Target intelligence / Profile preview

Sodium-calcium exchanger 1 (NCX1)

Target
NCX1
Molecular classification
Transporter, Ion exchanger
01

Overview

NCX1 is a ubiquitously expressed membrane protein that plays a critical role in cellular calcium homeostasis. It mediates the electrogenic exchange of one Ca(2+) ion for three to four Na+ ions across the plasma membrane, typically exporting Ca(2+) from the cytoplasm in exchange for Na+. This process is essential for cardiac muscle relaxation, control of neurosecretion, activity of photoreceptor cells, and maintenance of low cytoplasmic Ca(2+) concentration in various cell types. Dysregulation or abnormal activation can contribute to pathologies such as delayed afterdepolarization leading to arrhythmias in heart tissue due to aberrant depolarizing currents when excess intracellular calcium activates NCX-mediated sodium influx.

Other names
SLC8A1
02

Mechanism of action

Inhibition of Na+/Ca2+ exchange

03

Biological functions

Calcium homeostasisCardiac muscle relaxationNeurosecretion controlPhototransductionIon transport
04

Disease associations

ArrhythmiasIschemia/reperfusion injuryNeurodegenerative diseases
05

Safety considerations

Potential for pro-arrhythmic effectsOff-target effects of non-selective inhibitors
06

Interacting drugs

KB-R7943 mesylate

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