Knowledge Library
Oligonucleotide Therapeutics: Drug Discovery Through Tightly Coupled Chemistry and Biology
Designing effective oligonucleotide therapeutics for clinical applications involves understanding both the chemistry and biology of nucleic acids. In this white paper, learn about recent advances in chemical modifications for oligonucleotide therapeutics that improve stability and selectivity, biological screening assays to support lead optimization, and bioanalytical platforms that address the challenges of quantifying oligonucleotides. Check out …Read More >
Oncolytic Virus Platform
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 >
Discovery and preclinical profile of LX-039, a novel indole-based oral selective estrogen receptor degrader (SERD)
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 >
Inhibition of the hERG potassium ion channel by non-nucleoside CMV polymerase antiviral inhibitors
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 >
Recent Advances in Library Synthesis to Accelerate Medicinal Chemistry Research
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 >
Research Chemistry Services
Delivering synthetic and medicinal chemistry solutions to global pharma and biotech customers for the discovery of hits, leads, and preclinical candidates. Check out our comprehensive panel of integrated, discovery chemistry services.
Discovery of RNA Targeting Small Molecules – Our Toolbox for RNA Drug Discovery
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 >
Biophysical and Structural Biology Methods Enable Fragment-based Covalent Ligand Discovery of Human BTK
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 >
DNA-Encoded Libraries for the Discovery of Small-Molecule Hits
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 >