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Ras superfamily GEFs and GAPs: validated and tractable targets for cancer therapy?
Vigil, Dominico; Cherfils, Jacqueline; Rossman, Kent L; Der, Channing J.
Afiliación
  • Vigil D; University of North Carolina at Chapel Hill, Lineberger Comprehensive Cancer Center, Department of Pharmacology, Chapel Hill, North Carolina 27599, USA.
Nat Rev Cancer ; 10(12): 842-57, 2010 Dec.
Article en En | MEDLINE | ID: mdl-21102635
There is now considerable and increasing evidence for a causal role for aberrant activity of the Ras superfamily of small GTPases in human cancers. These GTPases function as GDP-GTP-regulated binary switches that control many fundamental cellular processes. A common mechanism of GTPase deregulation in cancer is the deregulated expression and/or activity of their regulatory proteins, guanine nucleotide exchange factors (GEFs) that promote formation of the active GTP-bound state and GTPase-activating proteins (GAPs) that return the GTPase to its GDP-bound inactive state. In this Review, we assess the association of GEFs and GAPs with cancer and their druggability for cancer therapeutics.
Asunto(s)

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Proteínas Activadoras de GTPasa / Factores de Intercambio de Guanina Nucleótido / Neoplasias Tipo de estudio: Etiology_studies Límite: Animals / Humans Idioma: En Revista: Nat Rev Cancer Asunto de la revista: NEOPLASIAS Año: 2010 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Proteínas Activadoras de GTPasa / Factores de Intercambio de Guanina Nucleótido / Neoplasias Tipo de estudio: Etiology_studies Límite: Animals / Humans Idioma: En Revista: Nat Rev Cancer Asunto de la revista: NEOPLASIAS Año: 2010 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido