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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
Cell-penetrating γ-peptide/antimicrobial undecapeptide conjugates with anticancer activity
Tetrahedron, Volume 68, No. 23, Year 2012
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Description
In this study, we combined a cell-penetrating γ-peptide, PEG-1, with antimicrobial undecapeptides in order to provide compounds with anticancer properties against MDA-MB-231 human breast cancer cells. We demonstrated that the conjugates were more cytotoxic than Ac-PEG-1 and the parent undecapeptides. We also evaluated the toxicity of the conjugates against non-malignant cells. The peptide conjugate with the best biological profile was BP77-PEG-1, which, at 10 μM, showed a 71% growth inhibition in MDA-MB-231 cells and only a 17% inhibition in non-malignant cells. Therefore, this study suggests that PEG-1 mediated the undecapeptide delivery into cancer cells and that these conjugates are the proof-of-concept of this strategy to generate improved anticancer drugs based on peptides. © 2011 Elsevier Ltd. All rights reserved.
Authors & Co-Authors
Carbajo López, Daniel
Spain, Barcelona
Combinatorial Chemistry Unit
Spain, Madrid
Centro de Investigación Biomédica en Red de Bioingeniería, Biomateriales y Nanomedicina
Cirac, J. Ignacio
Spain, Girona
Universitat de Girona
Bardají, Eduard R.
Spain, Girona
Universitat de Girona
Alberício, Fernando
Spain, Madrid
Centro de Investigación Biomédica en Red de Bioingeniería, Biomateriales y Nanomedicina
Spain, Barcelona
Irb Barcelona - Institute for Research in Biomedicine
Spain, Barcelona
Universitat de Barcelona
Royo, Míriam
Spain, Barcelona
Combinatorial Chemistry Unit
Spain, Madrid
Centro de Investigación Biomédica en Red de Bioingeniería, Biomateriales y Nanomedicina
Statistics
Citations: 13
Authors: 5
Affiliations: 6
Identifiers
Doi:
10.1016/j.tet.2012.02.003
ISSN:
14645416
Research Areas
Cancer