Some nice work from Ethan Toriki, James Papatzimas, Daniel Nomura and coauthors on bioRxiv https://www.biorxiv.org/content/10.1101/2022.11.04.512693v1

I think this is the first example in the “glue degraders” field where someone found a “degrading handle” that could be attached to multiple different inhibitors to give degradation of different proteins. A nice step forward in the rational design of molecular glue degraders!

#TPD #MedicinalChemistry #degraders

#SciComm friendly version

Most drugs work by sticking to a protein and blocking its function. Often, part of the drug protrudes out onto the protein surface.

Recently it’s been found that this sometimes causes the protein to be recognised by the cell’s garbage disposal system, meaning the protein is deleted.

In this paper by Nomura they find a “tag” that can be added to different drugs, causing protein deletion.

Finding general tags like this will let us use this approach more broadly!

I need to tell myself off here for writing “drugs” for some things that aren’t actually drugs, but chemicals or molecules or ligands has more characters…
@Chembellenie Thanks for sharing this study. Information flow is bigger than the Gulf stream, and it is hard to identify everything. Degraders are such a hot topic.