Knowledge Library

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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XPRESS Portfolio: Off-the-Shelf Crystallography

XPRESS Portfolio Over 150 targets enabled for off-the-shelf crystallography Broad range of targets and classes Established protocols for protein production and crystallization Average turn-around time of 2 months

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

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Resource Topics
× peptide, amino acid

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