Discovery of Novel KRAS-PDE delta Inhibitors by Fragment-Based Drug Design

作者：Chen Long; Zhuang Chunlin; Lu Junjie; Jiang Yan; Sheng Chunquan^*

来源：Journal of Medicinal Chemistry, 2018, 61(6): 2604-2610.

DOI：10.1021/acs.jmedchem.8b00057

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Targeting KRAS-PDE delta protein-protein interactions with small molecules represents a promising opportunity for developing novel antitumor agents. However, current KRAS-PDE delta inhibitors are limited by poor cellular antitumor potency and the druggability of the target remains to be validated by new inhibitors. To tackle these challenges, herein, novel, highly potent KRAS-PDE delta inhibitors were identified by fragment-based drug design, providing promising lead compounds or chemical probes for investigating the biological functions and druggability of KRAS-PDE delta interaction.

• 出版日期2018-3-22
• 单位中国人民解放军第二军医大学