Гель-электрофорез как метод классификации ингибиторов поли(АДФ-рибоза)-полимераз 1 и 2

Поли(АДФ-рибоза)-полимеразы 1 и 2 (PARP1 и PARP2) играют важную роль в репарации повреждений ДНК в клетке, а их ингибирование применяется для лечения некоторых онкологических заболеваний. Ведутся активные разработки новых ингибиторов PARP и изучение механизмов их действия. В настоящей работе на примере ингибиторов талазопариба, олапариба и велипариба показано, что электрофорез в полиакриламидном геле комплексов ДНК с PARP1 и PARP2 в присутствии ингибиторов позволяет выявить их влияние на сродство ферментов к ДНК, а после добавления субстрата НАД+ – оценить эффективность ингибирования каталитической активности ферментов. Учет данных механизмов действия важен для поиска новых ингибиторов PARP1 и PARP2.

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