A balancing act: using small molecules for therapeutic intervention of the p53 pathway in cancer
| Autor: | Christian Gaiddon, Jessica J. Miller, Tim Storr |
|---|---|
| Přispěvatelé: | Universite de Strasbourg, Inserm UMR_S 1113, IRFAC, Institut National de la Santé et de la Recherche Médicale (INSERM) |
| Jazyk: | angličtina |
| Rok vydání: | 2020 |
| Předmět: |
[SDV]Life Sciences [q-bio]
Antineoplastic Agents Bioinformatics medicine.disease_cause Genome Small Molecule Libraries 03 medical and health sciences 0302 clinical medicine Intervention (counseling) Neoplasms medicine Humans [CHIM]Chemical Sciences Molecular Targeted Therapy ComputingMilieux_MISCELLANEOUS 030304 developmental biology 0303 health sciences Mutation P53 pathway business.industry Cancer General Chemistry medicine.disease Small molecule 3. Good health 030220 oncology & carcinogenesis Personalized medicine Tumor Suppressor Protein p53 business Function (biology) |
| Zdroj: | Chemical Society Reviews Chemical Society Reviews, Royal Society of Chemistry, 2020, 49 (19), pp.6995-7014. ⟨10.1039/d0cs00163e⟩ |
| ISSN: | 0306-0012 1460-4744 |
| DOI: | 10.1039/d0cs00163e⟩ |
| Popis: | Referred to as the "guardian of the genome", p53 is the most frequently mutated protein in cancer and almost all cancers exhibit malfunction along the p53 pathway. As an overexpressed and tumour-specific target, the past two decades have seen considerable dedication to the development of small molecules that aim to restore wild-type function in mutant p53. In this review we collect and communicate the chemical principles involved in small molecule drug design for misfolded proteins in anticancer therapy. While this approach has met with significant challenges including off-target mechanisms that induce cytotoxicity independent of p53 status, major technological advancements in gene sequencing capability and a shift towards personalized medicine holds significant promise for p53 reactivating compounds and could have widespread benefits for the field of cancer therapy. |
| Databáze: | OpenAIRE |
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