Design and synthesis of novel cathepsin C inhibitors with anti-inflammatory activity
Xiaobao Shen(Fuyang Normal University), Nan Li(Fuyang Normal University), Miao Liu(Fuyang Normal University), Xuanzheng Han(Fuyang Normal University), Yazhi Wang(Fuyang Normal University), Jingwen Jia(Fuyang Normal University), Fufang Wu(Fuyang Normal University), Hongwei Chen(Fuyang Normal University), Xinhua Liu(Anhui Medical University)
Cited by 1Open Access
Abstract
value of 437 nM. It also showed a substantial enhancement in overall anti-inflammatory activity, achieving an inhibitory effect on NO release at 4.1 μM. Furthermore, molecular docking was conducted to analyze the mode of action with Cat C. And cell thermal shift analysis (CETSA) revealed that this compound increases the temperature tolerance of Cat C in a concentration-dependent manner, suggesting strong binding to the target Cat C. Prolonged pharmacological inhibition activity may result in the depletion of active NSPs.
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