The inhibitory effects of squalene-derived triterpenes on protein phosphatase PP2A.
This paper reports testing 15 polyether triterpenes with a squalene carbon skeleton for inhibitory effects on type 2A protein phosphatase. Two compounds, 16-hydroxydehydrothyrsiferol 10 and thyrsenol B 14, exhibited significant inhibitory action at a concentration of 10 microM. Comparison with thyrsiferyl-23-acetate 1 showed that a similar spatial disposition for the hydroxy group around C-15 or C-16 was the structural feature shared by these metabolites.
Souto
María L
ML
Instituto Universitario de Bio-Orgánica, Universidad de La Laguna, Astrofísico Francisco Sánchez 2, 38206 La Laguna, Spain.
Manríquez
Claudia P
CP
Norte
Manuel
M
Leira
Francisco
F
Fernández
José J
JJ
D004791:Enzyme Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D019319:Okadaic Acid / Q000494:pharmacology; D010749:Phosphoprotein Phosphatases / Q000037:antagonists & inhibitors*; D000461:Rhodophyta / Q000737:chemistry; D013185:Squalene / Q000031:analogs & derivatives* / Q000302:isolation & purification / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000302:isolation & purification / Q000494:pharmacology*
D004791:Enzyme Inhibitors; D014315:Triterpenes; D019319:Okadaic Acid; D013185:Squalene; D010749:Phosphoprotein Phosphatases