title: Tetraplex binding molecules as anti-cancer agents.
abstract: Increasing evidence suggests that four-stranded tetraplex structures spontaneously form under physiological conditions and these alternate DNA structures are likely to form in vivo. Alternate G-quadruplex DNA structures that may form in regulatory elements of oncogenes or G-rich telomere sequences are potential targets for cancer therapy since these sequence-specific structures are proposed to affect gene expression and telomerase activation, respectively. Small molecule compounds that specifically bind tetraplexes may be used to regulate cell cycle progression by modulating promotor activation or disrupting telomere maintenance, important processes of cellular transformation. In this review, we summarize the current research developments and associated patents that bear relevance to understanding the mechanism and clinical application of tetraplex binding molecules as anti-cancer agents.
authors.affiliation: Laboratory of Molecular Gerontology, National Institute on Aging, NIH, 5600 Nathan Shock Drive, Baltimore, MD 21224, USA.
authors.forename: Kevin M
authors.initials: KM
authors.lastname: Doherty
authors.forename: Sudha
authors.initials: S
authors.lastname: Sharma
authors.forename: Rigu
authors.initials: R
authors.lastname: Gupta
authors.forename: Robert M
authors.initials: RM
authors.lastname: Brosh
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D004265:DNA Helicases / Q000187:drug effects; D004261:DNA Replication / Q000187:drug effects; D004273:DNA, Neoplasm / Q000737:chemistry* / Q000187:drug effects*; D004791:Enzyme Inhibitors / Q000494:pharmacology; D006801:Humans; D008024:Ligands; D009690:Nucleic Acid Conformation; D010569:Perylene / Q000031:analogs & derivatives / Q000494:pharmacology; D019098:Telomerase / Q000037:antagonists & inhibitors; D016615:Telomere / Q000187:drug effects; D015533:Transcriptional Activation / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D004273:DNA, Neoplasm; D004791:Enzyme Inhibitors; D008024:Ligands; D010569:Perylene; D019098:Telomerase; D004265:DNA Helicases