Department of Synthetic Biology and Immunology, National Institute of Chemistry, Ljubljana 1000, Slovenia.
ACS Synth Biol. 2024 Mar 15;13(3):792-803. doi: 10.1021/acssynbio.3c00588. Epub 2024 Feb 26.
Protein degradation is a highly regulated cellular process crucial to enable the high dynamic range of the response to external and internal stimuli and to balance protein biosynthesis to maintain cell homeostasis. Within mammalian cells, hundreds of E3 ubiquitin ligases target specific protein substrates and could be repurposed for synthetic biology. Here, we present a systematic analysis of the four protein subunits of the multiprotein E3 ligase complex as scaffolds for the designed degrons. While all of them were functional, the fusion of a fragment of Skp1 with the target protein enabled the most effective degradation. Combination with heterodimerizing peptides, protease substrate sites, and chemically inducible dimerizers enabled the regulation of protein degradation. While the investigated subunits of E3 ligases showed variable degradation efficiency of the membrane and cytosolic and nuclear proteins, the bipartite SSD (SOCSbox-Skp1(ΔC111)) degron enabled fast degradation of protein targets in all tested cellular compartments, including the nucleus and plasma membrane, in different cell lines and could be chemically regulated. These subunits could be employed for research as well as for diverse applications, as demonstrated in the regulation of Cas9 and chimeric antigen receptor proteins.
蛋白质降解是一个高度调控的细胞过程,对于实现对外界和内部刺激的高动态范围响应以及平衡蛋白质生物合成以维持细胞内稳态至关重要。在哺乳动物细胞中,有数百种 E3 泛素连接酶靶向特定的蛋白质底物,可以被重新用于合成生物学。在这里,我们对多蛋白 E3 连接酶复合物的四个蛋白质亚基进行了系统分析,作为设计降解基序的支架。虽然它们都具有功能,但 Skp1 片段与靶蛋白的融合使降解最为有效。与异二聚化肽、蛋白酶底物位点和化学诱导二聚体的组合能够调节蛋白质降解。虽然研究的 E3 连接酶亚基对膜和细胞质及核蛋白的降解效率不同,但双部分 SSD(SOCSbox-Skp1(ΔC111))降解基序能够快速降解所有测试细胞区室中的蛋白质靶标,包括核和质膜,在不同的细胞系中,并可进行化学调节。这些亚基可用于研究和各种应用,如 Cas9 和嵌合抗原受体蛋白的调节。