PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

M He, C Cao, Z Ni, Y Liu, P Song, S Hao, Y He… - … and Targeted Therapy, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …

E3 ligase ligand chemistries: from building blocks to protein degraders

I Sosič, A Bricelj, C Steinebach - Chemical Society Reviews, 2022 - pubs.rsc.org
In recent years, proteolysis-targeting chimeras (PROTACs), capable of achieving targeted
protein degradation, have proven their great therapeutic potential and usefulness as …

Discovery of norbornene as a novel hydrophobic tag applied in protein degradation

S Xie, F Zhan, J Zhu, Y Sun, H Zhu, J Liu… - Angewandte …, 2023 - Wiley Online Library
Hydrophobic tagging (HyT) is a potential therapeutic strategy for targeted protein
degradation (TPD). Norbornene was discovered as an unprecedented hydrophobic tag in …

PROTAC therapy as a new targeted therapy for lung cancer

JW Li, G Zheng, FJ Kaye, L Wu - Molecular therapy, 2023 - cell.com
Despite recent advances in molecular therapeutics, lung cancer is still a leading cause of
cancer deaths. Currently, limited targeted therapy options and acquired drug resistance …

Small-Molecule Hydrophobic Tagging: A Promising Strategy of Druglike Technology for Targeted Protein Degradation: Miniperspective

S Xie, J Zhu, J Li, F Zhan, H Yao, J Xu… - Journal of Medicinal …, 2023 - ACS Publications
Targeted protein degradation (TPD) technologies have catalyzed a paradigm shift in
therapeutic strategies and offer innovative avenues for drug design. Hydrophobic tags …

Catalytic degraders effectively address kinase site mutations in EML4-ALK oncogenic fusions

Y Gao, B Jiang, H Kim, MJ Berberich… - Journal of Medicinal …, 2023 - ACS Publications
Heterobifunctional degraders, known as proteolysis targeting chimeras (PROTACs),
theoretically possess a catalytic mode-of-action, yet few studies have either confirmed or …

Targeted protein degradation in cancers: Orthodox PROTACs and beyond

J Li, X Chen, A Lu, C Liang - The Innovation, 2023 - cell.com
Targeted protein degradation (TPD) is emerging as a strategy to overcome the limitations of
traditional small-molecule inhibitors. Proteolysis-targeting chimera (PROTAC) technology …

Recent progress in degradation of membrane proteins by PROTACs and alternative targeted protein degradation techniques

S Chen, J Cui, H Chen, B Yu, S Long - European Journal of Medicinal …, 2023 - Elsevier
Targeted protein degradation (TPD) is one of the key strategies of current targeted cancer
therapy, and it can eliminate some of the root causes of cancer, and effectively avoid drug …

Unprecedented chemoselective Ru (III)-catalyzed [3+ 2] annulation of enaminones with iodonium ylides for the synthesis of functionalized 3a, 7a-dihydroxy hexahydro …

M Zhang, L Chen, Z Liu, J Huang, F Yu - Organic Chemistry Frontiers, 2023 - pubs.rsc.org
Herein, a straightforward and efficient method to obtain 3a, 7a-dihydroxy hexahydro-4H-
indol-4-ones via Ru (III)-catalyzed alkenyl C (sp2)–H bond functionalization/[3+ 2] …

Azaindole derivatives as potential kinase inhibitors and their SARs elucidation

G Fang, H Chen, Z Cheng, Z Tang, Y Wan - European Journal of Medicinal …, 2023 - Elsevier
Currently, heterocycles have occupied an important position in the fields of drug design.
Among them, azaindole moiety is regarded as one privileged scaffold to develop therapeutic …