多功能蛋白前体转化酶：其独特、冗余、互补和相反的功能。
The multifaceted proprotein convertases: their unique, redundant, complementary, and opposite functions.
机构信息
Laboratory of Biochemical Neuroendocrinology, Clinical Research Institute of Montreal (IRCM, affiliated with the University of Montreal), Montreal, Quebec H2W 1R7, Canada.
出版信息
J Biol Chem. 2013 Jul 26;288(30):21473-81. doi: 10.1074/jbc.R113.481549. Epub 2013 Jun 17.
Abstract
The secretory proprotein convertase (PC) family comprises nine members: PC1/3, PC2, furin, PC4, PC5/6, PACE4, PC7, SKI-1/S1P, and PCSK9. The first seven PCs cleave their substrates at single or paired basic residues, and SKI-1/S1P cleaves its substrates at non-basic residues in the Golgi. PCSK9 cleaves itself once, and the secreted inactive protease escorts specific receptors for lysosomal degradation. It regulates the levels of circulating LDL cholesterol and is considered a major therapeutic target in phase III clinical trials. In vivo, PCs exhibit unique and often essential functions during development and/or in adulthood, but certain convertases also exhibit complementary, redundant, or opposite functions.
摘要
分泌型蛋白前转化酶（PC）家族包括 9 个成员：PC1/3、PC2、furin、PC4、PC5/6、PACE4、PC7、SKI-1/S1P 和 PCSK9。前 7 种 PCs 在单一或成对碱性残基处切割其底物，而 SKI-1/S1P 在高尔基体中在非碱性残基处切割其底物。PCSK9 自身切割一次，分泌的无活性蛋白酶护送特定的受体进行溶酶体降解。它调节循环 LDL 胆固醇的水平，被认为是 III 期临床试验中的主要治疗靶点。在体内，PCs 在发育和/或成年期表现出独特且通常是必需的功能，但某些转化酶也表现出互补、冗余或相反的功能。
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