respiratory depressionCryo-EMG-proteinBinding sitesMOR agonistsEffective analgesicSafety profileEfficacy profileSubtype activationAnimal studiesDynamics simulationsOrthosteric pocketLofentanilIntracellular sidePlant-derivedAgonistsDiverse agonistsActive-state conformationSignaling snapshots of a serotonin receptor activated by the prototypical psychedelic LSD
Cao C, Barros-Álvarez X, Zhang S, Kim K, Dämgen M, Panova O, Suomivuori C, Fay J, Zhong X, Krumm B, Gumpper R, Seven A, Robertson M, Krogan N, Hüttenhain R, Nichols D, Dror R, Skiniotis G, Roth B. Signaling snapshots of a serotonin receptor activated by the prototypical psychedelic LSD. Neuron 2022, 110: 3154-3167.e7. PMID: 36087581, PMCID: PMC9583076, DOI: 10.1016/j.neuron.2022.08.006.Peer-Reviewed Original ResearchConceptsLysergic acid diethylamidePsychedelic lysergic acid diethylamideSerotonin receptorsPsychedelic drugsPsychedelic drug effectsAcid diethylamideSerotoninDrug effectsSignal snapshotsGq protein-coupledHTR2AHTR2BReceptorsActive stateDiethylamideSignaling mechanismsDrugCryo-EM structureModel receptor
2020
Angiotensin and biased analogs induce structurally distinct active conformations within a GPCR
Wingler L, Skiba M, McMahon C, Staus D, Kleinhenz A, Suomivuori C, Latorraca N, Dror R, Lefkowitz R, Kruse A. Angiotensin and biased analogs induce structurally distinct active conformations within a GPCR. Science 2020, 367: 888-892. PMID: 32079768, PMCID: PMC7171558, DOI: 10.1126/science.aay9813.Peer-Reviewed Original ResearchMeSH KeywordsAngiotensin IIbeta-ArrestinsHumansLigandsProtein ConformationReceptor, Angiotensin, Type 1Signal Transduction
2019
Antiviral immunity: a link to bile acids
Wang J, Flavell RA, Li HB. Antiviral immunity: a link to bile acids. Cell Research 2019, 29: 177-178. PMID: 30778178, PMCID: PMC6460437, DOI: 10.1038/s41422-019-0148-5.Peer-Reviewed Original Research
2014
Activation of N-methyl-d-aspartate receptor downregulates inflammasome activity and liver inflammation via a β-arrestin-2 pathway
Farooq A, Hoque R, Ouyang X, Farooq A, Ghani A, Ahsan K, Guerra M, Mehal WZ. Activation of N-methyl-d-aspartate receptor downregulates inflammasome activity and liver inflammation via a β-arrestin-2 pathway. AJP Gastrointestinal And Liver Physiology 2014, 307: g732-g740. PMID: 25104498, PMCID: PMC4187065, DOI: 10.1152/ajpgi.00073.2014.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsAnti-Inflammatory AgentsArrestinsAspartic Acidbeta-Arrestin 2beta-ArrestinsCarrier ProteinsCaspase 1Cell LineChemical and Drug Induced Liver InjuryDisease Models, AnimalExcitatory Amino Acid AgonistsHumansInflammasomesInterleukin-1betaLiverMacrophagesMaleMice, Inbred C57BLNLR Family, Pyrin Domain-Containing 3 ProteinPancreatitisProtein PrecursorsReceptors, N-Methyl-D-AspartateSignal TransductionTime FactorsConceptsNMDA receptorsAcute hepatitisLiver inflammationInflammasome activityAcute inflammatory liver injuryNOD-like receptor familyN-methyl-D-aspartate (NMDA) receptor familyChronic liver inflammationInflammatory liver injuryΒ-arrestinBrain NMDA receptorsReceptor familyNMDA receptor pathwayLigand-gated ion channelsLiver injuryNonalcoholic steatohepatitisImmune suppressionLimits injuryNF-kβImmune regulationInflammasome activationKupffer cellsInflammasome machineryPyrin domainNonneuronal cellsLactate Reduces Liver and Pancreatic Injury in Toll-Like Receptor– and Inflammasome-Mediated Inflammation via GPR81-Mediated Suppression of Innate Immunity
Hoque R, Farooq A, Ghani A, Gorelick F, Mehal WZ. Lactate Reduces Liver and Pancreatic Injury in Toll-Like Receptor– and Inflammasome-Mediated Inflammation via GPR81-Mediated Suppression of Innate Immunity. Gastroenterology 2014, 146: 1763-1774. PMID: 24657625, PMCID: PMC4104305, DOI: 10.1053/j.gastro.2014.03.014.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsAnti-Inflammatory AgentsArrestinsbeta-Arrestin 2beta-ArrestinsCarrier ProteinsCell LineCeruletideChemical and Drug Induced Liver InjuryCytoprotectionDisease Models, AnimalDose-Response Relationship, DrugDown-RegulationGalactosamineHumansImmunity, InnateInflammasomesInjections, IntraperitonealInterleukin-1betaLipopolysaccharidesLiverMacrophagesMaleMiceMice, Inbred C57BLMonocytesNF-kappa BNLR Family, Pyrin Domain-Containing 3 ProteinPancreasPancreatitisReceptors, G-Protein-CoupledRNA InterferenceRNA, Small InterferingSignal TransductionSodium LactateToll-Like Receptor 4Toll-Like ReceptorsTransfectionConceptsToll-like receptorsRelease of IL1βAdministration of lipopolysaccharideOrgan injuryNF-κBCaspase-1TLR inductionAcute pancreatitisPyrin domain-containing protein 3Administration of lactatePromising immunomodulatory therapyAcute liver injuryAcute organ injuryMacrophages of miceDomain-containing protein 3Production of IL1βRAW 264.7 cellsConcentration of lactateAcute hepatitisImmunomodulatory therapyImmune hepatitisPancreatic injuryLactate receptorLiver injuryNLRP3 inflammasome
2013
Characterization of Three Vasopressin Receptor 2 Variants: An Apparent Polymorphism (V266A) and Two Loss-of-Function Mutations (R181C and M311V)
Armstrong S, Seeber R, Ayoub M, Feldman B, Pfleger K. Characterization of Three Vasopressin Receptor 2 Variants: An Apparent Polymorphism (V266A) and Two Loss-of-Function Mutations (R181C and M311V). PLOS ONE 2013, 8: e65885. PMID: 23762448, PMCID: PMC3675069, DOI: 10.1371/journal.pone.0065885.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsAquaporin 2Arginine VasopressinArrestinsbeta-ArrestinsChlorocebus aethiopsCOS CellsCyclic AMPDiabetes Insipidus, NephrogenicGene Expression RegulationGenetic Diseases, X-LinkedGTP-Binding Protein alpha Subunits, GsHEK293 CellsHumansInappropriate ADH SyndromeInositol PhosphatesMutationPolymorphism, GeneticReceptors, VasopressinSignal TransductionConceptsNephrogenic diabetes insipidusArginine vasopressinWild-type receptorAquaporin-2 water channelsActivation of Gs proteinsIncreased inositol phosphate productionPartial agonismVasopressin V2 receptorInositol phosphate accumulationGain-of-function mutationsIncreased cAMP levelsBRET assayInositol phosphate productionLoss-of-function mutationsNephrogenic syndromeV2R mutationsLoss-of-functionDiabetes insipidusMutant V2RV2 receptorsCAMP accumulationMilder phenotypePosterior pituitaryB-arrestinControls water homeostasis
2011
Protective Effects of Glycyrrhizin against β2-Adrenergic Receptor Agonist-Induced Receptor Internalization and Cell Apoptosis
Shi Q, Hou Y, Yang Y, Bai G. Protective Effects of Glycyrrhizin against β2-Adrenergic Receptor Agonist-Induced Receptor Internalization and Cell Apoptosis. Biological And Pharmaceutical Bulletin 2011, 34: 609. PMID: 21532146, DOI: 10.1248/bpb.34.609.Peer-Reviewed Original ResearchConceptsAgonist-induced receptor internalizationG protein-coupled receptor kinasesReceptor internalizationCell apoptosisChronic obstructive pulmonary diseaseEffect of glycyrrhizinFixed-cell enzyme-linked immunosorbent assayEnzyme-linked immunosorbent assayClathrin heavy chainInhibition of receptor internalizationB-cell lymphoma 2Expression of B-cell lymphoma 2Protective effectLive cell confocal imagingLoss of pharmacological effectProtective effect of glycyrrhizinIncreased adverse cardiovascular eventsCardiac muscle cell apoptosisB2 adrenergic receptorAdverse cardiovascular eventsFamily genesMuscle cell apoptosisTransmembrane signalingEfficacy of bronchodilatorsBcl-2
2009
Agonist-Independent Interactions between β-Arrestins and Mutant Vasopressin Type II Receptors Associated with Nephrogenic Syndrome of Inappropriate Antidiuresis
Kocan M, See H, Sampaio N, Eidne K, Feldman B, Pfleger K. Agonist-Independent Interactions between β-Arrestins and Mutant Vasopressin Type II Receptors Associated with Nephrogenic Syndrome of Inappropriate Antidiuresis. Endocrinology 2009, 23: 559-571. PMID: 19179480, PMCID: PMC2667710, DOI: 10.1210/me.2008-0321.Peer-Reviewed Original ResearchConceptsAssociated with impaired signalingSyndrome of inappropriate antidiuresisImpaired signalingArginine vasopressin levelsNephrogenic diabetes insipidusAgonist-independent internalizationSevere symptomatic hyponatremiaPlasma membraneV2R R137HType II receptorMutation-dependent differencesDynamin-dependent internalizationInappropriate antidiuresisNephrogenic syndromeArginine to histidineVasopressin type II receptorSymptomatic hyponatremiaDiabetes insipidusVasopressin levelsBioluminescence resonance energy transferMale infantG-protein uncouplingCodon 137II receptorsKidney's ability
This site is protected by hCaptcha and its Privacy Policy and Terms of Service apply