phenyl-n-butylborinic acid (cas 100757-73-1) is a potent transition state analog inhibitor of lipolytic enzymes

Add time:08/09/2019    Source:sciencedirect.com

The cholesterol esterase and lipoprotein lipase catalyzed hydrolyses of the water-soluble substrate p-nitrophenyl butyrate are competitively inhibited by butaneboronic acid and phenylboronic acid. phenyl-n-butylborinic acid (cas 100757-73-1) has been synthesized and characterized as an ultrapotent transition state analog inhibitor: Ki = 2.9 ± 0.6 nM and 1.7 ± 0.3 μM for the cholesterol esterase and lipoprotein lipase reactions, respectively. These results are interpreted in terms of transition state structure and stabilization.

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