Tomorrow's anticancer agents: inhibitors of Ras farnesylation.
The purpose of this chapter is to concentrate on what can be considered as definite milestones on the way from examples of inhibitors of farnesyl-protein transferase (FPTase) to candidate drugs actually being considered for or already being evaluated in clinical trials. Emphasis will be placed on results obtained using experimental tumour models in vivo, with a detailed discussion of these results and of the questions which remain to be studied or are still unanswered. The data discussed here are almost exclusively based on published reports, with only brief reference, in the chapter "use of the FPTase inhibitors in the clinic", to some of the newer compounds reported on during recent meetings, details of which have not yet appeared in the peer-reviewed literature. For those requiring a more extensive review of the catalogue of FPTase inhibitors now discovered, some excellent reviews have been committed to this purpose [1-3].
Perrin
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Division de Cancérologie Expérimentale, Centre de Recherche Pierre Fabre, Castres, France.
Hill
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D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002455:Cell Division / Q000187:drug effects; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy; D017368:Protein Prenylation / Q000187:drug effects*; D015398:Signal Transduction; D018631:ras Proteins / Q000378:metabolism*
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D019883:Alkyl and Aryl Transferases; C064911:p21(ras) farnesyl-protein transferase; D018631:ras Proteins