Latest Science
USP7 Inhibitors Reveal a Differentiated Mechanism of p53-Driven Anti-Cancer Activity
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 >
Preclinical Evaluation of the SARS-CoV-2 Mpro Inhibitor RAY1216
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.
A µ-Opioid Receptor Modulator that Works Cooperatively with Naloxone
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 >
mRNA-Encoded Modulators Suppress Tumor Growth
Unlike conventional protein-targeted therapies, nucleic acid therapeutics have the potential for long-lasting effects and greater target specificity. WuXi AppTec provides a comprehensive platform to support the discovery of mRNA drugs. Our services include mRNA design and production, assessment of mRNA delivery systems, in vitro evaluation, and determination of in vivo efficacy and biodistribution. At AACR …Read More >
Clinical Drug Resistant PDX Models
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 >
Creating a Biological Switch Using DEL Technology
In addition to identifying chemical starting points for early drug discovery processes, DNA-encoded library (DEL) technology has now expanded to new applications, including the discovery of bifunctional affinity ligands historically considered difficult to develop. At the 2024 Gordon Research Conference, WuXi AppTec presented a poster describing how DEL can enable the rapid discovery of novel …Read More >
Recent Insights into Immuno-Oncology
The efficacy of CAR-T therapy is substantially influenced by the tumor microenvironment. This is particularly evident when PD-L1 is activated through CAR-T, leading to the inhibition of CAR-T cell activity via the PD-1 pathway. At the 2024 Recent Insights into Immuno-Oncology Conference, WuXi AppTec presented a poster describing an engineered CAR-T therapy that targets mesothelin …Read More >
Integrated Assay Platform Targeting HMPV Infection
Human metapneumovirus (HMPV) is a common cause of respiratory tract infections in young children, older adults, and people with weakened immune systems. HMPV is in the Pneumoviridae family along with the more commonly known respiratory syncytial virus (RSV). Currently, there is no specific antiviral therapy to treat HMPV and no vaccine to prevent HMPV. At …Read More >
Integrated Platform of siRNA Drug Discovery
RNA interference using small interfering RNA (siRNA) molecules has emerged as a promising therapeutic modality. To accelerate the discovery of novel siRNAs, WuXi AppTec has established an integrated platform encompassing siRNA sequence design, chemical synthesis/modification, delivery ligand exploration, and activity/off-target assessment. At the TIDES USA 2024 Conference, our scientists presented a poster showcasing the effectiveness …Read More >