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 >

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 >

WuXi AppTec provides a comprehensive platform of advanced biophysical assays and structural biology services to accelerate lead optimization efforts focused on GPCRs and membrane proteins. Our capabilities include high-quality protein production across all major target classes and nanodisc reconstitution of membrane proteins for screening. We also offer established protocols for cryo-EM structure determination and assessment …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 >

Introduction: 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 DNA-encoded library selection against a privileged scaffold to identify a compound with potent inhibition against human glutathione S-transferase Mu 2.  SAR studies, coupled with X-ray crystallography and …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 >

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 inhibitors, WuXi AppTec offers a comprehensive platform of biophysical and biochemical …Read More >