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Peptide TP10

Coupling the Antimalarial Cell Penetrating Peptide TP10 to Classical Antimalarial Drugs Primaquine and Chloroquine Produces Strongly Hemolytic Conjugates

December 23, 2019 - 14:59 -- Open Access
Author(s): 
Aguiar L, Biosca A, Lantero E, Gut J, Vale N, Rosenthal PJ, Nogueira F, Andreu D, Fernàndez-Busquets X, Gomes P
Reference: 
Molecules 2019, 24(24), 4559

Recently, we disclosed primaquine cell penetrating peptide conjugates that were more potent than parent primaquine against liver stage Plasmodium parasites and non-toxic to hepatocytes. The same strategy was now applied to the blood-stage antimalarial chloroquine, using a wide set of peptides, including TP10, a cell penetrating peptide with intrinsic antiplasmodial activity. Chloroquine-TP10 conjugates displaying higher antiplasmodial activity than the parent TP10 peptide were identified, at the cost of an increased hemolytic activity, which was further confirmed for their primaquine analogues.

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