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Farnesyltransferase inhibitors as anticancer agents: current status
Kuichun Zhu1, Andrew D Hamilton, Saïd M Sebti
1Drug Discovery Program, H Lee Moffitt Cancer Center & Research Institute, Department of Interdisciplinary Oncology, University of South Florida College of Medicine, 12902 Magnolia Drive, Tampa, FL 33612, USA.
Current Opinion in Investigational Drugs (London, England : 2000)
|February 7, 2004
Summary
Farnesyltransferase inhibitors (FTIs) target cancer cell signaling by blocking protein farnesylation. This review explores FTIs' mechanisms, targets beyond Ras, and clinical trial considerations for anticancer drug development.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- Farnesyltransferase (FTase) is a key target for anticancer drug development.
- Targeting FTase disrupts aberrant signal transduction in tumor cells.
- Ras oncoprotein farnesylation is crucial for its cancer-promoting activity.
Purpose of the Study:
- To review the mechanistic aspects of FTase inhibitors (FTIs).
- To discuss antiproliferative, pro-apoptotic, and anti-angiogenic effects of FTIs.
- To highlight potential FTI targets beyond Ras and clinical trial considerations.
Main Methods:
- Literature review of FTase inhibitors and their mechanisms.
- Analysis of preclinical and clinical data on FTIs.
- Discussion of signaling pathways affected by FTIs.
Main Results:
- FTIs exhibit antiproliferative, pro-apoptotic, and anti-angiogenic activities.
- Proteins other than Ras are also farnesylated and are potential FTI targets.
- Clinical translation of FTIs faces challenges related to target identification and trial design.
Conclusions:
- FTIs represent a promising class of anticancer agents with diverse mechanisms.
- Further research is needed to identify all relevant FTI targets and optimize clinical strategies.
- FTIs hold potential for treating various human cancers by modulating critical cellular pathways.
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