Галектины: потенциальная фармакологическая мишень

Целью работы является рассмотрение использования ингибиторов галектина-1 и галектина-3 как потенциальных лекарственных средств противоопухолевой и антифибротической терапии.

Лекция разработана на основе анализа экспериментальных и обзорных статей, представленных в базе данных PubMed. Дана краткая характеристика строения галектинов, представлены их общепринятая классификация и особенности структурной организации углевод-распознающего домена галектина-1 и галектина-3. В основной части лекции описаны результаты исследований по разработке молекул-ингибиторов углеводной (производные или аналоги β-галактозида) и неуглеводной (на основе пептидов, производные карбоксамида) структуры, способных взаимодействовать с галектином-1 и галектином-3.

Результаты экспериментов, выполненных на лабораторных животных и культурах опухолевых клеток, демонстрируют, что противоопухолевое действие антагонистов галектинов реализуется через подавление пролиферации, метастазирования, активацию апоптоза опухолевых клеток и модуляцию противоопухолевого иммунного ответа. Антагонисты галектина-1 и галектина-3 потенцируют действие противоопухолевых лекарственных средств и оказывают антифибротический эффект. Ряд рассмотренных соединений проходит фазу клинических исследований. Представленные в лекции данные открывают возможности для разработки и синтеза новых молекул – потенциальных ингибиторов галектина-1 и галектина -3.

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