Abstract: The present invention provides a screen which exploits mechanism-based activity probes that specifically and covalently modify the active site cysteine thiol residue of E3 Ub ligases including, but not limited to the HECT and RBR family. The activity probes are used to screen for activators and inhibitors of E3 Ub ligases, and to interrogate the functional state of E3 Ub ligases in human disease.
Type:
Grant
Filed:
May 2, 2014
Date of Patent:
October 11, 2016
Assignee:
E3X Bio, Inc.
Inventors:
Brigit Riley, Jennifer Johnston, David Morgans