Epigenetic Control and Cancer The Potential of Histone Demethylases as Therapeutic Targets.docVIP

Pharmaceuticals 2012, 5, 963-990; doi:10.3390/ph5090963 OPEN ACCESS pharmaceuticals ISSN 1424-8247 /journal/pharmaceuticals Review Epigenetic Control and Cancer: The Potential of Histone Demethylases as Therapeutic Targets Fernando Lizcano * and Jeison Garcia Center of Biomedical Research La Sabana University-CIBUS, School of Medicine, Universidad de La Sabana, Campus Del Puente del Común, km 7 Autopista Norte de Bogota, Chía 250001, Colombia; E-Mail: jeisongase@.co (J.G.) * Author to whom correspondence should be addressed; E-Mail: fernandoll@.co; Tel.: +571-861-5555 (ext. 23328); Fax: +571-861-5555 (ext. 10111). Received: 26 June 2012; in revised form: 21 July 2012 / Accepted: 17 August 2012 / Published: 12 September 2012 Abstract: The development of cancer involves an immense number of factors at the molecular level. These factors are associated principally with alterations in the epigenetic mechanisms that regulate gene expression profiles. Studying the effects of chromatin structure alterations, which are caused by the addition/removal of functional groups to specific histone residues, are of great interest as a promising way to identify markers for cancer diagnosis, classify the disease and determine its prognosis, and these markers could be potential targets for the treatment of this disease in its different forms. This manuscript presents the current point of view regarding members of the recently described family of proteins that exhibit histone demethylase activity; histone demethylases are genetic regulators that play a fundamental role in both the activation and repression of genes and whose expression has been observed to increase in many types of cancer. Some fundamental aspects of their association with the development of cancer and their relevance as potential targets for the development of new therapeutic strategies at the epigenetic leve