2014
Inverse 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
2012
Site-Directed Mutations and the Polymorphic Variant Ala160Thr in the Human Thromboxane Receptor Uncover a Structural Role for Transmembrane Helix 4
Chakraborty R, Pydi SP, Gleim S, Dakshinamurti S, Hwa J, Chelikani P. Site-Directed Mutations and the Polymorphic Variant Ala160Thr in the Human Thromboxane Receptor Uncover a Structural Role for Transmembrane Helix 4. PLOS ONE 2012, 7: e29996. PMID: 22272267, PMCID: PMC3260207, DOI: 10.1371/journal.pone.0029996.Peer-Reviewed Original ResearchMeSH Keywords15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic AcidAlanineAmino Acid SequenceAnimalsBinding SitesBinding, CompetitiveBridged Bicyclo Compounds, HeterocyclicCalciumChlorocebus aethiopsCOS CellsFatty Acids, UnsaturatedGlycineHEK293 CellsHumansHydrazinesMicroscopy, FluorescenceModels, MolecularMolecular Sequence DataMutagenesis, Site-DirectedMutant ProteinsMutation, MissensePolymorphism, Single NucleotideProtein Structure, SecondaryRadioligand AssayReceptors, Thromboxane A2, Prostaglandin H2Structure-Activity RelationshipTemperature