Knowledge Library
Xenograft and Syngeneic Tumor Models in Rats
Leverage our extensive panel of rat xenograft and syngeneic tumor models. Advantages for using rats in preclinical efficacy studies compared with mice include: more similar metabolism and physiology to human; easier use for orthotopic model surgery, vascular manipulation, and imaging; larger sampling sizes to ensure sufficient amount for bioanalysis; consistent animal species to toxicology studies …Read More >
Optimization and Mechanistic Investigations of Novel Allosteric Activators of PKG1α
WuXi AppTec scientists recently contributed to a research article in the Journal of Medicinal Chemistry describing the optimization of a piperidine series of small molecules as novel allosteric activators of PKG1α (a compelling drug target for treatment of cardiovascular diseases). This study reveals a mechanism of action for these compounds consistent with cGMP-induced activation, including …Read More >
Large-scale synthesis of a Notum inhibitor employing a modified Sakai reaction as the key step
WuXi AppTec scientists recently contributed to a research article in the Royal Society of Chemistry describing the large-scale synthesis of a potent and selective inhibitor of Notum carboxylesterase (an enzyme that suppresses Wnt signaling pathways). By employing a modified Sakai reaction as the key step, a one-pot synthesis of this Notum inhibitor was developed, enabling …Read More >
Discovery and Structural Characterization of Small Molecule Binders of the Human CTLH E3 Ligase Subunit GID4
Expansion of the E3 ligase toolbox has the potential to dramatically advance the field of targeted protein degradation. WuXi AppTec scientists recently contributed to a research article in the Journal of Medicinal Chemistry describing the discovery of novel small molecule binders of GID4, a substrate receptor in the human CTLH E3 ligase complex. Researchers used …Read More >
Fluoroalkane modified cationic polymers for personalized mRNA cancer vaccines
Delivery carriers are a critical component in the development of mRNA vaccines. Here, we describe the synthesis of a cationic polymer as a carrier for mRNA cancer vaccine delivery. In vivo results show that this polymer-based mRNA vaccine significantly delays tumor growth after vaccination of mice. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9743697/
KRAS-related Genetically Engineered Cell Lines and In Vivo Models
KRAS mutant proteins that drive cancer development are highly similar in sequence and structure. Direct inhibitors are most likely to bind to the catalytic domain of KRAS. However, recent studies have found that KRAS mutants can also be targeted by heterogeneous sites, to develop covalent inhibitors of KRAS mutants. The discovery of inhibitors that selectively …Read More >
WuXi Biology Fact Sheet
Expertise in all major disease areas and all major target classes, enabling discovery for all therapeutic modalities World class antiviral platform with an unequalled service capability and capacity in HBV and other viral diseases A global leader in DNA Encoded Library (DEL) screening, with innovative business models CAP-certified pathology and FACS capabilities supporting clinical biomarker …Read More >
Targeted Protein Degradation
WuXi AppTec utilizes state-of-the-art techniques to support drug discovery teams focused on targeted protein degradation. Our services include a broad range of ligand-finding methods, such as DEL, fragment screening, ASMS, and virtual screening. We provide custom linker design and complex synthesis for new linkers and E3 ligase ligands. To support lead optimization efforts, our platform …Read More >
In Vitro Imaging Services
Offering a comprehensive platform of in vitro imaging-based assays to screen compounds for cancer, inflammation, and autoimmune diseases. Our services include: Imaging assays for cell proliferation and apoptosis Imaging assays for cell cycle analysis Cell-based functional assays, including: Antibody internalization Live-cell immunocytochemistry Cellular movement and morphology monitoring Assays for 3D cell models, including: Spheroid growth …Read More >