Details of the Target

General Information of Target

Target ID LDTP04603
Target Name Chromaffin granule amine transporter (SLC18A1)
Gene Name SLC18A1
Gene ID 6570
Synonyms
VAT1; VMAT1; Chromaffin granule amine transporter; Solute carrier family 18 member 1; Vesicular amine transporter 1; VAT1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MLRTILDAPQRLLKEGRASRQLVLVVVFVALLLDNMLFTVVVPIVPTFLYDMEFKEVNSS
LHLGHAGSSPHALASPAFSTIFSFFNNNTVAVEESVPSGIAWMNDTASTIPPPATEAISA
HKNNCLQGTGFLEEEITRVGVLFASKAVMQLLVNPFVGPLTNRIGYHIPMFAGFVIMFLS
TVMFAFSGTYTLLFVARTLQGIGSSFSSVAGLGMLASVYTDDHERGRAMGTALGGLALGL
LVGAPFGSVMYEFVGKSAPFLILAFLALLDGALQLCILQPSKVSPESAKGTPLFMLLKDP
YILVAAGSICFANMGVAILEPTLPIWMMQTMCSPKWQLGLAFLPASVSYLIGTNLFGVLA
NKMGRWLCSLIGMLVVGTSLLCVPLAHNIFGLIGPNAGLGLAIGMVDSSMMPIMGHLVDL
RHTSVYGSVYAIADVAFCMGFAIGPSTGGAIVKAIGFPWLMVITGVINIVYAPLCYYLRS
PPAKEEKLAILSQDCPMETRMYATQKPTKEFPLGEDSDEEPDHEE
Target Bioclass
Transporter and channel
Family
Major facilitator superfamily, Vesicular transporter family
Subcellular location
Cytoplasmic vesicle, secretory vesicle membrane; Endoplasmic reticulum membrane
Function
[Isoform 1]: 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 catecholamines and indolamines with higher affinity for serotonin. Regulates the transvesicular monoaminergic gradient that determines the quantal size. Mediates presynaptic monoaminergic vesicle transport in the amygdala and prefrontal brain regions related with emotion processing in response to environmental stimuli.; [Isoform 2]: Unable to uptake serotonin.
Uniprot ID
P54219
Ensemble ID
ENST00000265808.11
HGNC ID
HGNC:10934
ChEMBL ID
CHEMBL1838

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
MDST8 SNV: p.G16E DBIA    Probe Info 
MFE319 SNV: p.F246Y DBIA    Probe Info 
NCIH1993 Insertion: p.A114PfsTer38 .
NCIH2170 SNV: p.R17I DBIA    Probe Info 
SKOV3 SNV: p.T39A DBIA    Probe Info 
U87MG SNV: p.M1? DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FBPP2
 Probe Info  		24.32  LDD0318  [1]
DBIA
 Probe Info  		C324(1.11); C50(1.87)  LDD3311  [2]
NAIA_5
 Probe Info  		N.A.  LDD2224  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 22RV1 C50(1.65)  LDD2243  [2]
 LDCM0023  KB03 22RV1 C50(2.17)  LDD2660  [2]
 LDCM0024  KB05 G361 C324(1.11); C50(1.87)  LDD3311  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Inactive pancreatic lipase-related protein 1 (PNLIPRP1) Lipase family P54315
Maltase-glucoamylase (MGAM) Glycosyl hydrolase 31 family O43451
Sialidase-1 (NEU1) Glycosyl hydrolase 33 family Q99519
Lysoplasmalogenase TMEM86A (TMEM86A) TMEM86 family Q8N2M4
GTPase IMAP family member 1 (GIMAP1) AIG1/Toc34/Toc159-like paraseptin GTPase family Q8WWP7
Transmembrane reductase CYB561D2 (CYB561D2) . O14569
Transporter and channel
Click To Hide/Show 24 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Sodium-coupled neutral amino acid transporter 7 (SLC38A7) Amino acid/polyamine transporter 2 family Q9NVC3
Proton-coupled zinc antiporter SLC30A2 (SLC30A2) Cation diffusion facilitator (CDF) transporter (TC 2.A.4) family Q9BRI3
Proton-coupled zinc antiporter SLC30A8 (SLC30A8) Cation diffusion facilitator (CDF) transporter (TC 2.A.4) family Q8IWU4
Gap junction beta-2 protein (GJB2) Connexin family P29033
Protein cornichon homolog 1 (CNIH1) Cornichon family O95406
Major facilitator superfamily domain-containing protein 6 (MFSD6) MFSD6 family Q6ZSS7
Lens fiber major intrinsic protein (MIP) MIP/aquaporin (TC 1.A.8) family P30301
B-lymphocyte antigen CD20 (MS4A1) MS4A family P11836
Membrane-spanning 4-domains subfamily A member 13 (MS4A13) MS4A family Q5J8X5
Nucleotide sugar transporter SLC35B4 (SLC35B4) Nucleotide-sugar transporter family Q969S0
Transferrin receptor protein 1 (TFRC) Peptidase M28 family P02786
Peroxisomal membrane protein PEX16 (PEX16) Peroxin-16 family Q9Y5Y5
Peripheral myelin protein 22 (PMP22) PMP-22/EMP/MP20 family Q01453
Small integral membrane protein 1 (SMIM1) SMIM1 family B2RUZ4
Transmembrane protein 14A (TMEM14A) TMEM14 family Q9Y6G1
Transmembrane protein 14B (TMEM14B) TMEM14 family Q9NUH8
Solute carrier family 35 member G1 (SLC35G1) TMEM20 family Q2M3R5
Transmembrane protein 218 (TMEM218) TMEM218 family A2RU14
Zinc transporter ZIP2 (SLC39A2) ZIP transporter (TC 2.A.5) family Q9NP94
Phospholipid transfer protein C2CD2L (C2CD2L) . O14523
Proteolipid protein 2 (PLP2) . Q04941
Transmembrane protein 203 (TMEM203) . Q969S6
Transmembrane protein 60 (TMEM60) . Q9H2L4
Transmembrane protein 65 (TMEM65) . Q6PI78
GPCR
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
G-protein coupled receptor 151 (GPR151) G-protein coupled receptor 1 family Q8TDV0
Cytokine and receptor
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
C-C motif chemokine 4 (CCL4) Intercrine beta (chemokine CC) family P13236
C-C motif chemokine 4-like (CCL4L1; CCL4L2) Intercrine beta (chemokine CC) family Q8NHW4
Other
Click To Hide/Show 14 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Apolipoprotein L2 (APOL2) Apolipoprotein L family Q9BQE5
Protein FAM3C (FAM3C) FAM3 family Q92520
MAL-like protein (MALL) MAL family Q13021
Nurim (NRM) Nurim family Q8IXM6
ORM1-like protein 1 (ORMDL1) ORM family Q9P0S3
Protein reprimo (RPRM) Reprimo family Q9NS64
Single-pass membrane and coiled-coil domain-containing protein 4 (SMCO4) SMCO4 family Q9NRQ5
Vesicle-associated membrane protein 5 (VAMP5) Synaptobrevin family O95183
Syntaxin-8 (STX8) Syntaxin family Q9UNK0
Transmembrane protein 120B (TMEM120B) TMEM120 family A0PK00
Protein YIPF4 (YIPF4) YIP1 family Q9BSR8
Protein YIPF6 (YIPF6) YIP1 family Q96EC8
Olfactomedin-4 (OLFM4) . Q6UX06
Transmembrane protein 42 (TMEM42) . Q69YG0

The Drug(s) Related To This Target

Approved
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Metamfetamine Small molecular drug DB01577
Norepinephrine Small molecular drug DB00368
Reserpine Small molecular drug DB00206
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ephedra Sinica Root Small molecular drug DB01363
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Mmda Small molecular drug DB01442

References

1 Tranylcypromine specificity for monoamine oxidase is limited by promiscuous protein labelling and lysosomal trapping. RSC Chem Biol. 2020 Aug 12;1(4):209-213. doi: 10.1039/d0cb00048e. eCollection 2020 Oct 1.
Mass spectrometry data entry: PXD018580
2 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
3 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264