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Transient receptor potential cation channel subfamily C member 2 (TRPC2) (TRPC2)

Target
TRPC2
Molecular classification
Ion channel, Transient receptor potential (TRP) channel, TRPC (canonical) subfamily
01

Overview

Transient receptor potential channel 2 (TRP-2), also known as TRPC2, is a non-selective cation channel belonging to the canonical (TRPC) subfamily of the transient receptor potential (TRP) superfamily [1, 13]. While TRPC2 is a pseudogene in humans and Old World monkeys, it is a functional and essential channel in many other organisms, including rodents and parasitic nematodes [11, 16]. In rodents, it is primarily expressed in the vomeronasal organ and is crucial for pheromone-mediated social and sexual behaviors [17]. In filarial nematodes such as Brugia malayi, TRP-2 is expressed in the body wall muscle and has been identified as the direct molecular target of the anthelmintic drug diethylcarbamazine (DEC) [2, 4, 6]. DEC acts as an agonist of the TRP-2 channel, triggering a rapid influx of calcium ions that leads to muscle contraction and spastic paralysis of the parasite [8, 9]. This mechanism facilitates the clearance of microfilariae by the host's immune system, making TRP-2 a significant target for the treatment of lymphatic filariasis and loiasis [7, 10]. It is important to distinguish this ion channel from Tyrosinase-related protein 2 (also called TRP-2), which is an enzyme involved in melanin synthesis and a target in melanoma immunotherapy [14, 15].

Other names
TRP-2Bm-TRP-2Bma-trp-2Transient receptor potential channel 2TRPC2-like channelShort transient receptor potential channel 2
02

Mechanism of action

Agonist activation of the channel leading to rapid calcium influx and spastic paralysis in parasitic nematodes.

03

Biological functions

Calcium signalingMuscle contractionPheromone sensingSensory transductionGerm cell development
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Disease associations

Lymphatic filariasisLoiasis
05

Safety considerations

Mazzotti reactionEncephalopathy in high-load Loa loa infectionsSevere inflammatory response to dying parasites
06

Interacting drugs

Diethylcarbamazine

2 more in the full profile.

07

Biomarkers

Microfilarial densityMicrofilariae count in peripheral blood

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