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

页码：716 / 721

页数：6

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