1. Actinoplanic acids A and B as novel inhibitors of farnesyl-protein transferase.
- Author
-
Silverman KC, Cascales C, Genilloud O, Sigmund JM, Gartner SE, Koch GE, Gagliardi MM, Heimbuch BK, Nallin-Omstead M, and Sanchez M
- Subjects
- Enzyme Inhibitors pharmacology, Farnesyltranstransferase, Lactones pharmacology, Actinomycetales chemistry, Alkyl and Aryl Transferases, Enzyme Inhibitors isolation & purification, Lactones isolation & purification, Streptomyces chemistry, Transferases antagonists & inhibitors
- 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.
- Published
- 1995
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