Glucagon‐like peptide‐1 (GLP-1) receptor agonists have emerged as promising therapeutic options for addressing type‐2 diabetes, obesity, and related conditions. However, because of the continued need for injectable administration, many GLP-1 agonists face compliance challenges. To improve the design and production of GLP-1 receptor biased agonists with enhanced druggability, a novel small molecule, designated SAL0112, was …Read More >

Introduction: OncoWuXi Express will continue to keep you informed about updates to our online tumor model database (OncoWuXi Database), as well as our recent progress in cancer and autoimmune research. In this issue, we present an evaluation of the efficacy of different JAK subtype inhibitors in a Type II collagen-induced arthritis model, along with corresponding …Read More >

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 >

WuXi AppTec scientists contributed to a research article in the journal Nature Microbiology, which characterized a peptidomimetic inhibitor of the SARS-CoV-2 main protease (Mpro).  In a human ACE2 transgenic mouse model, this inhibitor (designated RAY1216) exhibited antiviral activities against SARS-CoV-2 comparable to those of nirmatrelvir, but with improved pharmacokinetics.

G-protein coupled receptors (GPCRs) play a pivotal role in signaling pathways, and these transmembrane proteins represent an important drug target class. The majority of approved drugs that target GPCRs bind to traditional orthosteric sites. In a recent publication in Nature, Professor Brian Kobilka and his team at Stanford University successfully identified selective negative allosteric modulators …Read More >

The ErbB family of receptor tyrosine kinases are involved in key cellular functions, including cell growth and survival. ErbB family members are often overexpressed, amplified, or mutated in many forms of cancer, making them important therapeutic targets. To support research focused on ErbB receptors, WuXi AppTec offers a comprehensive platform of ready-to-go biophysical assays, high-quality …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. WuXi Biology has established gastric cancer and breast cancer cell lines that …Read More >

Within the phosphatidylinositol 3-kinase (PI3K) family, the heterodimer comprising the p110-α catalytic and p85-α regulatory subunits (encoded by PIK3CA and PIK3R1) is essential in the regulation of cellular proliferation and carcinogenesis. Kinases such as PIK3CA are mutated in many cancers and represent promising targets for therapeutics. To support drug discovery programs, we have established off-the-shelf …Read More >

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 >