The inhibition of the JAK/STAT signaling pathway is a promising approach for the treatment of cancers and inflammatory diseases. To support drug discovery programs, we have established off-the-shelf crystallization systems to enable the determination of high-resolution X-ray crystal structures with a short turnaround time. Together with our protein production service and off-the-shelf biochemical and biophysical …Read More >

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 >

Inhibition of the Werner syndrome RecQ helicase (WRN) is a promising approach for the treatment of cancers commonly associated with microsatellite instability. To support drug discovery programs, we have established off-the-shelf crystallization systems to enable the determination of high-resolution X-ray crystal structures with a short turnaround time. Together with our protein production service and off-the-shelf …Read More >

An inevitable challenge emerges over time as tumors develop drug resistance, resulting in treatment failure.  The development of targeted therapies for overcoming drug resistance represents an unmet medical need. Patient-derived xenografts (PDXs) represent a powerful platform for cancer drug screening and biomarker discovery and are considered the gold standard of in vivo models for their …Read More >

Estrogen receptor α (ERα) is considered the main driver in more than 70% of all breast cancers, making this transcription factor an important drug target.  Activating point mutations in the ERα gene, especially Y537S and D538G, have been linked to acquired resistance to endocrine therapies, and there is an urgent need to develop new strategies …Read More >

Protein kinase N3 (PKN3) is a serine/threonine kinase implicated in tumor progression across multiple cancer types.  PKN3 mRNA is almost undetectable in normal adult tissues but is upregulated in various cancer cells, indicating that siRNA may be a promising approach to inhibit tumor growth by reducing the expression of PKN3.  WuXi AppTec scientists established different siPKN3 molecules and evaluated …Read More >

Despite the excellent clinical response to paclitaxel therapy, drug resistance inevitably develops in subsequent treatments. The mechanisms for resistance to paclitaxel include drug efflux transporter overexpression, altered apoptotic gene expression, and changes associated with microtubules to reduce the influence of this chemotherapeutic agent. The development of targeted therapies for overcoming paclitaxel resistance represents an unmet medical …Read More >

NK cells are effector innate lymphoid cells (ILCs) that do not require antigen-specific priming. NK cells are not only killer cells that help to suppress tumors, but also are involved in the generation and maintenance of adaptive immune responses.  The process of antibody-dependent cell-mediated cytotoxicity (ADCC) makes use of innate immune cells which provide antitumor …Read More >

Rat tumor models are a better mimic of human pathology compared to mice. The tumor stroma component of rats is about 1.5 to 2-fold higher relative to mice. Rats are considered an ideal model for preclinical efficacy studies, as they are physiologically, metabolically, and genetically more similar to humans.  To support drug discovery teams, WuXi …Read More >