Knowledge Library

Application of ML-enriched ASMS for Hit Discovery

GLUT1 serves as the conduit for transporting glucose from the extracellular milieu into the cell, thereby fueling cellular physiological activities via glucose metabolism. Its overexpression has been documented in various tumor cells, establishing GLUT1 as a promising therapeutic target. During an ASMS screening of GLUT1, a counter screen was introduced to effectively mitigate false positives …Read More >

Resource Type: Poster
Resource Topic: Mass Spectrometry-based Assays Screening Libraries

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Application of ASMS for Molecular Glue Discovery

Molecular glues possess the remarkable ability to induce protein-protein interactions. In the pursuit of targeting the CDK12/CCNK/DDB1 complex, an ASMS screening strategy was employed, resulting in the successful identification of two active molecular glues from a subset of 2000 small molecules within the WuXi AppTec compound library. Validation efforts revealed compelling findings: the two small …Read More >

Resource Type: Poster
Resource Topic: Mass Spectrometry-based Assays Screening Libraries

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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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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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DNA-Compatible Cyclizations

The recent publication in the journal Organic Letters, ‘DNA-Compatible Cyclization Reaction to Access 1,3,4-Oxadiazoles & 1,2,4-Triazoles‘ by our WuXi Biology DEL team, introduces two novel DNA-compatible reactions, successfully incorporating bioactive cores 1,3,4-oxadiazoles and 1,2,4-triazoles into the DEL library. These cores are reported to show broad ranges of biological activities, such as antiviral, anti-inflammatory, anticancer, antifungal, …Read More >

Resource Type: Latest Science Publication
Resource Topic: Discovery Chemistry DNA-Encoded Library (DEL) Small Molecules

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High-Dimensional Flow Cytometry Platform

High-dimensional (HD) flow cytometry allows researchers to perform deep phenotyping of immune cells at the single cell level with increased accuracy and sensitivity.  This technology enables complex pathway characterization and data integration for the identification of biomarkers used in immunotherapy.  WuXi AppTec offers a comprehensive panel of HD flow cytometry services, with more than 100 …Read More >

Resource Type: Latest Science Presentation
Resource Topic: Autoimmune and Inflammatory Diseases Biomarkers Oncology Phenotypic Assays

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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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Emerging Drug Discovery Strategies for Targeted Protein Degradation

In the last decade, targeted protein degradation (TPD) technology has become one of the most promising methods to remove specific disease-related proteins using cellular self-destruction mechanisms.  In our latest White Paper, “Emerging Drug Discovery Strategies for Targeted Protein Degradation” we explore how DNA-encoded library (DEL) technology can be used for direct discovery of proteolysis-targeting chimeras …Read More >

Resource Type: Latest Science White Paper
Resource Topic: Discovery Chemistry DNA-Encoded Library (DEL) Targeted Protein Degradation

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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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