Effect of N- and C-Terminal Modifications on Cytotoxic Properties of Antimicrobial Peptide Tachyplesin I
- Authors: Kuzmin D.V.1, Emelianova A.A.1, Kalashnikova M.B.1, Panteleev P.V.1, Ovchinnikova T.V.1
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Affiliations:
- M. M. Shemyakin and Yu. A. Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences
- Issue: Vol 162, No 6 (2017)
- Pages: 754-757
- Section: Article
- URL: https://journals.rcsi.science/0007-4888/article/view/238528
- DOI: https://doi.org/10.1007/s10517-017-3705-2
- ID: 238528
Cite item
Abstract
We analyze the effects of N-terminal acetylation and C-terminal amidation on the cytotoxic properties of β-hairpin antimicrobial peptide tachyplesin I. MTT-assay showed that modified tachyplesin I exhibited increased cytotoxicity toward both tumor and normal human cells. Hemolytic activity of modified tachyplesin I was also higher than that of the initial molecule. In contrast to non-modified tachyplesin I, the peptide with C- and N-terminal modifications is resistant to proteolytic degradation in fresh human serum. C- and N-terminal modifications make tachyplesin I more attractive prototype of anticancer drug due to its more potent cytotoxic effect and better pharmacokinetic properties.
About the authors
D. V. Kuzmin
M. M. Shemyakin and Yu. A. Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences
Email: ovch@ibch.ru
Russian Federation, Moscow
A. A. Emelianova
M. M. Shemyakin and Yu. A. Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences
Email: ovch@ibch.ru
Russian Federation, Moscow
M. B. Kalashnikova
M. M. Shemyakin and Yu. A. Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences
Email: ovch@ibch.ru
Russian Federation, Moscow
P. V. Panteleev
M. M. Shemyakin and Yu. A. Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences
Email: ovch@ibch.ru
Russian Federation, Moscow
T. V. Ovchinnikova
M. M. Shemyakin and Yu. A. Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences
Author for correspondence.
Email: ovch@ibch.ru
Russian Federation, Moscow