《生命科学》 2017, 29(2): 138-145
摘 要：摘 要：SUMOs (small ubiquitin-like modifiers，小泛素类调节蛋白) 是最近发现的一类重要的翻译后修饰蛋白，通过共价修饰底物蛋白而调节细胞的功能。而SENPs (SUMO-specific proteases，SUMO- 特异性蛋白酶)通过催化SUMOs 前体的成熟启动SUMO化过程，通过催化SUMO化蛋白上SUMO的去除实现去SUMO化。最近研究发现，SENPs 与癌症、发育缺陷、神经变性等疾病密切相关，是潜在的药物靶标。SENPs 抑制剂及其测试方法也因此受到了越来越多的关注。现主要总结了SENPs 抑制剂的发展现状，探讨了目前可行的SENPs 抑制剂测试方法，这些将为SENPs 抑制剂的进一步发展和以SENPs 为靶标的药物开发奠定坚实的基础。
Abstract: Abstract: SUMOs (small ubiquitin-like modifiers) are discovered recently as a kind of proteins for posttranslational modification， which can alter the function of cells through conjugation to substrate proteins. SENPs (SUMO-specific proteases) initiate the process of SUMOylation by catalyzing the maturation of SUMO precursors and remove SUMO from substrates to achieve deSUMOylation. Recent studies show that SENPs are associated with a number of diseases such as cancers， developmental defects， neurodegenerative diseases， indicating SENPs are potential drug targets. Thus the development of SENP inhibitors and bioassay methods for SENP inhibitors attract more and more attentions. We reviewed the present progress of SENP inhibitors and their available bioassay methods， which will lay a good foundation for further discovery of SENP inhibitors and drug development for SENP related diseases.
