Synthesis of A 3-oxo-4(S)-amino acid analog of pepstatin. A new inhibitor of carboxyl (acid) proteases |
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| Authors: | Daniel H Rich Amrit S Boparai Michael S Bernatowicz |
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| Institution: | University of Wisconsin, School of Pharmacy 425 North Charter St., Madison, Wisconsin 53706 USA |
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| 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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