ssmuБюллетень сибирской медициныBulletin of Siberian Medicine1682-03631819-3684Siberian State Medical University, the Ministry of Healthcare of the Russian Federation10.20538/1682-0363-2024-3-155-162ssmu-5751Research ArticleОБЗОРЫ И ЛЕКЦИИREVIEW AND LECTURESГалектины: потенциальная фармакологическая мишеньGalectins: a potential pharmacological targethttps://orcid.org/0000-0001-7078-4988СеребряковаВ. А.SerebryakovaV. A.

Серебрякова Валентина Александровна – д-р мед. наук, доцент, профессор кафедры фармакологии 

2, Moscow Trakt, Tomsk, 634050

serebryakova-val@mail.ruhttps://orcid.org/0000-0003-4083-976XВаизоваО. Е.VaizovaO. E.

Ваизова Ольга Евгеньевна – д-р мед. наук, профессор, профессор кафедры фармакологии 

2, Moscow Trakt, Tomsk, 634050

vaizova@mail.ruhttps://orcid.org/0000-0001-6132-9617ГоловинаЕ. Л.GolovinaE. L.

Головина Евгения Леонидовна – канд. мед. наук, доцент кафедры фармакологии

2, Moscow Trakt, Tomsk, 634050

golovina.el@ssmu.ruhttps://orcid.org/0009-0003-8743-5022КочубейВ. В.KochubeyV. V.

Кочубей Вероника Владимировна – студентка, педиатрический факультет,

2, Moscow Trakt, Tomsk, 634050

veronica.kochubey@gmail.comСибирский государственный медицинский университетРоссияSiberian State Medical UniversityRussian Federation202411102024233155162Copyright © Серебрякова В.А., Ваизова О.Е., Головина Е.Л., Кочубей В.В., 20242024Серебрякова В.А., Ваизова О.Е., Головина Е.Л., Кочубей В.В.Serebryakova V.A., Vaizova O.E., Golovina E.L., Kochubey V.V.Данная работа распространяется под лицензией Creative Commons Attribution 4.0.This work is licensed under a Creative Commons Attribution 4.0 License.https://bulletin.ssmu.ru/jour/article/view/5751

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.

Aim. To consider the use of galectin-1 and galectin-3 inhibitors as potential pharmacological targets in antitumor and antifibrotic therapy.

The lecture includes the analysis of experimental research and review articles presented in the PubMed database. A brief description of the structure of galectins is given. Their generally accepted classification and features of the structure of the carbohydrate recognition domain in galectin-1 and galectin-3 are presented. The main part of the lecture describes the results of research on the development of carbohydrate-based (β-galactoside derivatives or analogues) and non-carbohydrate-based (peptide-based, carboxamide derivatives) inhibitors capable of interacting with galectin-1 and galectin-3.

The results of experiments performed on animal models and tumor cell cultures demonstrate that the antitumor effect of galectin antagonists is realized through the suppression of proliferation and metastasis, activation of tumor cell apoptosis, and modulation of the antitumor immune response. Antagonists of galectin-1 and galectin-3 potentiate the effect of antitumor drugs and have an antifibrotic effect. Some of the compounds discussed in the lecture are undergoing clinical trials. The data presented in the lecture open up opportunities for the development and synthesis of new molecules of potential galectin-1 and 3 inhibitors.

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The authors declare that there are no conflicts of interest present.