Knowledge Library

TLR8 Mouse Model to Evaluate anti-HBV Agents

Toll-like receptor 8 (TLR8) plays an essential role in human antiviral immunity by recognizing ssRNA of viruses. Upon activation by specific ligands, TLR8 can trigger potent antiviral responses. Development of an in vivo preclinical model has the potential to greatly accelerate research focused on new anti-HBV agents.  However, rodent TLR8 is unresponsive to human TLR8 …Read More >

Resource Type: Latest Science, Poster
Resource Topic: in vivo Pharmacology, Infectious Diseases

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Oncogenic Virus-associated Tumor Models

Viruses have well-established causal roles in numerous human cancers. Approximately 10% of cancers globally are attributed to viral infections, primarily from viruses like HPV, EBV, HBV, and HCV. The innate and adaptive immune systems play important roles in oncogenic viral infection and subsequent cancer development. As viral cancers have viral-specific targets and biomarkers, there is …Read More >

Resource Type: Presentation
Resource Topic: Infectious Diseases, Oncology, Tumor Models

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Discovery of SARS-CoV-2 Papain-like Protease Inhibitors

SARS-CoV-2 antivirals which have been clinically approved or are in late-stage development are directed against either the RNA-dependent RNA polymerase (RdRp) or the main protease (Mpro). With the possibility of resistance developing over time, there is a need for additional oral antivirals directed against currently undrugged viral targets. Conserved across coronaviruses, the SARS-CoV-2 papain-like protease …Read More >

Resource Type: Latest Science, Publication
Resource Topic: in silico services, Infectious Diseases, Small Molecules, Structural Biology, X-ray Crystallography

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Preclinical Evaluation of the SARS-CoV-2 Mpro Inhibitor RAY1216

WuXi AppTec scientists contributed to a research article in the journal Nature Microbiology, which characterized a peptidomimetic inhibitor of the SARS-CoV-2 main protease (Mpro).  In a human ACE2 transgenic mouse model, this inhibitor (designated RAY1216) exhibited antiviral activities against SARS-CoV-2 comparable to those of nirmatrelvir, but with improved pharmacokinetics.

Resource Type: Latest Science, Publication
Resource Topic: Infectious Diseases, Lead Optimization

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Integrated Assay Platform Targeting HMPV Infection

Human metapneumovirus (HMPV) is a common cause of respiratory tract infections in young children, older adults, and people with weakened immune systems. HMPV is in the Pneumoviridae family along with the more commonly known respiratory syncytial virus (RSV).  Currently, there is no specific antiviral therapy to treat HMPV and no vaccine to prevent HMPV. At …Read More >

Resource Type: Latest Science, Poster
Resource Topic: Infectious Diseases, Respiratory Diseases

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Infectious Disease Platform

Capacity Comprehensive virus, bacteria, fungi coverages Supporting drug and vaccine discovery from early research to clinical trials Capability 20+ various viruses Supporting discovery of antivirals and vaccines, including HBV, SARS-CoV, IFV, RSV, HCV, HIV, EV71, herpes, rabies, and other viruses 130+ different bacterial and fungal species Supporting discovery of antibacterial and antifungal therapeutics, including ESKAPE, …Read More >

Resource Type: Brochure
Resource Topic: Infectious Diseases

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Dianthus Platform: Screening for CRBN-DDB1 Proteolysis-Targeting Chimeras and Molecular Glues

Cereblon (CRBN) forms an E3 ligase complex together with DDB1, CUL4, and RBX1. CRBN functions as a substrate receptor of this complex for the recognition and binding of proteins targeted for ubiquitination and proteasomal degradation.  To support the discovery of CRBN-DDB1 proteolysis-targeting chimeras and molecular glues, WuXi AppTec offers an integrated platform of ready-to-go assays …Read More >

Resource Type: Brochure
Resource Topic: Biophysical Assays, Cardiovascular & Metabolic Diseases, Central Nervous System & Pain, Hit Finding, Hit-to-Lead, Immunology, Infectious Diseases, Oncology

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Inhibition of the hERG potassium ion channel by non-nucleoside CMV polymerase antiviral inhibitors

WuXi AppTec scientists collaborated on a study to characterize a series of pyrroloquinoline derivatives that were designed and synthesized to understand the effect of various substitutions on human cytomegalovirus (HCMV) polymerase activity, antiviral activity, and hERG inhibition.  Results suggest that substitutions can be fine-tuned to reduce hERG inhibition while maintaining HCMV antiviral potency. The abstract …Read More >

Resource Type: Latest Science, Publication
Resource Topic: Biochemical Assays, Discovery Chemistry, Hit-to-Lead, Infectious Diseases, Small Molecules

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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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Resource Topics
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