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Information × Registration Number 0225U000457, (0124U002143) , R & D reports Title Study of non-enzymatic activation of prothrombin popup.stage_title Характеристика активного центру, утвореного в ході неензиматичної активації протробіну. In silico пошук потенційних лігандів активаційної «Ile16»-комірки протромбіну; синтез пептидів. Дослідження впливу отриманих пептидів лігандів на активацію протромбіну. Head Ihor V. Komarov, Доктор хімічних наукChernyshenko Volodymyr O., Доктор біологічних наук Registration Date 12-01-2025 Organization Department for special training National academy of science of Ukraine at Kiev University popup.description1 The aim of the work is to study of non-enzymatic activation of prothrombin, as well as the search for peptides and/or low-molecular compounds that are potentially capable to activate prothrombin non-enzymatically. popup.description2  The subject of the research is non-enzymatic activation of prothrombin. It consists in exposing the thrombin-like active center in the prothrombin molecule without proteolytic modification. The aim of the work is to study the features of non-enzymatic activation of prothrombin and the search for peptides and/or low molecular weight compounds that are potentially capable of non-enzymatically activating prothrombin. During the work, a search for potential ligands of the activating "Ile16" cell of prothrombin was carried out using in silico methods. Peptides have been synthesized which, according to in silico data, are able to interact with the activation cell of prothrombin; the effect of the obtained peptides on the process of prothrombin activation was tested. The chromogenic thrombin substrate S2238 was used to determine thrombin-like activity. For the peptide with the sequence IIVSDYSKE, in all three types of experiments (primary activity screening, excess peptide, presence of streptokinase), a significant statistically significant increase in non-enzymatic activation of plasma prothrombin was observed compared to the control and the fragment of the N-terminal domain of the S. aureus coagulase peptide IVTKDYSKE. In the study on additional non-enzymatic activation of plasma prothrombin, the IVTSDYSDE peptide also demonstrated a significant effect compared to the control and the peptide of the original "wild-type" sequence IVTKDYSKE. IVFSDYSKE and IVVRDYSKE peptides also showed the ability to non-enzymatically activate plasma prothrombin, but in the experiment with an additional dose of peptides, the activity of the IVVRDYSKE peptide significantly exceeded the activity of the IIVSDYSKE peptide throughout the experiment. Peptides with the following sequences were identified as the most perspective: IIVSDYSKE, IVTSDYSDE and IVVRDYSKE. Product Description popup.authors Hrabovskyi Oleksii O. Lypenko Oleksii S. Pavlenko Anastasiia O. Tsuvariev Oleksandr Yu. Shevchenko Yeva V. popup.nrat_date 2025-01-12 Close