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.

Resource Type: Brochure
Resource Topic: Hit Finding Hit-to-Lead Lead Optimization Structural Biology

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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.

Resource Type: Brochure
Resource Topic: Biophysical Assays Mass Spectrometry-based Assays Structural Biology Target Identification and Validation

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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).  

Resource Type: Latest Science Newsletter
Resource Topic: Biochemical Assays Biophysical Assays Cell-based Assays Hit-to-Lead in vitro biology Infectious Diseases Lead Optimization Oncology Small Molecules Structural Biology Tumor Models

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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/

Resource Type: Latest Science Publication
Resource Topic: Biochemical Assays Cell-based Assays Discovery Chemistry Hit-to-Lead Infectious Diseases Lead Optimization Liver Diseases Small Molecules

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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 >

Resource Type: Latest Science Publication
Resource Topic: Biochemical Assays Biophysical Assays Cell-based Assays Discovery Chemistry Hit-to-Lead Infectious Diseases Lead Optimization Structural Biology

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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 >

Resource Type: Latest Science Presentation
Resource Topic: Lead Optimization Oncology Tumor Models

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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 >

Resource Type: Latest Science Publication
Resource Topic: Cell-based Assays Immunology Infectious Diseases Liver Diseases Small Molecules

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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 >

Resource Type: Latest Science Presentation
Resource Topic: Candidate Selection Oncology Tumor Models

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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 >

Resource Type: Latest Science Publication
Resource Topic: DNA-Encoded Library (DEL) Fragment-Based Drug Discovery Targeted Protein Degradation

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Resource Topics
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