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Published on: January 20, 2018
Multivalent effects of RGD peptides obtained by nanoparticle display
Xavier Montet1, Martin Funovics, Karin Montet-Abou
1Department of Radiology, Geneva Hospital, Geneva, Switzerland, and Department of Angiography and Interventional Radiology, Vienna Medical University, Vienna, Austria.
Attaching RGD peptides to nanoparticles significantly enhances their binding affinity to integrins, demonstrating strong multivalent effects. This nanoparticle formulation also extends peptide blood half-life, suggesting potent in vivo inhibition of alpha(V)beta(3) function.
Area of Science:
- Biomaterials Science
- Cell Biology
- Nanotechnology
Background:
- Integrins are cell surface receptors crucial for cell adhesion and signaling.
- RGD peptides are known ligands for integrins, particularly alpha(V)beta(3).
- Multivalency, the simultaneous binding of multiple ligands, can dramatically alter binding affinity.
Purpose of the Study:
- To investigate the impact of displaying RGD peptides on nanoparticle carriers on their binding affinity to integrins.
- To quantify the multivalent effects of RGD peptide-nanoparticle conjugates.
- To assess the in vivo potential of RGD nanoparticles as inhibitors of alpha(V)beta(3) function.
Main Methods:
- Synthesis of RGD peptide-conjugated nanoparticles.
- Measurement of endothelial cell adhesion using RGD nanoparticles and free RGD peptides.
- Calculation of the multivalent enhancement factor (MVE).
- Determination of blood half-life of RGD peptides with and without nanoparticle conjugation.
Main Results:
- RGD nanoparticles exhibited significantly enhanced binding affinity to endothelial cells compared to free peptides, with an IC50 of 1.0 nM for the nanoparticle and 20 nM for the peptide.
- A strong multivalent enhancement factor (MVE) of 38 was observed, indicating a substantial increase in binding affinity due to multivalency.
- Conjugation of RGD peptides to nanoparticles extended their blood half-life from 13 minutes to 180 minutes.
Conclusions:
- Multivalent display of RGD peptides on nanoparticles leads to a significant enhancement in binding affinity to integrins.
- The extended blood half-life and enhanced affinity suggest that RGD nanoparticle-sized materials are promising for potent in vivo inhibition of alpha(V)beta(3) function on endothelial cells.
