Sodium-dependent serotonin transporter
Also known as: HTT, SERT, SLC6A4
Function
Serotonin transporter that cotransports serotonin with one Na(+) ion in exchange for one K(+) ion and possibly one proton in an overall electroneutral transport cycle. Transports serotonin across the plasma membrane from the extracellular compartment to the cytosol thus limiting serotonin intercellular signaling. Essential for serotonin homeostasis in the central nervous system. In the developing somatosensory cortex, acts in glutamatergic neurons to control serotonin uptake and its trophic functions accounting for proper spatial organization of cortical neurons and elaboration of sensory circuits. In the mature cortex, acts primarily in brainstem raphe neurons to mediate serotonin uptake from the synaptic cleft back into the pre-synaptic terminal thus terminating serotonin signaling at the synapse (By similarity). Modulates mucosal serotonin levels in the gastrointestinal tract through uptake and clearance of serotonin in enterocytes. Required for enteric neurogenesis and gastrointestinal reflexes (By similarity). Regulates blood serotonin levels by ensuring rapid high affinity uptake of serotonin from plasma to platelets, where it is further stored in dense granules via vesicular monoamine transporters and then released upon stimulation. Mechanistically, the transport cycle starts with an outward-open conformation having Na1(+) and Cl(-) sites occupied. The binding of a second extracellular Na2(+) ion and serotonin substrate leads to structural changes to outward-occluded to inward-occluded to inward-open, where the Na2(+) ion and serotonin are released into the cytosol. Binding of intracellular K(+) ion induces conformational transitions to inward-occluded to outward-open and completes the cycle by releasing K(+) possibly together with a proton bound to Asp-98 into the extracellular compartment. Na1(+) and Cl(-) ions remain bound throughout the transport cycle. Additionally, displays serotonin-induced channel-like conductance for monovalent cations, mainly Na(+) ions. The channel activity is uncoupled from the transport cycle and may contribute to the membrane resting potential or excitability (By similarity).
Classification
- Family (Pfam)
- PF03491 5HT_transport_N, PF00209 SNF
- InterPro
- Na/ntran_symport, Na/ntran_symport_serotonin_N, SNS_sf
- Functional cluster
- Membrane Transporters & GPCRs
Experimental structures · PDB · 29
- 5I6X X-ray 3.14A
- 5I6Z X-ray 4.53A
- 5I71 X-ray 3.15A
- 5I73 X-ray 3.24A
- 5I74 X-ray 3.40A
- 5I75 X-ray 3.49A
- 6AWN X-ray 3.62A
- 6AWO X-ray 3.53A
- 6AWP X-ray 3.80A
- 6AWQ X-ray 4.05A
- 6DZV EM 4.20A
- 6DZW EM 4.30A
- … and 17 more
A predicted model is available from AlphaFold.
Gene Ontology · 54
- GO:0012505 endomembrane system
- GO:0010008 endosome membrane
- GO:0005925 focal adhesion
- GO:0005794 Golgi apparatus
- GO:0045121 membrane raft
- GO:0043005 neuron projection
- GO:0005886 plasma membrane
- GO:0045211 postsynaptic membrane
- GO:0042734 presynaptic membrane
- GO:0099154 serotonergic synapse
- GO:0045202 synapse
- GO:0051015 actin filament binding
- GO:0015297 antiporter activity
- GO:0019811 cocaine binding
- GO:0042802 identical protein binding
- GO:0005178 integrin binding
- GO:0008504 monoamine transmembrane transporter activity
- GO:0005261 monoatomic cation channel activity
- GO:0005326 neurotransmitter transmembrane transporter activity
- GO:0050998 nitric-oxide synthase binding
- GO:0051378 serotonin binding
- GO:0005335 serotonin:sodium:chloride symporter activity
- GO:0031402 sodium ion binding
- GO:0017075 syntaxin-1 binding
- GO:0006865 amino acid transport
- GO:0048148 behavioral response to cocaine
- GO:0048854 brain morphogenesis
- GO:0071321 cellular response to cGMP
- GO:0071300 cellular response to retinoic acid
- GO:0007623 circadian rhythm
- GO:1990708 conditioned place preference
- GO:0048484 enteric nervous system development
- GO:0060179 male mating behavior
- GO:0051899 membrane depolarization
- GO:0007613 memory
- GO:0015844 monoamine transport
- GO:0021941 negative regulation of cerebellar granule cell precursor proliferation
- GO:0045665 negative regulation of neuron differentiation
- GO:0046621 negative regulation of organ growth
- GO:0032227 negative regulation of synaptic transmission, dopaminergic
- GO:0006836 neurotransmitter transport
- GO:0070527 platelet aggregation
- GO:0045787 positive regulation of cell cycle
- GO:0010628 positive regulation of gene expression
- GO:0014064 positive regulation of serotonin secretion
- GO:0090067 regulation of thalamus size
- GO:0032355 response to estradiol
- GO:0001666 response to hypoxia
- GO:0007584 response to nutrient
- GO:0009636 response to toxic substance
- GO:0009410 response to xenobiotic stimulus
- GO:0051610 serotonin uptake
- GO:0035725 sodium ion transmembrane transport
- GO:0042310 vasoconstriction
Disease associations
- alcohol dependence MONDO:0007079
- obsessive-compulsive disorder MONDO:0008114
- anxiety MONDO:0011918
Drugs targeting this protein · 45
- AMOXAPINE inhibitor
- DESVENLAFAXINE inhibitor
- ESCITALOPRAM OXALATE inhibitor
- DULOXETINE HYDROCHLORIDE inhibitor
- PROTRIPTYLINE HYDROCHLORIDE inhibitor
- NEFAZODONE HYDROCHLORIDE inhibitor
- CHLORPHENTERMINE HYDROCHLORIDE substrate
- PAROXETINE MESYLATE inhibitor
- CLOMIPRAMINE HYDROCHLORIDE inhibitor
- CITALOPRAM HYDROBROMIDE inhibitor
- TRAZODONE HYDROCHLORIDE inhibitor
- METHAMPHETAMINE HYDROCHLORIDE inhibitor
- AMITRIPTYLINE HYDROCHLORIDE inhibitor
- VENLAFAXINE HYDROCHLORIDE inhibitor
- FLUOXETINE HYDROCHLORIDE inhibitor
- NORTRIPTYLINE HYDROCHLORIDE inhibitor
- DESVENLAFAXINE SUCCINATE inhibitor
- NOMIFENSINE MALEATE inhibitor
- FLUVOXAMINE MALEATE inhibitor
- DOTHIEPIN inhibitor
- VILAZODONE HYDROCHLORIDE inhibitor
- GSK163090 antagonist
- IMIPRAMINE HYDROCHLORIDE inhibitor
- SERTRALINE HYDROCHLORIDE inhibitor
- FAXELADOL inhibitor
- TEDATIOXETINE inhibitor
- LEVOMILNACIPRAN HYDROCHLORIDE inhibitor
- VORTIOXETINE HYDROBROMIDE inhibitor
- DAPOXETINE inhibitor
- LIAFENSINE inhibitor
- INDALPINE inhibitor
- DASOTRALINE inhibitor
- CENTANAFADINE inhibitor
- LUMATEPERONE inhibitor
- TESOFENSINE inhibitor
- SIBUTRAMINE HYDROCHLORIDE inhibitor
- IMIPRAMINE PAMOATE inhibitor
- DESVENLAFAXINE FUMARATE inhibitor
- MILNACIPRAN HYDROCHLORIDE inhibitor
- NS-2359 inhibitor
- MIDOMAFETAMINE releasing agent
- BICIFADINE inhibitor
- AMITIFADINE inhibitor
- PAROXETINE HYDROCHLORIDE inhibitor
- MAZINDOL inhibitor
Related proteins · sequence + function similarity
- Sodium-dependent serotonin transporter 1.00
- Sodium-dependent serotonin transporter 0.99
- Sodium-dependent serotonin transporter 0.99
- Sodium-dependent serotonin transporter 0.99
- Sodium-dependent serotonin transporter 0.99
- Sodium-dependent noradrenaline transporter 0.96
- Sodium- and chloride-dependent GABA transporter 2 0.96
- Sodium- and chloride-dependent GABA transporter 2 0.96
- Sodium-dependent noradrenaline transporter 0.96
- Sodium- and chloride-dependent GABA transporter 1 0.96
- Sodium- and chloride-dependent GABA transporter 1 0.96
- Sodium-dependent noradrenaline transporter 0.96
Co-cited proteins · studied together in the literature
- Sodium-dependent serotonin transporter 4 shared papers
- Sodium-dependent serotonin transporter 3 shared papers
- Sodium-dependent serotonin transporter 1 shared papers
- Vimentin 2 shared papers
- Secretory carrier-associated membrane protein 2 1 shared papers
- Integrin beta-3 1 shared papers
- Transforming growth factor beta-1-induced transcript 1 protein 1 shared papers
- Integrin beta-3 1 shared papers
Literature · 30 cited papers
- Illumination of serotonin transporter mechanism and role of the allosteric site. Sci. Adv. · 2021
- PMID 31201246 J. Biol. Chem. · 2019
- Retraction: The Cellular Distribution of Serotonin Transporter Is Impeded on Serotonin-Altered Vimentin Network. PLoS ONE · 2019
- Electrogenic Binding of Intracellular Cations Defines a Kinetic Decision Point in the Transport Cycle of the Human Serotonin Transporter. J. Biol. Chem. · 2016
- Serotonin transporter variant drives preventable gastrointestinal abnormalities in development and function. J. Clin. Invest. · 2016
- X-ray structures and mechanism of the human serotonin transporter. Nature · 2016
- Tyrosine phosphorylation of the human serotonin transporter: a role in the transporter stability and function. Mol. Pharmacol. · 2012
- A conserved asparagine residue in transmembrane segment 1 (TM1) of serotonin transporter dictates chloride-coupled neurotransmitter transport. J. Biol. Chem. · 2011
- The cellular distribution of serotonin transporter is impeded on serotonin-altered vimentin network. PLoS ONE · 2009
- Enhanced activity of human serotonin transporter variants associated with autism. Philos. Trans. R. Soc. Lond., B, Biol. Sci. · 2009
- Interactions between integrin alphaIIbbeta3 and the serotonin transporter regulate serotonin transport and platelet aggregation in mice and humans. J. Clin. Invest. · 2008
- Serotonin transamidates Rab4 and facilitates its binding to the C terminus of serotonin transporter. J. Biol. Chem. · 2008
- … and 18 more in the literature graph