Dianthus overcomes the top roadblocks faced during affinity screening of binary and ternary PROTAC complexes. Learn more.
Ternary complexproteolysis-targeting chimeras (PROTACs)The rapid and ever-growing advancements from within the field of proteolysis-targeting chimeras (PROTAC)-induced protein degradation have driven considerable development to gain a deeper understanding of their mode of action. The ternary complex formed...
Dianthus overcomes the top roadblocks faced during affinity screening of binary and ternary PROTAC complexes. Learn more.
Ternary PROTAC structures – necessary and sufficient?doi:10.1107/s0108767321097555C. ChungInternational Union of Crystallography (IUCr)Acta Crystallographica Section A Foundations and Advances
We and others have shown that a common explanation of PROTAC efficacy is the ability of the PROTAC to form a ternary complex between the E3 ubiquitin ligase and the target protein. In this chapter, we provide a simple in vitro method to quickly and inexpensively assess this property of ...
PROTACs recruit an E3 ubiquitin ligase, such as von Hippel-Lindau (VHL), to a protein of interest (POI) to form a ternary complex. Measuring the formation of this ternary species is important for understanding PROTAC mode of action. Proximity AlphaLISA assays can be used for this purpose ...
Native MS at high resolution allowed us to measure ternary complex formation as a function of PROTAC concentration to provide a measure of complex affinity and stability, whilst simultaneously measuring other intermediate protein species. Native MS provides a high‐throughput, low sample consumption, ...