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Literature summary for 2.7.1.227 extracted from

  • Norcliffe, J.; Mina, J.; Alvarez, E.; Cantizani, J.; De Dios-Anton, F.; Colmenarejo, G.; Valle, S.; Marco, M.; Fiandor, J.; Martin, J.; Steel, P.; Denny, P.
    Identifying inhibitors of the Leishmania inositol phosphorylceramide synthase with antiprotozoal activity using a yeast-based assay and ultra-high throughput screening platform (2018), Sci. Rep., 8, 8938 .
    View publication on PubMedView publication on EuropePMC
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Application

Application Comment Organism
analysis high-throughput screening of inhibitors via recombinant expression in Saccharomyces cerevisiae lacking IPC synthase activity Leishmania major

Inhibitors

Inhibitors Comment Organism Structure
3-[(4-fluorophenyl)methyl]-7-(1H-pyrrole-1-sulfonyl)-2,3,4,5-tetrahydro-1H-3-benzazepine selective, non-toxic benzazepane inhibitor, inhibits the enzyme at nanomolar concentrations Leishmania major
7-(4-fluoro-1H-indole-1-sulfonyl)-3-[(pyridin-3-yl)methyl]-2,3,4,5-tetrahydro-1H-3-benzazepine selective, non-toxic benzazepane inhibitor, inhibits the enzyme at nanomolar concentrations Leishmania major

Organism

Organism UniProt Comment Textmining
Leishmania major E9AFX2
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