Seven novel modulators of the analgesic target NaV 1.7 uncovered using a high-throughput venom-based discovery approach.

@article{Klint2015SevenNM,
  title={Seven novel modulators of the analgesic target NaV 1.7 uncovered using a high-throughput venom-based discovery approach.},
  author={Julie K. Klint and Jennifer J. Smith and Irina Vetter and Darshani B Rupasinghe and Sing Yan Er and Sebastian Senff and Volker Herzig and Mehdi Mobli and Richard J Lewis and Frank Bosmans and Glenn F. King},
  journal={British journal of pharmacology},
  year={2015},
  volume={172 10},
  pages={2445-58}
}
BACKGROUND AND PURPOSE Chronic 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 NaV 1.7 (hNaV 1.7) are indifferent to pain, making hNaV 1.7 a promising target for analgesic development. Since spider venoms are replete with NaV channel modulators, we examined their potential as a source of hNaV 1.7 inhibitors. EXPERIMENTAL APPROACH We developed a… CONTINUE READING