Knowledge Library

Heme Oxygenase-1-Targeting Molecules

WuXi AppTec scientists published a study in the open access archive ChemRxiv describing the discovery of highly selective, novel, heme oxygenase-1 (HO-1) targeting molecules. HO-1, primarily a heme-degrading enzyme, has been identified as a potential therapeutic target in diseases such as cancer and neurodegenerative disorders. Here, we report the discovery of five series of novel …Read More >

Resource Type: Latest Science Publication
Resource Topic: Central Nervous System & Pain DNA-Encoded Library (DEL) Hit Finding in silico services Oncology

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PROTAC Optimization Strategies

What if a constructed PROTAC with a confirmed high-affinity warhead doesn’t work as expected? That means we need to take a closer, more careful look at how it’s designed and how it works. In this video, our expert from WuXi Biology shares strategies to address such an R&D scenario.

Resource Type: Video
Resource Topic: Lead Optimization Targeted Protein Degradation

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Addition of Covalent Warhead and DEL-Generated Hit Fragmentation Empower FBDD

Fragment-based drug discovery (FBDD) is one of the most well-developed approaches for projects starting from small, low-affinity compounds.  At the SLAS 2024 meeting in Boston, WuXi AppTec presented a poster reporting on the assembly of a covalent fragment library that is suited to tackle protein targets via serine, lysine, and cysteine residues. In a case …Read More >

Resource Type: Latest Science Poster
Resource Topic: DNA-Encoded Library (DEL) Fragment-Based Drug Discovery Hit Finding Hit-to-Lead Lead Optimization Small Molecules

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DEL Insight: Novel Applications with the Bifunctional Linker of DNA-encoded Molecules

Due to the special configuration of the DNA encoded library (DEL), each DEL molecule carries a DNA sequence encoding its identity through a bifunctional linker. The linkers that are considered “redundant” and “troublesome” in traditional drug discovery actually offer innate advantages in many application scenarios. In this article, we review how to utilize DNA-encoded libraries …Read More >

Resource Type: Article Blog
Resource Topic: DNA-Encoded Library (DEL) Hit Finding Small Molecules

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Covalent Fragment-based Drug Discovery: BTK Inhibitors

At the Covalent Drug Discovery 2023 Summit and Fragments 2024 Conference, we presented a case study on Bruton’s tyrosine kinase (BTK) and demonstrated how biochemical, biophysical, and structural biology methods were used to confirm hits, characterize binding kinetics, and evaluate the mode of interaction of covalent BTK inhibitors. Our hit-to-lead workflow showcases the importance of bioanalytical …Read More >

Resource Type: Latest Science Poster
Resource Topic: Biochemical Assays Biophysical Assays Fragment-Based Drug Discovery Hit Finding Hit-to-Lead Structural Biology

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One Stop Target-to-Hit Platform: CDKs and CDK-Cyclin Complexes

Cyclin-dependent kinases (CDKs) and their cyclin regulatory subunits form complexes that are essential for driving abnormal growth processes in cancer cells, making these molecules important targets for cancer treatment. To support the discovery of novel CDK inhibitors, WuXi AppTec offers a comprehensive platform of biophysical and biochemical assays to accelerate hit finding and lead optimization …Read More >

Resource Type: Brochure
Resource Topic: Biochemical Assays Biophysical Assays Hit-to-Lead Lead Optimization Oncology Structural Biology

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Biophysical and Structural Biology Methods Enable Fragment-Based Ligand Discovery

Powerful biophysical and structural biology tools enable the study of large numbers of fragments and are opening new possibilities in the treatment of various diseases. In this webinar, WuXi AppTec presents the results of a conventional and covalent fragment-based drug discovery screen, and our expert speaker discusses how orthogonal biophysical and structural methods enable the …Read More >

Resource Type: Webinar
Resource Topic: Fragment-Based Drug Discovery Hit Finding Hit-to-Lead Lead Optimization

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Negative Allosteric Modulation of the µ-Opioid Receptor

DNA-encoded libraries from WuXi AppTec were used in a “steered” screening against either inactive or active μ-opioid receptors in parallel, to find novel negative allosteric modulators of this receptor. The molecule discovered via DEL screening not only shows direct and effective in vitro and in vivo potency, but also helps elucidate the mechanism of negative allosteric modulation of GPCRs. This discovery …Read More >

Resource Type: Latest Science Publication
Resource Topic: Central Nervous System & Pain DNA-Encoded Library (DEL) Hit Finding Small Molecules

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Discovery and Characterization of ZL-2201, a Potent, Highly Selective, and Orally Bioavailable Small-molecule DNA-PK Inhibitor

DNA-dependent protein kinase (DNA-PK) plays an important role in the overall survival and proliferation of cells, making this enzyme an intriguing target for the treatment of a variety of cancers.  In our latest publication, WuXi AppTec scientists contributed to the discovery and characterization of ZL-2201, a potent and highly selective small molecule DNA-PK inhibitor.  In …Read More >

Resource Type: Latest Science Publication
Resource Topic: Cell-based Assays Hit-to-Lead Lead Optimization Oncology Tumor Models

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