化学
平方毫米
药理学
效力
小分子
计算生物学
体外
生物化学
细胞凋亡
医学
生物
作者
Qianqian Ding,Zhuming Zhang,Jinjun Liu,Nan Jiang,Jing Zhang,Tina Morgan Ross,Xin‐Jie Chu,David Bartkovitz,Frank J. Podlaski,Cheryl A. Janson,Christian Tovar,Zoran Filipovic,Brian Higgins,Kelli Glenn,Kathryn Packman,Lyubomir T. Vassilev,Bradford Graves
摘要
Restoration of p53 activity by inhibition of the p53–MDM2 interaction has been considered an attractive approach for cancer treatment. However, the hydrophobic protein–protein interaction surface represents a significant challenge for the development of small-molecule inhibitors with desirable pharmacological profiles. RG7112 was the first small-molecule p53–MDM2 inhibitor in clinical development. Here, we report the discovery and characterization of a second generation clinical MDM2 inhibitor, RG7388, with superior potency and selectivity.
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