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.

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 >

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 >

Expansion of the E3 ligase toolbox has the potential to dramatically advance the field of targeted protein degradation.  WuXi AppTec scientists recently contributed to a research article in the Journal of Medicinal Chemistry describing the discovery of novel small molecule binders of GID4, a substrate receptor in the human CTLH E3 ligase complex.  Researchers used …Read More >

WuXi AppTec utilizes state-of-the-art techniques to support drug discovery teams focused on targeted protein degradation. Our services include a broad range of ligand-finding methods, such as DEL, fragment screening, ASMS, and virtual screening. We provide custom linker design and complex synthesis for new linkers and E3 ligase ligands. To support lead optimization efforts, our platform …Read More >

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 >

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 >

Challenging targets, such as membrane proteins or protein-protein interactions were considered undruggable in the past. However, today a variety of screening methods can be used to help develop drugs against these formerly undruggable targets.