2016
Control of serotonin transporter phosphorylation by conformational state
Zhang YW, Turk BE, Rudnick G. Control of serotonin transporter phosphorylation by conformational state. Proceedings Of The National Academy Of Sciences Of The United States Of America 2016, 113: e2776-e2783. PMID: 27140629, PMCID: PMC4878475, DOI: 10.1073/pnas.1603282113.Peer-Reviewed Original ResearchConceptsTransmembrane helix 5Cytoplasmic permeation pathwaysOutward open conformationIntact rat basophilic leukemia cellsCGMP-dependent phosphorylationInhibition of phosphorylationTM5 helicesTransporter phosphorylationSERT regulationOutward openingCysteine residuesHelix 5Open conformationCytoplasmic endHuman SERTPhosphorylationPermeation pathwayConformational statesHeLa cellsRat basophilic leukemia cellsBasophilic leukemia cellsSERT activityExocytotic releaseLeukemia cellsMutations
2012
The Mechanistic Basis for Noncompetitive Ibogaine Inhibition of Serotonin and Dopamine Transporters*
Bulling S, Schicker K, Zhang YW, Steinkellner T, Stockner T, Gruber CW, Boehm S, Freissmuth M, Rudnick G, Sitte HH, Sandtner W. The Mechanistic Basis for Noncompetitive Ibogaine Inhibition of Serotonin and Dopamine Transporters*. Journal Of Biological Chemistry 2012, 287: 18524-18534. PMID: 22451652, PMCID: PMC3365767, DOI: 10.1074/jbc.m112.343681.Peer-Reviewed Original ResearchConceptsSubstrate-induced currentsCell exteriorPermeation pathwayCytoplasmic permeation pathwaysSubstrate-binding site
2011
Cytoplasmic Permeation Pathway of Neurotransmitter Transporters
Rudnick G. Cytoplasmic Permeation Pathway of Neurotransmitter Transporters. Biochemistry 2011, 50: 7462-7475. PMID: 21774491, PMCID: PMC3164596, DOI: 10.1021/bi200926b.Peer-Reviewed Original ResearchConceptsCytoplasmic permeation pathwaysBacterial amino acid transporter LeuTNeurotransmitter transportersPermeation pathwayKingdoms of lifeMammalian serotonin transporterHigh-resolution crystal structuresFour-helix bundleRecent high-resolution crystal structureSubsequent crystal structureStructural repeatsLeuT structureProtein familyCommon structural featuresSolute transportersRelated proteinsLarge structural familyCytoplasmic oneConformational changesSubstrate siteFirst structureBiological membranesTransportersLeuTExtracellular pathways