Knowledge Library
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 >
Accelerating GPCR Drug Discovery and Development
GPCRs: Function, Structure, and Classifications G protein-coupled receptors (GPCRs) are a prevalent class of transmembrane proteins in animal cells, representing one of the largest families of membrane proteins in mammals. These receptors are widely distributed across numerous organs and regulate physiological functions by stimulating intracellular signaling pathways, thereby influencing cellular behavior. GPCRs have a central …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 >
DEL-Generated Endocytosis Receptor-Binding Peptides for Oligonucleotide Delivery
Despite the success of delivery technologies such as lipid nanoparticles and trivalent GalNAc conjugation, targeted delivery of oligonucleotides to extra hepatic tissues remains a challenge. WuXi AppTec presented a poster showing the utilization of our peptide-based DNA-encoded library screening platform to identify endocytosis receptor-binding peptides. The binding affinity of hit peptides was confirmed through biophysical …Read More >
iMN041: Prodrug with a Unique Antitumor Immune Response
WuXi AppTec scientists contributed to a research article in the journal Translational Medicine Communications which characterized the antitumor immune responses generated by iMN041, a prodrug of a DNA methyl transferase/ribonucleotide reductase inhibitor. This study also assessed the efficacy of iMN041 in mouse xenografts of human clear cell renal cell cancer, pancreatic cancer, and triple negative …Read More >
Expanded Applications of PDX Models
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 proven clinical relevance to human disease. WuXi AppTec offers a comprehensive platform of more than 1,400 well-annotated PDXs across 30 cancer types. We also provide expanded in vitro, ex …Read More >
OncoWuXi Express: Review of SITC 2023 Annual Meeting
Review of SITC 2023 Annual Meeting The 38th Annual Meeting of the Society for Immunotherapy of Cancer (SITC) was held this year in San Diego, CA, USA. As one of the most influential international conferences dedicated to cancer immunotherapy, SITC provides attendees with a cross-disciplinary educational and interactive platform. This meeting focuses on discussing and …Read More >
Preclinical platform for nucleic acid drug evaluation: siRNA and mRNA therapeutics
SITC Poster #59: Since the emergence of the COVID-19 pandemic, numerous nucleic-acid therapeutics have been approved for clinical use. Distinguished from conventional protein-targeted therapy, nucleic acid therapeutics offer the potential for sustained effects via gene modification or inhibition. In this study, we conducted a comprehensive evaluation of the activity and anti-tumor effects of PKN3-targeted siRNA …Read More >
Upregulation of drug metabolism enzymes mediates ADC resistance in a HER2-positive cancer cell line
SITC Poster #1162: Enhertu is currently approved for the treatment of patients with HER2-positive breast cancer, gastric cancer, or HER2-mutant non-small cell lung cancer. However, despite Enhertu’s clinical benefits, most patients inevitably experience disease progression and mortality. Understanding drug resistance mechanisms can aid in developing new treatment strategies for drug-resistant clinical patients. In this study, …Read More >