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 …

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 …

[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 …

[HTML][HTML] Aging-associated HELIOS deficiency in naive CD4+ T cells alters chromatin remodeling and promotes effector cell responses

H Zhang, RR Jadhav, W Cao, IN Goronzy, TV Zhao… - Nature …, 2023 - nature.com
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 …

From thalidomide to rational molecular glue design for targeted protein degradation

V Oleinikovas, P Gainza, T Ryckmans… - Annual Review of …, 2024 - annualreviews.org
Thalidomide and its derivatives are powerful cancer therapeutics that are among the best-
understood molecular glue degraders (MGDs). These drugs selectively reprogram the E3 …

Targeted protein degradation: from mechanisms to clinic

JM Tsai, RP Nowak, BL Ebert, ES Fischer - Nature Reviews Molecular …, 2024 - nature.com
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 …

The rise of degrader drugs

M Teng, NS Gray - Cell Chemical Biology, 2023 - cell.com
The cancer genomics revolution has served up a plethora of promising and challenging
targets for the drug discovery community. The field of targeted protein degradation (TPD) …

[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 …

[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 …

[HTML][HTML] Induced protein degradation for therapeutics: past, present, and future

H Yoon, JC Rutter, YD Li… - The Journal of Clinical …, 2024 - Am Soc Clin Investig
The concept of induced protein degradation by small molecules has emerged as a
promising therapeutic strategy that is particularly effective in targeting proteins previously …