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

SLC6A2 (P23975) - Overview - Molecular Target Synopsis

Protein


SLC6A2, Sodium-dependent noradrenaline transporter
UniProt P23975

Also Known as SC6A2_HUMAN, SLC6A2, NAT1, NET1, SLC6A5

Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals. Interacts with PRKCABP.

Isoforms / Transcripts (Protein Coding)


Drugs


SLC6A2 is targeted by Approved Drugs Amoxapine, Protriptyline, Dextroamphetamine Sulfate, Guanethidine, Desipramine, Sibutramine, Amphetamine, Venlafaxine, Desvenlafaxine Fumarate, Doxepin, Milnacipran, Dextroamphetamine, Trimipramine, Levomilnacipran, Bupropion, Bethanidine, Tapentadol, Sibutramine Hydrochloride, Maprotiline, IOBENGUANE I 131, Dextroamphetamine Saccharate, Guanadrel, Orphenadrine, Phendimetrazine Tartrate, Dextroamphetamine Adipate, Guanabenz, Desvenlafaxine, Amitriptyline, Atomoxetine, Dexmethylphenidate, Duloxetine. (see details)
Amoxapine
Protriptyline
Dextroamphetamine Sulfate
Guanethidine
Desipramine
Sibutramine
Amphetamine
Venlafaxine
Desvenlafaxine Fumarate
Doxepin
Milnacipran
Dextroamphetamine
Trimipramine
Levomilnacipran
Bupropion
Bethanidine
Tapentadol
Sibutramine Hydrochloride
Maprotiline
IOBENGUANE I 131
Dextroamphetamine Saccharate
Guanadrel
Orphenadrine
Phendimetrazine Tartrate
Dextroamphetamine Adipate
Guanabenz
Desvenlafaxine
Amitriptyline
Atomoxetine
Dexmethylphenidate
Duloxetine

Sub-cellular localization


UniProt: SLC6A2 is active in the following subcellular-locations: cell membrane.
GO terms: SLC6A2 is active in the following subcellular-locations: cell surface, integral component of plasma membrane, membrane, membrane raft, neuron projection, neuronal cell body membrane, plasma membrane, presynaptic membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project SLC6A2 has gain in 1 cell-lines, loss in 1 cell-lines and no signal in 1003 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: MOLT_4, TK_10, MCF7

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: MHH-NB-11, SK-N-FI, SK-N-SH

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, SK-N-SH_RA, NHLF

(see details)

3D Structures


At greater than 50% identity similarity to SLC6A2 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

SLC6A2 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


SLC6A2 has been screened with 4801 compounds (7577 bioactivities), 2071 compounds have bioactivities that show binding affinity of <= 500nM (2778 bioactivities). (see details)