Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors
Alteration of the epigenetic landscape has been implicated in several disease processes, where targeting histone modifiers may have therapeutic applications. Here the authors report a bifunctional small molecule inhibitor that simultaneously targets the deacetylase (HDAC1) and demethylase (LSD1) act...
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Nature Portfolio
2018
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oai:doaj.org-article:879832a39de54eeeb00cc6a12113408e2021-12-02T16:49:17ZTargeting the CoREST complex with dual histone deacetylase and demethylase inhibitors10.1038/s41467-017-02242-42041-1723https://doaj.org/article/879832a39de54eeeb00cc6a12113408e2018-01-01T00:00:00Zhttps://doi.org/10.1038/s41467-017-02242-4https://doaj.org/toc/2041-1723Alteration of the epigenetic landscape has been implicated in several disease processes, where targeting histone modifiers may have therapeutic applications. Here the authors report a bifunctional small molecule inhibitor that simultaneously targets the deacetylase (HDAC1) and demethylase (LSD1) activities of the CoREST complex.Jay H. KalinMuzhou WuAndrea V. GomezYun SongJayanta DasDawn HaywardNkosi AdejolaMingxuan WuIzabela PanovaHye Jin ChungEdward KimHolly J. RobertsJustin M. RobertsPolina PrusevichJeliazko R. JeliazkovShourya S. Roy BurmanLouise FairallCharles MilanoAbdulkerim ErogluCharlotte M. ProbyAlbena T. Dinkova-KostovaWayne W. HancockJeffrey J. GrayJames E. BradnerSergio ValenteAntonello MaiNicole M. AndersMichelle A. RudekYong HuByungwoo RyuJohn W. R. SchwabeAndrea MatteviRhoda M. AlaniPhilip A. ColeNature PortfolioarticleScienceQENNature Communications, Vol 9, Iss 1, Pp 1-13 (2018) |
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Science Q Jay H. Kalin Muzhou Wu Andrea V. Gomez Yun Song Jayanta Das Dawn Hayward Nkosi Adejola Mingxuan Wu Izabela Panova Hye Jin Chung Edward Kim Holly J. Roberts Justin M. Roberts Polina Prusevich Jeliazko R. Jeliazkov Shourya S. Roy Burman Louise Fairall Charles Milano Abdulkerim Eroglu Charlotte M. Proby Albena T. Dinkova-Kostova Wayne W. Hancock Jeffrey J. Gray James E. Bradner Sergio Valente Antonello Mai Nicole M. Anders Michelle A. Rudek Yong Hu Byungwoo Ryu John W. R. Schwabe Andrea Mattevi Rhoda M. Alani Philip A. Cole Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors |
description |
Alteration of the epigenetic landscape has been implicated in several disease processes, where targeting histone modifiers may have therapeutic applications. Here the authors report a bifunctional small molecule inhibitor that simultaneously targets the deacetylase (HDAC1) and demethylase (LSD1) activities of the CoREST complex. |
format |
article |
author |
Jay H. Kalin Muzhou Wu Andrea V. Gomez Yun Song Jayanta Das Dawn Hayward Nkosi Adejola Mingxuan Wu Izabela Panova Hye Jin Chung Edward Kim Holly J. Roberts Justin M. Roberts Polina Prusevich Jeliazko R. Jeliazkov Shourya S. Roy Burman Louise Fairall Charles Milano Abdulkerim Eroglu Charlotte M. Proby Albena T. Dinkova-Kostova Wayne W. Hancock Jeffrey J. Gray James E. Bradner Sergio Valente Antonello Mai Nicole M. Anders Michelle A. Rudek Yong Hu Byungwoo Ryu John W. R. Schwabe Andrea Mattevi Rhoda M. Alani Philip A. Cole |
author_facet |
Jay H. Kalin Muzhou Wu Andrea V. Gomez Yun Song Jayanta Das Dawn Hayward Nkosi Adejola Mingxuan Wu Izabela Panova Hye Jin Chung Edward Kim Holly J. Roberts Justin M. Roberts Polina Prusevich Jeliazko R. Jeliazkov Shourya S. Roy Burman Louise Fairall Charles Milano Abdulkerim Eroglu Charlotte M. Proby Albena T. Dinkova-Kostova Wayne W. Hancock Jeffrey J. Gray James E. Bradner Sergio Valente Antonello Mai Nicole M. Anders Michelle A. Rudek Yong Hu Byungwoo Ryu John W. R. Schwabe Andrea Mattevi Rhoda M. Alani Philip A. Cole |
author_sort |
Jay H. Kalin |
title |
Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors |
title_short |
Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors |
title_full |
Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors |
title_fullStr |
Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors |
title_full_unstemmed |
Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors |
title_sort |
targeting the corest complex with dual histone deacetylase and demethylase inhibitors |
publisher |
Nature Portfolio |
publishDate |
2018 |
url |
https://doaj.org/article/879832a39de54eeeb00cc6a12113408e |
work_keys_str_mv |
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