Drug intelligence / Profile preview

SAH-p53-8

Development stage
Preclinical
Lead developer
Dana-Farber Cancer Institute
Modality
Peptides
Administration
Intravenous, Intratumoral
01

Overview

SAH-p53-8 is a hydrocarbon-stapled alpha-helical peptide designed to mimic the transactivation domain of the p53 tumor suppressor protein. It functions as a dual inhibitor of the p53-MDM2 (HDM2) and p53-MDMX (HDMX) interactions. By competitively binding to the p53-binding pockets of these negative regulators, SAH-p53-8 prevents the ubiquitination and degradation of p53, thereby restoring its ability to induce cell cycle arrest and apoptosis in cancer cells harboring wild-type p53. Preclinical studies, particularly in metastatic melanoma, have shown that SAH-p53-8 can sensitize tumor cells to conventional chemotherapy and arrest tumor growth in vivo.

Other names
stapled p53 helix 8
02

Targets

MDM4 (Mouse double minute X homolog)MDM2 (Mouse double minute 2 homolog)

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