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Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers
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Cell-penetrating peptides: classes, origin, and current landscape.

Francesca Milletti1

  • 1Hoffmann-La Roche Inc., pRED Informatics, 340 Kingsland Street, Nutley, NJ, USA. francesca.milletti@roche.com

Drug Discovery Today
|April 3, 2012
PubMed
Summary
This summary is machine-generated.

Cell-penetrating peptides (CPPs) offer a promising therapeutic alternative by targeting intracellular proteins. This review classifies CPPs and provides a framework for discovering new therapeutic peptides.

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Last Updated: May 23, 2026

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Published on: September 19, 2022

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Drug Discovery

Background:

  • Peptides are increasingly FDA-approved therapeutics, offering an alternative to small molecules.
  • Current therapeutic peptides are limited to extracellular targets.
  • Cell-penetrating peptides (CPPs) can overcome this limitation by targeting intracellular proteins.

Purpose of the Study:

  • To present a classification scheme for CPPs.
  • To provide a framework for understanding and discovering novel CPPs.
  • To highlight the therapeutic potential of CPPs for intracellular targets.

Main Methods:

  • Literature review of existing CPPs.
  • Analysis of CPPs based on physical-chemical properties and origin.
  • Development of a classification system for CPPs.

Main Results:

  • A classification scheme for CPPs is proposed.
  • CPPs demonstrate potential for targeting intracellular proteins.
  • CPPs can facilitate the delivery of various cargoes into cells.

Conclusions:

  • CPPs represent a significant advancement in therapeutic drug development.
  • The proposed classification and framework can guide future CPP research.
  • CPPs hold great promise for treating diseases by targeting intracellular pathways.