mesЭкстремальная биомедицинаExtreme Medicine3033-89643033-8972Centre for Strategic Planning of the Federal Medical and Biological Agency10.47183/mes.2021.033mes-151Research ArticleОРИГИНАЛЬНОЕ ИССЛЕДОВАНИЕORIGINAL RESEARCHСовременные тенденции in vitro фармакологии прототипов противоопухолевых лекарств: библиометрический анализ за 2020–2021 гг.Current trends in anticancer drug prototype in vitro pharmacology: bibliometric analysis 2019–2021ЕршовП. В.ErshovP. V.

Павел Викторович Ершов

ул. Погодинская, д. 10, стр. 1, г. Москва, 119121

Pavel V. Ershov

Pogodinskaya, 10, korp 1, Moscow, 119121

pavel79@inbox.ruМакароваА. С.MakarovaA. S.

ул. Погодинская, д. 10, стр. 1, г. Москва, 119121

Pogodinskaya, 10, korp 1, Moscow, 119121

Центр стратегического планирования и управления медико-биологическими рисками Федерального медико-биологического агентстваРоссияCentre for Strategic Planning and Management of Biomedical Health Risks of the Federal Medical Biological AgencyRussian Federation2021261020242336983Copyright © Ершов П.В., Макарова А.С., 20242024Ершов П.В., Макарова А.С.Ershov P.V., Makarova A.S.Данная работа распространяется под лицензией Creative Commons Attribution 4.0.This work is licensed under a Creative Commons Attribution 4.0 License.https://www.extrememedicine.ru/jour/article/view/151

Выявление новых низкомолекулярных соединений, обладающих противоопухолевой активностью, является первым важным шагом на пути создания кандидатных лекарств и популярным направлением в in vitro фармакологии. Целью исследования было оценить ключевые тенденции и ранжировать научные приоритеты в области дизайна противоопухолевых лекарств с применением библиометрического анализа. Протокол предполагал использование панели библиографических баз данных (PubMed, Scopus, Cortellis) и аналитических ресурсов PubChem, FACTA+, ClustVis, Reaxys, PathwayStudio и VOSviewer для исследования выборки из 1657 публикаций за 2020–2021 гг. В работе также систематизирован материал по 70 новым перспективным производным на основе базовых химических структур, нацеленных на ингибирование отдельных про-опухолевых белковых молекул и сигнальных каскадов. Установлено, что серин-треониновые протеинкиназы, рецепторные тирозинкиназы, ДНК-топоизомеразы и тубулины, а также сигнальные пути PI3K, mTOR, AKT1, STAT3, HIF-1a и p53 составляют до 60% в общей структуре клеточных мишеней для дизайна противоопухолевых лекарств. Отмечен рост научного интереса к инновационным ингибиторам опухоль-ассоциированных белковых комплексов, факторов транскрипции и метаболических ферментов. Соединения из класса гетероциклов, гликозидов, хинонов и терпенов в 71% работ служат базовыми структурами для дизайна противоопухолевых производных. Лидирующие позиции по цитированию занимают вышедшие в 2019 г. публикации, в которых рассмотрены такие соединения, как лапахон, лютеолин, кверцетин, монастрол и кризоспленол D, в контексте дизайна новых прототипов лекарств. Системный библиометрический подход с использованием панели аналитических ресурсов позволяет оценить тенденции в области разработки и дизайна противоопухолевых лекарств и выявить приоритеты научного интереса, органично дополняя классические обзорные работы в периодических изданиях.

Identification of novel low molecular weight compounds with antitumor activity is the first important step towards the development of candidate drugs and a popular trend in in vitro pharmacology. The aim of the study was to assess the key trends and rank the scientific priorities in anticancer drug design using bibliometric analysis. The protocol involved using the panel of bibliographic databases (PubMed, Scopus, Cortellis) and analytical web-based tools PubChem, FACTA +, ClustVis, Reaxys, PathwayStudio and VOSviewer software to review a sample of 1657 papers issued 2020–2021.The work was also focused on 70 new promising basic structures and derivatives targeted at inhibiting both individual pro-tumor proteins and signaling cascades. It was found that serine-threonine protein kinases, receptor tyrosine kinases, DNA topoisomerases and tubulins as well as signaling pathways PI3K, mTOR, AKT1, STAT3, HIF-1a, and p53 account for up to 60% of the total structure of cellular targets for the design of anticancer drugs. The increasing scientific interest in innovative inhibitors of tumor-associated protein complexes, transcription factors and metabolic enzymes has been found. The compounds, which belong to heterocycles, glycosides, quinones and terpenes, were mentioned in 71% of papers as the basic structures for antitumor derivatives design. Papers, published in 2019, in which the compounds, such as lapachone, luteolin, quercetin, monastrol, and crisosplenol D are studied in the context of the design of new drug prototypes, have the highest citation rate. The systematic bibliometric approach involving the use of a panel of analytical resources makes it possible to assess R&D trends and scientific priorities in anticancer drug design, thus organically complementing the classic reviews in periodicals.

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