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pCAP-250 is a mutant-p53 reactivating peptide developed for the treatment of various cancers. It is a 9-amino acid peptide derived from the RAD9 protein, modified with an N-terminal myristic fatty acid to improve stability and pharmacokinetic properties. The peptide physically interacts with the DNA binding domain (DBD) of mutant p53, specifically targeting the L1 loop and Helix-2 regions to stabilize the wild-type protein conformation and restore transcriptional activity. In addition to its p53-dependent mechanism, pCAP-250 exhibits p53-independent anti-cancer activity. Preclinical studies have demonstrated efficacy in renal, colon, pancreatic, and ovarian cancer models, showing tumor regression and a favorable safety profile in non-transformed cells.
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