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 …
Emerging strategies for prospective discovery of molecular glue degraders
Molecular glue (MG) degraders are monovalent small molecule compounds that co-opt E3
ubiquitin ligases to target neo-substrates for proteasomal degradation. Here, we provide a …
ubiquitin ligases to target neo-substrates for proteasomal degradation. Here, we provide a …
Confounding factors in targeted degradation of short-lived proteins
Targeted protein degradation has recently emerged as a novel option in drug discovery.
Natural protein half-life is expected to affect the efficacy of degrading agents, but to what …
Natural protein half-life is expected to affect the efficacy of degrading agents, but to what …
[HTML][HTML] Alkylamine-tethered molecules recruit FBXO22 for targeted protein degradation
C Kagiou, JA Cisneros, J Farnung, J Liwocha… - Nature …, 2024 - nature.com
Targeted protein degradation (TPD) relies on small molecules to recruit proteins to E3
ligases to induce their ubiquitylation and degradation by the proteasome. Only a few of the …
ligases to induce their ubiquitylation and degradation by the proteasome. Only a few of the …
[HTML][HTML] Template-assisted covalent modification underlies activity of covalent molecular glues
Molecular glues are proximity-inducing small molecules that have emerged as an attractive
therapeutic approach. However, developing molecular glues remains challenging, requiring …
therapeutic approach. However, developing molecular glues remains challenging, requiring …
Combinatorial Ubiquitination REal-time PROteolysis (CURE-PROs): a modular platform for generating reversible, self-assembling bifunctional targeted degraders
Proteolysis-Targeting Chimeras (PROTACs) are bifunctional molecules that bring a target
protein and an E3 ubiquitin ligase into proximity to append ubiquitin, thus directing target …
protein and an E3 ubiquitin ligase into proximity to append ubiquitin, thus directing target …
TET3-overexpressing macrophages promote endometriosis
H Lv, B Liu, Y Dai, F Li, S Bellone, Y Zhou… - The Journal of Clinical …, 2024 - jci.org
Endometriosis is a debilitating, chronic inflammatory disease affecting~ 10% of reproductive
age women worldwide with no cure. While macrophages have been intrinsically linked to …
age women worldwide with no cure. While macrophages have been intrinsically linked to …
[HTML][HTML] Breaking Bad Proteins—Discovery Approaches and the Road to Clinic for Degraders
Proteolysis-targeting chimeras (PROTACs) describe compounds that bind to and induce
degradation of a target by simultaneously binding to a ubiquitin ligase. More generally …
degradation of a target by simultaneously binding to a ubiquitin ligase. More generally …
Extrapolating Lessons from Targeted Protein Degradation to Other Proximity-Inducing Drugs
GE Winter - ACS Chemical Biology, 2024 - ACS Publications
Targeted protein degradation (TPD) is an emerging pharmacologic strategy. It relies on
small-molecule “degraders” that induce proximity of a component of an E3 ubiquitin ligase …
small-molecule “degraders” that induce proximity of a component of an E3 ubiquitin ligase …
Overview of Class I HDAC Modulators: Inhibitors and Degraders
Z Huang, L Zeng, B Cheng, D Li - European Journal of Medicinal Chemistry, 2024 - Elsevier
Class I histone deacetylases (HDACs) are closely associated with the development of a
diverse array of diseases, including cancer, neurodegenerative disorders, HIV, and …
diverse array of diseases, including cancer, neurodegenerative disorders, HIV, and …