Generation of endosomolytic reagents by branching of cell-penetrating peptides: tools for the delivery of bioactive compounds to live cells in cis or trans. Academic Article

abstract

• We describe the synthesis and cellular delivery properties of multivalent and branched delivery systems consisting of cell-penetrating peptides assembled onto a peptide scaffold using native chemical ligation. A trimeric delivery system presenting three copies of the prototypical cell-penetrating peptide TAT shows an endosomolytic activity much higher than its monomeric and dimeric counterparts. This novel reagent promotes the endosomal release of macromolecules internalized into cells by endocytosis, and as a result, it can be used to achieve cytosolic delivery of bioactive but cell-impermeable macromolecules in either cis (covalent conjugation) or trans (simple coincubation).

authors

• Pellois, Jean-Philippe

published proceedings

• Bioconjug Chem

altmetric score

• 12

author list (cited authors)

• Angeles-Boza, A. M., Erazo-Oliveras, A., Lee, Y., & Pellois, J.

citation count

• 47

complete list of authors

• Angeles-Boza, Alfredo M||Erazo-Oliveras, Alfredo||Lee, Ya-Jung||Pellois, Jean-Philippe

publication date

• December 2010

publisher

• American Chemical Society (ACS)  Publisher

published in

• Bioconjugate Chemistry  Journal

keywords

• Amino Acid Sequence
• Biological Products
• Cell Membrane
• Cell-Penetrating Peptides
• Drug Delivery Systems
• Endocytosis
• Endosomes
• Female
• Fluorescein
• Hela Cells
• Humans
• Polymers
• Spectrometry, Fluorescence

PubMed Central ID

• 21043514

Digital Object Identifier (DOI)

• 10.1021/bc100130r

start page

• 2164

end page

• 2167

volume

• 21

issue

• 12

URL

• http%3A%2F%2Fdx.doi.org%2F10.1021%2Fbc100130r