Currently, there is a lack of efficient experimental strategies to collect high-quality proteome level data for protein-ligand interactions (PLIs).  At the 2024 ML Drug Discovery Symposium, WuXi AppTec presented a poster showcasing our advanced DELvision database, representing the first use of DNA-encoded library (DEL) technology for establishing a protein-DEL interaction database. The authors demonstrate how …Read More >

Targeted protein degradation (TPD) technology has become one of the most promising methods to remove specific disease-related proteins using cellular self-destruction mechanisms. This technology is enabling researchers to pursue targets that were previously considered undruggable and to address the resistance issue of small molecule inhibitors. Since 2016, WuXi AppTec has built a comprehensive TPD discovery …Read More >

With advancements in drug design, there is resurging interest in drugs that form covalent bonds with their targets, often referred to as targeted covalent inhibitors (TCIs).  In this webinar, experts discuss innovative approaches to screen for covalent binders, strategies for the synthesis of covalent warheads, and assays to optimize the ADME/DMPK properties of these molecules. …Read More >

Casein kinase 2-interacting protein-1 (CKIP-1) performs a critical negative role in the regulation of bone formation. Accumulated evidence strongly supports CKIP-1 as an attractive therapeutic target in osteoporosis.  As a scaffold protein lacking enzymatic activity, CKIP-1 seems to be an undruggable target, and the development of selective small molecule inhibitors targeting CKIP-1 has proven to …Read More >

The heme oxygenase (HO) family comprises the major isozymes HO-1 and HO-2, of which HO-1 is deemed as an emerging target for cancer therapy. HO-1 overexpression is often observed in prostate, renal, colon, lung, breast, and glioma cancers. In a publication in ACS Med Chem Letters, WuXi AppTec scientists report the discovery of five series …Read More >

The safe production of cultivated plants is threatened by various fungal diseases. NIS1 is a secreted effector protein produced by various fungal pathogens. BAK1 is a plant receptor-like kinase that plays a crucial role in recognizing pathogen-associated molecules like NIS1. Understanding the interaction between NIS1 and BAK1 is important for studying plant defense mechanisms against …Read More >

Casitas B lymphoma-b (Cbl-b), a RING finger E3 ubiquitin ligase, is a key regulator of T cell activation and plays an important role in immune responses against tumors.  Cbl-b has been identified as an attractive target for cancer immunotherapy due to its role in promoting an immunosuppressive tumor environment. WuXi AppTec contributed to a study …Read More >

In the last decade, targeted protein degradation (TPD) technology has become one of the most promising methods to remove specific disease-related proteins using cellular self-destruction mechanisms. WuXi AppTec has built a robust TPD discovery platform, allowing for in-depth biological and biophysical characterization of monovalent (molecular glue) and bivalent (PROTAC®) molecules through the use of target …Read More >

WuXi AppTec offers a comprehensive platform of in silico drug discovery services to accelerate the process of hit finding and hit-to-lead optimization.  We provide access to virtual chemical spaces built from our library of novel drug-like scaffolds, to support virtual screening and structure-based virtual screening (SBVS). Advances in ML-empowered virtual screening allows project teams to …Read More >