A small-molecule p53 activator induces apoptosis through inhibiting MDMX expression in breast cancer cells.

ABSTRACT: The tumor suppressor p53 is often inactivated in breast cancer cells because the overexpression of its repressors (e.g., MDM2 and MDMX). Restoration of p53 activity by small molecules through counteracting p53 repressors can lead to in vivo tumor regression and is therefore considered a promising strategy for treatments of cancer. Recent efforts in high-throughput drug screening and rational drug design have identified several structurally diverse small-molecule p53 activators, including a pseudourea derivative XI-011 (NSC146109). This small molecule strongly activates p53 while selectively inhibiting growth of transformed cells without inducing genotoxicity, indicating its potential as a drug lead for p53-targeted therapy. However, the mechanism(s) by which XI-011 activates p53 and the ef

SUBMITTER: Wang H 

PROVIDER: S-EPMC3132847 | biostudies-literature | 2011 Jul

REPOSITORIES: biostudies-literature