Structure-Guided Design of Novel, Potent, and Selective Macrocyclic Plasma Kallikrein Inhibitors.
ACS medicinal chemistry letters(2017)
摘要
A series of macrocyclic analogues were designed and synthesized based on the cocrystal structure of small molecule plasma kallikrein (pKal) inhibitor, , with the pKal protease domain. This led to the discovery of a potent macrocyclic pKal inhibitor , with an IC of 2 nM for one olefinic isomer and 42.3 nM for the other olefinic isomer.
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关键词
Hereditary angioedema,macrocycle,plasma kallikrein,protease inhibitor,structure-based design
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