Literature DB >> 26592812

Adenosine/guanosine preferring nucleoside ribohydrolase is a distinct, druggable antitrichomonal target.

Sierra Beck1, Samantha N Muellers1, Annie Laurie Benzie1, David W Parkin1, Brian J Stockman2.   

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.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Flavonoids; NIH Clinical Compound Collection; NMR; Nucleoside ribohydrolase; Trichomonas vaginalis

Mesh:

Substances:

Year:  2015        PMID: 26592812     DOI: 10.1016/j.bmcl.2015.10.030

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  6 in total

1.  Druggability of the guanosine/adenosine/cytidine nucleoside hydrolase from Trichomonas vaginalis.

Authors:  Rayyan Alam; Allen T Barbarovich; Wagma Caravan; Mirna Ismail; Angela Barskaya; David W Parkin; Brian J Stockman
Journal:  Chem Biol Drug Des       Date:  2018-06-19       Impact factor: 2.817

2.  NMR-Based Activity Assays for Determining Compound Inhibition, IC50 Values, Artifactual Activity, and Whole-Cell Activity of Nucleoside Ribohydrolases.

Authors:  Brian J Stockman; Abinash Kaur; Julia K Persaud; Maham Mahmood; Samantha F Thuilot; Melissa B Emilcar; Madison Canestrari; Juliana A Gonzalez; Shannon Auletta; Vital Sapojnikov; Wagma Caravan; Samantha N Muellers
Journal:  J Vis Exp       Date:  2019-06-30       Impact factor: 1.355

3.  Ligand-Efficient Inhibitors of Trichomonas vaginalis Adenosine/Guanosine Preferring Nucleoside Ribohydrolase.

Authors:  Samantha N Muellers; Juliana A Gonzalez; Abinash Kaur; Vital Sapojnikov; Annie Laurie Benzie; Dean G Brown; David W Parkin; Brian J Stockman
Journal:  ACS Infect Dis       Date:  2019-02-01       Impact factor: 5.084

4.  New Leishmania donovani nucleoside hydrolase inhibitors from Brazilian flora.

Authors:  Charlotte Nirma; Gregorio Torres Rangel; Marina Amaral Alves; Livia Marques Casanova; Mayara Monteiro Moreira; Luanna Monteiro Rodrigues; Lidilhone Hamerski; Luzineide Wanderley Tinoco
Journal:  RSC Adv       Date:  2019-06-13       Impact factor: 4.036

5.  Discovery of Ligand-Efficient Scaffolds for the Design of Novel Trichomonas vaginalis Uridine Nucleoside Ribohydrolase Inhibitors Using Fragment Screening.

Authors:  Shannon Auletta; Wagma Caravan; Julia K Persaud; Samantha F Thuilot; Dean G Brown; David W Parkin; Brian J Stockman
Journal:  ACS Omega       Date:  2019-09-16

Review 6.  Structure, Oligomerization and Activity Modulation in N-Ribohydrolases.

Authors:  Massimo Degano
Journal:  Int J Mol Sci       Date:  2022-02-25       Impact factor: 5.923

  6 in total

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