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Literature summary for 3.4.11.18 extracted from

  • Douangamath, A.; Dale, G.E.; D'Arcy, A.; Almstetter, M.; Eckl, R.; Frutos-Hoener, A.; Henkel, B.; Illgen, K.; Nerdinger, S.; Schulz, H.; MacSweeney, A.; Thormann, M.; Treml, A.; Pierau, S.; Wadman, S.; Oefner, C.
    Crystal structures of Staphylococcus aureus methionine aminopeptidase complexed with keto heterocycle and aminoketone inhibitors reveal the formation of a tetrahedral intermediate (2004), J. Med. Chem., 47, 1325-1328.
    View publication on PubMed
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Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with inhibitors 2-amino-4-(methylthio)-1-(1,3-thiazol-2-yl)butan-1-one, 2-amino-4-(methylthio)-1-pyridin-2-ylbutan-1-one, and 3-amino-1-(cyclopropylamino)heptan-2 Staphylococcus aureus

Inhibitors

Inhibitors Comment Organism Structure
2-amino-4-(methylthio)-1-(1,3-thiazol-2-yl)butan-1-one 50% inhibition at 0.019 mM, formation of uncleavable tetrahedral intermediate upon binding Staphylococcus aureus
2-amino-4-(methylthio)-1-pyridin-2-ylbutan-1-one 50% inhibition at 0.016 mM, formation of uncleavable tetrahedral intermediate upon binding Staphylococcus aureus
3-amino-1-(cyclopropylamino)heptan-2 -one 50% inhibition at 0.007 mM, formation of uncleavable tetrahedral intermediate upon binding Staphylococcus aureus

Organism

Organism UniProt Comment Textmining
Staphylococcus aureus P0A080 isoform I
-