Powerful biophysical and structural biology tools enable the study of large numbers of fragments and are opening new possibilities in the treatment of various diseases. In this webinar, WuXi AppTec presents the results of a conventional and covalent fragment-based drug discovery screen, and our expert speaker discusses how orthogonal biophysical and structural methods enable the …Read More >

DNA-dependent protein kinase (DNA-PK) plays an important role in the overall survival and proliferation of cells, making this enzyme an intriguing target for the treatment of a variety of cancers.  In our latest publication, WuXi AppTec scientists contributed to the discovery and characterization of ZL-2201, a potent and highly selective small molecule DNA-PK inhibitor.  In …Read More >

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 >

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 >

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 >

Screen your compounds across our comprehensive cell screening panel of over 600 authenticated, validated human cancer cell lines covering 50 cancer types.  We provide single agent and combination compound screening for potency and synergy, and bioinformatics analysis for mechanistic studies and biomarker discovery related to drug responses.  We also offer an extensive KRAS mutant cell …Read More >

The metabotropic glutamate receptor mGluR7 is widely expressed throughout the CNS and has been implicated in numerous CNS disorders.  WuXi AppTec scientists recently contributed to a study which led to the identification, optimization, and characterization of a highly potent, novel mGluR7 allosteric agonist, designated CVN636.  The authors show that CVN636 has high selectivity toward mGluR7, …Read More >

WuXi AppTec scientists recently contributed to a study which led to the discovery and optimization of a novel series of GST inhibitors. The authors used affinity mediated DEL selection against a privileged scaffold to identify a compound with potent inhibition against SjGST and GSTM2. SAR studies, coupled with X-ray crystallography and structural analysis, revealed that …Read More >

Within the PI3K family, the heterodimer protein comprising the p110-α and p85-α catalytic/regulatory subunits (encoded by PIK3CA and PIK3R1) are essential in the regulation of cellular proliferation and carcinogenesis.  To support the discovery of novel PI3K inhibitors, WuXi AppTec offers a comprehensive platform of biophysical and biochemical assays to accelerate hit finding and lead optimization …Read More >