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

Md Mizanur Rahaman, Fabio G. Reinders, David Koes, Anh T. Nguyen, Stephanie M. Mutchler, Courtney Sparacino-Watkins, Roger A. Alvarez, Megan P. Miller, Dongmei Cheng, Bill B. Chen, Edwin K. Jackson, Carlos J. Camacho, Adam C. Straub

Research output: Contribution to journalArticlepeer-review

19 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)16861-16872
Number of pages12
JournalJournal of Biological Chemistry
Volume290
Issue number27
DOIs
StatePublished - Jul 3 2015
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Cell Biology

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