Target intelligence / Profile preview

Polycystin 2-like 1 transient receptor potential cation channel (PKD2L1)

Target
PKD2L1
Molecular classification
Ion channel, Transient receptor potential (TRP) channel, Polycystin family
01

Overview

Polycystin 2-like 1 transient receptor potential cation channel (PKD2L1), also known as TRPP3, is a calcium-permeable non-selective cation channel belonging to the polycystin family of TRP channels (UniProt: Q9P0L9). It is primarily recognized for its role as a candidate sour taste receptor, where it forms a heteromeric complex with PKD1L3 in type III taste receptor cells to detect acidic stimuli (PMID: 16914744). Beyond the gustatory system, PKD2L1 is expressed in cerebrospinal fluid-contacting neurons (CSF-cNs) within the spinal cord, where it functions as a pH sensor and mechanoreceptor essential for maintaining spine curvature and regulating neuronal excitability (PMID: 30224625). It also plays a role in the cardiovascular system, contributing to cardiac sympathetic regulation and pacemaking, and has been implicated in conditions such as cardiac hypertrophy and seizure susceptibility (PMID: 22462525; PMID: 30224625). While recent evidence suggests OTOP1 is the primary proton channel for sour taste, PKD2L1 remains a critical component of sensory signaling pathways and a target for pharmacological research (PMID: 31533078). Modulators of PKD2L1 include the agonist calmidazolium and inhibitors such as capsaicin and QX-314, which are used to study its channel properties and therapeutic potential in taste and neurological disorders (PMID: 22462525; PMID: 35666144).

Other names
TRPP3Polycystin-LPolycystin-L1PCLPKDLTransient receptor potential cation channel subfamily P member 3
02

Mechanism of action

Modulation of non-selective cation channel activity, including activation by calmodulin antagonists and inhibition by pore-blocking agents or state-stabilizing molecules.

03

Biological functions

Sour taste perceptionpH sensingCalcium signalingMechanosensationRegulation of neuronal excitabilityMaintenance of spine curvatureCardiac sympathetic regulation
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Disease associations

Taste disorderCardiac hypertrophyPolycystic kidney diseaseSeizureAutism
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Safety considerations

Potential for cardiac arrhythmiaRisk of seizuresDisruption of cerebrospinal fluid pH sensingAlteration of spinal curvature
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Interacting drugs

Calmidazolium

3 more in the full profile.

07

Biomarkers

PKD2L1 mRNA expressionPKD2L1 protein expression

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