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...
Amiloride synergizes with EGFR PROTACs and inhibitors to overcome therapeutic resistance in NSCLC [0.03%]
氨氯地平与EGFR靶向蛋白降解剂联合应用可克服非小细胞肺癌的治疗耐药性
Xiaojuan Qu,Hongyue Ou,Yifan Wu et al.
Xiaojuan Qu et al.
Lung cancer remains the leading cause of cancer-related mortality worldwide, with non-small cell lung cancer (NSCLC) accounting for most cases. Among NSCLC patients, approximately 15-30 % harbor activating mutations in the Epidermal Growth ...
Corrigendum to "Design, synthesis, and biological evaluation of novel BTK-targeting proteolysis targeting chimeras (PROTACs) with enhanced pharmacokinetic properties" [Eur. J. Med. Chem. 289 (2025) 117420] [0.03%]
“新型BTK靶向蛋白降解嵌合体(PROTACs)的设计、合成及生物学评价”一文的勘误(刊载于《欧洲药理学杂志》289卷(2023)117420页)
Ying Lin,Jing Liu,Xinjian Tian et al.
Ying Lin et al.
Hypoxia-sensitive macrocycle inclusion complexes for targeted protein degradation [0.03%]
缺氧敏感大环包合物用于靶向蛋白降解
Jiachan Lin,Wenyan Wang,An-Kang Ying et al.
Jiachan Lin et al.
PROteolysis TArgeting Chimeras (PROTACs) have gained significant attention for targeted protein degradation in cancer therapy. However, their clinical application is limited by low bioavailability, poor tumor distribution, and potential off...
Razing the scaffolding: the elimination of non-catalytic functions of kinases through targeted protein degradation [0.03%]
拆除脚手架：通过靶向蛋白降解消除激酶的非催化功能
Sarah Pogash,Steven Fletcher
Sarah Pogash
Overexpression and activation of kinases often results in cancer initiation and progression through both catalytic and non-catalytic functions that promote rapid proliferation, growth, survival, and metastasis of cells. Catalytic functions ...
Unveiling p65 as the target of diphyllin in ameliorating metabolic dysfunction-associated steatotic liver disease via targeted protein degradation technology [0.03%]
揭秘大黄素甲醚通过靶向蛋白降解技术改善代谢紊乱相关肝脂肪变性疾病的分子机制
Xuejing Zhu,Lei Zhang,Wenqian Cui et al.
Xuejing Zhu et al.
Introduction: Metabolic dysfunction-associated steatotic liver disease (MASLD), characterized by hepatic steatosis, inflammation and fibrosis, is becoming a global epidemic. However, the currently available effective clin...
Marie Cornu,Thomas Lemaitre,Charline Kieffer et al.
Marie Cornu et al.
Proteolysis targeting chimera (PROTAC) technology has revolutionized targeted protein degradation via the ubiquitin-proteasome system. Despite their efficacy in degrading previously undruggable proteins, classical PROTACs face challenges su...
Selective steroid receptor modulators, degraders and PROTACs: Therapeutic strategies in management of endocrine-related cancers [0.03%]
选择性激素受体调节剂、降解剂和靶向蛋白降解嵌合物PROTACs在内分泌相关癌症治疗中的应用策略
Anjali Tripathi,Ayushi Chhabra,Sheeba Rizvi et al.
Anjali Tripathi et al.
Endocrine-related disorders are highly prevalent globally, affecting millions of people. Such diseases are multifactorial in origin and are influenced by the complex interplay of genetics, lifestyle, and environmental factors. Recurring dis...
Nanoparticle-Mediated Targeted Protein Degradation: An Emerging Therapeutics Technology [0.03%]
纳米颗粒介导的靶向蛋白降解：一种新兴的治疗技术
Andrew G Baker,Adrian Pui Ting Ho,Laura S Itzhaki et al.
Andrew G Baker et al.
Targeted protein degradation (TPD) has emerged as a transformative therapeutic strategy for eliminating disease-associated proteins, with relevance across disorders ranging from cancer to neurodegeneration. Since its inception nearly two de...
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