Knowledge Library

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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Parallel Purification of High-Quality Therapeutic Targets

Learn about our semi-automated chromatography platform for parallel purification of high-quality therapeutic targets.  At PEGS Europe 2023, WuXi AppTec scientists described an automated workflow integrated with a serial size exclusion platform, resulting in a complete purification scheme for the rapid purification of high-quality proteins expressed in E. coli, insect cells, and mammalian cells.  This approach …Read More >

Resource Type: Latest Science Poster
Resource Topic: Cells and Protein Science

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Combined Inhibition of KRAS G12C and PD1 Boosts Therapeutic Efficacy via Conditioning of Tumor Microenvironment

SITC Poster #466: Mutant KRAS is linked to PD-L1 expression, and oncogenic RAS signaling promotes an immunosuppressive tumor microenvironment by upregulating PD-L1 expression. Consequently, combining KRAS G12C inhibitors with immune checkpoint blockers shows promising benefits. To better understand the mechanisms underlying the combined inhibition of KRAS G12C inhibitor AMG 510, and anti-PD-1 antibody nivolumab, LU-01-0361 …Read More >

Resource Type: Latest Science Poster
Resource Topic: Antibodies Oncology Small Molecules Tumor Models

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AACR 2023: Comparison of two DTH models for T cell-mediated immunity

To characterize the immunity profile of the most widely used delayed-type hypersensitivity (DTH) models, WuXi AppTec scientists built 2,4-dinitrofluorobenzene (DNFB) and oxazolone-induced DTH models in both BALB/c and C57BL/6 mice with robust ear thickness as the readout. Check out our comprehensive panel of services related to autoimmune and inflammatory diseases

Resource Type: Latest Science Poster
Resource Topic: Autoimmune and Inflammatory Diseases in vivo Pharmacology Lead Optimization Respiratory Diseases

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Regenerable Surface Plasmon Resonance (SPR) Surfaces for Reliable, Cost-Effective, and Wide-Ranging Applications

Traditional SPR-based drug discovery efforts in the small-molecule space have revolved around single-use chips for screening and hit-to-lead efforts. Inspired by recent technological advances, we have established simple regenerable protocols that can (1) accommodate target-proteins with common tags such as His- and Avi-, (2) reach sufficient surface density for small-molecule testing, and (3) maintain a …Read More >

Resource Type: Latest Science Poster
Resource Topic: Biophysical Assays

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DDC 2023: Biophysical & Functional Characterization of Bifunctional Small Molecules Enables TPD Drug Discovery

Leverage our platform of biophysical methods to accelerate your research on targeted protein degradation. At DDC 2023, WuXi AppTec scientists presented an in-depth panel of assays to support the characterization of bifunctional small molecules. Our cutting-edge services include target protein ubiquitination and degradation assays, techniques to evaluate binary binding, and proximity assays to measure ternary …Read More >

Resource Type: Latest Science Poster
Resource Topic: Biochemical Assays Biophysical Assays Cell-based Assays Hit-to-Lead Lead Optimization Small Molecules Structural Biology Targeted Protein Degradation

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AACR 2023: Integrated platform enables KRAS-targeted drugs discovery

Discover our end-to-end KRAS services platform presented at AACR 2023! WuXi AppTec scientists have established a comprehensive panel of assays on key mutants of KRAS, including G12C and G12D, to empower KRAS-targeted drug discovery. Our suite of services includes 2D/3D cell proliferation assays (utilizing cell lines harboring single or double KRAS mutations) as well as …Read More >

Resource Type: Poster
Resource Topic: Biochemical Assays Biophysical Assays Cell-based Assays Hit Finding Hit-to-Lead Lead Optimization Oncology Small Molecules Structural Biology Tumor Models

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AACR 2023: Therapeutic potential of polatuzumab vedotin for the treatment of diffuse large B-cell lymphoma

In our latest AACR poster, WuXi AppTec scientists characterize the therapeutic potential of the antibody-drug conjugate (ADC) polatuzumab vedotin across a panel of established, in-house diffuse large B-cell lymphoma (DLBCL) patient-derived xenograft (PDX) models. Among our panel of lymphoma PDX models, three represent the germinal center B-cell (GCB) subtype. The authors show that 50% of …Read More >

Resource Type: Poster
Resource Topic: Antibody Drug Conjugate Lead Optimization Oncology Tumor Models

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AACR 2023: A tailored platform enables BRAF-targeted drug discovery and precision medicine

In our latest AACR poster, WuXi AppTec scientists showcase the development of a tailored platform of patient-derived xenograft (PDX) models based on the classification of BRAF mutations. This panel covers all 3 classes of BRAF mutants, including subtypes for which viable therapeutic options remain limited. The authors demonstrate that these PDX models are responsive to …Read More >

Resource Type: Poster
Resource Topic: Lead Optimization Oncology Small Molecules Tumor Models

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