Antibody‒drug conjugates (ADCs), which combine the advantages of monoclonal antibodies with precise targeting and payloads, show great potential as cancer therapies.  However, primary and secondary resistance is frequently observed, and development of next generation ADCs necessitates the establishment of resistant tumor models.  WuXi AppTec offers validated, Enhertu-induced resistant tumor models to support project teams focused …Read More >

The metabotropic glutamate receptor mGluR7 is widely expressed throughout the CNS and has been implicated in numerous CNS disorders.  WuXi AppTec scientists recently contributed to a study which led to the identification, optimization, and characterization of a highly potent, novel mGluR7 allosteric agonist, designated CVN636.  The authors show that CVN636 has high selectivity toward mGluR7, …Read More >

Introduction: Nucleic acid therapies can regulate the expression level or activity of disease-related targets at the genetic level, offering advantages such as a wide target range, programmability, and rapid iteration.  However, the wide application of nucleic acid drugs still faces many challenges, including delivery efficiency and off-target effects. To address these challenges, the Oncology-Immunology team …Read More >

Introduction: WuXi AppTec scientists recently contributed to a study which led to the discovery and optimization of a novel series of GST inhibitors. The authors used affinity mediated DNA-encoded library selection against a privileged scaffold to identify a compound with potent inhibition against human glutathione S-transferase Mu 2.  SAR studies, coupled with X-ray crystallography and …Read More >

WuXi AppTec scientists recently contributed to a study which led to the discovery and optimization of a novel series of GST inhibitors. The authors used affinity mediated DEL selection against a privileged scaffold to identify a compound with potent inhibition against SjGST and GSTM2. SAR studies, coupled with X-ray crystallography and structural analysis, revealed that …Read More >

Tissue transglutaminase (TG2) is a multifunctional enzyme activated in several pathological conditions, including cancer. WuXi AppTec recently contributed to a study which used a targeted protein degradation strategy to abolish TG2’s myriad of functions. The authors synthesized and characterized a series of VHL-based degraders that reduce TG2 in ovarian cancer cells in a proteasome-dependent manner.

Animal studies may provide a close approximation to humans when addressing the key challenge of clinical translatability. In the preclinical setting, new insights into disease models and mechanisms are crucial to efficacy studies. In this webinar, Dr. Deming Xu, Chief Pharmacologist, Executive Director, and Head of In Vivo Pharmacology of WuXi AppTec Discovery Biology will …Read More >

In this webinar, we present the latest advances and challenges facing researchers focused on new and emerging modalities in drug discovery. Topics include targeted protein degradation, targeted covalent inhibitors, and nucleic acid therapeutics. Our expert speaker, Dr. Tao Guo, discusses solutions for addressing the complexities in designing, synthesizing, and optimizing these molecules, with an added …Read More >

Designing effective oligonucleotide therapeutics for clinical applications involves understanding both the chemistry and biology of nucleic acids. In this white paper, learn about recent advances in chemical modifications for oligonucleotide therapeutics that improve stability and selectivity, biological screening assays to support lead optimization, and bioanalytical platforms that address the challenges of quantifying oligonucleotides. Check out …Read More >