Total Synthesis of Covalent Cysteine Protease Inhibitor <i>N</i>‑Desmethyl Thalassospiramide C and Crystallographic Evidence for Its Mode of Action
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A total synthesis of N-desmethyl thalassospiramide C, a unique strained macrocyclic proteobacterial depsipeptide, enabled a detailed crystallographic study of its covalent complex with cathepsin K, a member of a medicinally important family of cysteine proteases. The study provides support for the mechanism of action, and the insight gained can be used for structure-based drug design targeting these calpain proteases.
创建时间:
2019-01-09



