Next Article in Journal
The Role of Transport Mechanisms in Mycobacterium Tuberculosis Drug Resistance and Tolerance
Next Article in Special Issue
Cell Penetrating Peptoids (CPPos): Synthesis of a Small Combinatorial Library by Using IRORI MiniKans
Previous Article in Journal
Cyclooxygenase (COX) Inhibitors and the Newborn Kidney
Previous Article in Special Issue
Intranasal Delivery of Camptothecin-Loaded Tat-Modified Nanomicells for Treatment of Intracranial Brain Tumors
Article Menu

Export Article

Open AccessReview
Pharmaceuticals 2012, 5(11), 1177-1209; doi:10.3390/ph5111177

Improving the Endosomal Escape of Cell-Penetrating Peptides and Their Cargos: Strategies and Challenges

Department of Biochemistry and Biophysics, Texas A&M University, Room 430, 300 Olsen Blvd., College Station, TX 77843-2128, USA
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Received: 8 October 2012 / Revised: 25 October 2012 / Accepted: 26 October 2012 / Published: 1 November 2012
(This article belongs to the Special Issue Cell-penetrating Peptides 2012)
View Full-Text   |   Download PDF [526 KB, uploaded 1 November 2012]   |  

Abstract

Cell penetrating peptides (CPPs) can deliver cell-impermeable therapeutic cargos into cells. In particular, CPP-cargo conjugates tend to accumulate inside cells by endocytosis. However, they often remain trapped inside endocytic organelles and fail to reach the cytosolic space of cells efficiently. In this review, the evidence for CPP-mediated endosomal escape is discussed. In addition, several strategies that have been utilized to enhance the endosomal escape of CPP-cargos are described. The recent development of branched systems that display multiple copies of a CPP is presented. The use of viral or synthetic peptides that can disrupt the endosomal membrane upon activation by the low pH of endosomes is also discussed. Finally, we survey how CPPs labeled with chromophores can be used in combination with light to stimulate endosomal lysis. The mechanisms and challenges associated with these intracellular delivery methodologies are discussed.
Keywords: endosomal escape; cell-penetrating peptide; photochemical internalization; multivalent peptides; pH-dependent membrane-active peptides endosomal escape; cell-penetrating peptide; photochemical internalization; multivalent peptides; pH-dependent membrane-active peptides
Figures

This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

Erazo-Oliveras, A.; Muthukrishnan, N.; Baker, R.; Wang, T.-Y.; Pellois, J.-P. Improving the Endosomal Escape of Cell-Penetrating Peptides and Their Cargos: Strategies and Challenges. Pharmaceuticals 2012, 5, 1177-1209.

Show more citation formats Show less citations formats

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Pharmaceuticals EISSN 1424-8247 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top