Peptides for cell-selective drug delivery

Trends in Pharmacological Sciences
Nina SvensenMark Bradley

Abstract

The ability to target specific cell types to achieve optimal distribution of therapeutic entities into diseased tissues, while limiting possible adverse off-target effects, has long been a goal of many research groups and pharmaceutical organizations. This review focuses on peptidic tissue-specific biomarkers that allow peptides to act as homing devices for specific tissue types or organs, with a focus on homing peptides (HPs) and cell-penetrating homing peptides (CPHPs). These HPs, in addition to promoting cellular uptake, can deliver a variety of cargos (drugs, oligonucleotides and nanoparticles) into cells. Two such peptides that have entered clinical trials are the tumor-homing peptide asparagine-glycine-arginine (NGR) (fused to human tumor necrosis factor), which selectively binds CD13, an aminopeptidase that is overexpressed on tumor blood vessels, and cyclo[Arg-Gly-Asp-D-Phe-(NMeVal)] (cRGD, cilengitide), an anti-angiogenic agent that targets the α(v)β(3) and α(v)β(5) integrins.

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