Han Zhou,Tonglian Zhou,Wenli Yu et al.
Han Zhou et al.
Proteolysis-targeting chimeras (PROTACs) enable the selective and sub-stoichiometric elimination of pathological proteins, yet only two E3 ligases are routinely used for this purpose. Here, we expand the repertoire of PROTAC-compatible E3 l...
Polyvalent folate receptor-targeting chimeras for degradation of membrane proteins [0.03%]
一种用于降解膜蛋白的多价叶酸受体靶向嵌合体
Dian Xiao,Jingwen Dong,Fei Xie et al.
Dian Xiao et al.
Lysosome-targeting chimeras (LYTACs) represent a revolutionary targeted protein degradation technology. However, the advancement of LYTACs faces substantial challenges due to the limited diversity of lysosome-trafficking receptors.
Covalent Recruitment of NEDD4 for Targeted Protein Degradation: Rational Design of Small Molecular Degraders [0.03%]
共价招募NEDD4蛋白以实现靶向降解：理性设计小分子致蓄积化合物
Xiaoqiang He,Shihan Zeng,Yalei Wen et al.
Xiaoqiang He et al.
Targeted protein degradation (TPD) has emerged as a promising therapeutic strategy for treating various diseases. However, current small molecule degraders predominantly rely on a limited set of E3 ubiquitin ligases, such as CRBN and VHL, w...
Identification of Actionable Targeted Protein Degradation Effector Sites through Site-Specific Ligand Incorporation-Induced Proximity (SLIP) [0.03%]
基于位点特异性配体掺入诱导邻近(SLIP)效应器位点的识别以实现可操作的目标蛋白质降解
Zhangping Xiao,Efthymios S Gavriil,Fangyuan Cao et al.
Zhangping Xiao et al.
Targeted protein degradation (TPD) is a rapidly emerging and potentially transformative therapeutic modality. However, the large majority of >600 known ubiquitin ligases have yet to be exploited as TPD effectors by proteolysis-targeting chi...
In-Cell Approach to Evaluate E3 Ligases for Use in Targeted Protein Degradation [0.03%]
用于靶向蛋白降解的E3连接酶的在细胞内评估方法
Yunan Zheng,Anamika Singh,Zeqi Niu et al.
Yunan Zheng et al.
A major challenge in evaluating the suitability of ∼700 known and putative E3 ligases for target protein degradation (TPD) is the lack of ligase-specific binders. Here, we use genetic code expansion (GCE) to express in living cells an E3 l...
Development and characterization of endolysosomal trafficking targeting chimera degraders of α1A-adrenergic receptor [0.03%]
靶向内溶酶体转运的嵌合降解剂的研发及α1A肾上腺素受体降解机制研究
Jiwei Chen,Shuo Wang,Tong Li et al.
Jiwei Chen et al.
Introduction: Despite the booming targeted protein degradation technologies, degrading cell membrane proteins remains an enormous challenge. In particular, only a limited approach is appropriate for the degradation of the G protein-coupled receptor (GPCR) superfamily.
Innovative discovery and mechanistic validation of HyT-PD ligands for selective CDK9-targeted protein degradation [0.03%]
创新发现并验证针对CDK9的靶向HYT-PD配体的机制性蛋白质降解作用
Yizhan Zhai,Jianfeng Cai
Yizhan Zhai
Discovery and mechanism verification of first-in-class hydrophobic tagging-based degraders of HBV core protein [0.03%]
第一类乙肝病毒核心蛋白疏水标签降解剂的发现及机制验证
Shujing Xu,Ya Wang,Dazhou Shi et al.
Shujing Xu et al.
Novel anti-HBV agents are urgently needed to overcome drug resistance challenges, with targeted protein degradation (TPD) emerging as a hopeful strategy.
GPC3-mediated lysosome-targeting chimeras (GLTACs) for targeted degradation of membrane proteins [0.03%]
GPC3介导的溶酶体靶向嵌合体(GLTACs)，用于膜蛋白的降解
Yuxin Fang,Yaojin Zhu,Wei Wang et al.
Yuxin Fang et al.
Membrane protein degradation is a cutting-edge field in targeted protein degradation (TPD). Herein, we developed glypican-3 (GPC3)-mediated lysosome-targeting chimeras (GLTACs) as a novel strategy for the targeted degradation of tumor-specific membrane proteins.
Phototriggered LYTAC: Photoactive Bispecific Aptamer Chimera Enhances Targeted Degradation of Membrane Protein through Regulating Cell Autophagy [0.03%]
光触发的LYTACS：光活性双特异性适配体嵌合体通过调节细胞自噬增强膜蛋白靶向降解
Rongjun Zhang,Changjie Yang,Xiaobo Gao et al.
Rongjun Zhang et al.
In this study, we develop a multifunctional phototriggered LYTAC platform, named PT-LYTAC, to enhance targeted protein degradation using a photoactive bispecific aptamer chimera (PBAC)....By the combination of targeted protein degradation and spatiotemporally controllable regulation of intracellular oxidative stress, the function of tumor cells can be significantly inhibited.
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