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 >

Gene therapies are enabling a rapid expansion in the scope of treatable disease.  Adeno-associated viruses (AAVs) are particularly advantageous delivery vehicles for introducing functional genes to specific tissues or cells due to their simplicity, safety, and efficacy. A successful AAV discovery and development pipeline covers basic vector design, in vitro assays, in vivo biodistribution, immunogenicity, …Read More >

Since prostate cancer heavily depends on androgen hormones for growth, targeting the androgen receptor (AR) signaling pathway is a key therapeutic strategy for treating advanced metastatic prostate cancer. While AR antagonists like enzalutamide can significantly improve survival in prostate cancer patients, resistance often develops over time, largely driven by treatment-induced mutations within the ligand-binding domain …Read More >

Glucagon‐like peptide‐1 (GLP-1) receptor agonists have emerged as promising therapeutic options for addressing type‐2 diabetes, obesity, and related conditions. However, because of the continued need for injectable administration, many GLP-1 agonists face compliance challenges. To improve the design and production of GLP-1 receptor biased agonists with enhanced druggability, a novel small molecule, designated SAL0112, was …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 >

Rheumatoid arthritis (RA) is a prevalent, chronic, autoimmune disease. The onset and progression of RA are closely associated with an aberrant immune response, in which immune cells accumulate excessively in target joints.  Most current, anti-rheumatic drugs only alleviate disease progression or ameliorate inflammation. Development of new RA therapies with increased efficacy represents an unmet medical …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 >