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Modular Assembled Targeting Chimera Enables Multimodal Targeted Protein Degradation. [PDF]

JACS Au
Zhu W, Zhang W, Wang Y, Chen J, Xu F, Pang J.   +5 more
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Silica-based EGFR-degrading nano-PROTACs for efficient therapy of non-small cell lung cancer

European Journal of Pharmaceutics and Biopharmaceutics
Proteolysis targeting chimeras (PROTACs) technology is a promising strategy for degrading proteins of interest. Traditional PROTACs, however, often face challenges such as poor solubility, low stability, and off-target toxicity. To address these challenges, we integrated nanotechnology to enhance the delivery of target-protein degraders to the tumor ...
Lei, Fang, Ruixue, Zhu, Meijing, Li, Junhui, Ma, Sijun, Fan, Xuelian, He, Zhongrui, Yang, Yakai, Yan, Xiang, Ma, Guangya, Xiang   +9 more
exaly   +3 more sources

Self-Assembled Nano-PROTAC Enables Near-Infrared Photodynamic Proteolysis for Cancer Therapy

Journal of the American Chemical Society, 2023
Confining the protein degradation activity of proteolysis-targeting chimera (PROTAC) to cancer lesions ensures precision treatment. However, it still remains challenging to precisely control PROTAC function in tumor regions in vivo. We herein describe a near-infrared (NIR) photoactivatable nano-PROTAC (NAP) for remote-controllable proteolysis in tumor ...
Weishan Wang, Chenghong Zhu, Bin Zhang, Yi Feng, Yan Zhang, Jinbo Li   +5 more
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Cascade-responsive nano-PROTACs for tumor-specific ALK protein degradation and enhanced cancer therapy

Nano Today
Binlong Chen, Yiguang Wang
exaly   +2 more sources

Selective and spatiotemporal‑resolved nano-PROTAC for lung cancer therapy

Colloids and Surfaces B: Biointerfaces
The Proteolysis-Targeting Chimeras (PROTAC) technology has become a promising tool in lung cancer therapy. The PROTAC regents targeting to Bromodomain-containing Protein 4 (BRD4) showed effective induction of apoptosis in lung cancer cells. However, the application of this kind of PROTAC regents is still hindered by the low tissue specificity ...
Xiaowei Xu, Le Wang, Shitao Lin, Xiaoqing Wu, Xufeng Lin, Xiaoling Guan, Shiqi Tang, Ni Zhang, Yuxin Zhang, Lingmin Zhang, Dazhi Zhou   +10 more
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Ionizable Nano‐PROTAC Overcomes Endosomal Entrapment for Enhanced LRG1 Degradation and Tumor Suppression

Angewandte Chemie
Abstract Nanoscale proteolysis‐targeting chimeras (nano‐PROTACs) have emerged as a promising modality that circumvents conventional linker optimization using multivalent engineering. However, their therapeutic potential remains severely limited by inefficient cytosolic delivery caused by endosomal entrapment.
Huan Min, Ming Chao Sun, Kaijing Hu, Yana Zhang, Junyao Li, Yongzheng Li, Lin Du, Wei Ding, Yinlong Zhang, Guangjun Nie, Yingqiu Qi   +10 more
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New-generation advanced Nano-PROTACs as potential therapeutic agents in cancer therapy

Journal of Controlled Release
Proteolysis targeting chimeras (PROTACs) are catalytic degraders that eliminate pathogenic proteins via the ubiquitin-proteasome system (UPS). Building on this mechanism, nano-engineered PROTACs (Nano-PROTACs) integrate PROTACs with rationally designed nanomaterials to create an emerging therapeutic platform for cancer.
Jingjuan, Zhang, Yongzheng, Li, Huiyuan, Jin, Peizhen, Yang, Huan, Min, Jian, Song, Yingqiu, Qi   +6 more
openaire   +2 more sources

Tumor microenvironment responsive nano-PROTAC for BRD4 degradation enhanced cancer photo-immunotherapy

Biomaterials
Proteolysis Targeting Chimeras (PROTAC) technology has garnered great attention due to its advantages in targeted protein degradation, promising its potential for treating malignant cancer. Nevertheless, the inherent drawbacks of PROTAC technology hinder its clinical translation.
Zheng Li, Guodong Ren, Xuewei Wang, Xiaowan Li, Lingwen Ding, Jianwei Zhu, Yajie Zhang, Chengwu Zhang, Jianhua Zou, Xiaoyuan Chen   +9 more
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Innovative sarcoma therapy using multifaceted nano-PROTAC-induced EZH2 degradation and immunity enhancement

Biomaterials
Sarcomas are highly malignant tumors characterized by their heterogeneity and resistance to conventional therapies, which significantly limit treatment options. EZH2 is highly expressed in sarcomas, but targeting it is difficult. In this study, we uncovered the non-canonical transcriptional mechanisms of EZH2 in sarcoma and highlighted the essential ...
Zhihao Chen, Yi Tai, Chuangzhong Deng, Yameng Sun, Hongmin Chen, Tianqi Luo, Jiaming Lin, Weiqing Chen, Huaiyuan Xu, Guohui Song, Qinglian Tang, Jinchang Lu, Xiaojun Zhu, Shijun Wen, Jin Wang   +14 more
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De Novo Design of Hexamer‐Linker Dual‐Action Nano‐PROTAC for Tumor‐Specific Ferroptosis

Angewandte Chemie
Abstract Proteolysis‐Targeting Chimera (PROTAC) technology, a groundbreaking approach in drug discovery, leverages the ubiquitin‐proteasome system to degrade disease‐related proteins. Its efficacy mainly hinges on the linker design, which critically influences ternary complex (target protein‐PROTAC‐E3 ligase) stability and ...
Ni‐Yuan Zhang, Zhuan Wen, Ming‐Ze Cai, Ke‐Ting Zhou, Hao‐Ze Li, Yi‐xuan Liu, Shang Wu, Yu Xia, Hong‐Wei An, Hao Wang   +9 more
openaire   +2 more sources