title: Targeting G-quadruplexes in gene promoters: a novel anticancer strategy?
abstract: G-quadruplexes are four-stranded DNA structures that are over-represented in gene promoter regions and are viewed as emerging therapeutic targets in oncology, as transcriptional repression of oncogenes through stabilization of these structures could be a novel anticancer strategy. Many gene promoter G-quadruplexes have physicochemical properties and structural characteristics that might make them druggable, and their structural diversity suggests that a high degree of selectivity might be possible. Here, we describe the evidence for G-quadruplexes in gene promoters and discuss their potential as therapeutic targets, as well as progress in the development of strategies to harness this potential through intervention with small-molecule ligands.
authors: Department of Chemistry, University of Cambridge, Cambridge CB21EW, UK. sb10031@cam.ac.uk
authors: Shankar
authors: S
authors: Balasubramanian
authors: Laurence H
authors: LH
authors: Hurley
authors: Stephen
authors: S
authors: Neidle
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology; D016503:Drug Delivery Systems; D015195:Drug Design; D054856:G-Quadruplexes / Q000187:drug effects; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D011401:Promoter Regions, Genetic
chemical_list: D000970:Antineoplastic Agents