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. In this ...
LC-MS/MS-Based Metabolomics and Multivariate Statistical Analysis Reveal the Mechanism of Rhodotorula mucilaginosa Proteases on Myofibrillar Protein Degradation and the Evolution of Taste Compounds [0.03%]
基于LC-MS/MS的代谢组学和多元统计分析揭示了红假丝酵母蛋白酶对肌原纤维蛋白降解及风味物质演变的影响机制
Tianmeng Zhang,Qiang Xia,Daodong Pan et al.
Tianmeng Zhang et al.
Rhodotorula mucilaginosa plays a key role in developing the taste of dry-cured ham, while the mechanism of Rhodotorula mucilaginosa proteases on myofibrillar protein (MP) hydrolysis and the evolution of taste substances has not been studied...
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...
Extracellular HSP90-Facilitated Degradation of Extracellular and Membrane Proteins by Bifunctional Small Molecules [0.03%]
介导细胞外HSP90降解细胞外及膜蛋白的双功能小分子
Dongli Zhang,Jie Li,Yaqi Liang et al.
Dongli Zhang et al.
Lysosome-targeting chimeras represent a promising strategy for degrading extracellular and membrane proteins via the lysosomal pathway, but the available receptor options remain limited. Herein, we report a novel strategy utilizing extracel...
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...
Supramolecular Host-Guest Assemblies for Tunable and Modular Lysosome-Targeting Protein Degradation [0.03%]
超分子宿主-客体组装模块化调控溶酶体靶向蛋白质降解
Xuetao Chen,Tingting Wu,Yali Chen et al.
Xuetao Chen et al.
Heterobifunctional drugs have revolutionized chemical biology and therapeutic innovation, yet their fixed covalent linkages constrain dynamic adaptability. Here, we introduce Host-Guest Bridged Lysosome-Targeting Chimeras (HGTACs), a supram...
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
Wei Wang,Chunquan Sheng
Wei Wang
A single-chain antibody-based AID2 system for conditional degradation of GFP-tagged and untagged proteins [0.03%]
一种基于单链抗体的AID2系统 用于GFP标记及非标记蛋白质的条件性降解
Moutushi Islam,Takefumi Negishi,Naomi Kitamoto et al.
Moutushi Islam et al.
Protein knockdown using an improved auxin-inducible degron (AID2) technology has proven to be a powerful tool for studying protein function. The current approach requires the fusion of target proteins with a degron tag, a process typically ...
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