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Updated: Dec 24, 2025

Polymalic Acid-based Nano Biopolymers for Targeting of Multiple Tumor Markers: An Opportunity for Personalized Medicine?
Published on: June 13, 2014
Peptides for tumor-specific drug targeting: state of the art and beyond
Maurizio Roveri1, Michele Bernasconi, Jean-Christophe Leroux
1Institute of Pharmaceutical Sciences, ETH Zurich, 8093 Zurich, Switzerland.
Abstract:
Important elements for an efficient tumor targeted delivery are cancer-specific de novo- or over-expression of target receptors and their availability on the tumor cell surface. Peptides can be designed to selectively bind to such receptors and act as tumor-targeting ligands, as has been revealed in several preclinical studies. Notably, the amino acid sequences of these peptides can be chemically modified to prevent enzymatic degradation and improve the stability of the peptide. Furthermore, tumor-targeting peptides can be conjugated to the surface of nanosized drug carriers for the selective delivery of anticancer drugs to tumors. In this review, tumor receptors for which targeting peptides have been identified are described, and their targeting potential is considered. Various chemical modifications of peptides are thoroughly described, and targeting peptides as well as peptide-functionalized nanocarriers are critically discussed. The limitations of active targeting nanocarriers are evaluated in detail, and an outlook on the potential of tumor-targeting peptides and their clinical applications is provided.
Insights
Tumor-targeting peptides offer efficient drug delivery by binding to cancer cell receptors. Chemical modifications enhance peptide stability, enabling targeted delivery of anticancer drugs via nanocarriers.
Area of Science:
- Oncology
- Nanotechnology
- Biochemistry
Background:
- Efficient tumor targeted delivery relies on cancer-specific receptor expression.
- Peptides can be engineered as tumor-targeting ligands for selective binding.
- Chemical modifications improve peptide stability and prevent degradation.
Purpose of the Study:
- To review tumor receptors identified for targeting peptides.
- To discuss the targeting potential of these peptides.
- To evaluate peptide modifications and nanocarrier applications.
Main Methods:
- Literature review of tumor receptors and targeting peptides.
- Analysis of chemical modifications for peptide enhancement.
- Discussion of peptide-functionalized nanocarriers for drug delivery.
Main Results:
- Identified tumor receptors and their targeting peptide ligands.
- Described various chemical modifications for peptide optimization.
- Evaluated the role of peptide-functionalized nanocarriers in drug delivery.
Conclusions:
- Tumor-targeting peptides show significant potential for selective anticancer drug delivery.
- Chemical modifications and nanocarrier conjugation are crucial for efficacy.
- Further research is needed to overcome limitations for clinical applications.
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