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Naphthyridines as Novel BET Family Bromodomain Inhibitors
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… Expand
From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151.
- O. Mirguet, Yann Lamotte, +21 authors E. Nicodème
- Medicine, Chemistry
- Bioorganic & medicinal chemistry letters
- 15 April 2012
The discovery, synthesis and biological evaluation of a novel series of 7-isoxazoloquinolines is described. Several analogs are shown to increase ApoA1 expression within the nanomolar range in the… Expand
The first bromodomain of human BRD4 in complex with 3,5 dimethylisoxaxole ligand