title: Farnesyl protein transferase: a review of structural studies.
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.
authors: Schering-Plough Research Institute, Kenilworth, NJ 07033-0539, USA.
authors: C L
authors: CL
authors: Strickland
authors: P C
authors: PC
authors: Weber