In vitro and in vivo activity of a new small-molecule inhibitor of HDAC6 in mantle cell lymphoma

Cancer origin and development is associated not only with genetic alterations, but also with the disturbance of epigenetic profiles.1 In this regard, the tumoral epigenome is characterized by both specific and general shifts in the DNA methylation and histone-modification landscapes.1 However, in co...

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Detalhes bibliográficos
Autores: Pérez Salvia, Montserrat, Aldaba, Eneko, Vara, Yosu, Fabre, Myriam, Ferrer, Cristina, Masdeu, Carme, Zubia, Aizpea, San Sebastian, Eider, Otaegui, Dorleta, Llinàs-Arias, Pere, Rosselló-Tortella, Margalida, Berdasco, María, Moutinho, Cátia, Setién, Fernando, Villanueva Garatachea, Alberto, González Barca, Eva, Muncunill, Josep, Navarro, José-Tomás, Piris, Miguel A., Cossio, Fernando P., Esteller, Manel
Tipo de documento: artigo
Estado:Versão publicada
Data de publicação:2018
País:España
Recursos:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
Repositório:Recercat. Dipósit de la Recerca de Catalunya
OAI Identifier:oai:recercat.cat:2445/133681
Acesso em linha:https://hdl.handle.net/2445/133681
Access Level:Acceso aberto
Palavra-chave:Inhibidors enzimàtics
Histones
Cèl·lules T
Limfomes
Epigenètica
Enzyme inhibitors
T cells
Lymphomas
Epigenetics
Descrição
Resumo:Cancer origin and development is associated not only with genetic alterations, but also with the disturbance of epigenetic profiles.1 In this regard, the tumoral epigenome is characterized by both specific and general shifts in the DNA methylation and histone-modification landscapes.1 However, in contrast to genetic disruption, the effect of epigenetic modifications or marks may potentially be reversed by the use of drugs that target enzymes involved in adding, removing or signaling DNA methylation and histone modifications.1 This basic knowledge has been adopted into clinical practice, and inhibitors of histone deacetylases and DNA demethylating agents have been approved for use in the therapy of hematologic malignancies, such as cutaneous T-cell lymphoma and myelodysplastic syndrome, respectively.2 Other promising epigenetic drugs include inhibitors of histone methyltransferases,2 histone demethylases,2 histone kinases,3 and bromodomain proteins that interfere with the 'reading' of acetylated histone residues.

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