WuXi AppTec scientists recently contributed to a research study which utilized an affinity purification mass spectrometry approach to identify nuclear interacting partners of Transcriptional Enhanced Associate Domain (TEAD) proteins.  The authors found a significant enrichment of interacting proteins linked to DNA damage, and they showed that depletion of TEAD transcription factors makes cells more susceptible …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 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 >

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 >

Read our newest case study on enhancing predictivity of drug-target interactions. In collaboration with Cyclica, WuXi AppTec scientists engaged in a study to understand the synergies between DNA encoded library (DEL) screening and Cyclica’s MatchMaker™ deep-learning model for protein-ligand interactions. Our findings indicate that combining experimental DEL data with computational analysis from MatchMaker™ can lead …Read More >