Small molecules that reactivate mutant p53.
Around half of all human tumours carry mutant p53. This allows escape from p53-induced cell cycle arrest and apoptosis. Many tumours express mutant p53 proteins at elevated levels. Restoration of wild-type p53 function should trigger massive apoptosis in tumour cells and thus eradicate tumours. Various types of small molecules have been identified that can restore native conformation and wild-type function to mutant p53. Such molecules may serve as leads for the development of novel efficient anticancer drugs.
Bykov
V J N
VJ
Department of Oncology-Pathology, Cancer Center Karolinska, SE-171 76 Stockholm, Sweden.
Selivanova
G
G
Wiman
K G
KG
D000972:Antineoplastic Agents, Phytogenic / Q000627:therapeutic use; D017209:Apoptosis / Q000235:genetics; D001372:Aza Compounds / Q000627:therapeutic use; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000627:therapeutic use; D004611:Ellipticines / Q000627:therapeutic use; D015972:Gene Expression Regulation, Neoplastic; D016158:Genes, p53 / Q000235:genetics*; D015316:Genetic Therapy / Q000379:methods; D006801:Humans; D008624:Mercaptoethylamines / Q000627:therapeutic use; D018832:Molecular Chaperones / Q000502:physiology; D009154:Mutation / Q000235:genetics*; D009369:Neoplasms / Q000235:genetics* / Q000473:pathology / Q000628:therapy; D011743:Pyrimidines / Q000627:therapeutic use
D000972:Antineoplastic Agents, Phytogenic; D001372:Aza Compounds; D019086:Bridged Bicyclo Compounds, Heterocyclic; D004611:Ellipticines; D008624:Mercaptoethylamines; D018832:Molecular Chaperones; D011743:Pyrimidines; C020174:N-(2-mercaptoethyl)-1,3-diaminopropane; C451219:2,2-bis(hydroxymethyl)-1-azabicyclo(2,2,2,)octan-3-one; C402665:CP 31398