p53
The p53 tumor suppressor is a 53 kDa nuclear phosphoprotein of 393 amino acids that is encoded by the TP53 gene (20 kb with 11 exons and 10 introns) and characterized by the presence of several structural and functional domains, including a N-terminus, a central core domain, a C-terminal region, a strongly basic carboxyl-terminal regulatory domain, a nuclear localization signal sequence and three nuclear export signal sequence. The p53 is considered as a major “guardian of genome” for its activities in a wide range of cellular events, including cell-cycle regulation, induction of apoptosis, gene amplification, DNA recombination, chromosomal segregation and cellular senescence.
- A4208 NSC 319726Target: p53Summary: Reactivator of mutant p53
- A4228 Nutlin-3Target: MDM2Summary: MDM2 antagonist,inhibits MDM2-p53 interaction
- A4206 Pifithrin-α (PFTα)2 CitationTarget: p53Summary: p53 inhibitor
- A4204 JNJ-26854165 (Serdemetan)1 CitationTarget: p53|HDM2 ubiquitin ligaseSummary: P53 activator, blocking Mdm2-p53 interaction
- A4203 Tenovin-1Target: Sir2-like Family Deacetylases (Sirtuins)|p53|p21Summary: SIRT2 inhibitor, activates p53
- A4202 RITA (NSC 652287)Summary: Mdm2-p53 interaction and p53 ubiquitination blocking
- A3671 Nutlin-3a chiral2 CitationSummary: MDM2 inhibitor, antiproliferative and antiproapoptotic
- A3762 RG71125 CitationTarget: MDM2Summary: MDM2 inhibitor, first clinical
- A3763 RG73882 CitationSummary: MDM2 antagonist, oral, selective
- A8724 ONC201Summary: activates p53-independent apoptosis