A novel BK channel-targeted peptide suppresses sound evoked activity in the mouse inferior colliculus.

ABSTRACT: Large conductance calcium-activated (BK) channels are broadly expressed in neurons and muscle where they modulate cellular activity. Decades of research support an interest in pharmaceutical applications for modulating BK channel function. Here we report a novel BK channel-targeted peptide with functional activity in vitro and in vivo. This 9-amino acid peptide, LS3, has a unique action, suppressing channel gating rather than blocking the pore of heterologously expressed human BK channels. With an IC₅₀ in the high picomolar range, the apparent affinity is higher than known high affinity BK channel toxins. LS3 suppresses locomotor activity via a BK channel-specific mechanism in wild-type or BK channel-humanized Caenorhabditis elegans. Topical application on the dural surface of t

SUBMITTER: Scott LL 

PROVIDER: S-EPMC5307958 | biostudies-literature | 2017 Feb

REPOSITORIES: biostudies-literature