Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies

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 haematol...

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Autores principales:	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
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2017
Materias:	Science Q
Acceso en línea:	https://doaj.org/article/286f3156e84448249eb1c05f274be064
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spelling	oai:doaj.org-article:286f3156e84448249eb1c05f274be0642021-12-02T14:40:47ZDiscovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies10.1038/ncomms154242041-1723https://doaj.org/article/286f3156e84448249eb1c05f274be0642017-05-01T00:00:00Zhttps://doi.org/10.1038/ncomms15424https://doaj.org/toc/2041-1723Epigenetic 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.Edurne San José-EnérizXabier AgirreObdulia RabalAmaia Vilas-ZornozaJuan A. Sanchez-AriasEstibaliz MirandaAna UgarteSergio RoaBruno PaivaAnder Estella-Hermoso de MendozaRosa María AlvarezNoelia CasaresVictor SeguraJosé I. Martín-SuberoFrançois-Xavier OgiPierre SouleClara M. SantiveriRamón Campos-OlivasGiancarlo CastellanoMaite Garcia Fernandez de BarrenaJuan Roberto Rodriguez-MadozMaria José García-BarchinoJuan Jose LasarteMatias A AvilaJose Angel Martinez-ClimentJulen OyarzabalFelipe ProsperNature PortfolioarticleScienceQENNature Communications, Vol 8, Iss 1, Pp 1-10 (2017)
institution	DOAJ
collection	DOAJ
language	EN
topic	Science Q
spellingShingle	Science Q 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 Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies
description	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.
format	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
author_facet	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
author_sort	Edurne San José-Enériz
title	Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies
title_short	Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies
title_full	Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies
title_fullStr	Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies
title_full_unstemmed	Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies
title_sort	discovery of first-in-class reversible dual small molecule inhibitors against g9a and dnmts in hematological malignancies
publisher	Nature Portfolio
publishDate	2017
url	https://doaj.org/article/286f3156e84448249eb1c05f274be064
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Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies

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