학술논문
Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies
Document Type
article
Author
Edurne San José-Enériz; Xabier Agirre; Obdulia Rabal; Amaia Vilas-Zornoza; Juan A. Sanchez-Arias; Estibaliz Miranda; Ana Ugarte; Sergio Roa; Bruno Paiva; Ander Estella-Hermoso de Mendoza; Rosa María Alvarez; Noelia Casares; Victor Segura; José I. Martín-Subero; François-Xavier Ogi; Pierre Soule; Clara M. Santiveri; Ramón Campos-Olivas; Giancarlo Castellano; Maite Garcia Fernandez de Barrena; Juan Roberto Rodriguez-Madoz; Maria José García-Barchino; Juan Jose Lasarte; Matias A Avila; Jose Angel Martinez-Climent; Julen Oyarzabal; Felipe Prosper
Source
Nature Communications, Vol 8, Iss 1, Pp 1-10 (2017)
Subject
Language
English
ISSN
2041-1723
Abstract
Epigenetic drugs are emerging as a powerful therapeutic option for cancer treatment. Here, the authors synthesized selective chemical probes that simultaneously inhibit the G9a and DNMTs methyltransferase activity and demonstrate their anti-tumour activity usingin vitro and in vivomodels of haematological neoplasia.