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

Author:

Aguiar Luísa12345,Machado Marta678910,Sanches-Vaz Margarida678910,Prudêncio Miguel678910ORCID,Vale Nuno111213414,Gomes Paula12345ORCID

Affiliation:

1. LAQV-REQUIMTE

2. Departamento de Química e Bioquímica

3. Faculdade de Ciências

4. Universidade do Porto

5. P-4169-007 Porto

6. Instituto de Medicina Molecular João Lobo Antunes

7. Faculdade de Medicina

8. Universidade de Lisboa

9. P-1648-028 Lisboa

10. Portugal

11. Laboratório de Farmacologia

12. Departamento de Ciências do Medicamento

13. Faculdade de Farmácia

14. P-4050-313 Porto

Abstract

Novel primaquine–cell penetrating peptide conjugates were synthesised and testedin vitroagainst liver stagePlasmodium bergheiparasites, showing that generally the conjugates were more active than the parent peptides and, in some cases, than the parent drug.

Funder

Fundação para a Ciência e a Tecnologia

Publisher

Royal Society of Chemistry (RSC)

Subject

Pharmaceutical Science,Biochemistry,Drug Discovery,Molecular Medicine,Pharmacology,Organic Chemistry

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