2024
1734-P: ADP Privation of Human Beta-Cell Mitochondria by Pyruvate Kinase
RUZ-MALDONADO I, CARDONE R, KIBBEY R. 1734-P: ADP Privation of Human Beta-Cell Mitochondria by Pyruvate Kinase. Diabetes 2024, 73 DOI: 10.2337/db24-1734-p.Peer-Reviewed Original ResearchPyruvate kinaseBeta-cell mitochondriaInhibition of OXPHOSBeta-cellsHuman beta-cellsModulation of enzymesIntramitochondrial ADPPhosphoenolpyruvate inhibitionADP availabilityADP/ATP exchangeKATP channelsPhosphoenolpyruvate metabolismOxidative phosphorylationPhosphoenolpyruvateMitochondrial functionOXPHOSSubstrate transportComplex IATP/ADP ratioHuman isletsMitochondrial couplingOxygen consumption ratePyruvateMitochondriaDose-dependent manner
2023
A macrocyclic peptide inhibitor traps MRP1 in a catalytically incompetent conformation
Pietz H, Abbas A, Johnson Z, Oldham M, Suga H, Chen J. A macrocyclic peptide inhibitor traps MRP1 in a catalytically incompetent conformation. Proceedings Of The National Academy Of Sciences Of The United States Of America 2023, 120: e2220012120. PMID: 36893260, PMCID: PMC10089224, DOI: 10.1073/pnas.2220012120.Peer-Reviewed Original ResearchConceptsMultidrug resistance protein 1MRP1 overexpressionSubstrate transportAdenosine triphosphate-binding cassetteCatalytically incompetent conformationStructurally unrelated moleculesCpI1Small molecule inhibitorsAdenosine triphosphatePlasma membraneA-resolutionCryoelectron microscopyCryo-EMUnrelated moleculesConformational changesMultidrug resistanceMRP1 functionProtein 1Macrocyclic peptidesMultidrug transporter P-glycoproteinFlexible sidechainsXenobiotic compoundsNanomolar potencyCellular toxicityTherapeutic candidate
2018
Structural elements required for coupling ion and substrate transport in the neurotransmitter transporter homolog LeuT
Zhang YW, Tavoulari S, Sinning S, Aleksandrova AA, Forrest LR, Rudnick G. Structural elements required for coupling ion and substrate transport in the neurotransmitter transporter homolog LeuT. Proceedings Of The National Academy Of Sciences Of The United States Of America 2018, 115: e8854-e8862. PMID: 30181291, PMCID: PMC6156673, DOI: 10.1073/pnas.1716870115.Peer-Reviewed Original ResearchConceptsTransporter domainConformational changesOpen stateSodium symporter familyIon-substrate couplingTransmembrane ion gradientsSymporter familyNSS transportersSubstrate bindingLeuTIntracellular substratesCysteine accessibilitySubstrate transportAccessibility of substrateTyrosine residuesConformational responseNa2 siteUncoupled movementIon gradientsExtracellular pathwaysMechanistic componentsTransportersProteinTransport of ionsBinding
2008
A Competitive Inhibitor Traps LeuT in an Open-to-Out Conformation
Singh SK, Piscitelli CL, Yamashita A, Gouaux E. A Competitive Inhibitor Traps LeuT in an Open-to-Out Conformation. Science 2008, 322: 1655-1661. PMID: 19074341, PMCID: PMC2832577, DOI: 10.1126/science.1166777.Peer-Reviewed Original ResearchMeSH KeywordsAmino Acid Transport SystemsAmino AcidsBacterial ProteinsBinding SitesBinding, CompetitiveBiological TransportCrystallizationCrystallography, X-RayHydrogen BondingHydrophobic and Hydrophilic InteractionsKineticsLeucineLigandsModels, BiologicalModels, MolecularProtein ConformationProtein Structure, TertiarySodiumSymportersTryptophanConceptsNeurotransmitter sodium symportersPrimary substrate siteAmino acid substratesSodium symportersSecondary transportersExtracellular gateSubstrate passageLeucine transporterArginine 30Substrate transportCellular membranesConformational changesAcid substratesConformational statesSubstrate siteFunctional studiesIon gradientsLeuTWeak binding sitesTransportersBinding sitesSmall moleculesCompetitive inhibitorConformationTrp complex
2002
Examination of the Borrelia burgdorferi Transcriptome in Ixodes scapularis during Feeding
Narasimhan S, Santiago F, Koski RA, Brei B, Anderson JF, Fish D, Fikrig E. Examination of the Borrelia burgdorferi Transcriptome in Ixodes scapularis during Feeding. Journal Of Bacteriology 2002, 184: 3122-3125. PMID: 12003955, PMCID: PMC135063, DOI: 10.1128/jb.184.11.3122-3125.2002.Peer-Reviewed Original ResearchConceptsBorrelia burgdorferi gene expressionB. burgdorferi genesPeriplasmic proteinsSignal transductionChromosomal genesPutative lipoproteinSubstrate transportGene expressionDifferential expressionGenesEnergy metabolismIxodes scapularis ticksGlobal analysisIxodes scapularisScapularis ticksExpressionTranscriptomeTransductionTicksProteinFeedingMetabolismScapularis
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