Knowledge Library
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 a Novel Covalent Inhibitor Using DEL
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 >
Nephropathy Research Platform
Kidney diseases are complex conditions caused by a variety of factors, including autoimmune diseases, metabolic disorders, infections, drug side effects, and genetics. Kidney diseases can lead to a range of complications, including kidney failure, anemia, electrolyte imbalances, and nerve damage, thereby affecting the quality of life. To drive breakthroughs in this critical field, WuXi AppTec …Read More >
DEL Screening to Discover Small Molecule Ligands for RNA
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 >
Women’s Health Platform
Women’s health care is crucial not only for the well-being of individual women but also for the health and prosperity of families and communities. Despite significant medical advancements, there remains a concerning gap in the availability of effective drugs for common women-related diseases such as endometriosis, menopause syndromes, polycystic ovary syndrome (PCOS), and various forms …Read More >
Fibrosis Disease: Mechanisms, Therapeutic Targets, and Animal Models
Introduction: Fibrosis is a pathological process characterized by the excessive deposition of extracellular matrix (ECM) within an organ, leading to significant damage to its structure and function, which can potentially impact multiple organs such as the lungs, liver, heart, kidneys, and skin (Fig.1). Notable examples of fibrotic diseases include idiopathic pulmonary fibrosis (IPF), liver cirrhosis, …Read More >
Targeting FAK Improves the Tumor Uptake of ADCs
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 >
Strategies to Accelerate the Development of Antibody-Drug Conjugates
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 >
BRCA2 Deficient DLD-1 Model
BRCA1 and BRCA2 proteins are key components of the homologous recombination repair pathway for repairing double-stranded DNA breaks. Mutations in BRCA genes can significantly increase the risk of certain cancers such as breast, ovarian, pancreatic, and prostate cancer. To mimic the effects of BRCA2 deficiency in humans, WuXi Biology has constructed a BRCA2 deficient mouse …Read More >