Knowledge Library
Rational Design and Optimization of a Potent IDO1 PROTAC
Indoleamine 2,3-dioxygenase 1 (IDO1) is an enzyme that metabolizes tryptophan, and its activity can lead to immunosuppression, thereby allowing tumors to evade the immune system. IDO1 can also suppress the immune response through mechanisms independent of its enzyme activity, and this may be difficult to target with current inhibitors. Drugs targeting only IDO1 enzyme activity …Read More >
On-bead DEL Application and Case Study for Drug Discovery
DNA-encoded library (DEL) technology has been recognized as a major screening method with unique advantages for offering vast chemical diversity and multiplexed affinity-based screening. Recently, solid-phase On-bead DEL, also known as one bead one compound (OBOC), has been developed to further expand DEL screening from affinity-based screening into biochemical activity screening. At the 2025 SLAS …Read More >
Accelerating CIP Discovery with ASMS and DEL
Chemical inducers of proximity (CIPs) are small molecules that induce the proximity of two biological targets, usually proteins. Molecular glues and PROteolysis TArgeting Chimeras (PROTACs®) are among the best-known CIPs. These molecules utilize the endogenous E3-based proteolysis pathway to induce proximity between the target protein and E3 ligase, thereby triggering targeted protein degradation. At the …Read More >
Discovery of Molecular Glues: Challenges and Opportunities
Introduction: Molecular glues (MGs) are a class of small molecules that alter the surface properties of proteins to strengthen or induce protein-protein interactions (PPI), leading to specific biological effects like protein degradation, pathway inhibition, or activation. Their unique properties endow them with high selectivity and bioavailability, allowing for controlled drug release. Molecular glues show great …Read More >
Targeted Protein Degradation Platform
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 >
Discovery of a Specific CKIP-1 Ligand using DEL
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 >
Research Strategies for the Discovery of Targeted Protein Degraders
In this webinar, experts present research strategies for the discovery of targeted protein degraders. Over the past 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. Since 2016, WuXi AppTec has built a comprehensive TPD discovery service platform, adept in over 20 …Read More >
USP7 Inhibitors Reveal a Differentiated Mechanism of p53-Driven Anti-Cancer Activity
Ubiquitin-specific protease 7 (USP7) is a deubiquitinating enzyme that cleaves ubiquitin from a range of substrates, shielding them from degradation by the proteasome. USP7 activity has been implicated in cancer progression and its overexpression is associated with tumor aggressiveness and poor prognosis in a variety of cancer types, making USP7 inhibition an attractive strategy for …Read More >
CRBN Structural Biology Services
Targeted protein degradation of disease-causing proteins by the E3 ligase cereblon (CRBN) represents a new therapeutic strategy for addressing challenging-to-treat diseases. To support drug discovery programs, we have established off-the-shelf crystallization and cryo-EM systems to enable the determination of high-resolution X-ray crystal structures with a short turnaround time. Together with our protein production service and …Read More >