We serendipitously discovered that the degradation of glutathione S-transferase is accelerated when treated with a covalent ligand, ethacrynic acid, linked to tert-butyl carbamate-protected arginine moiety (Boc3Arg). Similarly, the degradation of E. coli dihydrofolate reductase is accelerated when treated with a noncovalent ligand, trimethoprim, linked to Boc3Arg. The Boc3Arg degron is another example of the hydrophobic degrons initially discovered by Crews and colleagues. Here we report progress on defining the affinity requirements of noncovalent ligands and further generalization of hydrophobic tagging to new targets and ligands.                                             

Greasing the wheels of destruction: Hydrophobic tagging

248th National Meeting (2014)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.