New fungal metabolite geranylgeranyltransferase inhibitors with antifungal activity.
NATURAL PRODUCT RESEARCH(2006)
摘要
Geranylgeranyltransferase I (GGTase 1) catalyzes the post-translational transfer of lyophilic diterpenoid geranylgeranyl to the cysteine residue of proteins terminating with a CaaX motif such as Rho1p and Cdc42p. It has been shown that GGTase I activity is essential for viability of Saccharomyces cerevisiae and hence its inhibition is a potential antifungal target. From natural product screening, a number of azaphilones including one novel analog were isolated as broad-spectrum inhibitors of GGTase I. Isolation, structure elucidation, GGTase I inhibitory activities and antifungal activities of these compounds are described.
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关键词
geranylgeranyltransferase I,antifungal activity,azaphilone
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