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

SCN5A (Q14524) - Overview - Molecular Target Synopsis

Protein


SCN5A, Sodium channel protein type 5 subunit alpha
UniProt Q14524

Also Known as SCN5A_HUMAN, SCN5A

This protein mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient (PubMed:1309946, PubMed:21447824, PubMed:25370050, PubMed:23420830, PubMed:23085483, PubMed:26279430, PubMed:26392562, PubMed:26776555). It is a tetrodotoxin-resistant Na(+) channel isoform (PubMed:1309946). This channel is responsible for the initial upstroke of the action potential. Channel inactivation is regulated by intracellular calcium levels (PubMed:19074138). Interacts with the PDZ domain of the syntrophin SNTA1, SNTB1 and SNTB2 (By similarity). Interacts with NEDD4, NEDD4L, WWP2 and GPD1L (PubMed:15217910, PubMed:15548568, PubMed:19666841). Interacts with CALM (PubMed:21167176, PubMed:22705208, PubMed:25370050). Interacts with FGF13; the interaction is direct and FGF13 may regulate SNC5A density at membranes and function (PubMed:21817159, PubMed:22705208, PubMed:26392562). May also interact with FGF12 and FGF14 (PubMed:26392562). Interacts with the spider toxin Jingzhaotoxin-I (AC P83974, AC B1P1B7, AC B1P1B8) (PubMed:26721415). Interacts with ANK3 (PubMed:15579534).

Isoforms / Transcripts (Protein Coding)


Drugs


SCN5A is targeted by Approved Drugs Indecainide, Flecainide, Ranolazine, Quinidine Sulfate, Merethoxylline Procaine, Propafenone, Eslicarbazepine, Mexiletine, Rufinamide, Moricizine, Eslicarbazepine Acetate. (see details)
Indecainide
Flecainide
Ranolazine
Quinidine Sulfate
Merethoxylline Procaine
Propafenone
Eslicarbazepine
Mexiletine
Rufinamide
Moricizine
Eslicarbazepine Acetate

Sub-cellular localization


UniProt: SCN5A is active in the following subcellular-locations: cell membrane, cytoplasm, perinuclear region, sarcolemma, t-tubule.
GO terms: SCN5A is active in the following subcellular-locations: axon, caveola, cell surface, endoplasmic reticulum, integral component of membrane, intercalated disc, intracellular, lateral plasma membrane, perinuclear region of cytoplasm, plasma membrane, sarcolemma, T-tubule, voltage-gated sodium channel complex, Z disc.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project SCN5A has gain in 3 cell-lines, loss in 3 cell-lines and no signal in 999 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SW_620, MDA_MB_231, UO_31

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SW 620, HT-55, LS1034

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: HSMM, SK-N-SH, NHLF

(see details)

3D Structures


For SCN5A there are:
7 structures (11 chains) solved
0 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


SCN5A has been screened with 1414 compounds (1733 bioactivities), 96 compounds have bioactivities that show binding affinity of <= 500nM (100 bioactivities). (see details)