Cell-Penetrating Peptides: From Basic Research to Clinics

Trends Pharmacol Sci. 2017 Apr;38(4):406-424. doi: 10.1016/j.tips.2017.01.003. Epub 2017 Feb 14.


The presence of cell and tissue barriers together with the low biomembrane permeability of various therapeutics often hampers systemic drug distribution; thus, most of the available molecules are of limited therapeutic value. Opportunities to increase medicament concentrations in areas that are difficult to access now exist with the advent of cell-penetrating peptides (CPPs), which can transport into the cell a wide variety of biologically active conjugates (cargoes). Numerous preclinical evaluations with CPP-derived therapeutics have provided promising results in various disease models that, in some cases, prompted clinical trials. The outcome of these investigations has thus opened new perspectives for CPP application in the development of unprecedented human therapies that are well tolerated and directed to intracellular targets.

Keywords: cell-penetrating peptides; clinical trials; internalization; therapy.

Publication types

  • Review
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell-Penetrating Peptides / classification
  • Cell-Penetrating Peptides / pharmacokinetics
  • Cell-Penetrating Peptides / pharmacology*
  • Cell-Penetrating Peptides / therapeutic use
  • Endocytosis
  • Humans
  • NF-kappa B / physiology
  • Reactive Oxygen Species / metabolism


  • Cell-Penetrating Peptides
  • NF-kappa B
  • Reactive Oxygen Species