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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Gepubliceerd in:Nat Commun
Hoofdauteurs: 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.
Formaat: Artigo
Taal:Inglês
Gepubliceerd in: Nature Publishing Group UK 2018
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Online toegang: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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