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 >

Dual leucine zipper kinase (DLK) and leucine zipper-bearing kinase (LZK) have emerged as key regulators of neuronal degeneration and axon growth.  WuXi AppTec scientists recently contributed to a research article in the Journal of Medicinal Chemistry demonstrating the use of ligand- and structure-based drug design approaches to discover an amino-pyrazine chemical series of DLK and …Read More >

Leverage our platform of biophysical methods to accelerate your research on targeted protein degradation. At DDC 2023, WuXi AppTec scientists presented an in-depth panel of assays to support the characterization of bifunctional small molecules. Our cutting-edge services include target protein ubiquitination and degradation assays, techniques to evaluate binary binding, and proximity assays to measure ternary …Read More >

Discover our end-to-end KRAS services platform presented at AACR 2023! WuXi AppTec scientists have established a comprehensive panel of assays on key mutants of KRAS, including G12C and G12D, to empower KRAS-targeted drug discovery. Our suite of services includes 2D/3D cell proliferation assays (utilizing cell lines harboring single or double KRAS mutations) as well as …Read More >