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 synthase. Furthermore, they also had broad spectrum in vitro antifungal activity.
Dawson
M J
MJ
Department of Natural Products Discovery, Glaxo Group Research Ltd., Greenford, Middlesex, UK.
Farthing
J E
JE
Marshall
P S
PS
Middleton
R F
RF
O'Neill
M J
MJ
Shuttleworth
A
A
Stylli
C
C
Tait
R M
RM
Taylor
P M
PM
Wildman
H G
HG
D000818:Animals; D000935:Antifungal Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D001643:Bridged Bicyclo Compounds / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D019086:Bridged Bicyclo Compounds, Heterocyclic; D013186:Farnesyl-Diphosphate Farnesyltransferase / Q000037:antagonists & inhibitors*; D005658:Fungi / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D051381:Rats; D014233:Tricarboxylic Acids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*
D000935:Antifungal Agents; D001643:Bridged Bicyclo Compounds; D019086:Bridged Bicyclo Compounds, Heterocyclic; D014233:Tricarboxylic Acids; C075117:squalestatin 1; D013186:Farnesyl-Diphosphate Farnesyltransferase