p53-MDM2小分子抑制剂的研究进展

Title:Recent Advances of p53-MDM2 Small Molecule Inhibitors (2011-Present)

Volume: 22 Issue: 5

Author(s): Peng-Cheng Lv, Juan Sun and Hai-Liang Zhu

Affiliation:

关键词: 抗癌药物筛选，晶体结构，p53-MDM2抑制剂，蛋白质偶联，构效关系，基于结构的药物设计，移植瘤模型

摘要: P53 is an important transcriptional factor that plays a pivotal role in different biological process (cell cycle, apoptosis, DNA repair, angiogenesis and cellular metabolism). While p53 binds to the promoter and increases the gene expression of Mdm2, MDM2 protein directly binds to p53 and inhibits its activity. Therefore, inhibitor of p53 and MDM2 has been considered as a potential cancer therapeutic agent due to the critical inhibitory role of MDM2 on p53. Small-molecule inhibitor of p53-MDM2 has been designed to serve as an effective way to treat cancer. Several compounds have moved into different phase of clinical trials based on major advances in the development of small-molecule inhibitors in recent years. Since there are few reviews covering the structure- activity relationship analysis of recent p53-MDM2 inhibitors reported from 2011 to the present time, in this review, attentions are focused on the development of p53-MDM2 inhibitors published from 2011 to the present time.

Cite this article as:

Peng-Cheng Lv, Juan Sun and Hai-Liang Zhu , Recent Advances of p53-MDM2 Small Molecule Inhibitors (2011-Present), Current Medicinal Chemistry 2015; 22 (5) . https://dx.doi.org/10.2174/0929867322666141128162557