THE SQUALESTATINS, NOVEL INHIBITORS OF SQUALENE SYNTHASE PRODUCED BY A SPECIES OF PHOMA I. TAXONOMY, FERMENTATION, ISOLATION, PHYSICO-CHEMICAL PROPERTIES AND BIOLOGICAL ACTIVITY

During the screening of fungi for inhibitors of squalene synthase, Phoma sp. 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 synt...

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Published inJournal of antibiotics Vol. 45; no. 5; pp. 639 - 647
Main Authors DAWSON, MICHAEL J., FARTHING, JOHN E., MARSHALL, PETER S., MIDDLETON, ROBERT F., O'NEILL, MELANIE J., SHUTTLEWORTH, ALAN, STYLLI, CHARI, TAIT, R. MURRAY, TAYLOR, PAM M., WILDMAN, HOWARD G., BUSS, ANTONY D., LANGLEY, DAVID, HAYES, MICHAEL V.
Format Journal Article
LanguageEnglish
Published Tokyo JAPAN ANTIBIOTICS RESEARCH ASSOCIATION 01.05.1992
Japan Antibiotics Research Association
Subjects
Animals
Antibiotics (antibacterial agents, antifungal agents)
Antibiotics, microbial producers, chemotherapic agents, antiseptics, disinfecting agents
Antifungal Agents - chemistry
Antifungal Agents - isolation & purification
Antifungal Agents - pharmacology
Applied microbiology
Biological and medical sciences
Bridged Bicyclo Compounds - chemistry
Bridged Bicyclo Compounds - isolation & purification
Bridged Bicyclo Compounds - pharmacology
Bridged Bicyclo Compounds, Heterocyclic
Farnesyl-Diphosphate Farnesyltransferase - antagonists & inhibitors
Fundamental and applied biological sciences. Psychology
Fungi - drug effects
Microbial Sensitivity Tests
Microbiology
Phoma
Rats
Tricarboxylic Acids - chemistry
Tricarboxylic Acids - isolation & purification
Tricarboxylic Acids - pharmacology
Enzyme
Enzyme inhibitor
Fermentation
In vitro
Biological activity
Fungi
Antifungal agent
Phoma
Farnesyltransferase
Isolation
Fungi Imperfecti
Physicochemical properties
Thallophyta
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Summary:During the screening of fungi for inhibitors of squalene synthase, Phoma sp. 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.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
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ISSN:0021-8820
1881-1469
DOI:10.7164/antibiotics.45.639