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