Target intelligence / Profile preview

Glutamate-gated chloride channel subunit alpha (CrGluCl-A)

Target
CrGluCl-A
Molecular classification
Ion channel, Cys-loop ligand-gated ion channel, Receptor, Glutamate-gated chloride channel
01

Overview

CrGluCl-A is a subunit of the glutamate-gated chloride channel (GluCl) found in the parasitic sea louse Caligus rogercresseyi, which is a significant pest in salmon aquaculture [1, 5]. As a member of the Cys-loop ligand-gated ion channel superfamily, it mediates inhibitory neurotransmission by allowing chloride ions to flow into neurons upon activation by the neurotransmitter glutamate [1, 2]. This receptor is a primary molecular target for avermectin-class antiparasitic drugs, such as ivermectin and emamectin, which act as allosteric activators to induce permanent channel opening and subsequent parasite paralysis [1, 4]. Research indicates that CrGluCl-A can form homomeric channels or heteromeric complexes with other subunits like CrGluCl-B, the latter of which can confer resistance to ivermectin [1, 5]. Understanding the functional properties and subunit composition of these channels is critical for managing drug resistance and developing novel treatment strategies in aquaculture settings [1, 5].

Other names
CrGluCl alphaCrGluClαGlutamate-gated chloride channel subunit ACaligus rogercresseyi GluCl-A
02

Mechanism of action

Allosteric activation of the chloride channel leading to hyperpolarization and paralysis.

03

Biological functions

Signal transductionInhibitory neurotransmissionChloride transport
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Disease associations

InfectionEctoparasitosis
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Safety considerations

Development of drug resistanceCross-resistance among avermectins
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Interacting drugs

Ivermectin

3 more in the full profile.

07

Biomarkers

CrGluCl-B expression levelGln15' mutation in M2 domain

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