Functional analysis of synthetic insectatachykinin analogs on recombinant neurokinin receptor expressing cell lines

H. Torfs, K.E. Akerman, R.J. Nachman, H.B. Oonk, M. Detheux, J. Poels, T. van Loy, A. Loof, R.H. Meloen, G. Vassart, M. Parmentier, J. van den Broeck

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Abstract

The activity of a series of synthetic tachykinin-like peptide analogs was studied by means of microscopic calcium imaging on recombinant neurokinin receptor expressing cell lines. A C-terminal pentapeptide (FTGMRa) is sufficient for activation of the stomoxytachykinin receptor (STKR) expressed in Schneider 2 cells. Replacement of amino acid residues at the position of the conserved phenylalanine (F) or arginine (R) residues by alanine (A) results in inactive peptides (when tested at 1 ¿M), whereas A-replacements at other positions do not abolish the biological activity of the resulting insectatachykinin-like analogs. Calcium imaging was also employed to compare the activity of C-terminally substituted tachykinin analogs on three different neurokinin receptors. The results indicate that the major pharmacological and evolutionary difference between tachykinin-related agonists for insect (STKR) and human (NK1 and NK2) receptors resides in the C-terminal amino acid residues (R versus M). A single C-terminal amino acid change can turn an STKR-agonist into an NK-agonist and vice versa
Original languageEnglish
Pages (from-to)1999-2005
JournalPeptides
Volume23
Issue number11
DOIs
Publication statusPublished - 2002

Keywords

  • tachykinin-related peptides
  • insect neuropeptides
  • urechis-unicinctus
  • myotropic peptides
  • echiuroid worm
  • identification
  • vertebrate
  • homology
  • family
  • cockroach

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    Torfs, H., Akerman, K. E., Nachman, R. J., Oonk, H. B., Detheux, M., Poels, J., van Loy, T., Loof, A., Meloen, R. H., Vassart, G., Parmentier, M., & van den Broeck, J. (2002). Functional analysis of synthetic insectatachykinin analogs on recombinant neurokinin receptor expressing cell lines. Peptides, 23(11), 1999-2005. https://doi.org/10.1016/S0196-9781(02)00187-0