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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。
SUMOs (small ubiquitin-like modifiers) are recently discovered class of important post-translational modifications that regulate the function of a cell by covalently modifying the substrate protein. SENPs (SUMO-specific proteases) initiate SUMOylation by catalyzing the maturation of SUMOs and de SUMOisation by catalyzing the removal of SUMO on SUMO proteins. Recent studies have found that SENPs are closely related to diseases such as cancer, developmental defects and neurodegeneration and are potential drug targets. SENPs inhibitors and their testing methods are therefore receiving more and more attention. The current status of SENPs inhibitors is summarized, and currently available SENPs inhibitors test methods are discussed, which will lay a solid foundation for the further development of SENPs inhibitors and drug development targeting SENPs.