Bromodomain and extra-terminal domain (BET) family proteins are key regulators of gene transcription and have been implicated in a wide range of diseases, making these proteins a potential therapeutic target.  Abnormal BET protein activity has been linked to cancer, inflammatory disorders, viral infections, and neurodegenerative conditions. In a recent publication, researchers highlight the discovery of …Read More >

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 >

Introduction Membrane proteins are essential for various cellular processes, including energy conversion, signal transduction, and disease progression. Efficient and accurate identification and screening of these proteins are vital for the development of small-molecule therapeutics targeting membrane proteins. In recent years, Affinity Selection Mass Spectrometry (ASMS) has become a powerful tool for studying membrane protein-small molecule …Read More >

Introduction: New modalities, such as molecular glues, require robust screening strategies to identify and develop the most promising candidates efficiently. In this article, we spotlight Affinity Selection Mass Spectrometry (ASMS), a versatile and cost-effective high-throughput screening technique used in drug discovery. ASMS: A Powerful High-throughput Screening Technology Since the mid-1990s, ASMS has emerged as a …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 >