Target intelligence / Profile preview

Ascaris suum nicotinic acetylcholine receptor subunit ACR-16 (Asu-ACR-16) (Asu-ACR-16)

Target
Asu-ACR-16
Molecular classification
Ion channel, Ligand-gated ion channel, Nicotinic acetylcholine receptor, Cys-loop receptor family
01

Overview

The Ascaris suum nicotinic acetylcholine receptor subunit ACR-16 (Asu-ACR-16) is a vital ligand-gated ion channel found in the neuromuscular system of the parasitic roundworm Ascaris suum (Abongwa et al., 2016; PubMed: 27103440). It belongs to the alpha-7-like class of nicotinic receptors and typically assembles into homomeric pentamers that function as excitatory cation channels (Williamson et al., 2009; PubMed: 19457115). In the parasite, Asu-ACR-16 is primarily located at the neuromuscular junction where it mediates fast synaptic transmission, a process essential for coordinated movement and muscle tone (Puttachary et al., 2013; PubMed: 23874366). This receptor is pharmacologically characterized as the N-type receptor due to its high sensitivity to nicotine, distinguishing it from the levamisole-sensitive L-type receptors (Baur et al., 2015; PubMed: 25637277). Asu-ACR-16 is a major target for anthelmintic therapy; for example, the drug derquantel acts as a potent antagonist at this site (Zamanian et al., 2011; PubMed: 21909104). By blocking the receptor, antagonists induce flaccid paralysis in the worm, facilitating its expulsion from the host's gastrointestinal tract. Conversely, agonists can cause spastic paralysis through overstimulation of the muscle cells. Research into Asu-ACR-16 is critical for addressing the growing challenge of anthelmintic resistance in veterinary and human medicine (Holden-Dye & Walker, 2014; WormBook).

Other names
ACR-16Alpha-7-like nicotinic acetylcholine receptorN-type nicotinic acetylcholine receptorAsu-ACR-16
02

Mechanism of action

Agonists (e.g., nicotine) induce persistent depolarization of muscle cells leading to spastic paralysis, while antagonists (e.g., derquantel) block cholinergic transmission leading to flaccid paralysis (Abongwa et al., 2016; Baur et al., 2015).

03

Biological functions

Neuromuscular transmissionSynaptic signalingMuscle contractionLocomotion
04

Disease associations

InfectionAscariasisHelminthiasis
05

Safety considerations

Potential cross-reactivity with host alpha-7 nicotinic acetylcholine receptorsDevelopment of anthelmintic resistance in parasite populationsLimited efficacy against non-motile life stages of the parasite
06

Interacting drugs

Nicotine

4 more in the full profile.

07

Biomarkers

Fecal egg count reduction test (FECRT)Parasite motility and migration assays (in vitro)Electrophysiological recording of muscle cell depolarization

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