Novel epoxysuccinyl peptides Selective inhibitors of cathepsin B, in vitro |
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Authors: | Mitsuo Murata Satsuki Miyashita Chihiro Yokoo Musaharu Tamai Kazunori Hanada Katsuo Hatayama Takae Towatari Takeshi Nikawa Nobuhiko Katunuma |
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Institution: | Research Center, Taisho Pharmaceutical Co., Saitama, Japan. |
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Abstract: | A series of new epoxysuccinyl peptides were designed and synthesized to develop a specific inhibitor of cathepsin B. Of these compounds, N-(L-3-trans-ethoxycarbonyloxirane-2-carbonyl)-L-isoleucyl-L-proline (compound CA-030) and N-(L-3-trans-propylcarbamoyloxirane-2-carbonyl)-L-isoleucyl-L-proline (compound CA-074) were the most potent and specific inhibitors of cathepsin B in vitro. The carboxyl group of proline and the ethyl ester group or n-propylamide group in the oxirane ring were necessary, the ethyl ester group or the n-propylamide group being particularly effective for distinguishing cathepsin B from other cysteine proteinases such as cathepsins L and H, and calpains. |
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Keywords: | Epoxysuccinyl peptide Cathepsin B Cysteine proteinase Specific inhibitor |
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