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

Trichomonas vaginalis infects approximately 300 million people worldwide annually. Infected individuals have a higher susceptibility to more serious conditions such as cervical and prostate cancer. The parasite has developed increasing resistance to current drug therapies, with an estimated 5% of cl...

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Veröffentlicht in:Chemical biology & drug design 2018-10, Vol.92 (4), p.1736-1742
Hauptverfasser: Alam, Rayyan, Barbarovich, Allen T., Caravan, Wagma, Ismail, Mirna, Barskaya, Angela, Parkin, David W., Stockman, Brian J.
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Sprache:eng
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Zusammenfassung:Trichomonas vaginalis infects approximately 300 million people worldwide annually. Infected individuals have a higher susceptibility to more serious conditions such as cervical and prostate cancer. The parasite has developed increasing resistance to current drug therapies, with an estimated 5% of clinical cases resulting from resistant strains, creating the need for new therapeutic strategies with novel mechanisms of action. Nucleoside salvage pathway enzymes represent novel drug targets as these pathways are essential for the parasite's survival. The guanosine/adenosine/cytidine nucleoside hydrolase (GACNH) may be particularly important as its expression is upregulated under glucose‐limiting conditions mimicking those that occur during infection establishment. GACNH was screened against the NIH Clinical Collection to explore its druggability. Seven compounds were identified with IC50 values
ISSN:1747-0277
1747-0285
DOI:10.1111/cbdd.13341