Knowledge Library

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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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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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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Osimertinib-Resistant Cell Lines and Models

Despite the robust clinical activity exerted by osimertinib, a majority of patients eventually exhibit disease progression while receiving this drug.  Resistance to osimertinib includes both on-target and off-target mechanisms.  With the use of osimertinib for advanced EGFR-mutant NSCLC increasing, the development of targeted therapies toward osimertinib resistance represents an unmet medical need.  To support research …Read More >

Resource Type: Latest Science, Presentation
Resource Topic: Lead Optimization, Oncology, Tumor Models

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OncoWuXi Express: Large-scale Cell Panel Screening Platform for Integrated Pharmacogenomics and Bioinformatics Research

Introduction: OncoWuXi Express will continue to keep you informed about updates to our on-line tumor model database (OncoWuXi Database), as well as our recent progress in cancer and autoimmune research. In this issue, we showcase our large-scale cell panel screening platform for integrated pharmacogenomics and bioinformatics research. Cell viability assessment is a commonly used in …Read More >

Resource Type: Article, Blog, Case Study
Resource Topic: Cell-based Assays, Hit-to-Lead, Lead Optimization, Oncology

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Structure-Based Design and Synthesis of Potent and Selective KRAS G12D Inhibitors

The KRAS G12D mutation subtype is present in over 40% of pancreatic ductal adenocarcinomas (PDAC), making this an important drug target.  WuXi AppTec scientists recently contributed to a research article in ACS Med. Chem. Letters describing the optimization of a series of potent and selective KRAS G12D inhibitors through a structure-based drug design approach.  The …Read More >

Resource Type: Latest Science, Publication
Resource Topic: Hit-to-Lead, Lead Optimization, Oncology, Small Molecules, Structural Biology

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Oncology Cell Panel Screening Platform

Screen your compounds across our comprehensive cell screening panel of over 600 authenticated, validated human cancer cell lines covering 50 cancer types.  We provide single agent and combination compound screening for potency and synergy, and bioinformatics analysis for mechanistic studies and biomarker discovery related to drug responses.  We also offer an extensive KRAS mutant cell …Read More >

Resource Type: Latest Science, Presentation
Resource Topic: Cell-based Assays, Hit-to-Lead, Lead Optimization, Oncology

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Resource Topics
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