4.1 Article

Design and synthesis of potent and selective inhibitors of BRD7 and BRD9 bromodomains

Journal

MEDCHEMCOMM
Volume 6, Issue 7, Pages 1381-1386

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c5md00152h

Keywords

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Funding

  1. AbbVie [1097737]
  2. Bayer
  3. Boehringer Ingelheim
  4. Canada Foundation for Innovation
  5. Canadian Institutes for Health Research
  6. Genome Canada
  7. GlaxoSmithKline
  8. Janssen
  9. Lilly Canada
  10. Merck
  11. Novartis Research Foundation
  12. Ontario Ministry of Economic Development and Innovation
  13. Pfizer
  14. Takeda
  15. Wellcome Trust [092809/Z/10/Z]
  16. European Union the Biotechnology and Biological Sciences Research Council (BBSRC)
  17. British Heart Foundation

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Emerging evidence suggests bromodomain-containing proteins 7 and 9 (BRD7 and BRD9) have roles in the regulation of human transcription and disease including cancer. We describe potent and selective inhibitors of the BRD7 and BRD9 bromodomains intended for use as tools to elucidate the biological roles of BRD7 and BRD9 in healthy and diseased cells.

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