Knowledge Library

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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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/  

Resource Type: Latest Science Publication
Resource Topic: Oncology Tumor Models

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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 >

Resource Type: Latest Science Presentation
Resource Topic: Biochemical Assays Biophysical Assays Cell-based Assays Cells and Protein Science Hit Finding Hit-to-Lead Lead Optimization Oncology Small Molecules Tumor Models

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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 >

Resource Type: Brochure Latest Science
Resource Topic: DRUG DISCOVERY AND INNOVATION TECHNOLOGY PLATFORMS THERAPEUTIC AREAS

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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 >

Resource Type: Brochure
Resource Topic: Biochemical Assays Biophysical Assays Cell-based Assays Mass Spectrometry-based Assays Small Molecules Structural Biology Targeted Protein Degradation

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