Adenosine/guanosine preferring nucleoside ribohydrolase is a distinct, druggable antitrichomonal target.
Basic Information
ID: ALA3632572
Journal: Bioorg Med Chem Lett
Title: Adenosine/guanosine preferring nucleoside ribohydrolase is a distinct, druggable antitrichomonal target.
Authors: Beck S, Muellers SN, Benzie AL, Parkin DW, Stockman BJ.
Abstract: Nucleoside salvage pathway enzymes used by Trichomonas vaginalis are distinct from the pathway involved in activation of existing 5-nitroimidazole drugs. They thus represent excellent targets for developing novel, mechanism-based antitrichomonal agents. The purine-specific adenosine/guanosine preferring ribohydrolase (AGNH) was screened against the NIH Clinical Collection to assess its druggability. Eight compounds, including five flavonoids, were identified with IC50 values ⩽10 μM and confirmed in counter screens run in the presence of detergent. The inhibitors are structurally distinct from inhibitors of the pyrimidine-specific uridine ribohydrolase (UNH) thus indicating that AGNH is a distinct, druggable target from UNH.
CiteXplore: 26592812
DOI: 10.1016/j.bmcl.2015.10.030
Patent ID: ┄