Targeted protein degradation (TPD) technology has become one of the most promising methods to remove specific disease-related proteins using cellular self-destruction mechanisms. This technology is enabling researchers to pursue targets that were previously considered undruggable and to address the resistance issue of small molecule inhibitors. Since 2016, WuXi AppTec has built a comprehensive TPD discovery …Read More >

The Son of Sevenless (SOS) protein is a guanine nucleotide exchange factor that acts as a key activator for KRAS function. The binding between KRAS and SOS helps facilitate the turnover of GDP-loaded KRAS (“off” state) into its GTP-loaded “on” state.  Disrupting the SOS1-KRAS complex with an SOS1 binder is a compelling strategy to help …Read More >

The RAS family of small GTPases are among the most frequently mutated oncogenes in human cancer. Previously viewed as undruggable, the recent FDA approval of two KRAS G12C-selective inhibitors has offered real promise to the development of anti-RAS therapies, including mutation-specific strategies. To support the discovery of novel KRAS inhibitors, WuXi AppTec offers a comprehensive …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 >

STAT proteins are key mediators of cellular immunity, proliferation, apoptosis, and differentiation.  STATs are known to play a role in the pathogenesis of many different diseases (including cancer) and the development of drugs directly or indirectly targeting STAT signaling has become a major focus for discovery teams.  WuXi AppTec offers a comprehensive platform of biophysical …Read More >

At the Covalent Drug Discovery 2023 Summit and Fragments 2024 Conference, we presented a case study on Bruton’s tyrosine kinase (BTK) and demonstrated how biochemical, biophysical, and structural biology methods were used to confirm hits, characterize binding kinetics, and evaluate the mode of interaction of covalent BTK inhibitors. Our hit-to-lead workflow showcases the importance of bioanalytical …Read More >

RecQ helicases (BLM, WRN, RECQL, RECQL4, and RECQL5) are an important family of surveillance proteins that play critical roles in genome maintenance and stability. Inherited mutations in these helicases are linked to distinct human disease syndromes, as well as cancer. To support the discovery of potent and selective RecQ helicase inhibitors, WuXi AppTec offers a …Read More >