Target intelligence / Profile preview

Volume-regulated anion channel subunit LRRC8E (LRRC8E)

Target
LRRC8E
Molecular classification
Ion channel, Volume-regulated anion channel (VRAC), Transmembrane protein
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Overview

Volume-regulated anion channel subunit LRRC8E (LRRC8E) is an integral membrane protein and one of five LRRC8 family members (LRRC8A-E) that assemble into heteromeric hexameric channels called VRAC. These channels are critical for maintaining cell homeostasis under hypotonic stress by mediating swelling-induced efflux of chloride ions and small organic solutes. Functional VRAC channels require LRRC8A and at least one other LRRC8 isoform—often including LRRC8E—to restore native currents. VRAC serves essential roles in regulating cell volume, cell proliferation, apoptosis, neurotransmitter (such as ATP and glutamate) release, and is involved in pathophysiological responses to chemotherapeutics and cell stress. LRRC8E contributes to the heterogeneity in channel selectivity and kinetic properties and participates in specialized functions such as cGAMP transport in immune signaling.

Other names
Leucine-rich repeat-containing protein 8ELeucine rich repeat containing 8 family member EFLJ23420
02

Mechanism of action

Facilitation of cell volume regulation and apoptosis via anion/solute efflux; modulation of cell response to platinum-based chemotherapeutics; participant in organic solute release affecting cellular signaling

03

Biological functions

Cell volume regulationAnion and osmolyte transportHomeostasis of membrane potentialRegulation of cell proliferationRegulation of apoptosisElectrical excitability of neuronsOrganic solute release (ATP, glutamate, cGAMP transport)
04

Disease associations

Cancer (role in apoptosis and cell proliferation)Neurological diseases (neuronal excitability, neurotransmitter release)Male infertility (linked to sperm development in mouse models)Chemotherapy response (cisplatin-induced cell death)
05

Safety considerations

Impairment in VRAC function may lead to defective cell volume regulationAltered apoptosis (potential cancer resistance/sensitivity)Neuronal dysfunctionInfertility
06

Interacting drugs

Cisplatin

2 more in the full profile.

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