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Updated: Jun 3, 2026

Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers
Published on: September 19, 2022
Cell penetrating peptides for tumor targeting
Young Suk Choi1, Jue Yeon Lee, Jin Sook Suh
1Department of Dental Regenerative Biotechnology, Dental Research Institute and School of Dentistry, Seoul National University, 28-2 Yongon-Dong, Chongno-Ku, Seoul 110-749, South Korea.
Abstract:
Anticancer drug delivery has been hindered due to cell membrane permeability and the lack of a selective marker for tumor cells. Cell permeability is related to the bioavailability of drugs and has therefore been considered to be an essential step for achieving therapeutic efficacy. While different types of transporters currently exist, cell penetrating peptides (CPPs) have become one of the most popular and effective tools for intracellular drug delivery. Most of the original CPPs are short peptides with basic residues. The mechanism of CPP cell entry remains to be established; however, the CPPs can deliver any type of molecular cargo including solid nanoparticles. Herein, this paper will discuss the classification of CPPs, the mechanism of cell entry, the application of CPPs in tumor therapy, and recent advances in targeted cell penetration that involve CPPs.
Insights
Cell penetrating peptides (CPPs) enhance anticancer drug delivery by improving cell membrane permeability. These peptides offer a promising strategy for targeted tumor therapy and intracellular delivery of various molecular cargoes.
Area of Science:
- Biochemistry
- Molecular Biology
- Nanotechnology
Background:
- Anticancer drug delivery faces challenges with cell membrane permeability and tumor cell targeting.
- Bioavailability of anticancer drugs is critically dependent on efficient cell permeability for therapeutic efficacy.
- Cell penetrating peptides (CPPs) are effective tools for intracellular drug delivery, overcoming traditional barriers.
Purpose of the Study:
- To discuss the classification and cell entry mechanisms of CPPs.
- To explore the application of CPPs in tumor therapy.
- To highlight recent advances in targeted cell penetration using CPPs.
Main Methods:
- Review of existing literature on CPP classification and mechanisms.
- Analysis of CPP applications in preclinical and clinical tumor models.
- Examination of novel strategies for targeted CPP-mediated delivery.
Main Results:
- CPPs, often short peptides with basic residues, facilitate intracellular delivery of diverse cargo, including nanoparticles.
- While CPP cell entry mechanisms require further elucidation, their utility in drug delivery is established.
- Targeted CPPs show potential for selective delivery to tumor cells, improving therapeutic outcomes.
Conclusions:
- CPPs represent a significant advancement in overcoming cell permeability barriers for anticancer drug delivery.
- Further research into CPP mechanisms and targeted delivery will enhance their role in oncology.
- CPPs offer a versatile platform for the intracellular delivery of therapeutic agents and nanoparticles in cancer treatment.
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