INHIBITORS OF RAS FARNESYLTRANSFERASES

Farnesyltransferase catalyses the post-translational modification of p roteins by a cholesterol precursor, farnesylpyrophosphate. One of the substrates of this enzyme is the product of the ras oncogene. Recently , inhibitors of farnesyltransferase have been identified through two d ifferent approaches: microbial screens for natural compounds, and subs trate analogues. These inhibitors may be useful in blocking the action of Ras proteins, in further characterizing protein prenyltransferases , and in elucidating the regulation of cholesterol metabolism.