De Novo-Designed APC/C Inhibitors Provide a Rationale for Targeting RING-Type E3 Ubiquitin Ligases

Alena's PhD paper is finally out Journal of Medicinal Chemistry: Targeting RING ubiquitin ligases is a major goal in cancer therapy — but their poorly defined active sites make them notoriously hard to drug. In an exciting collaboration led by the brilliant Alena Uvizl and Gloria Ruiz-Gomez (Pisabarro Lab, TU Dresden), we developed a rational design strategy to inhibit a specific, previously untargetable region of these enzymes using the key mitotic Ubiquitin E3 liagse APC/C as a proof of priciple..

Have a look here: https://lnkd.in/eJJkMj8q to read the paper!

I guess you have to work in the ubiquitin field to appreciate the quality of Alena's fully reconstituted APC/C activity assays :-)

Inhibition of securin ubiquitylation by our iAPC11 inhibitors molecules iAPC/C activity assays