Marco Antonio Meraz-Rodriguez, Manuel Humberto Cháirez-Ramírez, Karen Griselda de la Cruz-López, Rubén Francisco González-Laredo, Alejandro García-Carrancá
{"title":"Polyphenols bind G4-Quadruplex structures and act as epigenetic modifiers with anti-cancer effects.","authors":"Marco Antonio Meraz-Rodriguez, Manuel Humberto Cháirez-Ramírez, Karen Griselda de la Cruz-López, Rubén Francisco González-Laredo, Alejandro García-Carrancá","doi":"10.17179/excli2025-8507","DOIUrl":null,"url":null,"abstract":"<p><p>G4-quadruplexes (G4s) are non-canonical structures of nucleic acids that develop in guanine rich regions of DNA and RNA. Due to their presence in oncogenic promoters and telomeres, G4s represent attractive targets in anticancer drug designs. G4s have also been the subject of recent research regarding their role as epigenetic modulators, supporting their participation in epigenetic processes that control gene expression. The development of small compounds that preferentially target G4s have led to a better understanding of how G4s control these mechanisms. Natural products have greatly contributed to the development of many successful examples of compounds with excellent anticancer activities. Therefore, it is important to investigate ligands targeting G4-quadruplexes in natural products such as dietary polyphenols and their derivatives. In this review, we provide an overview of the latest research on natural compounds, with especial emphasis on dietary polyphenols, as G4-quadruplex targeted ligands. We also discuss dietary polyphenols' structural chemistry that could facilitate their characterization as G4 ligands, highlighting their potential in the development of anticancer drugs. Finally, we explore polyphenols' potential mechanisms of action in regulating epigenetic machinery through G4 binding, thereby providing insights for the development of safe and effective therapeutical tools against cancer.</p>","PeriodicalId":12247,"journal":{"name":"EXCLI Journal","volume":"24 ","pages":"957-991"},"PeriodicalIF":4.9000,"publicationDate":"2025-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12436681/pdf/","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"EXCLI Journal","FirstCategoryId":"99","ListUrlMain":"https://doi.org/10.17179/excli2025-8507","RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2025/1/1 0:00:00","PubModel":"eCollection","JCR":"Q1","JCRName":"BIOLOGY","Score":null,"Total":0}
引用次数: 0
Abstract
G4-quadruplexes (G4s) are non-canonical structures of nucleic acids that develop in guanine rich regions of DNA and RNA. Due to their presence in oncogenic promoters and telomeres, G4s represent attractive targets in anticancer drug designs. G4s have also been the subject of recent research regarding their role as epigenetic modulators, supporting their participation in epigenetic processes that control gene expression. The development of small compounds that preferentially target G4s have led to a better understanding of how G4s control these mechanisms. Natural products have greatly contributed to the development of many successful examples of compounds with excellent anticancer activities. Therefore, it is important to investigate ligands targeting G4-quadruplexes in natural products such as dietary polyphenols and their derivatives. In this review, we provide an overview of the latest research on natural compounds, with especial emphasis on dietary polyphenols, as G4-quadruplex targeted ligands. We also discuss dietary polyphenols' structural chemistry that could facilitate their characterization as G4 ligands, highlighting their potential in the development of anticancer drugs. Finally, we explore polyphenols' potential mechanisms of action in regulating epigenetic machinery through G4 binding, thereby providing insights for the development of safe and effective therapeutical tools against cancer.
期刊介绍:
EXCLI Journal publishes original research reports, authoritative reviews and case reports of experimental and clinical sciences.
The journal is particularly keen to keep a broad view of science and technology, and therefore welcomes papers which bridge disciplines and may not suit the narrow specialism of other journals. Although the general emphasis is on biological sciences, studies from the following fields are explicitly encouraged (alphabetical order):
aging research, behavioral sciences, biochemistry, cell biology, chemistry including analytical chemistry, clinical and preclinical studies, drug development, environmental health, ergonomics, forensic medicine, genetics, hepatology and gastroenterology, immunology, neurosciences, occupational medicine, oncology and cancer research, pharmacology, proteomics, psychiatric research, psychology, systems biology, toxicology