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 >

DELvision is a powerful DNA encoded library (DEL)-based toolset for AIphaFold-assisted drug discovery and target sciences. In contrast to conventional screens where the target space is low-dimensional, DELvision comprises a high-dimensional map of binding relationships between small molecules and protein targets. As such, this rich data universe enables simultaneous characterization of targets and exploration of …Read More >

As reported in Business Wire: DNA-Encoded Libraries (DELs) and NanoBRET Target Engagement Assays Accelerate Drug Discovery: “The authors demonstrate that DELs can benefit chemical biologists who require verification of live cell target engagement for their protein of interest. This is particularly beneficial for understudied protein classes that may not have existing chemical probes. Additionally, they …Read More >

WuXi AppTec scientists recently contributed to a research article in Cell Chemical Biology demonstrating the successful conversion of ligands identified from DNA-encoded library (DEL) screening into highly functional, cell-active, bioluminescence resonance energy transfer (BRET) probes. The authors show that analyzing preliminary DEL hits based on target occupancy data generated in live, intact cells is an …Read More >

Learn how parallel medicinal chemistry (PMC) and high throughput experimentation (HTE) combined with machine learning can provide a more focused approach to target molecules, resulting in a more concentrated set of compounds to make the process of lead selection easier. Our experts show how PMC can shorten the turnaround time of the design-synthesis-test cycle, providing …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 WuXi AppTec has developed technologies to facilitate RNA small molecule screening, an exciting frontier in drug discovery. SHAPE-MaP is applied to determine RNA structure and dynamics and verify small molecule binding. We utilize the “DNA-Zipper” strategy to enable DNA-encoded libraries to identify RNA binders. With other technologies including fragment-based drug …Read More >

Drug Discovery Chemistry Conference 2023 DNA-Encoded library (DEL) screening is now commonly used in the pharmaceutical industry to find novel chemical matter that modulates protein targets of interest.  Point-by-point, Dr. Alex Satz, Executive Director, WuXi Biology will discuss the primary challenges and limitations of DEL screening, and concisely state the current abilities of the technology …Read More >