Therapeutic Strategies to Activate p53

被引：18
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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