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Dipicolinic acid (DPA)-based chelators for zirconium-89 PET imaging applications
Siyuan Ren1, Haixing Wang1, Yujie Liu1
1Department of Chemistry, Illinois Institute of Technology, Chicago, IL, USA.
Bioorganic & Medicinal Chemistry Letters
|March 23, 2026
Summary
Researchers developed novel pyridine-based chelators for zirconium-89 (89Zr) PET imaging. Dipicolinic acid (DPA) derivatives, like TEG-DPA2, show rapid 89Zr complexation and favorable biodistribution for enhanced imaging applications.
Area of Science:
- Radiochemistry
- Nuclear Medicine
- Organic Chemistry
Background:
- Positron Emission Tomography (PET) imaging requires efficient radiolabeling agents.
- Zirconium-89 (89Zr) is a promising PET isotope but requires robust chelators for stable complexation.
Purpose of the Study:
- To synthesize and evaluate pyridine-based chelators for 89Zr radiolabeling.
- To identify effective chelators for 89Zr PET imaging applications.
Main Methods:
- Screening of pyridine-containing small molecule ligands for Zr(IV) complexation kinetics.
- Synthesis of a tetraethylene glycol (TEG) spacer-linked dipicolinic acid (DPA) derivative (TEG-DPA2).
- Radiolabeling with 89Zr, complex stability assays, and in vivo biodistribution studies in mice.
Main Results:
- Dipicolinic acid (DPA) identified as an effective donor system for 89Zr(IV).
- The acyclic chelator TEG-DPA2 rapidly formed a neutral 89Zr complex with high serum stability.
- 89Zr-TEG-DPA2 demonstrated rapid blood clearance and low normal tissue uptake via renal excretion in mice.
Conclusions:
- DPA-based donor systems show significant potential for 89Zr radiolabeling.
- TEG-DPA2 is a promising lead chelator for 89Zr PET imaging development.
