Cereblon (CRBN) forms an E3 ligase complex together with DDB1, CUL4, and RBX1. CRBN functions as a substrate receptor of this complex, and this protein is a key target for the action of small molecules.  Targeting of CRBN can modify its substrate specificity towards non-physiological proteins, which are subsequently ubiquitinated and degraded by the proteasome. …Read More >

TP53 is the most frequently mutated tumor suppressor gene in human cancer. Mutant p53 proteins not only lose wild-type p53-dependent tumor suppressive functions, but also frequently acquire oncogenic gain-of-functions that promote tumorigenesis.  Small molecules that can either protect p53 from negative regulators or restore the functionality of mutant p53 proteins are gaining interest, and potential drugs …Read More >

Targeted protein degradation of disease-causing proteins by the E3 ligase cereblon (CRBN) represents a new therapeutic strategy for addressing challenging-to-treat diseases. To support drug discovery programs, we have established off-the-shelf crystallization and cryo-EM systems to enable the determination of high-resolution X-ray crystal structures with a short turnaround time. Together with our protein production service and …Read More >

Inhibition of the Werner syndrome RecQ helicase (WRN) is a promising approach for the treatment of cancers commonly associated with microsatellite instability. To support drug discovery programs, we have established off-the-shelf crystallization systems to enable the determination of high-resolution X-ray crystal structures with a short turnaround time. Together with our protein production service and off-the-shelf …Read More >

WuXi Biology offers an integrated package of preclinical cancer pharmacology services for targeted oncology and immuno-oncology.  Our platform includes in vitro cell-free and cell-based assays, a comprehensive panel of in vivo tumor models, and multidisciplinary ex vivo PD analysis services. We have pioneered the development of over 1,500 PDX models across 30 cancer types, encompassing both …Read More >

Introduction: Diabetes is a chronic, metabolic disease resulting from defects in insulin secretion and varying degrees of insulin resistance. Early symptoms include increased thirst and urination, increased hunger, and blurred vision. Progressively, complications such as cardiovascular disease, peripheral neuropathy, nerve damage, myocardial disease, and kidney disease may occur. The prevalence of diabetes at younger ages …Read More >

GPCRs: Function, Structure, and Classifications G protein-coupled receptors (GPCRs) are a prevalent class of transmembrane proteins in animal cells, representing one of the largest families of membrane proteins in mammals. These receptors are widely distributed across numerous organs and regulate physiological functions by stimulating intracellular signaling pathways, thereby influencing cellular behavior. GPCRs have a central …Read More >

In addition to identifying chemical starting points for early drug discovery processes, DNA-encoded library (DEL) technology has now expanded to new applications, including the discovery of bifunctional affinity ligands historically considered difficult to develop. At the 2024 Gordon Research Conference, WuXi AppTec presented a poster describing how DEL can enable the rapid discovery of novel …Read More >

Despite the success of delivery technologies such as lipid nanoparticles and trivalent GalNAc conjugation, targeted delivery of oligonucleotides to extra hepatic tissues remains a challenge.  WuXi AppTec presented a poster showing the utilization of our peptide-based DNA-encoded library screening platform to identify endocytosis receptor-binding peptides.  The binding affinity of hit peptides was confirmed through biophysical …Read More >