A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors.

@article{Bronner2017AUA,
  title={A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors.},
  author={Sarah M Bronner and Jeremy M Murray and F Anthony Romero and Kwong Wah Lai and Vickie Tsui and Patrick Cyr and Maureen H. Beresini and Gladys de Leon Boenig and Zhongguo Chen and Edna F Choo and Kevin J. R. Clark and T. Daniel Crawford and H. Jayaram and Susan Kaufman and Ruina Li and Yingjie Li and Jiangpeng Liao and Xiaorong Liang and Wenfeng F. Liu and Justin Q. Ly and Jonathan M Maher and John Wai and Fei Wang and Aijun Zheng and Xiaoyu Zhu and Steven R Magnuson},
  journal={Journal of medicinal chemistry},
  year={2017},
  volume={60 24},
  pages={10151-10171}
}
The epigenetic regulator CBP/P300 presents a novel therapeutic target for oncology. Previously, we disclosed the development of potent and selective CBP bromodomain inhibitors by first identifying pharmacophores that bind the KAc region and then building into the LPF shelf. Herein, we report the "hybridization" of a variety of KAc-binding fragments with a… CONTINUE READING