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Braces for the Peptide Backbone: Insights into Structure–Activity Relationships of Protease Inhibitor Mimics with Locked Amide Conformations

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  • This research was supported by the Deutsche Forschungsgemeinschaft (grant Ko 1390/9-1) and LOEWE—Soft Control.

Abstract

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Flower power: Potent protease inhibitors containing triazolyl mimics of cis and trans backbone amides were engineered based on the structure of the sunflower trypsin inhibitor 1. The biologically relevant cis-Pro motif was successfully replaced with a non-prolyl unit. High-resolution crystal structures of 1,4- and 1,5-disubstituted 1,2,3-triazolyl peptidomimetics can serve in the design of tailor-made Bowman–Birk inhibitors.

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