Recent Synthetic Approaches towards Small Molecule Reactivators of p53

• Published in: Biomolecules (Basel, Switzerland) Vol. 10; no. 4; p. 635
• Main Authors: Silva, Jerson L., Lima, Carolina G. S., Rangel, Luciana P., Ferretti, Giulia D. S., Pauli, Fernanda P., Ribeiro, Ruan C. B., da Silva, Thais de B., da Silva, Fernando C., Ferreira, Vitor F.
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 20.04.2020; MDPI
• Subjects: Analysis; Animals; Humans; Low molecular weight heparin; MDM2; mutant p53; Mutation - genetics; Oncogenes; Production processes; Review; Signal Transduction - drug effects; Small Molecule Libraries - chemistry; Small Molecule Libraries - pharmacology; Synthetic Biology - methods; Tumor proteins; Tumor suppressor genes; tumor suppressor p53 protein; Tumor Suppressor Protein p53 - genetics; Tumor Suppressor Protein p53 - metabolism; wild-type p53; Brazil; MDM2; mutant p53; tumor suppressor p53 protein; wild-type p53
• ISSN: 2218-273X; 2218-273X
• DOI: 10.3390/biom10040635

The tumor suppressor protein p53 is often called “the genome guardian” and controls the cell cycle and the integrity of DNA, as well as other important cellular functions. Its main function is to trigger the process of apoptosis in tumor cells, and approximately 50% of all cancers are related to the inactivation of the p53 protein through mutations in the TP53 gene. Due to the association of mutant p53 with cancer therapy resistance, different forms of restoration of p53 have been subject of intense research in recent years. In this sense, this review focus on the main currently adopted approaches for activation and reactivation of p53 tumor suppressor function, focusing on the synthetic approaches that are involved in the development and preparation of such small molecules.