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Blocking damage due to the activation of the NADPH complex is a potential strategy for treating many diseases. Current NADPH oxidase inhibitors lack specificity or potency, thus there is need to develop alternative therapeutics suitable for clinical testing. Researchers at Cincinnati Children’s have designed inhibitors of the small GTPase Rac-p67phox interaction that interacts with p67phox such that it prevents the binding of activated Rac1, abrogating superoxide production. Disruption of the GTPase Rac-p67phox interaction inhibits NOX2 enzyme assembly, thereby preventing NADPH oxidase activation.
One inhibitor suppressed lipid oxidation and reduced inflammation in mouse lung tissue.
A novel confidential lead compound has a Kd ~0.1microM.
For an in-depth market overview, please click here.
US Non-Provisional Patent Pending14/378,089
Canada Patent PendingCA2864331
European Patent Pending13749793.9
Priority Date: 02/14/2012
Yi Zheng, PhD
Director, Division of Experimental Hematology and Cancer Biology
Co-Director, Cancer and Blood Diseases Institute
Professor, UC Department of Pediatrics
Bosco, E. E., Kumar, S., Marchioni, F., Biesiada, J., Kordos, M., Szczur, K., … Zheng, Y. (2012). Rational design of small molecule inhibitors targeting the Rac GTPase - p67phox signaling axis in inflammation. Chemistry & Biology, 19(2), 228–242. doi:10.1016/j.chembiol.2011.12.017
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