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The squalestatings, novel inhibitors of squalene synthase produced by a species of Phoma. I. Taxonomy, fermentation, isolation, physico-chemical properties and biological activity.

作者:Michael J. Dawson, John E. Farthing, Peter S. Marshall, Robert F. Middleton, Melanie J. O’Neill, ALAN SHUTTLEWORTH, C. Harri.Stylli, R. Murray Tait, PAM M. TAYLOR, Howard G. Wildman, Antony David Buss, David B. Langley, Michael V. Hayes · 发表于:The Journal of Antibiotics · 年份:1992 · DOI:10.7164/antibiotics.45.639 · 被引用次数:183 · 研究领域:Plant biochemistry and biosynthesis、Phytochemicals and Antioxidant Activities、Computational Drug Discovery Methods

During the screening of fungi for inhibitors of squalene synthase, Phomasp.C2932 was found to produce three structurally related novel inhibitors.These compounds,designated the squalestatins, exhibited potent activity against both mammalian (rat liver) and fungal {Candida albicans) squalene synthase.Furthermore, they also had broad spectrum in vitro antifungal activity.High serum cholesterol levels have been established as an important risk factor for atherosclerosis, and cholesterol lowering regimens have been shown to decrease the incidence of coronary heart disease morbidity and mortality1'2).In the search for agents which may lower cholesterol levels,