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Updated: May 6, 2026
Preparing a 68Ga-labeled Arginine Glycine Aspartate RGD-peptide for Angiogenesis
Published on: January 7, 2019
Development of RGD-based radiotracers for tumor imaging and therapy: translating from bench to bedside
1(Z. Liu) Medical Isotopes Research Center, Peking University, 38 Xueyuan Road, Beijing 100191, China. liuzf@bjmu.edu.cn.
Abstract:
The cell adhesion molecule integrin αvβ3 is an important player in the process of angiogenesis. In the last decades, a series of radiolabeled Arg-Gly-Asp (RGD) peptides targeting integrin αvβ3 has been prepared and optimized for positron emission tomography (PET) and single-photon-emission computed tomography (SPECT) imaging of integrin αvβ3 expression. Several promising radiotracers have been tested in clinical trials. In this review, we will introduce strategies that have been used to optimize and accelerate RGD radiotracers towards clinical translation; illustrate RGD-based radiotracers that have been investigated in clinical trials; and discuss the other applications of RGD radiotracers aside from tumor detection.
Insights
Radiolabeled Arg-Gly-Asp (RGD) peptides targeting integrin αvβ3 are crucial for imaging angiogenesis. This review details RGD radiotracer optimization, clinical trials, and diverse applications beyond tumor detection.
Area of Science:
- Biomedical imaging
- Molecular imaging
- Radiochemistry
Background:
- Integrin αvβ3 plays a key role in angiogenesis.
- Radiolabeled Arg-Gly-Asp (RGD) peptides target integrin αvβ3 for imaging.
- Positron Emission Tomography (PET) and Single-Photon Emission Computed Tomography (SPECT) are utilized.
Purpose of the Study:
- To review strategies for optimizing RGD radiotracers for clinical translation.
- To illustrate RGD-based radiotracers investigated in clinical trials.
- To discuss applications of RGD radiotracers beyond tumor detection.
Main Methods:
- Review of existing literature on RGD radiotracers.
- Analysis of optimization strategies for radiotracer development.
- Compilation of data from clinical trials involving RGD radiotracers.
Main Results:
- Various strategies have been employed to optimize RGD radiotracers.
- Several RGD-based radiotracers have undergone clinical evaluation.
- RGD radiotracers show potential in applications beyond oncology.
Conclusions:
- RGD radiotracers are valuable tools for imaging integrin αvβ3 expression.
- Continued optimization is essential for clinical translation of RGD radiotracers.
- The utility of RGD radiotracers extends to various non-oncological applications.
