Knowledge Library
Osimertinib-Resistant Cell Lines and Models
Despite the robust clinical activity exerted by osimertinib, a majority of patients eventually exhibit disease progression while receiving this drug. Resistance to osimertinib includes both on-target and off-target mechanisms. With the use of osimertinib for advanced EGFR-mutant NSCLC increasing, the development of targeted therapies toward osimertinib resistance represents an unmet medical need. To support research …Read More >
Empowering Small Molecule Drug Discovery by Automatic DEL Screening
In this webinar, our expert speakers showcase our automatic DNA-encoded library (DEL) screening device, DELman. DNA-encoded library technology has proven to be a powerful tool for drug discovery. There are now several DEL-derived candidates in clinical stage. DEL enables researchers to explore vast chemical space with millions to billions of compounds. With DELman and other …Read More >
OncoWuXi Express: Large-scale Cell Panel Screening Platform for Integrated Pharmacogenomics and Bioinformatics Research
Introduction: OncoWuXi Express will continue to keep you informed about updates to our on-line tumor model database (OncoWuXi Database), as well as our recent progress in cancer and autoimmune research. In this issue, we showcase our large-scale cell panel screening platform for integrated pharmacogenomics and bioinformatics research. Cell viability assessment is a commonly used in …Read More >
Structure-Based Design and Synthesis of Potent and Selective KRAS G12D Inhibitors
The KRAS G12D mutation subtype is present in over 40% of pancreatic ductal adenocarcinomas (PDAC), making this an important drug target. WuXi AppTec scientists recently contributed to a research article in ACS Med. Chem. Letters describing the optimization of a series of potent and selective KRAS G12D inhibitors through a structure-based drug design approach. The …Read More >
Dianthus Platform: Screening for Modulators of SIK3
Salt-inducible kinases (SIKs) have recently emerged as key regulators of oncogenesis, inflammation, and immune responses, making these enzymes an important drug target. The isoform SIK3 is a novel regulator of tumor-intrinsic resistance to cytotoxic T cell attack. To support the discovery of novel SIK3 modulators, WuXi AppTec offers an integrated platform of ready-to-go biophysical assays …Read More >
Dianthus Platform: Screening for CRBN-DDB1 Proteolysis-Targeting Chimeras and Molecular Glues
Cereblon (CRBN) forms an E3 ligase complex together with DDB1, CUL4, and RBX1. CRBN functions as a substrate receptor of this complex for the recognition and binding of proteins targeted for ubiquitination and proteasomal degradation. To support the discovery of CRBN-DDB1 proteolysis-targeting chimeras and molecular glues, WuXi AppTec offers an integrated platform of ready-to-go assays …Read More >
Dianthus Platform: Screening for Inhibitors of PIK3CA-PIK3R1
Within the PI3K family, the heterodimer comprising the p110-α catalytic and p85-α regulatory subunits (encoded by PIK3CA and PIK3R1) is essential in the regulation of cellular proliferation and carcinogenesis. To support the discovery of novel PI3K inhibitors, WuXi AppTec offers an integrated platform of ready-to-go assays and Spectral Shift technology within Dianthus, an affinity screening …Read More >
Dianthus Platform: Screening for Inhibitors of PRMT5-WDR77
Protein arginine methyltransferase 5 (PRMT5) is an enzyme which plays an essential role in a wide range of cellular processes. PRMT5 overexpression has been implicated in many diseases, including cancer, making this protein an important drug target. To support the discovery of novel PRMT5-WDR77 inhibitors, WuXi AppTec offers an integrated platform of ready-to-go assays and …Read More >
Dianthus Platform: Screening for Modulators of STING
The adaptor protein STING (stimulator of interferon genes) has emerged as an exciting target for both immunological conditions (STING inhibition) and cancer therapies (STING activation). To support drug discovery teams in the discovery of novel modulators of STING, WuXi AppTec offers an integrated platform of ready-to-go biophysical assays and Dianthus, a plate-based and microfluidics-free affinity …Read More >