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PLoS One. 2019 Mar 21;14(3):e0214160. doi: 10.1371/journal.pone.0214160. eCollection 2019.

Potent inhibitors of equine steroid isomerase EcaGST A3-3.

Author information

1
Department of Biochemistry and Biophysics, Arrhenius Laboratories, Stockholm University, Stockholm, Sweden.

Abstract

Equine glutathione transferase A3-3 (EcaGST A3-3) belongs to the superfamily of detoxication enzymes found in all higher organisms. However, it is also the most efficient steroid double-bond isomerase known in mammals. Equus ferus caballus shares the steroidogenic pathway with Homo sapiens, which makes the horse a suitable animal model for investigations of human steroidogenesis. Inhibition of the enzyme has potential for treatment of steroid-hormone-dependent disorders. Screening of a library of FDA-approved drugs identified 16 out of 1040 compounds, which at 10 μM concentration afforded at least 50% inhibition of EcaGST A3-3. The most potent inhibitors, anthralin, sennoside A, tannic acid, and ethacrynic acid, were characterized by IC50 values in the submicromolar range when assayed with the natural substrate Δ5-androstene-3,17-dione.

PMID:
30897163
PMCID:
PMC6428247
DOI:
10.1371/journal.pone.0214160
[Indexed for MEDLINE]
Free PMC Article

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