John Libbey Eurotext

Bulletin du Cancer


Inhibitors of Ras farnesylation: tomorrow’s anticancer agents? Volume 84, issue 6, Juin 1997


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Division de cancérologie expérimentale, Centre de recherche Pierre-Fabre, 17, avenue Jean-Moulin, 81106 Castres Cedex, France.

Des observations convergentes ont montré que l’activation constitutive de Ras joue un rôle important dans la cancérogenèse humaine, entraînant la recherche de produits inhibant Ras, à des fins thérapeutiquesAbstract – Increasing evidence implicates a critical role for aberrant Ras function in promoting the development of human tumours and has provided the impetus for identifying anti-Ras drugs for therapy. In order to be active the protooncogene ras must be associated with the plasma membrane. This feature depends crucially upon its farnesylation (addition of a 15 carbon moiety) by the enzyme farnesyl protein transferase. In the search for new anticancer strategies and agents, potent and selective inhibitors of this enzyme have been designed. The more recent of these compounds have produced impressive results in vivo against human tumours xenografted onto nude mice, without notable toxicity, making them promising candidates for clinical evaluation.