Madu Ikenna G, Chen Yuan
Department of Molecular Medicine, Beckman Research Institute of the City of Hope, Duarte, California, USA.
Curr Protoc Mol Biol. 2012 Jul;Chapter 10:Unit10.30. doi: 10.1002/0471142727.mb1030s99.
Post-translational modifications by the SUMO (Small Ubiquitin-like MOdifier) family of proteins are recently discovered essential regulatory mechanisms. All SUMO proteins are synthesized as larger precursors that are matured by SUMO-specific proteases, known as SENPs, which remove several C-terminal amino acids of SUMO to expose the Gly-Gly motif. SENPs also remove SUMO modifications from target proteins, making this modification highly dynamic. At least six deSUMOylation enzymes, all of which are encoded by essential genes, have been identified in mammals. SENP1 has been shown to play an important role in the development of prostate cancer and in angiogenesis. This unit describes and discusses methods for characterizing the deSUMOylation enzymes. These assays enable the identification of inhibitors of these enzymes and investigation of their mechanism of inhibition in order to develop research tools and future therapeutics.
由类泛素小修饰蛋白（SUMO）家族蛋白进行的翻译后修饰是最近发现的重要调控机制。所有SUMO蛋白最初都作为较大的前体合成，通过称为SENP的SUMO特异性蛋白酶成熟，这些蛋白酶去除SUMO的几个C末端氨基酸以暴露出甘氨酸-甘氨酸基序。SENP还从靶蛋白上去除SUMO修饰，使得这种修饰具有高度动态性。在哺乳动物中已鉴定出至少六种去SUMO化酶，它们均由必需基因编码。SENP1已被证明在前列腺癌的发展和血管生成中起重要作用。本单元描述并讨论了表征去SUMO化酶的方法。这些测定能够鉴定这些酶的抑制剂并研究其抑制机制，以便开发研究工具和未来的治疗方法。
