July 1st 2002
R115777 (Zarnestra) is an orally available methylquinolone derivative from Johnson & Johnson Pharmaceutical Research and Development L.L.C. that is a potent and selective nonpeptidomimetic farnesyltransferase inhibitor (FTI). FTIs represent a new class of agents that were originally developed to inhibit tumors by interfering with posttranslational processing of oncogenic Ras protein. The anticancer activity of FTIs might stem from their ability to effect various proteins other than Ras that can also mediate signal transduction, apoptosis, angiogenesis, and growth.