Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors
Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors
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Author / Creator
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. and Cole, Philip A.
Publisher
London: Nature Publishing Group UK
Journal title
Language
English
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Publication information
Publisher
London: Nature Publishing Group UK
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More information
Scope and Contents
Contents
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 with entinostat. Cell-based experiments demonstra...
Alternative Titles
Full title
Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors
Authors, Artists and Contributors
Author / Creator
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.
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Primary Identifiers
Record Identifier
TN_cdi_doaj_primary_oai_doaj_org_article_879832a39de54eeeb00cc6a12113408e
Permalink
https://devfeature-collection.sl.nsw.gov.au/record/TN_cdi_doaj_primary_oai_doaj_org_article_879832a39de54eeeb00cc6a12113408e
Other Identifiers
ISSN
2041-1723
E-ISSN
2041-1723
DOI
10.1038/s41467-017-02242-4