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Information × Registration Number 0220U101060, 0118U001128 , R & D reports Title Peptides with photo-directed biological activity - inhibitors of intracellular processes involved in the development of cancer diseases. popup.stage_title Head Komarov Igor V., Доктор хімічних наук Registration Date 31-01-2020 Organization Taras Shevchenko National University of Kyiv popup.description2 Object of study: Peptides with photocontrolled biological properties. Aim of work: design, synthesis, study of biological activity and development of approaches for use in the treatment of cancer diseases of such peptides, which are capable of photoisomerization of the diarylethene moiety and are analogues of known peptide inhibitors of PIN1 and p53-MDM2 protein-protein interaction. Research Methods: Organic synthesis, computer simulation, physical analysis. New peptides, inhibitors of the PIN1 enzyme, have been synthesized to further study their biological activity against the enzyme, including photosensitive derivatives of diarylethylene. Molecular docking and molecular dynamics have comprehensively investigated complexes of two photoforms of previously obtained diarylethylene-containing PIN1 inhibitors. Both structure and dynamic behavior of the complexes are found to be significant differ, which is consistent with the results of previous experimental measurements of the inhibitory activity of these compounds. Since the protein-protein interaction inhibitors p53-MDM2 found in the previous work stage did not show activity on cell bioassays, it was hypothesized that these inhibitors did not penetrate the cells. To test this hypothesis, a conjugate of the best cell-permeable peptide fragment inhibitor was synthesized for further cell bioassays. Diarylethylene-containing analogs of known cell-permeable peptides have been systematically investigated, and among them cell permeability can be effectively controlled by light.  Product Description popup.authors Harmonychuk Lyudmyla V. Komarov Igor V. popup.nrat_date 2020-04-02 Close