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
2005
Crystal structure of a bacterial homologue of Na+/Cl--dependent neurotransmitter transporters
Yamashita A, Singh SK, Kawate T, Jin Y, Gouaux E. Crystal structure of a bacterial homologue of Na+/Cl--dependent neurotransmitter transporters. Nature 2005, 437: 215-223. PMID: 16041361, DOI: 10.1038/nature03978.Peer-Reviewed Original ResearchMeSH KeywordsAmino Acid SequenceBacteriaBacterial ProteinsBinding SitesBiological TransportChloridesCrystallography, X-RayHydrophobic and Hydrophilic InteractionsLeucineMembrane Transport ProteinsModels, MolecularMolecular Sequence DataNeurotransmitter AgentsSequence AlignmentSodiumStructure-Activity RelationshipWaterConceptsBacterial homologueProtein coreDependent neurotransmitter transportersTransmembrane helicesTransmembrane segmentsAquifex aeolicusUptake of neurotransmittersSubstrate bindingNeurotransmitter transportersMain-chain atomsMembrane bilayerDependent transportersElectrochemical gradientIon binding siteTransportersHelix dipole