Therapeutic Strategies to Activate p53

Angelo Aguilar; Shaomeng Wang

doi:10.3390/ph16010024

Therapeutic Strategies to Activate p53

Pharmaceuticals (Basel). 2022 Dec 24;16(1):24. doi: 10.3390/ph16010024.

Authors

Angelo Aguilar¹, Shaomeng Wang¹

Affiliation

¹ The Rogel Cancer Center, Departments of Internal Medicine, Pharmacology and Medicinal Chemistry, University of Michigan, Ann Arbor, MI 48109, USA.

Abstract

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.

Keywords: MDM2; MDMX; PROTACS; Y220C; activators; degraders; inhibitors; molecular glue; mutant p53; wild-type p53.

Publication types

Review

Abstract

Publication types

Grants and funding