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Chembellenie · @Chembellenie

102 followers · 46 posts · Server scicomm.xyz

If you want to see the rest of this story so far, the later parts were published earlier (don’t ask):

https://pubs.acs.org/doi/10.1021/acs.jmedchem.9b02076
https://pubs.acs.org/doi/10.1021/acs.jmedchem.1c00946
https://pubs.acs.org/doi/full/10.1021/acs.jmedchem.1c02174
https://pubs.acs.org/doi/10.1021/acs.jmedchem.1c02175

These describe how we optimised those hit compounds through to potent inhibitors and #degraders

over 50 authors in total across these papers - #DrugDiscovery really does take a lot of team work, and this was no exception!

#drugdiscovery #degraders

Last updated 2 years ago

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Chembellenie · @Chembellenie

102 followers · 46 posts · Server scicomm.xyz

bioRxiv - Rational Chemical Design of Molecular Glue Degraders

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