Knowledge Library

STX-478, a Mutant-Selective, Allosteric PI3Kα Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3Kα-Mutant Xenografts

The contribution of the X-ray crystallography team from our WuXi AppTec site in Germany was acknowledged in a recent study published in the journal Cancer Discovery. In this study, the authors show that compound STX-478, an allosteric PI3Kα inhibitor, selectively targets prevalent PI3Kα helical- and kinase-domain mutant tumors. STX-478 demonstrated robust efficacy in human tumor …Read More >

Resource Type: Latest Science Publication
Resource Topic: Oncology Small Molecules Structural Biology Structural Biology X-ray Crystallography

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Cryo-EM

We offer established protocols for cryo-EM structure determination, with extensive experience in epitope mapping, formulation characterization, and structure-based drug discovery (SBDD). Our integrated services platform also includes: Biophysical and biochemical screening assays Crystal-grade protein production High-resolution X-ray crystallography

Resource Type: Brochure
Resource Topic: Cryo-EM Structural Biology

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One Stop Target-to-Hit Platform: STATs

STAT proteins are key mediators of cellular immunity, proliferation, apoptosis, and differentiation.  STATs are known to play a role in the pathogenesis of many different diseases (including cancer) and the development of drugs directly or indirectly targeting STAT signaling has become a major focus for discovery teams.  WuXi AppTec offers a comprehensive platform of biophysical …Read More >

Resource Type: Brochure
Resource Topic: Biochemical Assays Biophysical Assays Immunology Oncology Structural Biology

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Covalent Fragment-based Drug Discovery: BTK Inhibitors

At the Covalent Drug Discovery 2023 Summit, 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 methods, orthogonal assays, …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: Helicases

RecQ helicases (BLM, WRN, RECQL, RECQL4, and RECQL5) are an important family of surveillance proteins that play critical roles in genome maintenance and stability. Inherited mutations in these helicases are linked to distinct human disease syndromes, as well as cancer. To support the discovery of potent and selective RecQ helicase inhibitors, WuXi AppTec offers a …Read More >

Resource Type: Brochure
Resource Topic: Biochemical Assays Biophysical Assays Oncology Rare Diseases 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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GPCR-Membrane Protein Platform

WuXi AppTec provides a comprehensive platform of advanced biophysical assays and structural biology services to accelerate lead optimization efforts focused on GPCRs and membrane proteins. Our capabilities include high-quality protein production across all major target classes and nanodisc reconstitution of membrane proteins for screening. We also offer established protocols for cryo-EM structure determination and assessment …Read More >

Resource Type: Brochure
Resource Topic: Biophysical Assays Oncology Structural Biology

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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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Structural Biology Platform Facilitates Discovery of Glutathione S-Transferase Inhibitors, Offering Novel Pathways for Drug Development

Introduction: WuXi AppTec scientists recently contributed to a study which led to the discovery and optimization of a novel series of GST inhibitors. The authors used affinity mediated DNA-encoded library selection against a privileged scaffold to identify a compound with potent inhibition against human glutathione S-transferase Mu 2.  SAR studies, coupled with X-ray crystallography and …Read More >

Resource Type: Article Blog
Resource Topic: Small Molecules Structural Biology

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Resource Topics
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