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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Nature Publishing Group
2017-05-01
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| Series: | Nature Communications |
| Online Access: | https://doi.org/10.1038/ncomms15424 |
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doaj-286f3156e84448249eb1c05f274be0642021-05-11T07:26:04ZengNature Publishing GroupNature Communications2041-17232017-05-018111010.1038/ncomms15424Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignanciesEdurne San José-Enériz0Xabier Agirre1Obdulia Rabal2Amaia Vilas-Zornoza3Juan A. Sanchez-Arias4Estibaliz Miranda5Ana Ugarte6Sergio Roa7Bruno Paiva8Ander Estella-Hermoso de Mendoza9Rosa María Alvarez10Noelia Casares11Victor Segura12José I. Martín-Subero13François-Xavier Ogi14Pierre Soule15Clara M. Santiveri16Ramón Campos-Olivas17Giancarlo Castellano18Maite Garcia Fernandez de Barrena19Juan Roberto Rodriguez-Madoz20Maria José García-Barchino21Juan Jose Lasarte22Matias A Avila23Jose Angel Martinez-Climent24Julen Oyarzabal25Felipe Prosper26Area de Hemato-Oncología, Centro de Investigación Médica Aplicada, IDISNA, Ciberonc, Universidad de NavarraArea de Hemato-Oncología, Centro de Investigación Médica Aplicada, IDISNA, Ciberonc, Universidad de NavarraSmall Molecule Discovery Platform, Molecular Therapeutics Program, Center for Applied Medical Research, University of NavarraArea de Hemato-Oncología, Centro de Investigación Médica Aplicada, IDISNA, Ciberonc, Universidad de NavarraSmall Molecule Discovery Platform, Molecular Therapeutics Program, Center for Applied Medical Research, University of NavarraArea de Hemato-Oncología, Centro de Investigación Médica Aplicada, IDISNA, Ciberonc, Universidad de NavarraSmall Molecule Discovery Platform, Molecular Therapeutics Program, Center for Applied Medical Research, University of NavarraArea de Hemato-Oncología, Centro de Investigación Médica Aplicada, IDISNA, Ciberonc, Universidad de NavarraArea de Hemato-Oncología, Centro de Investigación Médica Aplicada, IDISNA, Ciberonc, Universidad de NavarraSmall Molecule Discovery Platform, Molecular Therapeutics Program, Center for Applied Medical Research, University of NavarraSmall Molecule Discovery Platform, Molecular Therapeutics Program, Center for Applied Medical Research, University of NavarraArea de Terapia Génica y Hepatología, Centro de Investigación Médica Aplicada, Universidad de NavarraUnidad de Bioinformática, Centro de Investigación Médica Aplicada, Universidad de NavarraDepartamento de Fundamentos Clínicos, Universitat de Barcelona, Institut d’Investigacions Biomèdiques August Pi i SunyerNanotemper Technologies GmbHNanotemper Technologies GmbHSpectroscopy and NMR Unit, Spanish National Cancer Research Center (CNIO)Spectroscopy and NMR Unit, Spanish National Cancer Research Center (CNIO)Departamento de Fundamentos Clínicos, Universitat de Barcelona, Institut d’Investigacions Biomèdiques August Pi i SunyerArea de Terapia Génica y Hepatología, Centro de Investigación Médica Aplicada, Universidad de NavarraArea de Hemato-Oncología, Centro de Investigación Médica Aplicada, IDISNA, Ciberonc, Universidad de NavarraArea de Hemato-Oncología, Centro de Investigación Médica Aplicada, IDISNA, Ciberonc, Universidad de NavarraArea de Terapia Génica y Hepatología, Centro de Investigación Médica Aplicada, Universidad de NavarraArea de Terapia Génica y Hepatología, Centro de Investigación Médica Aplicada, Universidad de NavarraArea de Hemato-Oncología, Centro de Investigación Médica Aplicada, IDISNA, Ciberonc, Universidad de NavarraSmall Molecule Discovery Platform, Molecular Therapeutics Program, Center for Applied Medical Research, University of NavarraArea de Hemato-Oncología, Centro de Investigación Médica Aplicada, IDISNA, Ciberonc, Universidad de NavarraEpigenetic 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.https://doi.org/10.1038/ncomms15424 |
| collection |
DOAJ |
| language |
English |
| format |
Article |
| sources |
DOAJ |
| 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 |
| spellingShingle |
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 Nature Communications |
| 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 Publishing Group |
| series |
Nature Communications |
| issn |
2041-1723 |
| publishDate |
2017-05-01 |
| 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. |
| url |
https://doi.org/10.1038/ncomms15424 |
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