Recent research revealed that mutations in ras genes contribute to tumorigenesis in a number of tissues. In order to achieve a biologically active state during mitosis, Ras proteins need to undergo a number of post-translational modifications of which farnesylation is the most important one. Mutation of ras genes blocks the physiological dephosphorylating process of Ras proteins. This can result in tumour development and growth. Inhibition of farnesylation by farnesyltransferase inhibitors may prevent these processes. Several types of farnesyltransferase inhibitors have been developed, each with its own unique mechanism of interference. Pre-clinical studies revealed promising tumour regression in several models as well as limited side-effects. Several phase I Studies have been completed and currently phase II and III investigations are in progress focused on pancreatic and colon cancer. However, prior to routine use of these agents more clinical research is required to demonstrate efficacy and safety.
|Number of pages||6|
|Publication status||Published - 23 Feb 2001|