Novel epoxysuccinyl peptides selective inhibitors of cathepsin B, in vitro
M Murata, S Miyashita, C Yokoo, M Tamai, K Hanada… - FEBS letters, 1991 - Elsevier
M Murata, S Miyashita, C Yokoo, M Tamai, K Hanada, K Hatayama, T Towatari, T Nikawa…
FEBS letters, 1991•ElsevierA 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 …
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 …
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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