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Information × Registration Number 0220U100520, 0118U100240 , R & D reports Title Enhancement of anticancer activity of landomycin A by its immobilization on the poly-2-oxazoline nanocarrier: effects in vitro and in vivo popup.stage_title Head Panchuk Rostyslav Ruslanovych, Доктор біологічних наук Registration Date 21-01-2020 Organization Institute of Cell Biology popup.description2 During the implementation of Phase I of the project, in silico studies of potential molecular targets of landomycin A in malignant cells were performed and their in vitro verification was performed by flow cytometry. Molecular docking of 3 landomycin family members, characterized by different length of the oligosaccharide chain, was performed to the virtual models of NADPH-dehydrogenases NQO1 and NQO2. It has been shown that landomycin A containing 6 residues of dideoxysugars in its molecule, is characterized by the highest affinity for the NQO1 enzyme. Other landomycins with shorter hydrocarbon chain cannot attach to the additional NQO1 binding site, which explains twice lower ROS production under their action on target cells compared to LA. For verification of these studies specific NQO1 inhibitor (dicumarol) was addressed, decreasing therapeutic effect of LA by 25-30%. The obtained results indicate on the important role of NQO1 in the implementation of the antitumor action of landomycin antibiotics in vitro, which may be important in further clinical studies of these compounds. Product Description popup.authors Kozak Yuliya S. Skorokhyd Nadiya R. popup.nrat_date 2020-04-02 Close