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Allosteric Modulation of PARP1-DNA Binding with Small Molecule Inhibitors: A Potential None Synthetic Lethal Therapeutic Strategy for Treating Ewing Sarcoma and Other Solid Tumors for Treating Ewing Sarcoma and Other Solid Tumors

SummaryResearchers at OHSU have developed a novel PARP1 inhibitors that demonstrate a novel dual mode of action to inhibit catalytic activity while also allosterically trapping PARP1 at the DNA binding stage. This strategy offers a significant advantage over existing PARP1 inhibitors by increasing replication stress and cytotoxicity, potentially eliminating...

Published: 7/29/2019 | Inventor(s): Moriah Arnold, Michael Cohen, Anang Shelat

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Category(s): Therapeutics