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 >
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).
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/
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 >
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 >
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 >
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 >
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 >
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