Naphthyridines as novel BET family bromodomain inhibitors.

  title={Naphthyridines as novel BET family bromodomain inhibitors.},
  author={Olivier Mirguet and Yann Lamotte and Chun-Wa Chung and Paul Bamborough and Delphine Delann{\'e}e and Anne M Bouillot and Françoise J Gellibert and Gael Krysa and Antonia J Lewis and Jason Witherington and Pascal Huet and Yann Dudit and Lionel Trottet and Edwige Nicod{\`e}me},
  volume={9 3},
Bromodomains (BRDs) are small protein domains found in a variety of proteins that recognize and bind to acetylated histone tails. This binding affects chromatin structure and facilitates the localisation of transcriptional complexes to specific genes, thereby regulating epigenetically controlled processes including gene transcription and mRNA elongation. Inhibitors of the bromodomain and extra-terminal (BET) proteins BRD2-4 and T, which prevent bromodomain binding to acetyl-modified histone… CONTINUE READING


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Published online on

  • R. G. Gould, W. A. Jacobs, J. Am
  • Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim…
  • 1939
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