Abstract
Quadruplex nucleic acids (G4s) are higher-order formed by the folding of short G-tracts in DNA or RNA. They are non-randomly distributed in the human genome, occurring disproportionally in cancer-related genes, notably in promoter regions. When stabilized by a suitable small-molecule ligand, they can impede the transcription, translation or replication of a gene, depending on the location of the G4(s) within the gene. This can ultimately lead to apoptosis, DNA damage and an anti-cancer effect. Many G4 ligands have been studied: there are currently over 4500 in the literature. This review focusses on the background to, and the current status as of mid-2024, of the two such compounds that have progressed to clinical trials, CX-5461 and QN-302. Their very different chemical structures have resulted in distinct pre-clinical and (as far as is known) clinical profiles. Prospects for their future development and potential as approved anti-cancer drugs are discussed, together with possible directions for the more general G4-drug field.
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