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 >

Peptides, and in particular macrocyclic peptides, are well known for their ability to disrupt protein-protein interactions (PPIs).  In this webinar, learn how DNA encoded library (DEL) screening can be used to discover peptide macrocycles that disrupt PPIs.  Our speakers present a case study using the oncoprotein murine double minute 2 (MDM2). We will also highlight the …Read More >

RNA molecules are promising drug targets due to their genomic prevalence, disease involvement, and druggable complex structures. Successful examples include RNA-targeting small molecule drugs for spinal muscular atrophy (SMA), with on-going efforts in other RNA-related diseases. Here, Dr. Zhifeng Yu presents our toolbox for discovering RNA-targeting small molecules, with a focus on unique DNA-encoded libraries …Read More >

WuXi AppTec scientists recently contributed to a study which led to the discovery and optimization of a novel series of GST inhibitors. The authors used affinity mediated DEL selection against a privileged scaffold to identify a compound with potent inhibition against SjGST and GSTM2. SAR studies, coupled with X-ray crystallography and structural analysis, revealed that …Read More >

Within the PI3K family, the heterodimer protein comprising the p110-α and p85-α catalytic/regulatory subunits (encoded by PIK3CA and PIK3R1) are essential in the regulation of cellular proliferation and carcinogenesis.  To support the discovery of novel PI3K inhibitors, WuXi AppTec offers a comprehensive platform of biophysical and biochemical assays to accelerate hit finding and lead optimization …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 inhibitors, WuXi AppTec offers a comprehensive platform of biophysical and biochemical …Read More >