Discovery of a Novel Na_v1.7 Inhibitor From Cyriopagopus albostriatus Venom With Potent Analgesic Efficacy.

ABSTRACT: Spider venoms contain a vast array of bioactive peptides targeting ion channels. A large number of peptides have high potency and selectivity toward sodium channels. Na_v1.7 contributes to action potential generation and propagation and participates in pain signaling pathway. In this study, we describe the identification of μ-TRTX-Ca2a (Ca2a), a novel 35-residue peptide from the venom of Vietnam spider Cyriopagopus albostriatus (C. albostriatus) that potently inhibits Na_v1.7 (IC₅₀ = 98.1 ± 3.3 nM) with high selectivity against skeletal muscle isoform Na_v1.4 (IC₅₀ > 10 μM) and cardiac muscle isoform Na_v1.5 (IC₅₀ > 10 μM). Ca2a did not significantly alter the voltage-dependent activation or fast inactiv

SUBMITTER: Zhang Y 

PROVIDER: S-EPMC6198068 | biostudies-literature | 2018

REPOSITORIES: biostudies-literature