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Tomorrow's anticancer agents: inhibitors of Ras farnesylation
1Division de Cancérologie Expérimentale, Centre de Recherche Pierre Fabre, Castres, France.
Abstract:
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].
Insights
This chapter reviews milestones in developing farnesyl-protein transferase (FPTase) inhibitors from experimental models to clinical trials. It emphasizes in vivo tumor model results and remaining research questions for these anticancer drug candidates.
Area of Science:
- Oncology
- Pharmacology
- Biochemistry
Background:
- Farnesyl-protein transferase (FPTase) inhibitors represent a class of compounds investigated for their therapeutic potential.
- The development pathway from initial discovery to clinical application involves rigorous preclinical and clinical evaluation.
- Understanding milestones in this process is crucial for advancing cancer drug development.
Purpose of the Study:
- To outline key milestones in the progression of farnesyl-protein transferase (FPTase) inhibitors.
- To focus on the transition from early inhibitor examples to drug candidates in clinical trials.
- To critically discuss results from experimental in vivo tumor models.
Main Methods:
- Review of published literature on farnesyl-protein transferase (FPTase) inhibitors.
- Emphasis on data derived from experimental in vivo tumor models.
- Discussion of results and identification of unanswered questions in the field.
Main Results:
- Identification of significant advancements in FPTase inhibitor development.
- Detailed analysis of efficacy and challenges observed in preclinical tumor models.
- Highlighting the current status of FPTase inhibitors in clinical evaluation.
Conclusions:
- Farnesyl-protein transferase (FPTase) inhibitors have progressed through distinct developmental stages.
- In vivo experimental models provide critical data for advancing these compounds.
- Further research is needed to address remaining questions and optimize clinical application.