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Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors

Here we report corin, a synthetic hybrid agent derived from the class I HDAC inhibitor (entinostat) and an LSD1 inhibitor (tranylcypromine analog). Enzymologic analysis reveals that corin potently targets the CoREST complex and shows more sustained inhibition of CoREST complex HDAC activity compared...

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Detalhes bibliográficos
Publicado no:Nat Commun
Main Authors: Kalin, Jay H., Wu, Muzhou, Gomez, Andrea V., Song, Yun, Das, Jayanta, Hayward, Dawn, Adejola, Nkosi, Wu, Mingxuan, Panova, Izabela, Chung, Hye Jin, Kim, Edward, Roberts, Holly J., Roberts, Justin M., Prusevich, Polina, Jeliazkov, Jeliazko R., Roy Burman, Shourya S., Fairall, Louise, Milano, Charles, Eroglu, Abdulkerim, Proby, Charlotte M., Dinkova-Kostova, Albena T., Hancock, Wayne W., Gray, Jeffrey J., Bradner, James E., Valente, Sergio, Mai, Antonello, Anders, Nicole M., Rudek, Michelle A., Hu, Yong, Ryu, Byungwoo, Schwabe, John W. R., Mattevi, Andrea, Alani, Rhoda M., Cole, Philip A.
Formato: Artigo
Idioma:Inglês
Publicado em: Nature Publishing Group UK 2018
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC5754352/
https://ncbi.nlm.nih.gov/pubmed/29302039
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/s41467-017-02242-4
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