Knowledge Library
Targeted Protein Degradation of Mutant ER-alpha
Estrogen receptor α (ERα) is considered the main driver in more than 70% of all breast cancers, making this transcription factor an important drug target. Activating point mutations in the ERα gene, especially Y537S and D538G, have been linked to acquired resistance to endocrine therapies, and there is an urgent need to develop new strategies …Read More >
PROTAC Optimization Strategies
What if a constructed PROTAC with a confirmed high-affinity warhead doesn’t work as expected? That means we need to take a closer, more careful look at how it’s designed and how it works. In this video, our expert from WuXi Biology shares strategies to address such an R&D scenario.
How to Accelerate the Synthesis of PROTACs: Strategies and Case Studies
Introduction: Targeted Protein Degradation (TPD) has emerged as a promising therapeutic modality due to its potential to develop therapeutics for previously undruggable targets and address the resistance issues of small molecule inhibitors. Central to this strategy is the novel protein-degradation approach represented by proteolysis-targeting-chimeras (PROTACs), which induce targeted protein degradation through the ubiquitin-proteasome system (UPS). …Read More >
Emerging Drug Discovery Strategies for Targeted Protein Degradation
In the last decade, targeted protein degradation (TPD) technology has become one of the most promising methods to remove specific disease-related proteins using cellular self-destruction mechanisms. In our latest White Paper, “Emerging Drug Discovery Strategies for Targeted Protein Degradation” we explore how DNA-encoded library (DEL) technology can be used for direct discovery of proteolysis-targeting chimeras …Read More >
Novel Approaches to Targeted Protein Degradation
In the last decade, targeted protein degradation (TPD) technology has become one of the most promising methods to remove specific disease-related proteins using cellular self-destruction mechanisms. As of now, over 20 targeted protein degraders have advanced into clinical development. WuXi AppTec has built a robust TPD discovery chemistry platform. We deliver synthetic and medicinal chemistry …Read More >
Pioneering Advanced Modalities in Early Drug Discovery
New modalities such as peptides, oligonucleotides, and cell and gene therapies have revolutionized healthcare industry innovation. To meet these evolving needs, WuXi Biology has proactively developed a broad range of capabilities, offering integrated solutions to global pharmaceutical and biotech companies for challenging targets. We have established major capabilities for new modalities in the early discovery …Read More >
Discovery and Characterization of Proteolysis Targeting Chimeras: Tissue Transglutaminase
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.
Emerging Modalities in Drug Discovery
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 >
DDC 2023: Biophysical & Functional Characterization of Bifunctional Small Molecules Enables TPD Drug Discovery
Leverage our platform of biophysical methods to accelerate your research on targeted protein degradation. At DDC 2023, WuXi AppTec scientists presented an in-depth panel of assays to support the characterization of bifunctional small molecules. Our cutting-edge services include target protein ubiquitination and degradation assays, techniques to evaluate binary binding, and proximity assays to measure ternary …Read More >