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Acid-sensing ion channel-3 (ASIC3; ACCN3)

In vitro and mouse studies suggest a peptide inhibitor of ASIC3 could help treat inflammatory and acid-induced pain. Electrophysiological testing in transgenic Xenopus laevis oocytes expressing human ASIC3 identified a 29-mer sea anemone peptide as a low micromolar inhibitor of the ASIC3 current. In mouse models for thermal hyperalgesia and acid-induced pain, the peptide decreased hypersensitivity to thermal and acidic stimulus compared with vehicle. Next steps include optimizing the peptide to improve its potency.
Theralpha S.A.S. and Flamel Technologies S.A. have THA902, a long-acting formulation ASIC3 inhibitor using Medusa technology, in preclinical testing to treat pain.

SciBX 6(30); doi:10.1038/scibx.2013.800
Published online Aug. 8, 2013

Patented by the M.M. Shemyakin and Yu.A. Ovchinnikov Institute of Bioorganic Chemistry of the Russian Academy of Sciences; available for licensing and partnering

Osmakov, D.I. et al. J. Biol. Chem.; published June 25, 2013;
Contact: Yaroslav A. Andreev, M.M. Shemyakin and Yu.A. Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Moscow, Russia