Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

SLC6A3 (Q01959) - Overview - Molecular Target Synopsis

Protein


SLC6A3, Sodium-dependent dopamine transporter
UniProt Q01959

Also Known as SC6A3_HUMAN, SLC6A3, DAT1

Amine transporter. Terminates the action of dopamine by its high affinity sodium-dependent reuptake into presynaptic terminals. Homooligomer; disulfide-linked (Ref.14). Interacts with PRKCABP and TGFB1I1 (PubMed:11343649, PubMed:12177201). Interacts (via N-terminus) with SYNGR3 (via N-terminus). Interacts with SLC18A2. Interacts with TOR1A (ATP-bound); TOR1A regulates SLC6A3 subcellular location (By similarity). Interacts with alpha-synuclein/SNCA (PubMed:26442590).

Isoforms / Transcripts (Protein Coding)


Drugs


SLC6A3 is targeted by Approved Drugs Modafinil, Dextroamphetamine Sulfate, Armodafinil, Sibutramine, Droperidol, Phendimetrazine, Amphetamine, Mazindol, Dextroamphetamine, Diethylpropion, Phenmetrazine, Bupropion, Phenmetrazine Hydrochloride, Sibutramine Hydrochloride, Dextroamphetamine Saccharate, Dextroamphetamine Saccharate, Methamphetamine, Phendimetrazine Tartrate, Dextroamphetamine Adipate, Methylphenidate, Lisdexamfetamine, Dexmethylphenidate. (see details)
Modafinil
Dextroamphetamine Sulfate
Armodafinil
Sibutramine
Droperidol
Phendimetrazine
Amphetamine
Mazindol
Dextroamphetamine
Diethylpropion
Phenmetrazine
Bupropion
Phenmetrazine Hydrochloride
Sibutramine Hydrochloride
Dextroamphetamine Saccharate
Dextroamphetamine Saccharate
Methamphetamine
Phendimetrazine Tartrate
Dextroamphetamine Adipate
Methylphenidate
Lisdexamfetamine
Dexmethylphenidate

Sub-cellular localization


Gene Copy Number Variation


In COSMIC - Cell Lines Project SLC6A3 has gain in 30 cell-lines, loss in 0 cell-lines and no signal in 975 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: A498, SF_539, LOXIMVI

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: HCC1319, NCI-H209, DMS 53

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: SK-N-SH, NHLF, HSMM

(see details)

3D Structures


At greater than 50% identity similarity to SLC6A3 there are:
28 structures (28 chains) solved
28 are solved in complex with at least one small molecule ligand
24 are solved with an approved drug

SLC6A3 is solved in complex with the approved drug(s):

CLR/CHOLESTEROL (4M48_A, 4XNU_A, 4XNX_A, 4XP1_A, 4XP4_A, 4XP5_A, 4XP6_A, 4XP9_C, 4XPA_A, 4XPB_A, 4XPF_A, 4XPG_A, 4XPH_A, 4XPT_A, 5I6X_A, 5I71_A, 5I73_A, 5I74_A, 5I75_A, 6AWN_A, 6AWO_A, 6AWP_A, 6AWQ_A),
1WE/DEXTROAMPHETAMINE (4XP9_C),
FVX/FLUVOXAMINE (6AWP_A),
8PR/PAROXETINE (5I6X_A, 6AWN_A, 6DZW_A),
B40/METHAMPHETAMINE (4XP6_A),
21B/NORTRIPTYLINE (4M48_A),
ACA/AMINOCAPROIC ACID (5I73_A),
68P/ESCITALOPRAM (5I71_A, 5I73_A, 5I75_A),
LDP/DOPAMINE (4XP1_A),
SRE/SERTRALINE (6AWO_A, 6AWQ_A),
COC/COCAINE (4XP4_A, 4XPB_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


SLC6A3 has been screened with 5093 compounds (8357 bioactivities), 1635 compounds have bioactivities that show binding affinity of <= 500nM (2354 bioactivities). (see details)