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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In Vivo Pharmacology for Ophthalmic Drug Development

Introduction The number of people with vision impairment has increased due to the continuously expanding and aging population, as well as lifestyle changes. According to the Lancet Global Health, by 2050, myopia is expected to affect 5 billion people. Additionally, the number of individuals with distance vision impairment is projected to reach 895 million, including …Read More >

Resource Type: Article, Blog
Resource Topic: in vivo Pharmacology

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Radionuclide Drug Conjugates

Radiopharmaceuticals have proven to be effective agents since they can be successfully applied for both diagnostics and therapy. Radionuclide drug conjugates (RDCs) combine a radioactive compound, a tailored-targeting molecule for specific receptors enriched on diseased cells, and a linker for stable attachment, enabling more effective radiation delivery and significantly reducing side effects by attacking only …Read More >

Resource Type: Video
Resource Topic: in vivo Pharmacology, Oncology

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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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Resource Topics
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