Wed, 14 Oct 2020, 09:00 CEST (Berlin)

Dr. Jessica Holien, Vice Chancellor’s Research Fellow, RMIT University, Melbourne, Australia

Structure-based drug design of selective Drp1 inhibitors

The mitochondrial protein dynamin-related protein (Drp1) has been implicated in the development of a number of diseases, including cancer, heart disease and dementia. To date, no direct small molecule inhibitors of human Drp1 have been identified. Using a virtual screening method, we identified three “hit” compounds (OB-27, OB-37 and OB-47), from three alternate chemical classes, which interacted with Drp1 directly and inhibited its activity in cell-based assays. Using BioSolveIT software, we have purchased and assaysed compound analogues and are using this software to guide our medicinal chemistry campaign.

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