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Updated: Jun 21, 2026

Förster Resonance Energy Transfer Mapping: A New Methodology to Elucidate Global Structural Features
Published on: March 16, 2022
Farnesyl protein transferase: a review of structural studies
1Schering-Plough Research Institute, Kenilworth, NJ 07033-0539, USA.
Abstract:
Emerging therapies for the treatment of cancer rely on detailed knowledge of cell growth mechanisms. It is hoped that mechanism-based inhibitors will prove more effective and exhibit fewer side effects than current treatments. Among the first, non-cytotoxic anticancer agents to enter clinical trials are the farnesyl protein transferase inhibitors, which prevent attachment of the farnesyl isoprenoid side chain to Ras. This post-translational modification is essential for the function of Ras, a protein exhibiting unregulated activity in nearly one-third of human cancers. Here structural studies of farnesyl protein transferase and strategies for discovery of its inhibitors are reviewed.
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