Chasing molecular glue degraders: screening approaches
A Domostegui, L Nieto-Barrado… - Chemical Society …, 2022 - pubs.rsc.org
Protein–protein interactions (PPIs) govern all biological processes. Some small molecules
modulate PPIs through induced protein proximity. In particular, molecular glue degraders …
modulate PPIs through induced protein proximity. In particular, molecular glue degraders …
E3 ligase ligand chemistries: from building blocks to protein degraders
In recent years, proteolysis-targeting chimeras (PROTACs), capable of achieving targeted
protein degradation, have proven their great therapeutic potential and usefulness as …
protein degradation, have proven their great therapeutic potential and usefulness as …
[PDF][PDF] Discovery and characterization of a selective IKZF2 glue degrader for cancer immunotherapy
S Bonazzi, E d'Hennezel, REJ Beckwith, L Xu… - Cell Chemical …, 2023 - cell.com
Malignant tumors can evade destruction by the immune system by attracting immune-
suppressive regulatory T cells (Treg) cells. The IKZF2 (Helios) transcription factor plays a …
suppressive regulatory T cells (Treg) cells. The IKZF2 (Helios) transcription factor plays a …
[HTML][HTML] Aging-associated HELIOS deficiency in naive CD4+ T cells alters chromatin remodeling and promotes effector cell responses
Immune aging combines cellular defects in adaptive immunity with the activation of
pathways causing a low-inflammatory state. Here we examined the influence of age on the …
pathways causing a low-inflammatory state. Here we examined the influence of age on the …
From thalidomide to rational molecular glue design for targeted protein degradation
Thalidomide and its derivatives are powerful cancer therapeutics that are among the best-
understood molecular glue degraders (MGDs). These drugs selectively reprogram the E3 …
understood molecular glue degraders (MGDs). These drugs selectively reprogram the E3 …
Targeted protein degradation: from mechanisms to clinic
Targeted protein degradation refers to the use of small molecules to induce the selective
degradation of proteins. In its most common form, this degradation is achieved through …
degradation of proteins. In its most common form, this degradation is achieved through …
[HTML][HTML] Cereblon covalent modulation through structure-based design of histidine targeting chemical probes
JT Cruite, GP Dann, J Che, KA Donovan… - RSC Chemical …, 2022 - pubs.rsc.org
Electrophilic biocompatible warheads, particularly cysteine-reactive acrylamides, have
enabled the development of covalent inhibitor drugs and chemical biology probes, but …
enabled the development of covalent inhibitor drugs and chemical biology probes, but …
[HTML][HTML] Applications of protein ubiquitylation and deubiquitylation in drug discovery
Y Chen, H Xue, J Jin - Journal of Biological Chemistry, 2024 - Elsevier
The ubiquitin-proteasome system (UPS) is the major machinery mediating specific protein
turnover in eukaryotic cells. By ubiquitylating unwanted, damaged, or harmful proteins and …
turnover in eukaryotic cells. By ubiquitylating unwanted, damaged, or harmful proteins and …
[HTML][HTML] Induced protein degradation for therapeutics: past, present, and future
The concept of induced protein degradation by small molecules has emerged as a
promising therapeutic strategy that is particularly effective in targeting proteins previously …
promising therapeutic strategy that is particularly effective in targeting proteins previously …