General Information of Target

Target ID LDTP05469
Target Name Synaptic vesicular amine transporter (SLC18A2)
Gene Name SLC18A2
Gene ID 6571
Synonyms
SVMT; VMAT2; Synaptic vesicular amine transporter; Monoamine transporter; Solute carrier family 18 member 2; Vesicular amine transporter 2; VAT2
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MALSELALVRWLQESRRSRKLILFIVFLALLLDNMLLTVVVPIIPSYLYSIKHEKNATEI
QTARPVHTASISDSFQSIFSYYDNSTMVTGNATRDLTLHQTATQHMVTNASAVPSDCPSE
DKDLLNENVQVGLLFASKATVQLITNPFIGLLTNRIGYPIPIFAGFCIMFVSTIMFAFSS
SYAFLLIARSLQGIGSSCSSVAGMGMLASVYTDDEERGNVMGIALGGLAMGVLVGPPFGS
VLYEFVGKTAPFLVLAALVLLDGAIQLFVLQPSRVQPESQKGTPLTTLLKDPYILIAAGS
ICFANMGIAMLEPALPIWMMETMCSRKWQLGVAFLPASISYLIGTNIFGILAHKMGRWLC
ALLGMIIVGVSILCIPFAKNIYGLIAPNFGVGFAIGMVDSSMMPIMGYLVDLRHVSVYGS
VYAIADVAFCMGYAIGPSAGGAIAKAIGFPWLMTIIGIIDILFAPLCFFLRSPPAKEEKM
AILMDHNCPIKTKMYTQNNIQSYPIGEDEESESD
Target Type
Successful
Target Bioclass
Transporter and channel
Family
Major facilitator superfamily, Vesicular transporter family
Subcellular location
Cytoplasmic vesicle, secretory vesicle, synaptic vesicle membrane
Function
Electrogenic antiporter that exchanges one cationic monoamine with two intravesicular protons across the membrane of secretory and synaptic vesicles. Uses the electrochemical proton gradient established by the V-type proton-pump ATPase to accumulate high concentrations of monoamines inside the vesicles prior to their release via exocytosis. Transports a variety of catecholamines such as dopamine, adrenaline and noradrenaline, histamine, and indolamines such as serotonin. Regulates the transvesicular monoaminergic gradient that determines the quantal size. Mediates somatodendritic dopamine release in hippocampal neurons, likely as part of a regulated secretory pathway that integrates retrograde synaptic signals. Acts as a primary transporter for striatal dopamine loading ensuring impulse-dependent release of dopamine at the synaptic cleft. Responsible for histamine and serotonin storage and subsequent corelease from mast cell granules.
TTD ID
T48873
Uniprot ID
Q05940
DrugMap ID
TTNZRI3
Ensemble ID
ENST00000644641.2
HGNC ID
HGNC:10935
ChEMBL ID
CHEMBL1893

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HCC1806 Substitution: p.T68M .
HUCCT1 Deletion: p.L143PfsTer68 .
JURKAT SNV: p.R10H; p.P404H .
MDAMB231 SNV: p.M310T .
MFE319 Deletion: p.F238SfsTer48 .
NCIN87 Substitution: p.T68M .
SNU1 SNV: p.M1? .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C488(2.06)  LDD3340  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 Kelly C488(3.42)  LDD2417  [1]
 LDCM0023  KB03 Kelly C488(10.24)  LDD2834  [1]
 LDCM0024  KB05 NB1 C488(2.06)  LDD3340  [1]

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840