General Information of Target

Target ID LDTP01303
Target Name Solute carrier family 22 member 3 (SLC22A3)
Gene Name SLC22A3
Gene ID 6581
Synonyms
EMTH; OCT3; Solute carrier family 22 member 3; Extraneuronal monoamine transporter; EMT; Organic cation transporter 3; OCT3
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MPSFDEALQRVGEFGRFQRRVFLLLCLTGVTFAFLFVGVVFLGTQPDHYWCRGPSAAALA
ERCGWSPEEEWNRTAPASRGPEPPERRGRCQRYLLEAANDSASATSALSCADPLAAFPNR
SAPLVPCRGGWRYAQAHSTIVSEFDLVCVNAWMLDLTQAILNLGFLTGAFTLGYAADRYG
RIVIYLLSCLGVGVTGVVVAFAPNFPVFVIFRFLQGVFGKGTWMTCYVIVTEIVGSKQRR
IVGIVIQMFFTLGIIILPGIAYFIPNWQGIQLAITLPSFLFLLYYWVVPESPRWLITRKK
GDKALQILRRIAKCNGKYLSSNYSEITVTDEEVSNPSFLDLVRTPQMRKCTLILMFAWFT
SAVVYQGLVMRLGIIGGNLYIDFFISGVVELPGALLILLTIERLGRRLPFAASNIVAGVA
CLVTAFLPEGIAWLRTTVATLGRLGITMAFEIVYLVNSELYPTTLRNFGVSLCSGLCDFG
GIIAPFLLFRLAAVWLELPLIIFGILASICGGLVMLLPETKGIALPETVDDVEKLGSPHS
CKCGRNKKTPVSRSHL
Target Type
Literature-reported
Target Bioclass
Transporter and channel
Family
Major facilitator (TC 2.A.1) superfamily, Organic cation transporter (TC 2.A.1.19) family
Subcellular location
Cell membrane
Function
Electrogenic voltage-dependent transporter that mediates the transport of a variety of organic cations such as endogenous bioactive amines, cationic drugs and xenobiotics. Cation cellular uptake or release is driven by the electrochemical potential, i.e. membrane potential and concentration gradient. Functions as a Na(+)- and Cl(-)-independent, bidirectional uniporter. Implicated in monoamine neurotransmitters uptake such as dopamine, adrenaline/epinephrine, noradrenaline/norepinephrine, histamine, serotonin and tyramine, thereby supporting a role in homeostatic regulation of aminergic neurotransmission in the brain. Transports dopaminergic neuromodulators cyclo(his-pro) and salsolinol with low efficiency. May be involved in the uptake and disposition of cationic compounds by renal clearance from the blood flow. May contribute to regulate the transport of cationic compounds in testis across the blood-testis-barrier (Probable). Mediates the transport of polyamine spermidine and putrescine. Mediates the bidirectional transport of polyamine agmatine. Also transports guanidine. May also mediate intracellular transport of organic cations, thereby playing a role in amine metabolism and intracellular signaling.
TTD ID
T55948
Uniprot ID
O75751
DrugMap ID
TTG2UMS
Ensemble ID
ENST00000275300.3
HGNC ID
HGNC:10967
ChEMBL ID
CHEMBL2073673

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IPM
 Probe Info 
C127(1.31)  LDD1701  [1]
DBIA
 Probe Info 
C127(0.34); C541(0.29)  LDD2236  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C127(1.19)  LDD1702  [1]
 LDCM0023  KB03 MDA-MB-231 C127(1.31)  LDD1701  [1]

References

1 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
2 Global profiling of phosphorylation-dependent changes in cysteine reactivity. Nat Methods. 2022 Mar;19(3):341-352. doi: 10.1038/s41592-022-01398-2. Epub 2022 Feb 28.
Mass spectrometry data entry: PXD026730