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Coupling the cell-penetrating peptides transportan and transportan 10 to primaquine enhances its activity against liver-stage malaria parasites

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Abstract

Novel primaquine–cell penetrating peptide conjugates were synthesised and tested in vitro against liver stage Plasmodium berghei parasites. Generally, the conjugates were more active than the parent peptides and, in some cases, than the parent drug. These are unprecedented findings that may open a new route towards antimalarial drug rescuing.

Graphical abstract: Coupling the cell-penetrating peptides transportan and transportan 10 to primaquine enhances its activity against liver-stage malaria parasites

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Publication details

The article was received on 05 Sep 2018, accepted on 13 Nov 2018 and first published on 16 Nov 2018


Article type: Research Article
DOI: 10.1039/C8MD00447A
Citation: Med. Chem. Commun., 2018, Advance Article
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    Coupling the cell-penetrating peptides transportan and transportan 10 to primaquine enhances its activity against liver-stage malaria parasites

    L. Aguiar, M. Machado, M. Sanches-Vaz, M. Prudêncio, N. Vale and P. Gomes, Med. Chem. Commun., 2018, Advance Article , DOI: 10.1039/C8MD00447A

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