Nature Communications (Jan 2018)
Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors
- 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
Affiliations
- Jay H. Kalin
- Division of Genetics, Departments of Medicine and Biological Chemistry and Molecular Pharmacology, Harvard Medical School and Brigham and Women’s Hospital
- Muzhou Wu
- Department of Dermatology, Boston University School of Medicine
- Andrea V. Gomez
- Department of Biology and Biotechnology, University of Pavia
- Yun Song
- Department of Molecular and Cell Biology, University of Leicester
- Jayanta Das
- Department of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine
- Dawn Hayward
- Department of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine
- Nkosi Adejola
- Department of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine
- Mingxuan Wu
- Division of Genetics, Departments of Medicine and Biological Chemistry and Molecular Pharmacology, Harvard Medical School and Brigham and Women’s Hospital
- Izabela Panova
- Department of Dermatology, Boston University School of Medicine
- Hye Jin Chung
- Department of Dermatology, Boston University School of Medicine
- Edward Kim
- Department of Dermatology, Boston University School of Medicine
- Holly J. Roberts
- Department of Dermatology, Boston University School of Medicine
- Justin M. Roberts
- Department of Medical Oncology, Dana-Farber Cancer Institute
- Polina Prusevich
- Department of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine
- Jeliazko R. Jeliazkov
- Program in Molecular Biophysics, Johns Hopkins University
- Shourya S. Roy Burman
- Department of Chemical and Biomolecular Engineering, Johns Hopkins University
- Louise Fairall
- Department of Molecular and Cell Biology, University of Leicester
- Charles Milano
- Department of Molecular and Cell Biology, University of Leicester
- Abdulkerim Eroglu
- Department of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine
- Charlotte M. Proby
- Division of Cancer Research, Jacqui Wood Cancer Centre, University of Dundee
- Albena T. Dinkova-Kostova
- Department of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine
- Wayne W. Hancock
- Department of Pathology and Laboratory Medicine, University of Pennsylvania School of Medicine
- Jeffrey J. Gray
- Program in Molecular Biophysics, Johns Hopkins University
- James E. Bradner
- Department of Medical Oncology, Dana-Farber Cancer Institute
- Sergio Valente
- Pasteur Institute, Cenci-Bolognetti Foundation, Department of Drug Chemistry and Technologies, Sapienza University of Rome
- Antonello Mai
- Pasteur Institute, Cenci-Bolognetti Foundation, Department of Drug Chemistry and Technologies, Sapienza University of Rome
- Nicole M. Anders
- Sidney Kimmel Comprehensive Cancer Center, Johns Hopkins University School of Medicine
- Michelle A. Rudek
- Sidney Kimmel Comprehensive Cancer Center, Johns Hopkins University School of Medicine
- Yong Hu
- Department of Oncology, BioDuro LLC
- Byungwoo Ryu
- Department of Dermatology, Boston University School of Medicine
- John W. R. Schwabe
- Department of Molecular and Cell Biology, University of Leicester
- Andrea Mattevi
- Department of Biology and Biotechnology, University of Pavia
- Rhoda M. Alani
- Department of Dermatology, Boston University School of Medicine
- Philip A. Cole
- Division of Genetics, Departments of Medicine and Biological Chemistry and Molecular Pharmacology, Harvard Medical School and Brigham and Women’s Hospital
- DOI
- https://doi.org/10.1038/s41467-017-02242-4
- Journal volume & issue
-
Vol. 9,
no. 1
pp. 1 – 13
Abstract
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.
