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Título del libro: Epigenetic Technological Applications
Título del capítulo: DNA Methyltransferase Inhibitors for Cancer Therapy

Autores UNAM:
JOSE LUIS MEDINA FRANCO; ALFONSO DUEÑAS GONZALEZ;
Autores externos:

Idioma:
Inglés
Año de publicación:
2015
Palabras clave:

Chemoinformatics; DNA hypermethylation; DNA hypomethylation; Drug repositioning; Epi-Informatics; High-throughput screening; Nutri-epigenetics; Virtual screening


Resumen:

DNA methyltransferases (DNMTs) are promising epigenetic targets for the development of novel anticancer drugs and other diseases. 5-Azacytidine and decitabine are DNMT inhibitors (DNMTi) approved by the Food and Drug Administration of the United States for the treatment of myelodysplastic syndromes. These two drugs have demonstrated significant, although usually transient, improvement in patient survival. The promising clinical success and limitations of these approved drugs have prompted the search for novel agents targeting DNMTs using a blend of complementary methods including chemical synthesis, rational search in natural sources and food components, and high-throughput screening. This chapter discusses the therapeutic significance of DNMTs in cancer and successful applications of DNMTi in the clinic. We also present advances on experimental assays to screen compound collections and the current status of DNMTi development. Additionally, we elaborate on data sources and recent applications of chemoinformatics and molecular modeling that exemplify the significance of ChemEpinformatics in translational epigenetics. © 2015 Elsevier Inc. All rights reserved.


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