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  • Title: Aaptamines as sortase A inhibitors from the tropical sponge Aaptos aaptos.
    Author: Jang KH, Chung SC, Shin J, Lee SH, Kim TI, Lee HS, Oh KB.
    Journal: Bioorg Med Chem Lett; 2007 Oct 01; 17(19):5366-9. PubMed ID: 17716892.
    Abstract:
    Four aaptamines (1-4), 1H-benzo[de][1,6]-naphthyridine alkaloids, were isolated from the marine sponge Aaptos aaptos and their inhibitory activities against sortase A (SrtA), an enzyme that plays a key role in cell wall protein anchoring and virulence in Staphylococcus aureus, were evaluated. Isoaaptamine (2) was a potent inhibitor of SrtA, with an IC(50) value of 3.7+/-0.2 microg/mL. The suppression of fibronectin-binding activity by isoaaptamine (2) highlights its potential for the treatment of S. aureus infections via inhibition of SrtA activity. Our studies have identified a series of SrtA inhibitors, providing the basis for further development of potent inhibitors.
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