In this webinar, we present the latest advances and challenges facing researchers focused on new and emerging modalities in drug discovery. Topics include targeted protein degradation, targeted covalent inhibitors, and nucleic acid therapeutics. Our expert speaker, Dr. Tao Guo, discusses solutions for addressing the complexities in designing, synthesizing, and optimizing these molecules, with an added …Read More >

WuXi AppTec scientists contributed to a study which identified a novel, indole-based, selective estrogen receptor degrader (SERD), designated LX-039. The authors show that LX-039 exhibits potent activity in ER degradation and proliferation assays. With favorable ADME/PK properties, LX-039 also exhibits higher efficacy in a tamoxifen-resistant MCF7 CDX model compared to fulvestrant, with up to 90% inhibition …Read More >

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 >

Learn how parallel medicinal chemistry (PMC) and high throughput experimentation (HTE) combined with machine learning can provide a more focused approach to target molecules, resulting in a more concentrated set of compounds to make the process of lead selection easier. Our experts show how PMC can shorten the turnaround time of the design-synthesis-test cycle, providing …Read More >

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Drug Discovery Chemistry Conference 2023 Powerful biophysical and structural biology tools enable the study of large numbers of covalent fragments and are opening up new possibilities in the treatment of various diseases. Here, Dr. Moran Jerabek-Willemsen, Head of Biophysics & Screening in WuXi Biology reports the results of a covalent FBDD project on Bruton’s Tyrosine …Read More >

Dual leucine zipper kinase (DLK) and leucine zipper-bearing kinase (LZK) have emerged as key regulators of neuronal degeneration and axon growth.  WuXi AppTec scientists recently contributed to a research article in the Journal of Medicinal Chemistry demonstrating the use of ligand- and structure-based drug design approaches to discover an amino-pyrazine chemical series of DLK and …Read More >

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/

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 >