A Synthetic Strategy for Conjugation of Paromomycin to Cell-Penetrating Tat(48-60) for Delivery and Visualization into Leishmania Parasites

Defaus, Sira; Gallo, María, 1989-; Abengózar, María Ángeles; Rivas, Luis; Andreu Martínez, David

doi:http://dx.doi.org/10.1155/2017/4213037

A Synthetic Strategy for Conjugation of Paromomycin to Cell-Penetrating Tat(48-60) for Delivery and Visualization into Leishmania Parasites

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Defaus S, Gallo M, Abengózar MA, Rivas L, Andreu Martínez D. A Synthetic Strategy for Conjugation of Paromomycin to Cell-Penetrating Tat(48-60) for Delivery and Visualization into Leishmania Parasites. International Journal of Peptides. 2017;2017:4213037. DOI: 10.1155/2017/4213037

Abstract

A successful approach to deliver paromomycin, a poorly absorbed aminoglycoside antibiotic, to parasite cells is reported, based on selective protection of amino and hydroxyl groups followed by conjugation to a fluorolabeled, PEG-functionalized cell-penetrating Tat(48-60) peptide. The resulting construct is efficiently internalized into Leishmania cells, evidencing the fitness of cell-penetrating peptides as vectors for efficiently transporting low-bioavailability drugs into cells.