Seven novel modulators of the analgesic target NaV1.7 uncovered using a high-throughput venom-based discovery approach

Abstract

Background and PurposeChronic pain is a serious worldwide health issue, with current analgesics having limited efficacy and dose-limiting side effects. Humans with loss-of-function mutations in the voltage-gated sodium channel Na(V)1.7 (hNa(V)1.7) are indifferent to pain, making hNa(V)1.7 a promising target for analgesic development. Since spider venoms are replete with Na-V channel modulators, we examined their potential as a source of hNa(V)1.7 inhibitors