Knowledge Library
Cardiac Manifestations of Fabry Disease
Lysosomal storage disorders are rare genetic conditions that cause a buildup of toxic materials in the cells of various organs. Fabry disease (FD) is an X-linked disorder of glycosphingolipid metabolism caused by mutations in the GLA gene encoding alpha-galactosidase A. Manifestations of FD include life-threatening renal, cardiovascular, and cerebrovascular dysfunctions. Current treatments can preserve kidney …Read More >
Dianthus Platform: Screening for CRBN-DDB1 Proteolysis-Targeting Chimeras and Molecular Glues
Cereblon (CRBN) forms an E3 ligase complex together with DDB1, CUL4, and RBX1. CRBN functions as a substrate receptor of this complex for the recognition and binding of proteins targeted for ubiquitination and proteasomal degradation. To support the discovery of CRBN-DDB1 proteolysis-targeting chimeras and molecular glues, WuXi AppTec offers an integrated platform of ready-to-go assays …Read More >
Translational Pharmacology of CNS and Metabolic Disorders for Testing New Modality Therapies
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 >
Optimization and Mechanistic Investigations of Novel Allosteric Activators of PKG1α
WuXi AppTec scientists recently contributed to a research article in the Journal of Medicinal Chemistry describing the optimization of a piperidine series of small molecules as novel allosteric activators of PKG1α (a compelling drug target for treatment of cardiovascular diseases). This study reveals a mechanism of action for these compounds consistent with cGMP-induced activation, including …Read More >
Large-scale synthesis of a Notum inhibitor employing a modified Sakai reaction as the key step
WuXi AppTec scientists recently contributed to a research article in the Royal Society of Chemistry describing the large-scale synthesis of a potent and selective inhibitor of Notum carboxylesterase (an enzyme that suppresses Wnt signaling pathways). By employing a modified Sakai reaction as the key step, a one-pot synthesis of this Notum inhibitor was developed, enabling …Read More >
Ligand Finding and Chemistry Workflows for Targeted Protein Degradation
This webinar will focus on aspects related to PROTAC discovery and chemistry workflows, such as ligand finding strategies, synthesis optimization, and linker design. Successful development of bifunctional molecules requires a deep understanding of multiple processes, including biophysical events which dictate induced proximity and how technologies such as DNA-encoded libraries (DEL) can be leveraged to identify …Read More >
Biological Characterization and Development Workflows for Targeted Protein Degradation
This webinar will focus on PROTAC biology workflows, such as in vitro screening assays, in vivo testing, and optimization of DMPK properties. Topics will include the best use of biochemical assays to measure binary/ternary complex formation, cell-based assays to assess target engagement and degradation, strategies for enhancing drug delivery and formulation, and PK/PD evaluation of …Read More >
How Does It Work? | RNAi
As part of our dedication to providing an #openaccess platform, so our entire ecosystem can come together to share #science & #collaborate to better the lives of all #patientsfirst. We’ve created MoA animations in our new series exploring biotech topics on a molecular level. Protein malfunctions cause many diseases, but a new approach is emerging …Read More >
WuXi AppTec Discovery Services
Delivering comprehensive end-to-end solutions for creating, identifying, and supporting preclinical candidates, from discovery to development, with our integrated chemistry and biology research platforms.