[HTML][HTML] 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 …

Developments of CRBN-based PROTACs as potential therapeutic agents

C Wang, Y Zhang, Y Wu, D Xing - European journal of medicinal chemistry, 2021 - Elsevier
Protease-targeted chimeras (PROTACs) are a new technology that is receiving much
attention in the treatment of diseases. The mechanism is to inhibit protein function by …

Proteolysis-targeting chimera (PROTAC) delivery system: advancing protein degraders towards clinical translation

Y Chen, I Tandon, W Heelan, Y Wang… - Chemical Society …, 2022 - pubs.rsc.org
Proteolysis Targeting Chimeras (PROTACs), an emerging therapeutic entity designed to
degrade target proteins by hijacking the ubiquitin–proteasome system, have the potential to …

Unlocking the potential of PROTACs: A comprehensive review of protein degradation strategies in disease therapy

RP Bhole, PR Kute, RV Chikhale, CG Bonde, A Pant… - Bioorganic …, 2023 - Elsevier
The technology known asPROTACs (PROteolysisTArgeting Chimeras) is a method of
protein degradation. Utilising bifunctional small molecules, the ubiquitin-proteosome system …

AZD5438-PROTAC: a selective CDK2 degrader that protects against cisplatin-and noise-induced hearing loss

S Hati, M Zallocchi, R Hazlitt, Y Li… - European journal of …, 2021 - Elsevier
Abstract Cyclin-dependent kinase 2 (CDK2) is a potential therapeutic target for the treatment
of hearing loss and cancer. Previously, we identified AZD5438 and AT7519-7 as potent …

Proteolysis-targeting chimeras in biotherapeutics: Current trends and future applications

Q Li, L Zhou, S Qin, Z Huang, B Li, R Liu… - European Journal of …, 2023 - Elsevier
The success of inhibitor-based therapeutics is largely constrained by the acquisition of
therapeutic resistance, which is partially driven by the undruggable proteome. The …

Therapeutic targeting of eukaryotic initiation factor (eIF) 4E

J Pelletier, N Sonenberg - Biochemical Society Transactions, 2023 - portlandpress.com
Fundamental studies unraveled the role of eukaryotic initiation factor (eIF) 4E in mRNA
translation and its control. Under physiological conditions, regulation of translation by eIF4E …

Medicinal chemistry approaches to target the MNK–eIF4E axis in cancer

A Fernandez, PJ Monsen, LC Platanias… - RSC Medicinal …, 2023 - pubs.rsc.org
Aberrant translation of proteins that promote cell proliferation is an essential factor that
defines oncogenic processes and cancer. The process for ribosomal translation of proteins …

Inhibition of Eukaryotic Initiating Factor eIF4E Overcomes Abemaciclib Resistance in Gastric Cancer

H Zha, W Chen, W Shi, Y Liao - Current Medical Science, 2023 - Springer
Objective Aberrant activating mutations in cyclin-dependent kinases 4 and 6 (CDK4/6) are
common in various cancers, including gastroesophageal malignancies. Although CDK4/6 …

[HTML][HTML] miR-483-5p orchestrates the initiation of protein synthesis by facilitating the decrease in phosphorylated Ser209eIF4E and 4E-BP1 levels

S Nagaraj, A Stankiewicz-Drogon, E Darzynkiewicz… - Scientific Reports, 2024 - nature.com
Eukaryotic initiation factor 4E (eIF4E) is a pivotal protein involved in the regulatory
mechanism for global protein synthesis in both physiological and pathological conditions …