Welcome to your October Newsletter!
WuXi Discovery Services
Driving drug discovery through world-class capabilities, dedicated collaborative teams, and scientific excellence.
View the Video | PROTAC? Optimization Strategies?
Targeted protein degradation technology has become one of the most promising methods to remove specific disease-related proteins using cellular self-destruction mechanisms.? But what if a constructed PROTAC with a confirmed high-affinity warhead doesn't work as expected? In such a scenario, we need to take a closer, more careful look at how the molecule is designed and how it works. In this video we share strategies to address this type of R&D challenge.
On-Demand Webinar?| Empowering Early Discovery of Peptide Drugs
In this webinar, we discuss recent advancements in peptide drug discovery, including new technologies for hit generation and selection, as well as novel cyclization techniques for peptide conformational rigidity. This webinar offers a comprehensive perspective on strategies that are crucial to achieve the desired binding affinity and efficacy for developing potent and orally available peptide drugs.
eBook | Quantum Mechanics for Organic Chemists - 4th Edition
Would you like to predict organic reaction outcomes accurately? Quantum mechanics (QM) tools for chemistry are evolving at a tremendously fast pace and have proven to be invaluable for organic and medicinal chemists. We are excited to announce that the latest edition of our QM eBook, “Quantum Mechanics for Organic Chemists, an Experimentalist Approach” is now available!
Chemical Insights Article | Ni-Catalyzed Reductive Cross-Coupling
Given the experimental nature of chemistry, each substrate modification may require fine-tuning of reaction conditions. In our latest chemical insights article, we show how our Reaction Condition Screening platform can enhance drug development efficiency by identifying optimal reaction conditions for Ni-catalyzed reductive cross-coupling, a powerful tool in synthetic chemistry.
领英推荐
Publication | Discovery of Potent and Selective IRE1 alpha Inhibitors
Inositol-requiring enzyme 1α (IRE1α) is a sensor protein that plays a key role in multiple myeloma (MM). WuXi AppTec contributed to a study which identified a potent and selective IRE1α inhibitor, designated G-5758, that was well tolerated following multiday oral administration. G-5758 demonstrated comparable pharmacodynamic effects to induced IRE1 knockdown in a KMS-11 multiple myeloma model.
Publication | Recognition of NIS1 by BRI1-Associated Receptor Kinase 1
In the?International Journal of Biological Macromolecules, a recent publication describes the identification of a novel molecule discovered directly from WuXi AppTec’s DNA-encoded library (DEL) product.?The authors demonstrate that this molecule can block the interaction of NIS1-BAK1 and significantly inhibit the virulence of the rice blast fungus, Magnaporthe oryzae.
Poster | TLR8 Mouse Model to Evaluate anti-HBV Agents
Toll-like receptor 8 (TLR8) plays an essential role in human antiviral immunity by recognizing ssRNA of viruses. Development of an in vivo preclinical model has the potential to greatly accelerate research focused on new anti-HBV agents.?However, rodent TLR8 is unresponsive to human TLR8 ligands unless polyT-oligodeoxynucleotides are present. To overcome this hurdle, WuXi Biology has established a human TLR8 transgenic mouse model of AAV/HBV infection, showing that treatment of a TLR8 agonist in this model resulted in significant reductions of plasma HBV DNA, hepatitis B surface antigen (HBsAg) and hepatitis B e-antigen (HBeAg) levels.
Spotlight on Services | Anti-Tumor mRNA Drugs
The development of nucleic acid drugs faces numerous challenges, including reducing immunogenicity, improving stability, enhancing in vivo delivery efficiency, and achieving appropriate biodistribution. To address these challenges, WuXi Biology has established a preclinical pharmacology and efficacy platform aiming to specifically support the research and development of mRNA and other nucleic acid drugs.?In our latest issue of OncoWuXi Express, we showcase how the WuXi Biology team designed and synthesized an mRNA sequence encoding human Interleukin-12 and encapsulated it in lipid nanoparticles to prepare IL-12 mRNA LNPs for assessing their antitumor efficacy.