Inhibition of lipoprotein lipase by alkanesulfonyl fluorides.
A number of alkanesulfonyl halides (chlorides and fluorides) and esters were synthesized and their effect on the activity of lipoprotein lipase (LPL) was studied. Sulfonyl fluorides proved to be efficient inhibitors of LPL when the enzyme was incubated with a 10-fold molar excess of the inhibitors in a buffer containing bile salts (deoxycholate). Hexadecane- and dodecanesulfonyl fluorides caused 50% inhibition of LPL activity at concentrations of 10 to 20 microM.
Kokotos
G
G
Department of Chemistry, University of Athens, Greece. gkokotos@cc.uoa.gr
Kotsovolou
S
S
Constantinou-Kokotou
V
V
Wu
G
G
Olivecrona
G
G
D000476:Alkanesulfonates / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D002417:Cattle; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D007700:Kinetics; D008055:Lipids / Q000138:chemical synthesis / Q000494:pharmacology; D008071:Lipoprotein Lipase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D012995:Solubility; D013329:Structure-Activity Relationship; D013441:Sulfinic Acids / Q000138:chemical synthesis / Q000494:pharmacology*
D000476:Alkanesulfonates; D004791:Enzyme Inhibitors; D008055:Lipids; D013441:Sulfinic Acids; C015518:sulfolipids; C048899:sulfuryl fluoride; C044255:sulfonyl chloride; D008071:Lipoprotein Lipase