Inhibition of farnesyltransferase: A rational approach to treat cancer?

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.

Keywords::

• Farnesyltransferase (FTase)
• farnesyltransferase inhibitors (FTIs)
• Comparative Molecular Field Analysis (CoMFA)

Acknowledgements

The work was supported by the All India Council for Technical Education, New Delhi, India, Grant No: 8021/RID/NPROJ/TAP-201/2002-03). One of the authors (DSP) would like to thank the University Grants Commission for the award of a junior research fellowship.