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- Lindström, HelenaStockholms universitet,Institutionen för biokemi och biofysik (author)
Potent inhibitors of equine steroid isomerase EcaGST A3-3
- Article/chapterEnglish2019
Publisher, publication year, extent ...
- 2019-03-21
- Public Library of Science (PLoS),2019
- printrdacarrier
Numbers
- LIBRIS-ID:oai:DiVA.org:su-168366
- https://urn.kb.se/resolve?urn=urn:nbn:se:su:diva-168366URI
- https://doi.org/10.1371/journal.pone.0214160DOI
Supplementary language notes
- Language:English
- Summary in:English
Part of subdatabase
- SwePubSwePub
Classification
Notes
- 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 mu M 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 Delta(5)-androstene-3,17-dione.
Subject headings and genre
- NATURVETENSKAP Biologi hsv//swe
- NATURAL SCIENCES Biological Sciences hsv//eng
- neurokemi med molekylär neurobiologi
- Neurochemistry with Molecular Neurobiology
Added entries (persons, corporate bodies, meetings, titles ...)
- Mazari, Aslam M. A.Stockholms universitet,Institutionen för biokemi och biofysik (author)
- Musdal, YamanStockholms universitet,Institutionen för biokemi och biofysik (author)
- Mannervik, BengtStockholms universitet,Institutionen för biokemi och biofysik(Swepub:su)bmann (author)
- Stockholms universitetInstitutionen för biokemi och biofysik (creator_code:org_t)
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- In:PLOS ONE: Public Library of Science (PLoS)14:31932-6203
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