School of Medicine, Zhejiang University City College, Hangzhou, Zhejiang Province, 310015, People's Republic of China.
Department of Pharmaceutical Preparation, Hangzhou Xixi Hospital, Hangzhou, Zhejiang Province, 310023 People's Republic of China.
Drug Des Devel Ther. 2020 Oct 19;14:4327-4342. doi: 10.2147/DDDT.S265793. eCollection 2020.
Proteasome is vital for intracellular protein homeostasis as it eliminates misfolded and damaged protein. Inhibition of proteasome has been validated as a powerful strategy for anti-cancer therapy, and several drugs have been approved for treatment of multiple myeloma. Recent studies indicate that proteasome has potent therapeutic effects on a variety of diseases besides cancer, including parasite infectious diseases, bacterial/fungal infections diseases, neurodegenerative diseases and autoimmune diseases. In this review, recent developments of proteasome inhibitors for various diseases and related structure activity relationships are going to be summarized.
蛋白酶体对于细胞内蛋白质的稳态至关重要,因为它可以消除错误折叠和受损的蛋白质。抑制蛋白酶体已被证实是一种有效的抗癌治疗策略,并且已经有几种药物被批准用于治疗多发性骨髓瘤。最近的研究表明,蛋白酶体除了癌症之外,对多种疾病(包括寄生虫感染性疾病、细菌/真菌感染性疾病、神经退行性疾病和自身免疫性疾病)也具有强大的治疗作用。在这篇综述中,将总结蛋白酶体抑制剂在各种疾病中的最新发展和相关的构效关系。