2014
Dextromethorphan Mediated Bitter Taste Receptor Activation in the Pulmonary Circuit Causes Vasoconstriction
Upadhyaya J, Singh N, Sikarwar A, Chakraborty R, Pydi S, Bhullar R, Dakshinamurti S, Chelikani P. Dextromethorphan Mediated Bitter Taste Receptor Activation in the Pulmonary Circuit Causes Vasoconstriction. PLOS ONE 2014, 9: e110373. PMID: 25340739, PMCID: PMC4207743, DOI: 10.1371/journal.pone.0110373.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsDextromethorphanFluorescent Antibody TechniqueGene Expression RegulationGene Knockdown TechniquesHumansIn Vitro TechniquesInositol 1,4,5-TrisphosphateLungMyocytes, Smooth MuscleMyographyMyosin Light ChainsPhosphorylationPulmonary ArteryReceptors, G-Protein-CoupledReverse Transcriptase Polymerase Chain ReactionRNA, MessengerSuperoxidesSus scrofaTasteVasoconstrictionConceptsPulmonary artery smooth muscle cellsArtery smooth muscle cellsHuman pulmonary artery smooth muscle cellsSmooth muscle cellsAirway ringsMuscle cellsVascular tonePulmonary circuitCalcium responseHuman airway smooth muscle cellsAirway smooth muscle cellsExpression of T2RsPulmonary vascular toneBitter taste receptor activationTaste receptor activationEx vivo studyVasoconstrictor responsesBitter taste receptorsMyographic studiesMuscle relaxationReceptor activationDextromethorphanSpecific shRNART-PCRVivo studiesInverse Agonism of SQ 29,548 and Ramatroban on Thromboxane A2 Receptor
Chakraborty R, Bhullar RP, Dakshinamurti S, Hwa J, Chelikani P. Inverse Agonism of SQ 29,548 and Ramatroban on Thromboxane A2 Receptor. PLOS ONE 2014, 9: e85937. PMID: 24465800, PMCID: PMC3900440, DOI: 10.1371/journal.pone.0085937.Peer-Reviewed Original ResearchMeSH KeywordsAmino Acid SubstitutionBlood PlateletsBridged Bicyclo Compounds, HeterocyclicCalcium SignalingCarbazolesDrug Evaluation, PreclinicalFatty Acids, UnsaturatedHEK293 CellsHumansHydrazinesInositol 1,4,5-TrisphosphateMutagenesis, Site-DirectedReceptors, Thromboxane A2, Prostaglandin H2SulfonamidesConceptsThromboxane A2 receptorG protein-coupled receptorsA2 receptorsBasal activityPathophysiological conditionsImportant pathophysiological roleInverse agonist propertiesHuman platelet functionSuch constitutive activityTP dysfunctionConstitutive activityPlatelet hyperactivityProtein-coupled receptorsCardiovascular diseaseThromboxane A2Pathophysiological roleT cellsPlatelet functionImportant therapeutic applicationsAgonist propertiesRamatrobanPlatelet activationInverse agonistInverse agonismNeutral antagonists
2013
New Insights into Structural Determinants for Prostanoid Thromboxane A2 Receptor- and Prostacyclin Receptor-G Protein Coupling
Chakraborty R, Pydi SP, Gleim S, Bhullar RP, Hwa J, Dakshinamurti S, Chelikani P. New Insights into Structural Determinants for Prostanoid Thromboxane A2 Receptor- and Prostacyclin Receptor-G Protein Coupling. Molecular And Cellular Biology 2013, 33: 184-193. PMID: 23109431, PMCID: PMC3554117, DOI: 10.1128/mcb.00725-12.Peer-Reviewed Original ResearchMeSH KeywordsAmino Acid SequenceBinding SitesCalciumFluorescent Antibody TechniqueGTP-Binding ProteinsHEK293 CellsHumansInositol 1,4,5-TrisphosphateLigandsModels, MolecularMolecular Sequence DataMutagenesis, Site-DirectedNonlinear DynamicsProtein BindingProtein ConformationReceptors, EpoprostenolReceptors, Thromboxane A2, Prostaglandin H2Signal TransductionConceptsG protein-coupled receptorsG protein specificityThromboxane A2 receptorProtein interactionsProtein specificityIntracellular loopChimeric receptorsG proteinsGPCR-G protein interactionsProtein couplingHeterotrimeric G proteinsCognate G-proteinSite-directed mutagenesisNew molecular insightsProtein-coupled receptorsG protein couplingReceptor-G protein interactionG protein activationA2 receptorsReceptor-G protein couplingStructural basisMolecular insightsProtein activationMolecular natureStructural determinants