Knowledge Library
Heme Oxygenase-1-Targeting Molecules
WuXi AppTec scientists published a study in the open access archive ChemRxiv describing the discovery of highly selective, novel, heme oxygenase-1 (HO-1) targeting molecules. HO-1, primarily a heme-degrading enzyme, has been identified as a potential therapeutic target in diseases such as cancer and neurodegenerative disorders. Here, we report the discovery of five series of novel …Read More >
Addition of Covalent Warhead and DEL-Generated Hit Fragmentation Empower FBDD
Fragment-based drug discovery (FBDD) is one of the most well-developed approaches for projects starting from small, low-affinity compounds. At the SLAS 2024 meeting in Boston, WuXi AppTec presented a poster reporting on the assembly of a covalent fragment library that is suited to tackle protein targets via serine, lysine, and cysteine residues. In a case …Read More >
DNA-Compatible Cyclizations
The recent publication in the journal Organic Letters, ‘DNA-Compatible Cyclization Reaction to Access 1,3,4-Oxadiazoles & 1,2,4-Triazoles‘ by our WuXi Biology DEL team, introduces two novel DNA-compatible reactions, successfully incorporating bioactive cores 1,3,4-oxadiazoles and 1,2,4-triazoles into the DEL library. These cores are reported to show broad ranges of biological activities, such as antiviral, anti-inflammatory, anticancer, antifungal, …Read More >
High-Dimensional Flow Cytometry Platform
High-dimensional (HD) flow cytometry allows researchers to perform deep phenotyping of immune cells at the single cell level with increased accuracy and sensitivity. This technology enables complex pathway characterization and data integration for the identification of biomarkers used in immunotherapy. WuXi AppTec offers a comprehensive panel of HD flow cytometry services, with more than 100 …Read More >
DEL Insight: Novel Applications with the Bifunctional Linker of DNA-encoded Molecules
Due to the special configuration of the DNA encoded library (DEL), each DEL molecule carries a DNA sequence encoding its identity through a bifunctional linker. The linkers that are considered “redundant” and “troublesome” in traditional drug discovery actually offer innate advantages in many application scenarios. In this article, we review how to utilize DNA-encoded libraries …Read More >
Emerging Drug Discovery Strategies for Targeted Protein Degradation
In the last decade, targeted protein degradation (TPD) technology has become one of the most promising methods to remove specific disease-related proteins using cellular self-destruction mechanisms. In our latest White Paper, “Emerging Drug Discovery Strategies for Targeted Protein Degradation” we explore how DNA-encoded library (DEL) technology can be used for direct discovery of proteolysis-targeting chimeras …Read More >
Covalent Fragment-based Drug Discovery: BTK Inhibitors
At the Covalent Drug Discovery 2023 Summit and Fragments 2024 Conference, we presented a case study on Bruton’s tyrosine kinase (BTK) and demonstrated how biochemical, biophysical, and structural biology methods were used to confirm hits, characterize binding kinetics, and evaluate the mode of interaction of covalent BTK inhibitors. Our hit-to-lead workflow showcases the importance of bioanalytical …Read More >
Pioneering Advanced Modalities in Early Drug Discovery
New modalities such as peptides, oligonucleotides, and cell and gene therapies have revolutionized healthcare industry innovation. To meet these evolving needs, WuXi Biology has proactively developed a broad range of capabilities, offering integrated solutions to global pharmaceutical and biotech companies for challenging targets. We have established major capabilities for new modalities in the early discovery …Read More >
Biophysical and Structural Biology Methods Enable Fragment-Based Ligand Discovery
Powerful biophysical and structural biology tools enable the study of large numbers of fragments and are opening new possibilities in the treatment of various diseases. In this webinar, WuXi AppTec presents the results of a conventional and covalent fragment-based drug discovery screen, and our expert speaker discusses how orthogonal biophysical and structural methods enable the …Read More >