Results 21 to 30 of about 7,362 (230)

Targeted Degradation of Picornaviral 3C Protease via PROTACs Confers High Barrier to Viral Resistance and Broad-Spectrum Antiviral Activity. [PDF]

Adv Sci (Weinh)
This study reports D34 as the first PROTAC degrader that targets the 3C protease of picornaviruses. D34 effectively degrades EV71 3C protease via the ubiquitin‐proteasome pathway. More importantly, D34 exhibits a high resistance barrier and shows broad‐spectrum antiviral activity against multiple picornaviruses, highlighting its potential as a novel ...
Deng W, Chen J, Pang Y, Zhang Y, Chen S, You G, Tian X, Xu Z, Wang J, Shang L.   +9 more
europepmc   +2 more sources

Proteolysis-targeting chimeras (PROTACs) in cancer therapy

Molecular Cancer, 2022
Proteolysis-targeting chimeras (PROTACs) are engineered techniques for targeted protein degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits target protein and E3 ubiquitin ligase together to trigger proteasomal ...
Xinyi Li, Wenchen Pu, Qingquan Zheng, Min Ai, Song Chen, Yong Peng   +5 more
doaj   +1 more source

Reversible Covalent PROTACs: Novel and Efficient Targeted Degradation Strategy

Frontiers in Chemistry, 2021
The proteolysis targeting chimeras (PROTACs), which are composed of a target protein binding moiety, a linker, and an E3 ubiquitin ligase binder, have been a promising strategy for drug design and discovery.
Minghua Yuan, Minghua Yuan, Yanan Chu, Yanan Chu, Yongtao Duan   +4 more
doaj   +1 more source

PROTAC-Design-Evaluator (PRODE): An Advanced Method for In-Silico PROTAC Design

ACS Omega, 2023
Abstract PROTAC (proteolysis-targeting chimeras) is a rapidly evolving technology to target undruggable targets. The mechanism by which this happens is when a bifunctional molecule binds to a target protein and also brings in proximity an E3 ubiquitin ligase to trigger ubiquitination and degradation of the target protein.
Ben Geoffrey A S, Deepak Agrawal, Nagaraj M. Kulkarni, Rajappan Vetrivel, Kishan Gurram   +4 more
openaire   +3 more sources

The clinical advances of proteolysis targeting chimeras in oncology

Exploration of Targeted Anti-tumor Therapy, 2021
Proteolysis targeting chimeras (PROTACs) are a class of small molecules designed to target proteins for degradation. Their novel and unique modes of action provide PROTACs with the potential for their application in the management of both solid and ...
Hao Xie, Junjia Liu, Diego M. Alem Glison, Jason B. Fleming   +3 more
doaj   +1 more source

Proteolysis-targeting chimaeras (PROTACs) as pharmacological tools and therapeutic agents: advances and future challenges

Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Proteolysis-targeting chimaeras (PROTACs) have been developed to be an emerging technology for targeted protein degradation and attracted the favour of academic institutions, large pharmaceutical enterprises, and biotechnology companies. The mechanism is
Chao Wang, Yujing Zhang, Tingting Zhang, Lingyu Shi, Zhongmin Geng, Dongming Xing   +5 more
doaj   +1 more source

PROTACs– a game-changing technology [PDF]

Expert Opinion on Drug Discovery, 2019
Introduction: Proteolysis - targeting chimeras (PROTACs) have emerged as a new modality with the potential to revolutionize drug discovery. PROTACs are heterobifunctional molecules comprising of a ligand targeting a protein of interest, a ligand targeting an E3 ligase and a connecting linker.
Konstantinidou, Markella, Li, Jingyao, Zhang, Bidong, Wang, Zefeng, Shaabani, Shabnam, Ter Brake, Frans, Essa, Khaled, Dömling, Alexander   +7 more
openaire   +2 more sources

Tackling Drug Resistance in EGFR Exon 20 Insertion Mutant Lung Cancer

Pharmacogenomics and Personalized Medicine, 2021
Laura Pacini,* Andrew D Jenks,* Simon Vyse,* Christopher P Wilding, Amani Arthur, Paul H Huang Division of Molecular Pathology, The Institute of Cancer Research, London, UK*These authors contributed equally to this workCorrespondence: Paul H ...
Pacini L, Jenks AD, Vyse S, Wilding CP, Arthur A, Huang PH   +5 more
doaj  

Light-Activating PROTACs in Cancer: Chemical Design, Challenges, and Applications

Applied Sciences, 2022
Nonselective cell damage remains a significant limitation of radiation therapies in cancer. Decades of successful integration of radiation therapies with other medicinal chemistry strategies significantly improved therapeutic benefits in cancer ...
Arvind Negi, Kavindra Kumar Kesari, Anne Sophie Voisin-Chiret   +2 more
doaj   +1 more source

Protacs for Treatment of Cancer [PDF]

Pediatric Research, 2010
Protein degradation is the cell's mechanism of eliminating misfolded or unwanted proteins. The pathway by which proteins are degraded occurs through the ubiquitin-proteasome system. Ubiquitin is a small 9-kD (kDa) protein that is attached to proteins. A minimum of four ubiquitins are required for proteins to be recognized by the degradation machinery ...
openaire   +2 more sources