Abstract
This article presents in brief the development of farnesyltransferase inhibitors (FTIs) and their preclinical and clinical status. In this review the mechanism of action of FTIs is discussed and their selectivity issue towards tumor cells is also addressed. The significant efficacy of FTIs as single or combined agents in preclinical studies stands in contrast with only moderate effects in Clinical Phase II-III studies. This suggests that there is a need to further explore and understand the complex mechanism of action of FTIs and their interaction with cytotoxic agents.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / pharmacology
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Antineoplastic Agents / therapeutic use*
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Cell Cycle / drug effects
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Drug Design*
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Drug Evaluation, Preclinical
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Enzyme Inhibitors / chemistry*
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Enzyme Inhibitors / pharmacology
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Enzyme Inhibitors / therapeutic use*
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Farnesyltranstransferase / antagonists & inhibitors*
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Farnesyltranstransferase / chemistry
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Humans
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Models, Molecular
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Neoplasms / drug therapy
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Neoplasms / enzymology
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Protein Conformation
Substances
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Antineoplastic Agents
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Enzyme Inhibitors
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Farnesyltranstransferase