Abstract
Efficient cellular delivery, including plasma membrane permeability and intracellular metabolic stability, is a crucial factor determining the success of therapeutic agents. Cell-penetrating peptides (CPPs) have been widely used for the intracellular delivery of various bioactive molecules into cells to modify cellular functions. We have developed an improved CPP-based cellular delivery vector, named lipo-oligoarginine peptide (LOAP), by conjugating an oligoarginine peptide with a fatty acid moiety. The prepared LOAPs were further stabilized by introducing different combinations of d-Arg residues into the peptide backbone and were systematically evaluated for their membrane-penetrating properties and metabolic stabilities in cells.
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Abbreviations
- MBHA:
-
4-Methylbenzhydrylamine
- Fmoc:
-
9-Fluorenylmethyloxycarbonyl
- Pbf:
-
2,2,4,6,7-Pentamethyldihydrobenzofuran-5-sulfonyl
- Mtt:
-
Methyltrityl
- TA:
-
Thioanisole
- EDT:
-
Ethandithiol
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Acknowledgment
This work was supported in part by NIH CA135312, CA114149, and CA126752.
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Lee, J.S., Tung, CH. (2013). Lipo-oligoarginine-Based Intracellular Delivery. In: Weissig, V., Elbayoumi, T., Olsen, M. (eds) Cellular and Subcellular Nanotechnology. Methods in Molecular Biology, vol 991. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-62703-336-7_26
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DOI: https://doi.org/10.1007/978-1-62703-336-7_26
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