Farnesyltransferase/Geranylgeranyltransferase Inhibitor L-778,123

**Semantic type:** Organic Chemical|Pharmacologic Substance

**Definition:** A benzonitrile derivative capable of inhibiting some prenyltransferases. L-778,123 is a dual inhibitor of farnesyl:protein and geranylgeranyl:protein transferases; both enzymes catalyze prenylation of oncoprotein KRAS, a prerequisite step in activation of KRAS in signal transduction pathway of apoptosis. Although this agent was developed in part as an anti-KRAS agent, L-778,123 failed in a Phase I trial to inhibit KRAS, which is associated with many types of solid tumors.

**Synonyms:** - 4-[[5-[[4-(3-Chlorophenyl)-3-oxo-1-piperazinyl]methyl]-1H-imidazol-1-yl]methyl]benzonitrile Monohydrochloride - 4-[[5-[[4-(3-Chlorophenyl)-3-oxo-1-piperazinyl]methyl]-1H-imidazol-1-yl]methyl]benzonitrile Monohydrochloride - L 778123 - L-778,123 - L-778123 - L-778123