Structure guided chemical modifications of propylthiouracil reveal novel small molecule inhibitors of cytochrome b5 reductase 3 that increase nitric oxide bioavailability

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Abstract

Background: Cytochrome b5 reductase 3 (CYB5R3) regulates nitric oxide (NO) diffusion in the artery wall. Results: Novel CYB5R3 small molecule inhibitors were discovered that increase NO bioavailability. Conclusion: A potent new CYB5R3 inhibitor improves vascular function. Significance: These data provide a platform for further drug development and new tools for understanding CYB5R3 function.

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Rahaman, M. M., Reinders, F. G., Koes, D., Nguyen, A. T., Mutchler, S. M., Sparacino-Watkins, C., … Straub, A. C. (2015). Structure guided chemical modifications of propylthiouracil reveal novel small molecule inhibitors of cytochrome b5 reductase 3 that increase nitric oxide bioavailability. Journal of Biological Chemistry, 290(27), 16861–16872. https://doi.org/10.1074/jbc.M114.629964

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