Actinoplanic acids A and B as novel inhibitors of farnesyl-protein transferase

Applied Microbiology and Biotechnology
K C SilvermanM Sanchez

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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Citations

Apr 21, 2020·Journal of Enzyme Inhibition and Medicinal Chemistry·Xiaohan DaiGao Hongwei
Oct 1, 1996·Journal of Enzyme Inhibition·D PerrinB T Hill
Feb 8, 2007·Organic & Biomolecular Chemistry·Marc A Boudreau, John C Vederas
Mar 17, 1997·Biochemical and Biophysical Research Communications·K C SilvermanR B Lingham

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