Fragment-based drug discovery (FBDD) is one of the most well-developed approaches for projects starting from small, low-affinity compounds.  At the SLAS 2024 meeting in Boston, WuXi AppTec presented a poster reporting on the assembly of a covalent fragment library that is suited to tackle protein targets via serine, lysine, and cysteine residues. In a case …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 >

Cyclin-dependent kinases (CDKs) and their cyclin regulatory subunits form complexes that are essential for driving abnormal growth processes in cancer cells, making these molecules important targets for cancer treatment. To support the discovery of novel CDK inhibitors, WuXi AppTec offers a comprehensive platform of biophysical and biochemical assays to accelerate hit finding and lead optimization …Read More >

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 >