Knowledge Library

One Stop Target-to-Hit Platform: p53

TP53 is the most frequently mutated tumor suppressor gene in human cancer. Mutant p53 proteins not only lose wild-type p53-dependent tumor suppressive functions, but also frequently acquire oncogenic gain-of-functions that promote tumorigenesis.  Small molecules that can either protect p53 from negative regulators or restore the functionality of mutant p53 proteins are gaining interest, and potential drugs …Read More >

Resource Type: Brochure
Resource Topic: Biophysical Assays, Structural Biology, X-ray Crystallography

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CRBN Structural Biology Services

Targeted protein degradation of disease-causing proteins by the E3 ligase cereblon (CRBN) represents a new therapeutic strategy for addressing challenging-to-treat diseases. To support drug discovery programs, we have established off-the-shelf crystallization and cryo-EM systems to enable the determination of high-resolution X-ray crystal structures with a short turnaround time. Together with our protein production service and …Read More >

Resource Type: Presentation
Resource Topic: Biophysical Assays, Cryo-EM, Structural Biology, Targeted Protein Degradation, X-ray Crystallography

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WRN Helicase: Structural Biology Services

Inhibition of the Werner syndrome RecQ helicase (WRN) is a promising approach for the treatment of cancers commonly associated with microsatellite instability. To support drug discovery programs, we have established off-the-shelf crystallization systems to enable the determination of high-resolution X-ray crystal structures with a short turnaround time. Together with our protein production service and off-the-shelf …Read More >

Resource Type: Presentation
Resource Topic: Biophysical Assays, Cryo-EM, Structural Biology, X-ray Crystallography

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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 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: 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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Resource Topics
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