Abstract
Farnesyltransferase (FTase) is a major molecular target for the development of novel anticancer drugs that are designed to disrupt the aberrant signal transduction circuitry of tumor cells. The discovery more than a decade ago that farnesylation of Ras, one of the most prevalent oncoproteins in human cancers, is required for its cancer-causing activity was the initial stimulus to target FTase. However, it is now clear that yet to be identified farnesylated proteins other than Ras also play a pivotal role as targets for FTase inhibitors (FTIs). In this review, important mechanistic issues on the antiproliferative, pro-apoptotic and anti-angiogenic activities of FTIs, with an emphasis on potential FTI targets, will be discussed. Important clinical issues associated with translational aspects of hypotheses-driven clinical trials will also be discussed.
Original language | English (US) |
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Pages (from-to) | 1428-1435 |
Number of pages | 8 |
Journal | Current Opinion in Investigational Drugs |
Volume | 4 |
Issue number | 12 |
State | Published - Dec 2003 |
Keywords
- Farnesyltransferase
- Farnesyltransferase inhibitor
- Prenylation
- Ras
- RhoB
ASJC Scopus subject areas
- Pharmacology
- Drug Discovery