A Synthetic Strategy for Conjugation of Paromomycin to Cell-Penetrating Tat(48-60) for Delivery and Visualization into Leishmania Parasites
Author(s) -
Sira Defaus,
Maria Gallo,
María Ángeles Abengózar,
Luís Rivas,
David Andreu
Publication year - 2017
Publication title -
international journal of peptides
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.239
H-Index - 25
eISSN - 1687-9775
pISSN - 1687-9767
DOI - 10.1155/2017/4213037
Subject(s) - paromomycin , aminoglycoside , leishmania , cell penetrating peptide , peptide , cell , antibiotics , microbiology and biotechnology , bioavailability , leishmaniasis , medicine , biology , pharmacology , chemistry , biochemistry , parasite hosting , immunology , world wide web , computer science
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.
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