Sumoylation
SUMO:SIM
Since the enzymatic steps of the sumoylation process are all catalyzed by a single set of enzymes for the different sumoylation targets, the PPIs that drive the specificity are potentially an important target. There is an interest for the development of druglike molecules inhibiting the SUMO:SIM interaction to study the poorly understood role of PPIs in the sumoylation process as well as potential therapeutic applications. The SUMO:SIM is a challenging protein-protein interaction drug target. We have used a virtual screening approach incorporating the consensus of protein interactions that led to the discovery of non-peptidic inhibitors. The most potent inhibitors have low micromolar potency and the binding affinity and interface was validated using multiple assays and HSQC-NMR. This work has been published in MedChemComm (publication).
