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 >

Cyclin-dependent kinase 2 (CDK2) and its respective cyclin E1 and cyclin A2 complexes are essential to driving abnormal growth processes in cancer cells, making these proteins important targets for cancer treatment.  To support the discovery of novel CDK2 inhibitors, WuXi AppTec offers a comprehensive platform of biophysical and biochemical assays to accelerate hit finding and …Read More >

Werner syndrome helicase (WRN) is a key drug target for cancers with microsatellite instability.  To support the discovery of potent and selective WRN inhibitors, WuXi AppTec offers a comprehensive platform of biophysical and biochemical assays to support hit finding and lead optimization efforts targeting WRN.  Our panel of services also include high-quality WRN protein production …Read More >

Macrocyclic peptides are an emerging molecular class for targeting intracellular protein–protein interactions (PPIs) and for providing an oral modality for drug targets. Herein, we use DNA-encoded cyclic peptide libraries to discover a neutral nonapeptide, UNP-6457, that inhibits MDM2–p53 interaction with an IC50 of 8.9 nM. These studies showcase how tailored DEL libraries can directly yield …Read More >

Drug Discovery Chemistry Conference 2023 Powerful biophysical and structural biology tools enable the study of large numbers of covalent fragments and are opening up new possibilities in the treatment of various diseases. Here, Dr. Moran Jerabek-Willemsen, Head of Biophysics & Screening in WuXi Biology reports the results of a covalent FBDD project on Bruton’s Tyrosine …Read More >