Article ; Online: G-quadruplexes in cancer-related gene promoters: from identification to therapeutic targeting.
Expert opinion on therapeutic patents
2024 Volume 33, Issue 11, Page(s) 745–773
Abstract: ... structures called G-quadruplexes (G4s) which are widely distributed in functional regions of the human genome ...
Abstract | Introduction: Guanine-rich DNA sequences can fold into four-stranded noncanonical secondary structures called G-quadruplexes (G4s) which are widely distributed in functional regions of the human genome, such as telomeres and gene promoter regions. Compelling evidence suggests their involvement in key genome functions such as gene expression and genome stability. Notably, the abundance of G4-forming sequences near transcription start sites suggests their potential involvement in regulating oncogenes. Areas covered: This review provides an overview of current knowledge on G4s in human oncogene promoters. The most representative G4-binding ligands have also been documented. The objective of this work is to present a comprehensive overview of the most promising targets for the development of novel and highly specific anticancer drugs capable of selectively impacting the expression of individual or a limited number of genes. Expert opinion: Modulation of G4 formation by specific ligands has been proposed as a powerful new tool to treat cancer through the control of oncogene expression. Actually, most of G4-binding small molecules seem to simultaneously target a range of gene promoter G4s, potentially influencing several critical driver genes in cancer, thus producing significant therapeutic benefits. |
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MeSH term(s) | Humans ; G-Quadruplexes ; DNA/chemistry ; DNA/genetics ; DNA/metabolism ; Patents as Topic ; Promoter Regions, Genetic ; Antineoplastic Agents/pharmacology ; Ligands ; Neoplasms/drug therapy ; Neoplasms/genetics |
Chemical Substances | DNA (9007-49-2) ; Antineoplastic Agents ; Ligands |
Language | English |
Publishing date | 2024-01-11 |
Publishing country | England |
Document type | Journal Article ; Review |
ZDB-ID | 1186201-4 |
ISSN | 1744-7674 ; 0962-2594 ; 1354-3776 |
ISSN (online) | 1744-7674 |
ISSN | 0962-2594 ; 1354-3776 |
DOI | 10.1080/13543776.2023.2271168 |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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