Natural product scaffolds as inspiration for the design and synthesis of 20S human proteasome inhibitors,RSC Chemical Biology

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Natural product scaffolds as inspiration for the design and synthesis of 20S human proteasome inhibitors
RSC Chemical Biology ( IF 4.2 ) Pub Date : 2020-09-16 , DOI: 10.1039/d0cb00111b
Grace E Hubbell ₁ , Jetze J Tepe ₁

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The 20S proteasome is a valuable target for the treatment of a number of diseases including cancer, neurodegenerative disease, and parasitic infection. In an effort to discover novel inhibitors of the 20S proteasome, many reseaarchers have looked to natural products as potential leads for drug discovery. The following review discusses the efforts made in the field to isolate and identify natural products as inhibitors of the proteasome. In addition, we describe some of the modifications made to natural products in order to discover more potent and selective inhibitors for potential disease treatment.

中文翻译：

天然产物支架作为20S人类蛋白酶体抑制剂设计和合成的灵感

20S 蛋白酶体是治疗多种疾病的重要靶点，包括癌症、神经退行性疾病和寄生虫感染。为了发现 20S 蛋白酶体的新型抑制剂，许多研究人员将天然产物视为药物发现的潜在先导。以下综述讨论了该领域为分离和鉴定天然产物作为蛋白酶体抑制剂所做的努力。此外，我们描述了对天然产物进行的一些修饰，以便发现用于潜在疾病治疗的更有效和选择性的抑制剂。

更新日期：2020-11-03

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