Powerful biophysical and structural biology tools enable the study of large numbers of fragments and are opening new possibilities in the treatment of various diseases. In this webinar, WuXi AppTec presents the results of a conventional and covalent fragment-based drug discovery screen, and our expert speaker discusses how orthogonal biophysical and structural methods enable the …Read More >

DNA-encoded libraries from WuXi AppTec were used in a “steered” screening against either inactive or active μ-opioid receptors in parallel, to find novel negative allosteric modulators of this receptor. The molecule discovered via DEL screening not only shows direct and effective in vitro and in vivo potency, but also helps elucidate the mechanism of negative allosteric modulation of GPCRs. This discovery …Read More >

In this webinar, our expert speakers showcase our automatic DNA-encoded library (DEL) screening device, DELman. DNA-encoded library technology has proven to be a powerful tool for drug discovery. There are now several DEL-derived candidates in clinical stage. DEL enables researchers to explore vast chemical space with millions to billions of compounds. With DELman and other …Read More >

Salt-inducible kinases (SIKs) have recently emerged as key regulators of oncogenesis, inflammation, and immune responses, making these enzymes an important drug target. The isoform SIK3 is a novel regulator of tumor-intrinsic resistance to cytotoxic T cell attack. To support the discovery of novel SIK3 modulators, WuXi AppTec offers an integrated platform of ready-to-go biophysical assays …Read More >

Cereblon (CRBN) forms an E3 ligase complex together with DDB1, CUL4, and RBX1. CRBN functions as a substrate receptor of this complex for the recognition and binding of proteins targeted for ubiquitination and proteasomal degradation.  To support the discovery of CRBN-DDB1 proteolysis-targeting chimeras and molecular glues, WuXi AppTec offers an integrated platform of ready-to-go assays …Read More >

Within the 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.  To support the discovery of novel PI3K inhibitors, WuXi AppTec offers an integrated platform of ready-to-go assays and Spectral Shift technology within Dianthus, an affinity screening …Read More >

Protein arginine methyltransferase 5 (PRMT5) is an enzyme which plays an essential role in a wide range of cellular processes.  PRMT5 overexpression has been implicated in many diseases, including cancer, making this protein an important drug target.  To support the discovery of novel PRMT5-WDR77 inhibitors, WuXi AppTec offers an integrated platform of ready-to-go assays and …Read More >

The adaptor protein STING (stimulator of interferon genes) has emerged as an exciting target for both immunological conditions (STING inhibition) and cancer therapies (STING activation).  To support drug discovery teams in the discovery of novel modulators of STING, WuXi AppTec offers an integrated platform of ready-to-go biophysical assays and Dianthus, a plate-based and microfluidics-free affinity …Read More >

The metabotropic glutamate receptor mGluR7 is widely expressed throughout the CNS and has been implicated in numerous CNS disorders.  WuXi AppTec scientists recently contributed to a study which led to the identification, optimization, and characterization of a highly potent, novel mGluR7 allosteric agonist, designated CVN636.  The authors show that CVN636 has high selectivity toward mGluR7, …Read More >