title: G-quadruplexes as potential therapeutic targets for embryonal tumors.
abstract: Embryonal tumors include a heterogeneous group of highly malignant neoplasms that primarily affect infants and children and are characterized by a high rate of mortality and treatment-related morbidity, hence improved therapies are clearly needed. G-quadruplexes are special secondary structures adopted in guanine (G)-rich DNA sequences that are often present in biologically important regions, e.g. at the end of telomeres and in the regulatory regions of oncogenes such as MYC. Owing to the significant roles that both telomeres and MYC play in cancer cell biology, G-quadruplexes have been viewed as emerging therapeutic targets in oncology and as tools for novel anticancer drug design. Several compounds that target these structures have shown promising anticancer activity in tumor xenograft models and some of them have entered Phase II clinical trials. In this review we examine approaches to DNA targeted cancer therapy, summarize the recent developments of G-quadruplex ligands as anticancer drugs and speculate on the future direction of such structures as a potential novel therapeutic strategy for embryonal tumors of the nervous system.
authors.affiliation: Division of Oncology, University Children's Hospital of Zurich, Zurich 8032, Switzerland. tarek.shalaby@kispi.uzh.ch.
authors.forename: Tarek
authors.initials: T
authors.lastname: Shalaby
authors.forename: Giulio
authors.initials: G
authors.lastname: Fiaschetti
authors.forename: Kazuo
authors.initials: K
authors.lastname: Nagasawa
authors.forename: Kazuo
authors.initials: K
authors.lastname: Shin-ya
authors.forename: Martin
authors.initials: M
authors.lastname: Baumgartner
authors.forename: Michael
authors.initials: M
authors.lastname: Grotzer
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D004247:DNA / Q000235:genetics; D015195:Drug Design; D054856:G-Quadruplexes; D006801:Humans; D008024:Ligands; D058990:Molecular Targeted Therapy; D009373:Neoplasms, Germ Cell and Embryonal / Q000188:drug therapy* / Q000235:genetics; D009423:Nervous System Neoplasms / Q000188:drug therapy* / Q000235:genetics; D016615:Telomere / Q000235:genetics; D059505:Telomere Homeostasis / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D008024:Ligands; D004247:DNA