Gout is a common type of inflammatory arthritis caused by elevated uric acid levels in the blood. When uric acid levels are too high, monosodium urate (MSU) crystals can form in the body, especially in and around joints. These MSU crystals are sharp and can cause inflammation when they are deposited in the joints, leading …Read More >

In our latest publication, WuXi AppTec scientists introduce two new methods that utilize readily accessible aldehydes to create substituted isoxazolines and isoxazoles by the 1,3-dipolar cycloaddition reaction. Isoxazoles and isoxazolines, known for their diverse bioactivities—including antibacterial, antifungal, and insecticidal properties—are now accessible through a novel DNA-compatible method developed in this study. This approach enables the …Read More >

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 >

Despite the excellent clinical response to paclitaxel therapy, drug resistance inevitably develops in subsequent treatments. The development of targeted therapies for overcoming paclitaxel resistance represents an unmet medical need. Although not fully understood, the mechanisms for resistance to paclitaxel include drug efflux transporter overexpression, altered apoptotic gene expression, and changes associated with microtubules to reduce …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 >

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 >

Tuberculosis is the leading cause of death from an infectious disease and is caused by Mycobacterium tuberculosis (MTB). Inosine-5′-monophosphate dehydrogenase (GuaB) is an enzyme that performs the rate-limiting step in the de novo biosynthesis of guanine, which is critical for growth of bacteria, including MTB. The development of a novel antibiotic that inhibits GuaB could …Read More >

Mutant p53 is one of the most attractive targets for new anti-cancer drugs. Although traditionally regarded as difficult to drug, several new strategies have recently become available for targeting the mutant protein. One of the most promising of these involves the use of low molecular weight compounds that promote refolding and reactivation of mutant p53 …Read More >