2017
Chapter 8 Characterization of GPCR signaling in hypoxia
Chakraborty R, Sikarwar A, Hinton M, Dakshinamurti S, Chelikani P. Chapter 8 Characterization of GPCR signaling in hypoxia. Methods In Cell Biology 2017, 142: 101-110. PMID: 28964329, DOI: 10.1016/bs.mcb.2017.07.005.Peer-Reviewed Original ResearchConceptsThromboxane A2 receptorG protein-coupled receptorsPrimary pulmonary artery smooth muscle cellsPulmonary artery smooth muscle cellsArtery smooth muscle cellsPersistent pulmonary hypertensionPulmonary arterial responsesKey G‐protein‐coupled receptorsSmooth muscle cellsPulmonary hypertensionProtein-coupled receptorsArterial responseTissue hypoxiaCardiovascular diseaseA2 receptorsT cellsProstanoid receptorsCell responsesMuscle cellsHypoxic experimentsGPCR signalingHypoxiaHEK293T cellsReceptorsOxygen supply
2016
The Pharmacochaperone Activity of Quinine on Bitter Taste Receptors
Upadhyaya J, Chakraborty R, Shaik F, Jaggupilli A, Bhullar R, Chelikani P. The Pharmacochaperone Activity of Quinine on Bitter Taste Receptors. PLOS ONE 2016, 11: e0156347. PMID: 27223611, PMCID: PMC4880206, DOI: 10.1371/journal.pone.0156347.Peer-Reviewed Original ResearchConceptsBitter taste receptorsBitter taste signal transductionTaste receptorsTaste signal transductionControl untreated cellsQuinine treatmentAgonist treatmentCell surface expressionCalcium responsePharmacological techniquesAgonist activityTaste sensationBitter agonistsBasic taste sensationsReceptor internalizationSurface expressionUntreated cellsQuinineTreatmentDesensitizationReceptorsSignal transductionObserved actions
2015
Chapter Twelve Expression of G Protein-Coupled Receptors in Mammalian Cells
Chakraborty R, Xu B, Bhullar R, Chelikani P. Chapter Twelve Expression of G Protein-Coupled Receptors in Mammalian Cells. Methods In Enzymology 2015, 556: 267-281. PMID: 25857786, DOI: 10.1016/bs.mie.2014.12.013.Peer-Reviewed Original Research
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
2013
High-Level Expression, Purification and Characterization of a Constitutively Active Thromboxane A2 Receptor Polymorphic Variant
Xu B, Chakraborty R, Eilers M, Dakshinamurti S, O’Neil J, Smith S, Bhullar R, Chelikani P. High-Level Expression, Purification and Characterization of a Constitutively Active Thromboxane A2 Receptor Polymorphic Variant. PLOS ONE 2013, 8: e76481. PMID: 24086743, PMCID: PMC3781061, DOI: 10.1371/journal.pone.0076481.Peer-Reviewed Original ResearchConceptsG protein-coupled receptorsHigh-level expressionThromboxane A2 receptorSuccessful high-level expressionCell linesHigh-resolution crystal structuresProper expression systemMammalian cell linesResolution crystal structureProtein-coupled receptorsSingle-step affinity purificationStep affinity purificationCircular dichroism spectropolarimetryMembrane proteinsActive mutantAffinity purificationExpression systemBiophysical characterizationConstitutive signalingT geneSecondary structure changesT mutantGenetic variantsDiffusible ligandsHomogeneous glycosylationNew 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
2012
Role of rhodopsin N-terminus in structure and function of rhodopsin-bitter taste receptor chimeras
Pydi S, Chakraborty R, Bhullar R, Chelikani P. Role of rhodopsin N-terminus in structure and function of rhodopsin-bitter taste receptor chimeras. Biochemical And Biophysical Research Communications 2012, 430: 179-182. PMID: 23159609, DOI: 10.1016/j.bbrc.2012.11.029.Peer-Reviewed Original ResearchConceptsG protein-coupled receptorsBitter taste receptorsTaste receptorsProtein-coupled receptorsBitter taste sensationReceptor expressionLow-level expressionCalcium imagingReceptor functionFlow cytometryReceptorsTaste sensationAllosteric ligand bindingT2RsReceptor chimerasAmino acidsExpressionReceptor structureN-terminal 33N-terminal 33 amino acidsN-terminal sequenceCytometrySite-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
2011
Structural and functional roles of small group-conserved amino acids present on helix-H7 in the β2-adrenergic receptor
Arakawa M, Chakraborty R, Upadhyaya J, Eilers M, Reeves P, Smith S, Chelikani P. Structural and functional roles of small group-conserved amino acids present on helix-H7 in the β2-adrenergic receptor. Biochimica Et Biophysica Acta 2011, 1808: 1170-1178. PMID: 21262196, PMCID: PMC3062665, DOI: 10.1016/j.bbamem.2011.01.012.Peer-Reviewed Original ResearchAdrenergic beta-AgonistsAdrenergic beta-AntagonistsAmino Acid SubstitutionAmino AcidsAnimalsBinding SitesChlorocebus aethiopsCOS CellsCricetinaeCyclic AMPDihydroalprenololGlycineHEK293 CellsHumansHydrogen BondingIsoproterenolModels, MolecularMutationProtein BindingProtein Structure, SecondaryProtein Structure, TertiaryRadioligand AssayReceptors, Adrenergic, beta-2SerineStructure-Activity Relationship