RGD-based PET tracers for imaging receptor integrin αv β3 expression

Area of Science:

• Nuclear medicine
• Radiochemistry
• Molecular imaging

Background:

• Integrin αv β3 receptor expression is crucial in cancer and cardiovascular diseases.
• Positron emission tomography (PET) imaging offers vital diagnostic and therapeutic monitoring capabilities.
• Advances in PET chemistry have enabled the development of novel imaging tracers.

Purpose of the Study:

• To review the radiochemistry development of PET tracers targeting integrin αv β3.
• To provide an overview of strategies for preparing arginine-glycine-aspartic acid (RGD) peptide-based PET tracers.
• To highlight recent advances in RGD-based PET tracer development.

Main Methods:

• Focus on radiochemistry of RGD peptide-based PET tracers.
• Overview of general strategies for RGD-based PET tracer preparation.
• Review of recent advances in (18)F, (64)Cu, and (68)Ga-labeled RGD tracers.

Main Results:

• Significant progress in developing RGD-based PET tracers for integrin αv β3 imaging.
• Development of multivalent and multimodality RGD-based PET probes.
• Demonstrated potential for early disease detection and therapeutic evaluation.

Conclusions:

• RGD peptide-based PET tracers are valuable tools for imaging integrin αv β3 expression.
• Ongoing advancements facilitate improved diagnostic and therapeutic applications.
• These tracers are critical for anti-angiogenic drug discovery and development.