Farnesyl Protein Transferase Inhibition: A Novel Approach to Anti-tumor
Abstract:Farnesyl protein transferase (FPT) inhibition is an interesting and promising approach to non-cytotoxic anticancer therapy. Research in this area has resulted in several orally active compounds that are currently in clinical evaluation. This review focuses on FPT inhibitors in clinical trials and concentrates on the benzocycloheptapyridine class, with details on the discovery and development of SCH 66336, currently in Phase II clinical trials.
Keywords: Anti-tumor Therapy; COS Assay; FPT Enzyme Assay; Farnesyl Protein Transferase Inhibition; Farnesylation; Geranlylgeranylation; Pharmacokinetic Assay (PK); Potent FPT Inhibitors; carboxymethyl transferase; farnesyl protein transferase
Document Type: Review Article
Publication date: October 1, 2001
- Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.