Current advances and development strategies of orally bioavailable PROTACs
S Zeng, Y Ye, H Xia, J Min, J Xu, Z Wang, Y Pan… - European Journal of …, 2023 - Elsevier
Proteolysis-targeting chimeras (PROTACs) have been an area of intensive research with the
potential to extend drug space not target to traditional molecules. In the last half decade, we …
potential to extend drug space not target to traditional molecules. In the last half decade, we …
Leveraging aptamers for targeted protein degradation
Z Yang, Q Pang, J Zhou, C Xuan, S Xie - Trends in pharmacological …, 2023 - cell.com
Targeted protein degradation (TPD) technologies, particularly proteolysis-targeting chimeras
(PROTACs), have emerged as a significant advancement in drug discovery. However …
(PROTACs), have emerged as a significant advancement in drug discovery. However …
[HTML][HTML] Regulation of EZH2 protein stability: new mechanisms, roles in tumorigenesis, and roads to the clinic
Y Guo, R Cheng, Y Wang, ME Gonzalez, H Zhang… - …, 2024 - thelancet.com
The importance of EZH2 as a key methyltransferase has been well documented
theoretically. Practically, the first EZH2 inhibitor Tazemetostat (EPZ6438), was approved by …
theoretically. Practically, the first EZH2 inhibitor Tazemetostat (EPZ6438), was approved by …
[HTML][HTML] PROTAC-Based Protein Degradation as a Promising Strategy for Targeted Therapy in Sarcomas
C Mancarella, A Morrione, K Scotlandi - International Journal of …, 2023 - mdpi.com
Sarcomas are heterogeneous bone and soft tissue cancers representing the second most
common tumor type in children and adolescents. Histology and genetic profiling discovered …
common tumor type in children and adolescents. Histology and genetic profiling discovered …
Journey of von hippel-lindau (VHL) E3 ligase in PROTACs design: From VHL ligands to VHL-based degraders
N Setia, HTA Almuqdadi, M Abid - European Journal of Medicinal Chemistry, 2023 - Elsevier
The scientific community has shown considerable interest in proteolysis-targeting chimeras
(PROTACs) in the last decade, indicating their remarkable potential as a means of achieving …
(PROTACs) in the last decade, indicating their remarkable potential as a means of achieving …
Application and challenges of nitrogen heterocycles in PROTAC linker
Y Li, J Qu, L Jiang, X Peng, K Wu, M Chen… - European Journal of …, 2024 - Elsevier
The absence of effective active pockets makes traditional molecularly targeted drug
strategies ineffective against 80% of human disease-related proteins. The PROTAC …
strategies ineffective against 80% of human disease-related proteins. The PROTAC …
ZX703: a small-molecule degrader of GPX4 inducing ferroptosis in human cancer cells
M Hu, X Li, L Wang, Y Zhang, Y Sun… - ACS Medicinal …, 2024 - ACS Publications
Ferroptosis is a novel form of oxidative cell death triggered by iron-dependent lipid
peroxidation. The induction of ferroptosis presents an attractive therapeutic strategy for …
peroxidation. The induction of ferroptosis presents an attractive therapeutic strategy for …
Efficient, multi-hundred-gram scale access to E3 ubiquitin ligase ligands for degrader development
MS Cooper, MC Norley, S Armitage… - Organic & …, 2023 - pubs.rsc.org
Small molecule heterobifunctional degraders (commonly also known as PROTACs) offer
tremendous potential to deliver new therapeutics in areas of unmet medical need. To deliver …
tremendous potential to deliver new therapeutics in areas of unmet medical need. To deliver …
Novel Amphiphilic PROTAC with Enhanced Pharmacokinetic Properties for ALK Protein Degradation
S Wang, Z Feng, C Qu, S Yu, H Zhang… - Journal of Medicinal …, 2024 - ACS Publications
Advancements in anticancer strategies spotlight proteolysis targeting chimera (PROTAC)
technology, yet it is hindered by poor water solubility and bioavailability. This study …
technology, yet it is hindered by poor water solubility and bioavailability. This study …
Use of ionic liquids in amidation reactions for proteolysis targeting chimera synthesis
M Eleuteri, J Desantis, G Cruciani, R Germani… - Organic & …, 2024 - pubs.rsc.org
Selective degradation of disease-causing proteins using proteolysis targeting chimeras
(PROTACs) has gained great attention, thanks to its several advantages over traditional …
(PROTACs) has gained great attention, thanks to its several advantages over traditional …