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Drug platforms

Structure-based design of peptide inhibitors and activators of ubiquitin enzymes

In vitro studies identified a strategy to develop peptide inhibitors and activators of ubiquitin pathway enzymes that could help treat various diseases. The crystal structures of ubiquitin with deubiquitinases or ligases were used to identify ubiquitin variants that could act as competitive inhibitors, allosteric inhibitors or activators of the enzymes. In human embryonic kidney cells, a ubiquitin variant with high binding affinity for the ubiquitin-specific peptidase 21 (USP21) blocked deubiquitination. Next steps include developing therapeutic delivery methods for the proteins.

SciBX 6(4); doi:10.1038/scibx.2013.103
Published online Jan. 31, 2013

Provisional patent application filed covering inhibitors and activators of deubiquitinases and ubiquitin ligases; available for licensing

Ernst, A. et al. Science; published online Jan. 3, 2013;
Contact: Sachdev S. Sidhu, University of Toronto, Toronto, Ontario, Canada