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 >

Oncolytic viruses (OVs) are emerging as a promising therapeutic approach for treating cancer. OVs are capable of both tumor-specific cell lysis and immune stimulation and can be optimized for enhanced tumor selectivity.  WuXi AppTec offers a comprehensive platform of OV-related services, including virus engineering and validation, immune profiling and lysis assays, tumor cell selectivity assays, …Read More >

WuXi AppTec scientists contributed to a study which identified a novel, indole-based, selective estrogen receptor degrader (SERD), designated LX-039. The authors show that LX-039 exhibits potent activity in ER degradation and proliferation assays. With favorable ADME/PK properties, LX-039 also exhibits higher efficacy in a tamoxifen-resistant MCF7 CDX model compared to fulvestrant, with up to 90% inhibition …Read More >

WuXi AppTec scientists collaborated on a study to characterize a series of pyrroloquinoline derivatives that were designed and synthesized to understand the effect of various substitutions on human cytomegalovirus (HCMV) polymerase activity, antiviral activity, and hERG inhibition.  Results suggest that substitutions can be fine-tuned to reduce hERG inhibition while maintaining HCMV antiviral potency. The abstract …Read More >

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 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 >