Novel Prenyl Transferase Inhibitors

A series of farnesol and geranylgeraniol analogs that block the prenylation of proteins in cells. The diphosphate derivatives of these compounds are potent inhibitors of protein prenyltransferases in vitro.  One allylfarnesol compound specifically inhibits the farnesylation of proteins and one allylgeranylgeraniol compound specifically inhibits the geranylgeranylation of proteins in cells. 

The allylfarnesol compound is potentially useful as an inhibitor of protein farnesyltransferase. Structurally different protein prenyltransferase inhibitors have demonstrated anticancer properties both in cell culture and in animal studies.  It has been recently proposed that a selective protein geranylgeranyltransferase inhibitor, such as the allylgeranylgeraniol compound, may also be useful as an anticancer agent.  Furthermore, protein geranylgeranyltransferase inhibitors may also have potential application as inhibitors of restenosis following cardiac catheterization. 

 

Issued U.S. patent application 6,586,461