Journal of medicinal chemistryAnimalsProteasome InhibitorsHumansMiceStructure-Activity Relationship
Discovery of Novel Potent and Safe Immunoproteasome Inhibitors with Bridged Ring for Anti-Inflammatory Therapy.
Jian Wu, Shi Cai, Jincai Su, Xiaojun Ji, Qiuhua Zhou, Zehong Chen, Yiqing Fan, Xuefei Li, Jiang Liu, Wanting Dong, Changyou Ma, Dan Xu, Hai Qian
Published: 202510.1021/acs.jmedchem.5c02583
Abstract
Current clinical proteasome inhibitors suffer from nonselective pan-inhibition, leading to severe toxicity. Selective immunoproteasome inhibition offers a safer therapeutic strategy for autoimmune diseases. However, the inadequate LMP7/β5 selectivity…
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