Lipo-oligoarginine-based intracellular delivery

Methods Mol Biol. 2013:991:281-92. doi: 10.1007/978-1-62703-336-7_26.

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.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Arginine / chemistry*
  • Drug Delivery Systems*
  • Humans
  • Jurkat Cells
  • Microscopy, Confocal
  • Microscopy, Fluorescence

Substances

  • Arginine