From conception to development: investigating PROTACs features for improved cell permeability and successful protein degradation
C Cecchini, S Pannilunghi, S Tardy… - Frontiers in …, 2021 - frontiersin.org
Proteolysis Targeting Chimeras (PROTACs) are heterobifunctional degraders that
specifically eliminate targeted proteins by hijacking the ubiquitin-proteasome system (UPS) …
specifically eliminate targeted proteins by hijacking the ubiquitin-proteasome system (UPS) …
Decoding the messaging of the ubiquitin system using chemical and protein probes
LT Henneberg, BA Schulman - Cell chemical biology, 2021 - cell.com
Post-translational modification of proteins by ubiquitin is required for nearly all aspects of
eukaryotic cell function. The numerous targets of ubiquitylation, and variety of ubiquitin …
eukaryotic cell function. The numerous targets of ubiquitylation, and variety of ubiquitin …
Development of BromoTag: a “Bump-and-Hole”–PROTAC system to induce potent, rapid, and selective degradation of tagged target proteins
Small-molecule-induced protein depletion technologies, also called inducible degrons,
allow degradation of genetically engineered target proteins within cells and animals. Here …
allow degradation of genetically engineered target proteins within cells and animals. Here …
[HTML][HTML] Molecular glues modulate protein functions by inducing protein aggregation: A promising therapeutic strategy of small molecules for disease treatment
Molecular glues can specifically induce aggregation between two or more proteins to
modulate biological functions. In recent years, molecular glues have been widely used as …
modulate biological functions. In recent years, molecular glues have been widely used as …
Design, synthesis, and evaluation of trivalent PROTACs having a functionalization site with controlled orientation
Y Huang, H Yokoe, A Kaiho-Soma… - Bioconjugate …, 2021 - ACS Publications
Trivalent PROTACs having a functionalization site with controlled orientation were designed,
synthesized, and evaluated. Based on the X-ray structure of BRD protein degrader MZ1 (1) …
synthesized, and evaluated. Based on the X-ray structure of BRD protein degrader MZ1 (1) …
A Reliable and Sustainable Multicomponent Access to Protein Degraders
The use of small molecules to induce targeted protein degradation is increasingly growing in
the drug discovery landscape and protein degraders have progressed rapidly through the …
the drug discovery landscape and protein degraders have progressed rapidly through the …