We offer a comprehensive platform of biophysical screening assays to measure protein binding, thermodynamics, stoichiometry, protein quality, and kinetics to accelerate your drug discovery programs.

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.

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).  

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/

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 >

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 >

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 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 >

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 >