Conversed mutagenesis of an inactive peptide to ASIC3 inhibitor for active sites determination.

@article{Osmakov2016ConversedMO,
  title={Conversed mutagenesis of an inactive peptide to ASIC3 inhibitor for active sites determination.},
  author={Dmitry I Osmakov and Sergey G. Koshelev and Yaroslav A. Andreev and Igor A. Dyachenko and Dmitry A Bondarenko and Arkadii N. Murashev and Eugene V. Grishin and Sergey A Kozlov},
  journal={Toxicon : official journal of the International Society on Toxinology},
  year={2016},
  volume={116},
  pages={11-6}
}
Peptide Ugr9-1 from the venom of sea anemone Urticina grebelnyi selectively inhibits the ASIC3 channel and significantly reverses inflammatory and acid-induced pain in vivo. A close homolog peptide Ugr 9-2 does not have these features. To find the pharmacophore residues and explore structure-activity relationships of Ugr 9-1, we performed site-directed mutagenesis of Ugr 9-2 and replaced several positions by the corresponding residues from Ugr 9-1. Mutant peptides Ugr 9-2 T9F and Ugr 9-2 Y12H… CONTINUE READING
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