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 >

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 >

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 >

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 >

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 >

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 >

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 >