Knowledge Library
Cutting-Edge Crystallography Services
Discover our comprehensive structure generation platform for challenging targets, with our high resolution and high throughput crystallization services to support hit finding through to lead optimization.
Crystal-Grade Protein Production
With a focus on quality and stability, gain access to our established systems, strategies, and advanced co-expression vectors to address even the most significant challenges of recombinant protein production.
Discovery Newsletter: April 2023
In this month’s newsletter, learn more about our comprehensive panel of CDK4/6 inhibitor-resistant breast cancer models and in vitro imaging assays for compound profiling. We also showcase our recent publications describing the development of HBV antigen inhibitors and noncovalent inhibitors of the SARS-CoV-2 3C-like protease (3CLpro).
Discovery and preclinical evaluations of GST-HG131, a novel HBV antigen inhibitor for the treatment of chronic hepatitis B infection
Chronic HBV infection (CHB) is a major contributor to liver-related deaths worldwide. The ultimate endpoint of CHB treatment is sustained HBV surface antigen (HBsAg) loss. Here, we report the design of a series of HBV surface antigen inhibitors which promotes reduction of HBV antigens in vitro and in vivo. https://pubmed.ncbi.nlm.nih.gov/36089112/
Development of Highly Potent Noncovalent Inhibitors of SARS-CoV-2 3CLpro
The 3C-like protease (3CLpro) is an essential enzyme for the replication of SARS-CoV-2 and thus is a target for drug discovery teams. Nearly all inhibitors of coronavirus 3CLpro reported so far are covalent inhibitors. Here, we report the development of specific, noncovalent inhibitors of 3CLpro with high in vivo efficacy in mice. One compound, WU-04, …Read More >
BRAF-Related In Vivo Models
Discover our comprehensive platform of CDX and PDX tumor models, carrying BRAF mutations across multiple cancer types: 18 CDX models carrying BRAF mutation (V600E, G469A, G464V, G466V, G596R or N581Y), covering melanoma, breast cancer, lung cancer and colorectal cancer 18 PDX models carrying BRAF mutation (V600E, G469A, G469E, D594N or N581S), covering melanoma, pancreatic cancer, …Read More >
Alpha‐kinase 1 (ALPK1) agonist DF‐006 demonstrates potent efficacy in mouse and primary human hepatocyte models of hepatitis B
WuXi AppTec scientists recently contributed to a research study published in the journal Hepatology, characterizing the efficacy of prodrug DF-006 for treating chronic hepatitis B infection. DF-006 is an orally active agonist of alpha‐kinase 1, a pattern recognition receptor involved in the stimulation of innate immunity. The authors show that DF‐006 is efficacious in hepatitis …Read More >
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 >
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 >