Open-channel block of human TRPV6 by polyamine spermine - PubMed
5 hours ago
- #ion channel block
- #TRPV6
- #spermine
- Polyamines modulate TRP channels and are involved in pain, inflammation, and cancer.
- Spermine blocks human TRPV6 channels in a voltage-dependent manner.
- Cryo-EM shows spermine binds in the open pore, spanning the selectivity filter and central cavity.
- Mutagenesis and MD simulations identify the selectivity filter as the main binding site and suggest a stepwise blocking mechanism.
- The study provides insights into TRPV6 regulation and potential therapeutic targeting.