构建肿瘤靶向 ANM-PROTACs 以降解转录因子的方案。
Protocol for constructing tumor-targeting ANM-PROTACs for degradation of transcription factors.
机构信息
Department of Systems Biology, School of Life Sciences, Southern University of Science and Technology, Shenzhen 518055, China.
Department of Systems Biology, School of Life Sciences, Southern University of Science and Technology, Shenzhen 518055, China; Institute of Integrated Bioinfomedicine and Translational Science (IBTS), School of Chinese Medicine, Hong Kong Baptist University, Hong Kong SAR 999077, China; State Key Laboratory of Proteomics, National Center for Protein Sciences (Beijing), Beijing Institute of Lifeomics, Beijing 100850, China.
出版信息
STAR Protoc. 2024 Sep 20;5(3):103220. doi: 10.1016/j.xpro.2024.103220. Epub 2024 Jul 27.
AS1411-NCL-MDM2-based proteolysis-targeting chimeras (ANM-PROTACs) are capable of inducing selective degradation of transcription factors (TFs) in tumor cells. Here, we present a protocol for constructing ANM-PROTACs. We describe steps for molecular design of the ANM-PROTACs, assembly and characterization of the ANM-PROTACs, and initial assessment of in vitro TF degradation potency. We then detail procedures for validation of selective degradation of TFs via proteomic analysis. This protocol has been successfully applied to degrade various TFs across multiple tumor cell lines. For complete details on the use and execution of this protocol, please refer to Fu et al..
AS1411-NCL-MDM2 基蛋白水解靶向嵌合体 (ANM-PROTACs) 能够诱导肿瘤细胞中转录因子 (TFs) 的选择性降解。在这里，我们提供了构建 ANM-PROTACs 的方案。我们描述了 ANM-PROTACs 的分子设计步骤、ANM-PROTACs 的组装和表征，以及体外 TF 降解效力的初步评估。然后，我们详细介绍了通过蛋白质组学分析验证 TF 选择性降解的程序。该方案已成功应用于降解多种肿瘤细胞系中的各种 TF。有关该方案使用和执行的完整详细信息，请参阅 Fu 等人的研究。
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