Publication: Structure-based discovery of selective BRPF1 bromodomain inhibitors
Structure-based discovery of selective BRPF1 bromodomain inhibitors
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Zhu, J., Zhou, C., & Caflisch, A. (2018). Structure-based discovery of selective BRPF1 bromodomain inhibitors. European Journal of Medicinal Chemistry, 155, 337–352. https://doi.org/10.1016/j.ejmech.2018.05.037
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Abstract
Bromodomain and plant homeodomain (PHD) finger containing protein 1 (BRPF1) is a member of subfamily IV of the human bromodomains. Experimental evidence suggests that BRPF1 is involved in leukemia. In a previous high-throughput docking campaign we identified several chemotypes targeting the BRPF1 bromodomain. Here, pharmacophore searches using the binding modes of two of these chemotypes resulted in two new series of ligands of the BRPF1 bromodomain. The 2,3-dioxo-quinoxaline 21 exhibits a 2-μM affinity for the BRPF1 bromodomain in tw
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- Zhu, Jian
- Zhou, Chunxian
- Caflisch, Amedeo
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Zhu, J., Zhou, C., & Caflisch, A. (2018). Structure-based discovery of selective BRPF1 bromodomain inhibitors. European Journal of Medicinal Chemistry, 155, 337–352. https://doi.org/10.1016/j.ejmech.2018.05.037