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Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
Published on: January 26, 2016
Modeling, synthesis and in vitro testing of peptides based on unusual amino acids as potential antibacterial agents
A S Sargsyan1, L T Karapetyan1, A V Mkhitaryan1
1Scientific and Production Center "Armbiotechnology" NAS RA, Yerevan, Armenia.
Abstract:
Currently non-protein amino acids and synthetic peptides are widely used as blocks in drug design. Many proteases are of great interest for pharmacology due to their key role in various pathologies. Bacterial collagenase (EC 3.4.24.3) is quite an attractive target for drug development as the inhibitors of bacterial collagenolytic protease may stop propagation of diseases caused by infections. The interaction of peptides containing unusual amino acids with Clostridium histolyticum collagenase has been evaluated by molecular docking followed by the measurement of enzyme inhibition by selected compounds. According to the docking analysis, 4 compounds were selected and synthesized for further research. Measurement of enzyme activity revealed that all tested compounds inhibited collagenase activity with IC50 values ranging within 1.45-2.08 μM. The antibacterial activity of synthesized compounds against some resistant strains was characterized by MICs values ranging within 4.6-9.2 μg/ml.
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