Abstract

Over the last couple of years, the number of original papers and reviews discussing various applications of cell penetrating peptides (CPPs) has grown exponentially. This is not remarkable since CPPs are capable of transporting the most varying cargo across cell membranes which is one of the biggest problems in drug delivery and targeted therapy. In this review, we focus on the use of CPPs and related peptides for delivery of imaging contrast agents and radionuclides to cells and tissues with the ultimate goal of in vivo molecular imaging and molecular radiotherapy of intracellular and even intranuclear targets.

Highlights

  • Since their discovery in 1988, cell penetrating peptides (CPPs) have been extensively studied and in2009 alone, over 200 papers were published, including 10 reviews [1,2,3,4,5,6,7,8]

  • The success of CPPs lies in their potential to unlock intracellular targets for drug delivery and molecular imaging, by the adaption of a wide variety of agents ranging from

  • In contrast to the variety of papers that describe the delivery of oligopeptide/protein and nucleic acids or analogs, this review will focus on the use of CPPs in molecular imaging with applications diverse from optical, magnetic resonance and nuclear medicine imaging

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Summary

Introduction

Since their discovery in 1988, cell penetrating peptides (CPPs) have been extensively studied and in. Pharmaceuticals 2010, 3 peptides to antibodies and (drug-loaded) nanoparticles This can provide a new approach to molecular imaging and therapy as many targets aren’t located on the cell surface but intracellular or even intranuclear. It was clear that these results could eventually open new possibilities for direct delivery of proteins into patients in the context of protein therapy Despite their tremendous potential, the majority of CPP research to date is limited to elucidating their cell uptake mechanisms and to the exploration of novel compounds or intracellular targets in cell-based systems. CPPs don’t seem to be toxic to cells and organisms, only a few papers report on the use of CPPs for in v ivo applications such as delivery of peptides and proteins to target different diseases including cancer, asthma, apoptosis, ischemia, stimulating cytotoxic immunity and diabetes [17,18,19,20,21]. In contrast to the variety of papers that describe the delivery of oligopeptide/protein and nucleic acids or analogs, this review will focus on the use of CPPs in molecular imaging with applications diverse from optical, magnetic resonance and nuclear medicine imaging

Uptake Mechanisms and Repercussions for Applications
Applicatiions of CPP
The Direct Approach
CPP Constructs with an Intracellular or Intranuclear Target
CPP Constructs with an Extracellular Target
Activatable CPP Constructs
Use of CPP to Track Prelabelled Cells
Findings
Future Applications
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