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Bestatin is an inhibitor of amino peptidases and a potent, irreversible inhibitor of LTA4 hydrolase. It inhibits the amino peptidase activity of LTA4 hydrolase with a Ki value of 201 nM. It offers promise as a novel analgesic because it protects endogenous opioid peptides against degradation. It does not inhibit carboxypeptidases.
Mei-Rong Jia; Tao Wei; Wen-Fang Xu. The Analgesic Activity of Bestatin as a Potent APN Inhibitor. Frontiers in Neuroscience.2010, 4, 50.
Donald L Gardiner; Katharine R Trenholme; Tina S Skinner-Adams; Colin M Stack; John P Dalton. Overexpression of leucyl aminopeptidase in Plasmodium falciparum parasites. Target for the antimalarial activity of bestatin. Journal of Biological Chemistry. 2006, 281 (3), 1741-1745.