Therapeutic Strategies to Activate p53

被引：20

作者：

Aguilar, Angelo ^{[1
]}

Wang, Shaomeng ^{[1
]}

机构：

[1] Univ Michigan, Dept Internal Med Pharmacol & Med Chem, Rogel Canc Ctr, Ann Arbor, MI 48109 USA

来源：

PHARMACEUTICALS | 2023年 / 16卷 / 01期

基金：

美国国家卫生研究院;

关键词：

wild-type p53; mutant p53; activators; MDM2; MDMX; Y220C; inhibitors; PROTACS; degraders; molecular glue; STRUCTURE-BASED DESIGN; PHASE-I TRIAL; MOLECULE MDM2 INHIBITOR; MUTANT P53; STRUCTURAL BASIS; HIGHLY POTENT; DNA-BINDING; SUBSTITUTED PIPERIDINES; FUNCTIONAL-PROPERTIES; P53-MDM2; INTERACTION;

D O I：

10.3390/ph16010024

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The p53 protein has appropriately been named the "guardian of the genome". In almost all human cancers, the powerful tumor suppressor function of p53 is compromised by a variety of mechanisms, including mutations with either loss of function or gain of function and inhibition by its negative regulators MDM2 and/or MDMX. We review herein the progress made on different therapeutic strategies for targeting p53.

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页数：39

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