Abstract

A ketone analog of pepstatin, in which the 3S hydroxyl group is oxidized to a ketone group, has been synthesized and shown to be a potent inhibitor of pepsin. Kinetics of inhibition of pepsin provide evidence that the ketone pepstatin analog binds to pepsin differently than pepstatin. The relationship of these complexes to crystal complexes of pepstatin-carboxyl proteases is discussed.

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