Results 21 to 30 of about 5,184,182 (156)

Targeted Protein Degradation via a Covalent Reversible Degrader Based on Bardoxolone [PDF]

, 2020
Targeted protein degradation (TPD) has emerged as a powerful tool in drug discovery for the perturbation of protein levels using heterobifunctional small molecules (i.e. PROTACs).
John A., Tallarico, Jessica, Spradlin, Mai, Luo, Yi, Xie, Bingqi, Tong, Daniel, Nomura, Markus, Schirle, Thomas J., Maimone, Jeffrey M., McKenna   +8 more
core   +3 more sources

Discovery of Norbornene as a Novel Hydrophobic Tag Applied in Protein Degradation [PDF]

, 2023
Hydrophobic tagging (HyT) is a potential therapeutic strategy for targeted protein degradation (TPD). Norbornene was discovered as an unprecedented hydrophobic tag in this study and was used to degrade the anaplastic lymphoma kinase (ALK) fusion protein ...
Sun, Yuan, Zhu, Huajian, Chen, Zhe-Sheng, Zhe‐Sheng Chen, Jinyi Xu, Liu, Jie, Yuan Sun, Dong‐Hua Yang, Xie, Shaowen, Hong Yao, Yang, Dong-Hua, Zhu, Zheying, Jie Liu, Huajian Zhu, Jingjie Zhu, Chen, Jian, Zhan, Feiyan, Zheying Zhu, Xu, Jinyi, Xu, Shengtao, Yao, Hong, Jian Chen, Shaowen Xie, Zhu, Jingjie, Feiyan Zhan, Shengtao Xu   +25 more
core   +1 more source

Targeted Protein Degradation Induced by HEMTACs Based on HSP90

, 2022
Targeted protein degradation (TPD) strategies open up new avenues for therapeutics and provide powerful tools for biological inquiry. Herein, we present a brand-new approach, termed heat shock protein 90 (HSP90)–mediated targeting chimeras (HEMTACs), to ...
Zhenzhen Li, Ling Zhang, Lupei Du (1376673), Zhao Ma (655370), Siyue Ma (7866746), Shuxin Zhang, Siyue Ma, Zhao Ma, Zhenzhen Li (112901), Lupei Du, Minyong Li (69472), Shuxin Zhang (669853), Ling Zhang (18071), Minyong Li   +13 more
core   +3 more sources

Recent advancements in targeted protein knockdown technologies—emerging paradigms for targeted therapy

Exploration of Targeted Anti-tumor Therapy, 2023
A generalized therapeutic strategy for various disease conditions, including cancer, is to deplete or inactivate harmful protein targets. Various forms of protein or gene silencing molecules, e.g., small molecule inhibitors, RNA interference (RNAi), and ...
Mansi Joshi, Pranay Dey, Abhijit De
doaj   +1 more source

Targeted Protein Degradation via Lysosomes [PDF]

, 2023
In the scope of targeted protein degradation (TPD), proteolysis-targeting chimeras (PROTACs), leveraging the ubiquitin-proteasome system, have been extensively studied.
Jin Wang, Rishi R. Paudel, Erika Y. Monroy, Paudel, Rishi R, Wang, Jin, Dong Lu, Lu, Dong, Sandipan Roy Chowdhury, Roy Chowdhury, Sandipan, Monroy, Erika Y   +9 more
core   +1 more source

Targeted protein degradation in mammalian cells: A promising avenue toward future

Computational and Structural Biotechnology Journal, 2022
In the eukaryotic cellular milieu, proteins are continuously synthesized and degraded effectively via endogenous protein degradation machineries such as the ubiquitin–proteasome and lysosome pathways.
Tianyi Zhang, Chuanyang Liu, Wenying Li, Jingyu Kuang, Xin-yuan Qiu, Lu Min, Lingyun Zhu   +6 more
doaj   +1 more source

Proteomic approaches advancing targeted protein degradation [PDF]

, 2023
Targeted protein degradation (TPD) is an emerging modality for research and therapeutics. Most TPD approaches harness cellular ubiquitin-dependent proteolytic pathways.
Gajanan Sathe, Gopal P. Sapkota, Sathe, Gajanan, Sapkota, Gopal P.   +3 more
core   +1 more source

The Potential of Proteolytic Chimeras as Pharmacological Tools and Therapeutic Agents

Molecules, 2020
The induction of protein degradation in a highly selective and efficient way by means of druggable molecules is known as targeted protein degradation (TPD).
Bernat Coll-Martínez, Antonio Delgado, Bernat Crosas   +2 more
doaj   +1 more source

Native Mass Spectrometry: Insights and Opportunities for Targeted Protein Degradation

, 2023
Native mass spectrometry (nMS) is one of the most powerful biophysical methods for the direct observation of noncovalent protein interactions with both small molecules and other proteins.
Sternicki, Louise M, Poulsen, Sally-Ann
core   +1 more source

Targeted protein degradation and multicomponent reactions in drug discovery [PDF]

, 2022
Multicomponent reaction (MCR) chemistry is a promising and useful tool for building the chemical library in a manner of high-efficiency, low-cost and mild conditions. Targeted protein degradation (TPD) as a hopeful technology has attracted much attention
Wang, Zefeng
core   +7 more sources