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Pharmacological rescue of mutant p53 conformation and function.
Foster, B A; Coffey, H A; Morin, M J; Rastinejad, F.
Afiliación
  • Foster BA; Department of Genomics, Targets, and Cancer Research, Pfizer Central Research, Eastern Point Road, Groton, CT 06340, USA.
Science ; 286(5449): 2507-10, 1999 Dec 24.
Article en En | MEDLINE | ID: mdl-10617466
Compounds that stabilize the DNA binding domain of p53 in the active conformation were identified. These small synthetic molecules not only promoted the stability of wild-type p53 but also allowed mutant p53 to maintain an active conformation. A prototype compound caused the accumulation of conformationally active p53 in cells with mutant p53, enabling it to activate transcription and to slow tumor growth in mice. With further work aimed at improving potency, this class of compounds may be developed into anticancer drugs of broad utility.
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirimidinas / Proteína p53 Supresora de Tumor / Neoplasias Experimentales / Antineoplásicos Límite: Animals / Humans Idioma: En Revista: Science Año: 1999 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos
Buscar en Google
Añadir a Mi BVS
Imprimir
XML
PubMed Links

Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirimidinas / Proteína p53 Supresora de Tumor / Neoplasias Experimentales / Antineoplásicos Límite: Animals / Humans Idioma: En Revista: Science Año: 1999 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos