PROTACs: emerging targeted protein degradation approaches for advanced druggable strategies

NI Sincere, K Anand, S Ashique, J Yang, C You - Molecules, 2023 - mdpi.com
A potential therapeutic strategy to treat conditions brought on by the aberrant production of a
disease-causing protein is emerging for targeted protein breakdown using the PROTACs …

[HTML][HTML] Emerging protein degradation strategies: expanding the scope to extracellular and membrane proteins

J Lin, J Jin, Y Shen, L Zhang, G Gong, H Bian… - Theranostics, 2021 - ncbi.nlm.nih.gov
Classic small molecule inhibitors that directly target pathogenic proteins typically rely on the
accessible binding sites to achieve prolonged occupancy and influence protein functions …

Catalytic in vivo protein knockdown by small-molecule PROTACs

DP Bondeson, A Mares, IED Smith, E Ko… - Nature chemical …, 2015 - nature.com
The current predominant therapeutic paradigm is based on maximizing drug-receptor
occupancy to achieve clinical benefit. This strategy, however, generally requires excessive …

Targeted protein degradation in vivo with Proteolysis Targeting Chimeras: Current status and future considerations

GF Watt, P Scott-Stevens, L Gaohua - Drug Discovery Today: Technologies, 2019 - Elsevier
Proteolysis Targeting Chimeras (PROTACs) are a rapidly expanding new therapeutic
modality inducing selective protein degradation and offering the potential of a differentiated …

Target protein degradation by protacs: A budding cancer treatment strategy

D Choudhary, A Kaur, P Singh, G Chaudhary… - Pharmacology & …, 2023 - Elsevier
Cancer is one of the most common causes of death. So, its lethal effect increases with time.
Near about hundreds of cancers are known in humans. Cancer treatment is done to cure or …

Small molecule PROTACs: an emerging technology for targeted therapy in drug discovery

H Pei, Y Peng, Q Zhao, Y Chen - RSC advances, 2019 - pubs.rsc.org
Curing malignant carcinomas is a grand ambition in the development of human health. Over
the past decades, targeted therapies have become one of the most successful ways of …

The role of reversible and irreversible covalent chemistry in targeted protein degradation

H Kiely-Collins, GE Winter, GJL Bernardes - Cell chemical biology, 2021 - cell.com
Proteolysis-targeting chimeras (PROTACs) that degrade disease-causing proteins by
hijacking the endogenous ubiquitin-proteasome system have emerged as an exciting and …

Proteolysis targeting chimeras (PROTACs): a perspective on integral membrane protein degradation

C Ruffilli, S Roth, M Rodrigo, H Boyd… - ACS Pharmacology & …, 2022 - ACS Publications
Targeted protein degradation (TPD) is a promising therapeutic modality to modulate protein
levels and its application promises to reduce the “undruggable” proteome. Among TPD …

Stimuli-activatable PROTACs for precise protein degradation and cancer therapy

J Gao, L Yang, S Lei, F Zhou, H Nie, B Peng, T Xu… - Science bulletin, 2023 - Elsevier
The proteolysis targeting chimeras (PROTACs) approach has attracted extensive attention in
the past decade, which represents an emerging therapeutic modality with the potential to …

E3 ligase ligands for PROTACs: how they were found and how to discover new ones

T Ishida, A Ciulli - … Advancing the Science of Drug Discovery, 2021 - journals.sagepub.com
Bifunctional degrader molecules, also called proteolysis-targeting chimeras (PROTACs), are
a new modality of chemical tools and potential therapeutics to understand and treat human …