Target intelligence / Profile preview

Transient receptor potential melastatin-related channel (TRPMPZQ) (TRPMPZQ)

Target
TRPMPZQ
Molecular classification
Ion channel, Transient receptor potential channel
01

Overview

The parasite calcium ion channels, specifically the tegumental calcium handling mechanisms, are essential for the survival and physiological function of flatworms such as Schistosoma. The primary molecular component of this system is the Transient receptor potential melastatin-related channel (TRPMPZQ), which regulates the flow of calcium ions across the parasite's tegument and into its muscle cells (Park et al., 2019). This channel is the definitive target of praziquantel, the primary drug used to treat schistosomiasis and other trematode infections. Activation of TRPMPZQ by praziquantel triggers a massive, rapid influx of calcium, leading to immediate muscle contraction and severe damage to the parasite's tegumental surface (Marchant et al., 2020). This disruption not only paralyzes the worm but also exposes its internal antigens to the host's immune system, facilitating its clearance from the body (Greenberg, 2005). Understanding the specific structure and function of these channels is critical for developing new anthelmintics that can overcome emerging resistance and target juvenile stages of the parasite (Le Clec'h et al., 2021).

Other names
SmTRPMPZQPraziquantel-activated TRP channelSchistosoma mansoni TRP channelVoltage-gated calcium channel beta subunitTegumental calcium channel
02

Mechanism of action

Activation of the TRPMPZQ channel causes a rapid influx of calcium ions, leading to muscle paralysis and tegumental damage in the parasite (Park et al., 2019).

03

Biological functions

Signal transductionMuscle contractionIon transportTegumental maintenance
04

Disease associations

InfectionSchistosomiasisHelminthiasis
05

Safety considerations

Emerging drug resistanceInefficacy against juvenile parasitesHost immune-mediated reactions to dying parasites
06

Interacting drugs

Praziquantel
07

Biomarkers

Egg reduction rate (ERR)Circulating anodic antigen (CAA)Circulating cathodic antigen (CCA)

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