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Modular Synthesis of Peptide-Based Single- and Multimodal Targeted Molecular Imaging Agents.
Hans F Schmitthenner1, Taylor M Barrett1, Stephanie A Beach1
1School of Chemistry and Materials Science, Rochester Institute of Technology, Rochester, New York 14623, United States.
ACS Applied Bio Materials
|January 10, 2022
Summary
A new modular synthesis creates targeted molecular imaging agents for optical, MRI, and PET scans. This method uses protected lysines and novel metal protecting groups, enabling versatile single- or dual-modal imaging probe assembly.
Area of Science:
- Molecular imaging
- Medicinal chemistry
- Organic synthesis
Background:
- Targeted molecular imaging agents (TMIAs) are crucial for disease diagnosis and monitoring.
- Existing synthesis methods can be complex and lack modularity.
- Developing versatile platforms for multimodal imaging agents is an ongoing challenge.
Purpose of the Study:
- To develop a practical, modular synthesis for targeted molecular imaging agents (TMIAs).
- To create agents capable of optical molecular imaging (OMI), magnetic resonance imaging (MRI), and positron emission tomography (PET).
- To demonstrate the utility of novel protecting group strategies for chelators and metals.
Main Methods:
- A modular synthesis approach attaching imaging agents to protected lysine side chains.
- Utilizing gadolinium (Gd) as a protecting group for 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA).
- Employing lanthanide metals (La, Ce) as protecting and placeholder metals for transmetalation with PET metals.
- Conjugating imaging modules to linkers and targeting groups, exemplified by c(RGDyK) for integrin targeting.
Main Results:
- Successful synthesis of single- and dual-modal imaging agents (MRI-OMI, PET-OMI, PET-MRI).
- Demonstrated efficacy of Gd-based modules for MRI via NMR spin-lattice relaxivity measurements.
- Validated functional imaging of dual-modal agents targeting cancer cells using confocal fluorescence microscopy.
- Enabled synthesis of probes with combinations of dyes and/or metals.
Conclusions:
- The developed modular synthesis provides a versatile platform for constructing diverse TMIAs.
- Novel metal-based protecting group strategies simplify the assembly of complex imaging agents.
- The method facilitates the creation of single- and dual-modal probes for various imaging applications.
- This approach holds significant potential for advancing molecular imaging and personalized medicine.
