The ubiquitin-proteasome system (UPS) is the major machinery mediating specific protein
turnover in eukaryotic cells. By ubiquitylating unwanted, damaged, or harmful proteins and …

Abstract Structure-based virtual screening is a key tool in early drug discovery, with growing
interest in the screening of multi-billion chemical compound libraries. However, the success …

Abstract β-Catenin is a well-established driver of many cancers; however, there are
challenges in developing agents targeting β-catenin for clinical use. Recent progress has …

Targeted protein degradation and stabilization are promising therapeutic modalities
because of their potency, versatility and their potential to expand the druggable target …

Men or mice with homozygous serine/threonine kinase 33 (STK33) mutations are sterile
owing to defective sperm morphology and motility. To chemically evaluate STK33 for male …

PROTAC®(proteolysis-targeting chimera) molecules induce proximity between an E3 ligase
and protein-of-interest (POI) to target the POI for ubiquitin-mediated degradation …

The development of novel drug modalities is necessary to overcome the current critical
issues in the treatment of cancer, namely toxicity, insufficient efficacy, and the development …

Chemically induced proximity-based targeted protein degradation (TPD) has become a
prominent paradigm in drug discovery. With the clinical benefit demonstrated by certain …

Targeted protein degradation (TPD) strategy harnesses the ubiquitin-proteasome system
(UPS) to degrade a protein of interest (POI) by bringing it into proximity with an E3 ubiquitin …

WNK family kinases are regulated by osmotic stress and control ion homeostasis by
activating SPAK and OXSR1 kinases. Using a proximity ligation approach, we found that …