Target intelligence / Profile preview

Polycystic kidney disease 2-like 1 protein (PKD2L1) (PKD2L1)

Target
PKD2L1
Molecular classification
Ion channel, Transient receptor potential channel, Polycystin family, TRPP subfamily
01

Overview

Polycystic kidney disease 2-like 1 protein (PKD2L1), also known as TRPP3, is a member of the polycystin family of transient receptor potential (TRP) ion channels [UniProt: P67564]. It functions as a non-selective cation channel, facilitating the transport of calcium, sodium, and potassium ions across the cell membrane [PubMed: 29899445]. PKD2L1 is prominently known for its role in sour taste perception, where it forms a functional heteromeric complex with PKD1L3 in Type III taste receptor cells to sense acidic stimuli [PubMed: 16929298]. Additionally, it is expressed in cerebrospinal fluid-contacting neurons (CSF-cNs) and primary cilia, where it acts as a chemo- or mechanosensor to monitor the local environment [PubMed: 28834701]. While PKD2L1 is not the primary gene associated with autosomal dominant polycystic kidney disease (ADPKD), its structural similarity to PKD2 and its role in calcium signaling make it a subject of interest in renal and cardiovascular research [PubMed: 21106692]. Currently, there are no FDA-approved drugs specifically targeting PKD2L1, but experimental modulators like amiloride and ruthenium red are used in research to study its channel properties [PubMed: 15331798].

Other names
TRPP3PKDLPolycystin-LPolycystin-2L1PKD2LTransient receptor potential cation channel subfamily P member 3
02

Mechanism of action

Inhibition of cation conductance through the channel pore, blocking the influx of calcium and sodium ions in response to acidic or mechanical stimuli.

03

Biological functions

Sour taste transductionCalcium-activated non-selective cation channel activitypH sensingCiliary signalingMechanotransduction
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Disease associations

Taste disordersPolycystic kidney diseaseCardiovascular diseaseNeurological disorders
05

Safety considerations

Dysgeusia (taste distortion)Potential systemic electrolyte imbalanceOff-target effects in the central nervous system
06

Interacting drugs

Amiloride (experimental)

3 more in the full profile.

07

Biomarkers

PKD2L1 protein expression in Type III taste cellsPKD2L1 mRNA levels in cerebrospinal fluid-contacting neurons

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