Keywords
KRAS
аллостерическое ингибирование
дизайн лекарств
молекулярное моделирование
панселективность
рак легкого
Abstract
Представлен подробный обзор последних достижений в разработке ингибиторов мутантных форм гуанозинтрифосфатазы KRAS, которая играет ключевую роль в патогенезе различных онкологических заболеваний. Сделан акцент на сложности и ограничениях таргетирования KRAS из-за его структурных особенностей и высокой частоты мутаций. Основное внимание уделено панселективным ингибиторам, способным действовать на несколько различных мутаций KRAS, что важно для преодоления резистентности опухолей к терапии. Приведены примеры перспективных молекулярных структур, анализ механизмов действия и возможных причин селективности.
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