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Inhibition of lipoprotein lipase by alkanesulfonyl fluorides
G Kokotos1, S Kotsovolou, V Constantinou-Kokotou
1Department of Chemistry, University of Athens, Greece. gkokotos@cc.uoa.gr
Bioorganic & Medicinal Chemistry Letters
|January 2, 2001
Abstract:
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.