Engineering potent and selective analogues of GpTx-1, a tarantula venom peptide antagonist of the Na(V)1.7 sodium channel.

@article{Murray2015EngineeringPA,
  title={Engineering potent and selective analogues of GpTx-1, a tarantula venom peptide antagonist of the Na(V)1.7 sodium channel.},
  author={Justin K. Murray and Joseph A. Ligutti and Dong Liu and Anruo Zou and Leszek Poppe and Hongyan Li and Kristin L. Andrews and Bryan D Moyer and Stefan I. McDonough and Philippe S. Favreau and Reto St{\"o}cklin and Les P. Miranda},
  journal={Journal of medicinal chemistry},
  year={2015},
  volume={58 5},
  pages={
          2299-314
        }
}
NaV1.7 is a voltage-gated sodium ion channel implicated by human genetic evidence as a therapeutic target for the treatment of pain. Screening fractionated venom from the tarantula Grammostola porteri led to the identification of a 34-residue peptide, termed GpTx-1, with potent activity on NaV1.7 (IC50 = 10 nM) and promising selectivity against key NaV subtypes (20× and 1000× over NaV1.4 and NaV1.5, respectively). NMR structural analysis of the chemically synthesized three disulfide peptide was… CONTINUE READING
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