ACTINOPLANIC-ACID-A AND ACTINOPLANIC-ACID-B AS NOVEL INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE

Actinoplanic acids A and B are macrocyclic polycarboxylic acids that a re potent reversible inhibitors of farnesyl-protein transferase. Actin oplanic acids A and B were isolated from Actinoplanes sp. MA 7066 whil e actinoplanic acid B was isolated from both MA 7066 and Streptomyces sp. MA 7099. Actinoplanic acids A and B are competitive with respect t o farnesyl diphosphate and are selective inhibitors of farnesyl-protei n transferase because they do not inhibit geranylgeranyl-protein trans ferase type 1 or squalene synthase, MA 7066 is believed to be a novel species of actinomycetes while MA 7099 is believed to be a novel strai n of Streptomyces violaceusniger on the basis of morphological, bioche mical and chemotaxonomic characteristics as well as its production of actinoplanic acids.