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Abstract Supplement HIV Glasgow 8–11 November 2026, Glasgow, UK/Virtual

Journal of the International AIDS Society, Volume 29, Issue S6, November 2026.
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E3 Ligase Ligand Chemistries: From Building Blocks to Protein Degraders

Chemical Society Reviews, 2022
In recent years, proteolysis-targeting chimeras (PROTACs), capable of achieving targeted protein degradation, have proven their great therapeutic potential and usefulness as molecular biology tools.
Christian Steinebach, Izidor Sosič, Aleša Bricelj   +2 more
exaly   +4 more sources

Optimization of Potent Ligands for the E3 Ligase DCAF15 and Evaluation of Their Use in Heterobifunctional Degraders.

Journal of Medicinal Chemistry
Unlocking novel E3 ligases for use in heterobifunctional PROTAC degraders is of high importance to the pharmaceutical industry. Over-reliance on the current suite of ligands used to recruit E3 ligases could limit the potential of their application.
Simon C C Lucas, Afshan Ahmed, S. Ashraf, A. Argyrou, Matthias R Bauer, G. D. de Donatis, Sylvain Demanze, Frederik Eisele, Lucia Fusani, Andreas K Hock, Ganesh Kadamur, Shuyou Li, Abigail L Macmillan-Jones, Iacovos N. Michaelides, Christopher Phillips, Marie Rehnström, Magdalena Richter, Monica C. Rodrigo-Brenni, Fiona Shilliday, Peng Wang, R. Storer   +20 more
semanticscholar   +5 more sources

A C-Degron Structure-Based Approach for the Development of Ligands Targeting the E3 Ligase TRIM7.

ACS Chemical Biology
TRIM7 is a ubiquitin E3 ligase with key regulatory functions, mediating viral infection, tumor biology, innate immunity, and cellular processes, such as autophagy and ferroptosis. It contains a PRYSPRY domain that specifically recognizes degron sequences
C. J. Muñoz Sosa, Christopher Lenz, Anton Hamann, Frederic Farges, Johannes Dopfer, Andreas Krämer, Veronika Cherkashyna, Andrey Tarnovskiy, Yurii S. Moroz, E. Proschak, Václav Němec, S. Mueller, Krishna Saxena, S. Knapp   +13 more
semanticscholar   +4 more sources

Fragment-Based Approaches to Discover Ligands for Tumor-Specific E3 Ligases

Expert Opinion on Drug Discovery
Introduction Targeted protein degradation (TPD) has emerged as an innovative therapeutic strategy through selective degradation of specific proteins by harnessing the cellular ubiquitin-proteasome system (UPS), which involves over 600 E3 ubiquitin ...
Jongmin Park
exaly   +4 more sources

High Throughput E3 Ligase Degron Binding Assays for Novel PROTAC Ligand Discovery

Methods in Enzymology, 2023
The discovery of new small molecule ligands for E3 ligases will enable the creation of novel proteolysis targeting chimeras (PROTACs) and molecular glues to tackle traditionally undruggable proteins. Diversifying both the chemical matter for each E3 ligase and the type of ligases will be important to fully capture the potential of these targeted ...
Patrick Ryan Potts
exaly   +4 more sources

DNA‐Encoded Libraries for the Discovery of E3 Ligase Ligands

ChemMedChem
DNA‐encoded library (DEL) technology has emerged as a powerful tool to accelerate drug discovery, and its application has expanded to challenging targets such as E3 ubiquitin ligases, whose ligands are essential for the development of targeted therapies,
Lu-Lu Wen, Qing-Qing Zhang, Zhi-Qiang Duan, Rui Jin, Xiao-Jie Lu   +4 more
semanticscholar   +3 more sources