Results 191 to 200 of about 11,335 (243)

Bifunctional Molecules beyond PROTACs

Journal of Medicinal Chemistry, 2020
Heterobifunctional molecules, which recruit E3 ligases to ubiquitinate a target protein of interest, have found wide application as both biological tools and molecules with the potential to have clinical effects. In their recent paper, Yamazoe et al. report a heterobifunctional molecule that recruits the phosphatase PP1 to promote the dephosphorylation
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PROTAC 2.0: Expanding the frontiers of targeted protein degradation.

Drug Discovery Today
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 such as poor ...
Marie Cornu, Thomas Lemaitre, Charline Kieffer, A. Voisin‐Chiret   +3 more
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PROTACs: past, present and future

Chemical Society Reviews, 2022
This review highlights important milestones in the evolution of PROTACs, briefly discusses recent lessons about targeted protein degradation, and conjectures on the efforts still needed to expand the toolbox for PROTAC discovery.
Ke Li, Craig M. Crews
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Chemistries of bifunctional PROTAC degraders

Chemical Society Reviews, 2022
Proteolysis targeting chimeras (PROTACs) technology is a novel and promising therapeutic strategy using small molecules to induce ubiquitin-dependent degradation of proteins.
Chaoguo Cao, Ming He, Liguo Wang, Yuna He, Yu Rao   +4 more
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A PROTAC‐Based Cuproptosis Sensitizer in Lung Cancer Therapy

Advances in Materials
As an autonomous form of regulated cell death, cuproptosis depends on copper (Cu) and mitochondrial metabolism. However, the principle metabolic pathway known as glycolysis (Warburg effect) and high glutathione (GSH) levels of tumor cells inevitably lead
Yu Wang, Xiaoyang Yao, Yingying Lu, Juan Ruan, Zhao Yang, Chunhui Wang, Niantong Yang, Yan Gao, Shuo Shi   +8 more
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The therapeutic potential of PROTACs

Expert Opinion on Therapeutic Patents, 2021
PROTACs represent a novel class of heterobifunctional molecules that simultaneously bind to a target protein and to an E3 ligase complex, resulting in the transfer of ubiquitin and initiating a process ultimately causing the proteasomal degradation of the target protein.
Andrew B, Benowitz, Katherine L, Jones, John D, Harling   +2 more
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The Peptide PROTAC Modality: A New Strategy for Drug Discovery

MedComm
In recent years, proteolysis targeting chimera (PROTAC) technology has made significant progress in the field of drug development. Traditional drugs mainly focus on inhibiting or activating specific proteins, while PROTAC technology provides new ideas ...
Youmin Zhu, Yu Dai, Yuncai Tian
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Journey of PROTAC: From Bench to Clinical Trial and Beyond.

Biochemistry
Proteolysis-targeting chimeras (PROTACs) represent a transformative advancement in drug discovery, offering a method to degrade specific intracellular proteins.
Kyli Berkley, Julian Zalejski, Nidhi Sharma, Ashutosh Sharma   +3 more
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Self‐Oxygenating PROTAC Microneedle for Spatiotemporally‐Confined Protein Degradation and Enhanced Glioblastoma Therapy

Advances in Materials
Glioblastoma (GBM) is the most aggressive subtype of primary brain tumors, which marginally respond to standard chemotherapy due to the blood‐brain barrier (BBB) and the low tumor specificity of the therapeutics. Herein, a double‐layered microneedle (MN)
Xingyu Jiang, Yi Lai, Wenzheng Xia, Wenfang Yang, Junjue Wang, Jiaxing Pan, Qiang Zhao, Fengqi Zhou, Shiqin Li, Shunan Zhang, Jing Gao, Yinyan Wang, T. Zan, Z. Xu, Haijun Yu, Z. Xu   +15 more
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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
Zheng Li, Guodong Ren, Xuewei Wang, Xiaowan Li, Lingwen Ding, Jianwei Zhu, Yajie Zhang, Chengwu Zhang, Jianhua Zou, Xiaoyuan Chen   +9 more
semanticscholar   +1 more source