Discovery of Potent and Selective p53-MDM2 Protein-Protein Interaction Inhibitors as Anticancer Drugs

被引：15
|
作者：
Holzer, Philipp [1 ]
机构：
[1] Novartis Inst BioMed Res, CH-4002 Basel, Switzerland
来源：
CHIMIA | 2017年 / 71卷 / 10期
关键词：
Clinical trial; HDM2; Inhibitor; MDM2; NVP-CGM097; NVP-HDM201; p53; Protein-protein interaction; PPI; STRUCTURE-BASED DESIGN; P53; PATHWAY; MDM2-P53; INTERACTION; HIGHLY POTENT; ANTAGONISTS; CANCER; TUMORS;
D O I：
10.2533/chimia.2017.716
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
As a result of our persistent efforts to discover novel inhibitors of the p53-MDM2 protein-protein interaction useful for the treatment of cancer, the potent and selective MDM2 inhibitors NVP-CGM097 and NVP-HDM201 with excellent in vitro and in vivo profile were selected as clinical candidates and are currently in phase 1 clinical development. This short review article provides a summary of the program history, the applied pharmacophore model and the discovery story of these novel p53-MDM2 inhibitor investigational drugs.
引用
收藏
页码：716 / 721
页数：6
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