2. Academic Validation
  3. Identification of proton-pump inhibitor drugs that inhibit Trichomonas vaginalis uridine nucleoside ribohydrolase

Identification of proton-pump inhibitor drugs that inhibit Trichomonas vaginalis uridine nucleoside ribohydrolase

  • Bioorg Med Chem Lett. 2014 Feb 15;24(4):1080-4. doi: 10.1016/j.bmcl.2014.01.014.
Tara A Shea 1,  Paola J Burburan 1,  Vivian N Matubia 1,  Sandy S Ramcharan 1,  Irving Rosario Jr 1,  David W Parkin 1,  Brian J Stockman 2
Affiliations

Affiliations

  • 1 Department of Chemistry, Adelphi University, 1 South Avenue, Garden City, NY 11530, United States.
  • 2 Department of Chemistry, Adelphi University, 1 South Avenue, Garden City, NY 11530, United States. Electronic address: [email protected].
PMID: 24468412 DOI: 10.1016/j.bmcl.2014.01.014
Abstract

Trichomonas vaginalis continues to be a major health problem with drug-resistant strains increasing in prevalence. Novel antitrichomonal agents that are mechanistically distinct from current therapies are needed. The NIH Clinical Compound Collection was screened to find inhibitors of the uridine ribohydrolase Enzyme required by the Parasite to scavenge uracil for its growth. The proton-pump inhibitors omeprazole, pantoprazole, and rabeprazole were identified as inhibitors of this Enzyme, with IC50 values ranging from 0.3 to 14.5 μM. This suggests a molecular mechanism for the in vitro antitrichomonal activity of these proton-pump inhibitors, and may provide important insights toward structure-based drug design.

Keywords

NIH Clinical Compound Collection; NMR; Proton-pump inhibitors; Trichomonas vaginalis; Uridine ribohydrolase.

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