Target intelligence / Profile preview

Cation channel sperm-associated protein 2 (CATSPER2)

Target
CATSPER2
Molecular classification
Ion channel, Voltage-gated calcium channel (sperm-specific)
01

Overview

Cation channel sperm-associated protein 2 (CATSPER2) is a pore-forming subunit of the CatSper calcium channel, a sperm-specific voltage-gated ion channel essential for the calcium influx required for sperm hyperactivation, chemotaxis, and successful fertilization. CATSPER2 localizes to the principal piece of the sperm flagellum and forms a critical component of the heteromeric CatSper channel complex composed of four pore-forming subunits (CatSper1–4) and several auxiliary proteins. Disruption, mutation, or deletion of CATSPER2 leads to abolition of calcium influx through CatSper, failure of sperm hyperactivation, and male infertility, and is also implicated in human deafness-infertility syndrome. The channel is expressed only in spermatozoa and testis, and its activity is regulated by pH, intracellular signaling events, and exogenous factors such as progesterone and prostaglandins in humans. Although there are no approved drugs currently targeting CATSPER2, several small molecules and metal ions can block its activity in experimental studies.

Other names
CatSper2CATSPER2Cation channel sperm associated 2Sperm ion channel
02

Mechanism of action

Channel block (by certain small molecules/metals, as above)

03

Biological functions

Sperm motility regulationCalcium influx in sperm flagellumSperm hyperactivationFertilizationSperm chemotaxisAcrosome reaction
04

Disease associations

Male infertilityDeafness-infertility syndrome
05

Safety considerations

High specificity to spermatozoa may minimize off-target effects, but targeting may affect male fertility and potentially sensory functions (as in deafness-infertility syndrome)
06

Interacting drugs

Cadmium (inhibitor, experimental)

4 more in the full profile.

07

Biomarkers

Loss or mutation of CATSPER2 (for male infertility and deafness-infertility syndrome)

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