• Trends Pharmacol. Sci. · Sep 2014

    Review

    Siderophore-drug complexes: potential medicinal applications of the 'Trojan horse' strategy.

    • Agnieszka Górska, Anna Sloderbach, and Michał Piotr Marszałł.
    • Department of Medicinal Chemistry, Faculty of Pharmacy, Nicolaus Copernicus University, Jurasza 2, 85-089 Bydgoszcz, Poland.
    • Trends Pharmacol. Sci. 2014 Sep 1; 35 (9): 442-9.

    AbstractThe ability of bacteria to develop resistance to antimicrobial agents poses problems in the treatment of numerous bacterial infections. One method to circumvent permeability-mediated drug resistance involves the employment of the 'Trojan horse' strategy. The Trojan horse concept involves the use of bacterial iron uptake systems to enter and kill bacteria. The siderophore-drug complex is recognized by specific siderophore receptors and is then actively transported across the outer membrane. The recently identified benefits of this strategy have led to the synthesis of a series of siderophore-based antibiotics. Several studies have shown that siderophore-drug conjugates make it possible to design antibiotics with improved cell transport and reduce the frequency of resistance mutants. Growing interest in siderophore-drug conjugates for the treatment of human diseases including iron overload, cancer, and malaria has driven the search for new siderophore-drug complexes. This strategy may have special importance for the development of iron oxide nanoparticle-based therapeutics. Copyright © 2014 Elsevier Ltd. All rights reserved.

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