The tarantula toxin β/δ-TRTX-Pre1a highlights the importance of the S1-S2 voltage-sensor region for sodium channel subtype selectivity.

ABSTRACT: Voltage-gated sodium (Na_V) channels are essential for the transmission of pain signals in humans making them prime targets for the development of new analgesics. Spider venoms are a rich source of peptide modulators useful to study ion channel structure and function. Here we describe β/δ-TRTX-Pre1a, a 35-residue tarantula peptide that selectively interacts with neuronal Na_V channels inhibiting peak current of hNa_V1.1, rNa_V1.2, hNa_V1.6, and hNa_V1.7 while concurrently inhibiting fast inactivation of hNa_V1.1 and rNa_V1.3. The DII and DIV S3-S4 loops of Na_V channel voltage sensors are important for the interaction of Pre1a with Na_V channels but cannot account for its unique subtype sele

SUBMITTER: Wingerd JS 

PROVIDER: S-EPMC5430537 | biostudies-literature | 2017 Apr

REPOSITORIES: biostudies-literature