Venom Peptides with Dual Modulatory Activity on the Voltage-Gated Sodium Channel Na_V1.1 Provide Novel Leads for Development of Antiepileptic Drugs.

ABSTRACT: Voltage-gated sodium (Na_V) channels play a fundamental role in normal neurological function, especially via the initiation and propagation of action potentials. The Na_V1.1 subtype is found in inhibitory interneurons of the brain and it is essential for maintaining a balance between excitation and inhibition in neuronal networks. Heterozygous loss-of-function mutations of SCN1A, the gene encoding Na_V1.1, underlie Dravet syndrome (DS), a severe pediatric epilepsy. We recently demonstrated that selective inhibition of Na_V1.1 inactivation prevents seizures and premature death in a mouse model of DS. Thus, selective modulators of Na_V1.1 might be useful therapeutics for treatment of DS as they target the underlying molecular deficit.

SUBMITTER: Chow CY 

PROVIDER: S-EPMC7088997 | biostudies-literature | 2020 Feb

REPOSITORIES: biostudies-literature