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 >

Approximately 20-40% of diffuse large B-cell lymphoma (DLBCL) patients experience relapsed or refractory disease after initial treatment with R-CHOP (a combination therapy regimen for DLBCL that combines chemotherapy drugs with rituximab). Polatuzumab vedotin is an antibody-drug conjugate (ADC) used to treat DLBCL, both in first-line treatment and for relapsed or refractory cases. At the 2025 …Read More >

Antibody‒drug conjugates (ADCs), which combine the advantages of monoclonal antibodies with precise targeting and payloads, show great potential as cancer therapies.  However, primary and secondary resistance is frequently observed.  The successful development of next generation ADCs necessitates the establishment of tumor models that address the mechanism of action underlying this resistance. At the 2025 World …Read More >

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 >

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 >

With advancements in drug design, there is resurging interest in drugs that form covalent bonds with their targets. Covalent drugs have the potential to provide enhanced potency and prolonged duration of action compared to non-covalent drugs. Emerging areas of interest include the development of reversible covalent inhibitors, covalent degraders, and covalent targeting of non-cysteine amino …Read More >

RNA-targeted therapeutics are highly intriguing due to their unique physiological properties and novel modes of action in drug R&D. Developing methods to target RNA can lead to new therapeutic options, especially for conditions where RNA plays a pivotal role, such as genetic disorders, viral infections, and cancer. Over the past decade, discovering novel chemical matter …Read More >

Antibody-drug conjugates (ADCs), exemplified by HER2-targeted Enhertu and TROP2-targeted Trodelvy, have demonstrated significant therapeutic potential in cancers. However, a subset of patients remains refractory to ADC treatment.  WuXi AppTec contributed to a research article which demonstrated that excessive cancer-associated fibroblasts (CAFs) can form a fibrotic barrier within a tumor microenvironment, impeding the tissue uptake of …Read More >

Antibody-drug conjugates (ADCs) hold great promise as targeted cancer therapeutics, but their complex structure poses significant development and safety challenges for project teams.  In our latest webinar, experts discuss methodologies for evaluating ADC efficacy, resistance, and immunogenicity that address both antibody-specific and payload-specific mechanisms through various multi-dimensional assays. This webinar offers a comprehensive perspective on …Read More >