Knowledge Library

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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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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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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How Does It Work? | Protein Based Vaccines

When a new pathogen invades, it’s a race against time for your immune system to stop it from multiplying out of control. This week, we explore Protein Based Vaccines as part of our “How Does It Work?” series. Fortunately, #vaccines give your immune system a head start against dangerous pathogens. A protein-based vaccine, like this …Read More >

Resource Type: Video
Resource Topic: Cells and Protein Science Infectious Diseases Target Identification and Validation

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How Does It Work? | Adenovirus Vaccines

This week, we delve into Adenovirus Vaccines as part of our “How Does It Work?” 3D MoA animation series examining biotech topics on a molecular level. In 2020, the World Health Organization declared the Covid-19 outbreak a pandemic, but not all viruses are bad news. Adenoviruses are a family of viruses that can be used …Read More >

Resource Type: Video
Resource Topic: DRUG DISCOVERY AND INNOVATION Gene Therapies Infectious Diseases Target Identification and Validation

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How Does It Work? | mRNA Vaccines

If you’ve ever read about mRNA vaccines and wondered, “How Does It Work?” This week’s installment of our video series was made with you in mind. To understand how mRNA vaccines work, let’s take a close look at the immune system. Your immune system can recognize that the structures on bacteria or viruses are different …Read More >

Resource Type: Video
Resource Topic: Infectious Diseases Oligonucleotides Target Identification and Validation

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WuXi AppTec Discovery Services

Delivering comprehensive end-to-end solutions for creating, identifying, and supporting preclinical candidates, from discovery to development, with our integrated chemistry and biology research platform. Integrated Chemistry and Biology Research Platform | From Discovery to Candidate Selection and Beyond

Resource Type: Brochure
Resource Topic: Antibodies Antibody Drug Conjugate Autoimmune and Inflammatory Diseases Biochemical Assays Biomarkers Biophysical Assays Candidate Selection CAR-T Cell Cardiovascular & Metabolic Diseases Cell Therapies Cell-based Assays Cells and Protein Science Central Nervous System & Pain Chemical Biology and Proteomics CRISPR/Cas9 Dermatology Discovery Chemistry DNA-Encoded Library (DEL) DRUG DISCOVERY AND INNOVATION Fragment-Based Drug Discovery Gene Manipulation Gene Therapies High-throughput screening (HTS) Hit Finding Hit-to-Lead Immunology in silico services in vitro biology in vivo Pharmacology in vivo Toxicology Infectious Diseases Lead Optimization Liver Diseases Mass Spectrometry-based Assays Metabolic Diseases NASH Oligonucleotides Oncology Oncolytic Viruses Ophthalmology Phenotypic Assays Quantum Mechanics Rare Diseases Respiratory Diseases Safety and Early Toxicity Screening Libraries Screening Services Small Molecules Structural Biology Target Identification and Validation Target-Specific Assays Targeted Protein Degradation TECHNOLOGY PLATFORMS THERAPEUTIC AREAS THERAPEUTIC MODALITIES Tumor Models

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