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Information × Registration Number 0221U101020, 0120U104883 , R & D reports Title Enzymes of post-translational modifications of microtubule proteins as targets for inhibition of the excitability of primary nociceptive neurons popup.stage_title Head Karpov Pavlo A., Кандидат біологічних наук Registration Date 12-01-2021 Organization Institute of Food Biotechnology and Genomics of the National Academy of Sciences of Ukraine popup.description2  As a result of the project in 2020, methods of virtual screening, as well as electrophysiological studies were established and tested, the algorithm of ion channel assembly in a membrane fragment was developed on the example of Nav1.5 sodium channel and the molecular mechanism of Nav1.5 open and closed state formation was established. Refined 3D-models of associated enzymes: HDAC6, ATAT, ELP3, TTLL1 were also obtained and the topology of their sites was determined. Conformations of apo- and holoenzyme forms of targets in complex with reference compounds were established. The primary screening of the concentration dependence of the effect of colchicine on P2X channel currents using the HEK-293 cell line was performed and it was found that the dynamic competition of colchicine and ATP varies depending on the concentration of these compounds. Threshold concentrations of colchicine toxicity (≥1 mm) and the optimal protocol for testing future inhibitors in the model of excitable cells of the central and peripheral nervous system and interpretation of the obtained data were determined. Product Description popup.authors Karpov Pavlo A. Novozhilov Dmitry О. Rabokon Anastasiya M. Samofalova Dariya O. Stikhilyas Mariya M. popup.nrat_date 2021-01-12 Close