Knowledge Library
Production and Characterization of Protein Biologics
At the 2024 Protein & Antibody Engineering Summit (PEGS) Europe, Crelux presented a poster highlighting its drug discovery platform for the production and characterization of protein biologics and their antigens. This platform combines construct and expression scouting, customizable high-throughput protein purification, and affinity/kinetics determination using various biophysical techniques, as well as paratope and epitope mapping …Read More >
Discovery of SARS-CoV-2 Papain-like Protease Inhibitors
SARS-CoV-2 antivirals which have been clinically approved or are in late-stage development are directed against either the RNA-dependent RNA polymerase (RdRp) or the main protease (Mpro). With the possibility of resistance developing over time, there is a need for additional oral antivirals directed against currently undrugged viral targets. Conserved across coronaviruses, the SARS-CoV-2 papain-like protease …Read More >
Fibroblast Growth Factor Receptors
Fibroblast growth factor receptor (FGFR) signaling pathways represent promising targets for therapeutics owing to their role in development, tissue, and whole-body homeostasis, as well as in many cancers. 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 …Read More >
USP7 Inhibitors Reveal a Differentiated Mechanism of p53-Driven Anti-Cancer Activity
Ubiquitin-specific protease 7 (USP7) is a deubiquitinating enzyme that cleaves ubiquitin from a range of substrates, shielding them from degradation by the proteasome. USP7 activity has been implicated in cancer progression and its overexpression is associated with tumor aggressiveness and poor prognosis in a variety of cancer types, making USP7 inhibition an attractive strategy for …Read More >
ErbB Receptor Tyrosine Kinase Platform
The ErbB family of receptor tyrosine kinases are involved in key cellular functions, including cell growth and survival. ErbB family members are often overexpressed, amplified, or mutated in many forms of cancer, making them important therapeutic targets. To support research focused on ErbB receptors, WuXi AppTec offers a comprehensive platform of ready-to-go biophysical assays, high-quality …Read More >
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 >
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 >
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 >
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 >