Actinoplanic acids A and B as novel inhibitors of farnesyl-protein transferase |
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Authors: | KC Silverman C Cascales O Genilloud JM Sigmund SE Gartner GE Koch MM Gagliardi BK Heimbuch M Nallin-Omstead M Sanchez |
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Affiliation: | Merck and Company, Rahway, NJ 07065, USA. |
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Abstract: | Actinoplanic acids A and B are macrocyclic polycarboxylic acids that are potent reversible inhibitors of farnesyl-protein transferase. Actinoplanic acids A and B were isolated from Actinoplanes sp. MA 7066 while actinoplanic acid B was isolated from both MA 7066 and Streptomyces sp. MA 7099. Actinoplanic acids A and B are competitive with respect to farnesyl diphosphate and are selective inhibitors of farnesyl-protein transferase because they do not inhibit geranylgeranyl-protein transferase 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 strain of Streptomyces violaceusniger on the basis of morphological, biochemical and chemotaxonomic characteristics as well as its production of actinoplanic acids. |
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