Knowledge Library

Phosphatidylinositol Kinases: Structural Biology Services

Within the phosphatidylinositol 3-kinase (PI3K) family, the heterodimer comprising the p110-α catalytic and p85-α regulatory subunits (encoded by PIK3CA and PIK3R1) is essential in the regulation of cellular proliferation and carcinogenesis. Kinases such as PIK3CA are mutated in many cancers and represent promising targets for therapeutics. To support drug discovery programs, we have established off-the-shelf …Read More >

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

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Janus Kinases: Structural Biology Services

The inhibition of the JAK/STAT signaling pathway is a promising approach for the treatment of cancers and inflammatory diseases. 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 biochemical and biophysical …Read More >

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

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One Stop Target-to-Hit Platform: SOS1

The Son of Sevenless (SOS) protein is a guanine nucleotide exchange factor that acts as a key activator for KRAS function. The binding between KRAS and SOS helps facilitate the turnover of GDP-loaded KRAS (“off” state) into its GTP-loaded “on” state.  Disrupting the SOS1-KRAS complex with an SOS1 binder is a compelling strategy to help …Read More >

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

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One Stop Target-to-Hit Platform: RAS Family

The RAS family of small GTPases are among the most frequently mutated oncogenes in human cancer. Previously viewed as undruggable, the recent FDA approval of two KRAS G12C-selective inhibitors has offered real promise to the development of anti-RAS therapies, including mutation-specific strategies. To support the discovery of novel KRAS inhibitors, WuXi AppTec offers a comprehensive …Read More >

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

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One Stop Target-to-Hit Platform: CRBN-DDB1

Cereblon (CRBN) forms an E3 ligase complex together with DDB1, CUL4, and RBX1. CRBN functions as a substrate receptor of this complex, and this protein is a key target for the action of small molecules.  Targeting of CRBN can modify its substrate specificity towards non-physiological proteins, which are subsequently ubiquitinated and degraded by the proteasome. …Read More >

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

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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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Resource Topics
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