Small-molecule modulators of p53 family signaling and antitumor effects in p53-deficient human colon tumor xenografts.

ABSTRACT: p53 deficiency is common in almost all human tumors and contributes to an aggressive chemo- or radiotherapy-resistant phenotype, therefore providing a target for drug development. Molecular targeting to restore wild-type p53 activity has been attempted in drug development and has led to the identification of CP-31398, PRIMA1, and the Nutlins. However, strategies targeting p53-activated transcriptional responses or p53 family member expression in p53-deficient tumors have yet to be explored. Here we demonstrate the use of noninvasive bioluminescence imaging in a high-throughput cell-based screen of small molecules that activate p53 responses and cell death in human tumor cells carrying a mutant p53. We isolated a number of small molecules that activate p53 reporter activity, increase expres

SUBMITTER: Wang W 

PROVIDER: S-EPMC1544164 | biostudies-literature | 2006 Jul

REPOSITORIES: biostudies-literature