Journal article
Evaluation of macrocyclic hydroxyisophthalamide ligands as chelators for zirconium-89
PloS one, Vol.12(6), pp.e0178767-e0178767
2017
DOI: 10.1371/journal.pone.0178767
PMCID: PMC5456358
PMID: 28575044
Abstract
The development of bifunctional chelators (BFCs) for zirconium-89 immuno-PET applications is an area of active research. Herein we report the synthesis and evaluation of octadentate hydroxyisophthalamide ligands (1 and 2) as zirconium-89 chelators. While both radiometal complexes could be prepared quantitatively and with excellent specific activity, preparation of 89Zr-1 required elevated temperature and an increased reaction time. 89Zr-1 was more stable than 89Zr-2 when challenged in vitro by excess DTPA or serum proteins and in vivo during acute biodistribution studies. Differences in radiometal complex stability arise from structural changes between the two ligand systems, and suggest further ligand optimization is necessary to enhance 89Zr chelation.
Details
- Title: Subtitle
- Evaluation of macrocyclic hydroxyisophthalamide ligands as chelators for zirconium-89
- Creators
- Nikunj B Bhatt - Wake Forest UniversityDarpan N Pandya - Wake Forest UniversityJide Xu - LumiphoreDavid Tatum - LumiphoreDarren Magda - LumiphoreThaddeus J Wadas - Wake Forest University
- Resource Type
- Journal article
- Publication Details
- PloS one, Vol.12(6), pp.e0178767-e0178767
- DOI
- 10.1371/journal.pone.0178767
- PMID
- 28575044
- PMCID
- PMC5456358
- NLM abbreviation
- PLoS One
- ISSN
- 1932-6203
- eISSN
- 1932-6203
- Grant note
- UL1 TR001420 / NCATS NIH HHS
- Language
- English
- Date published
- 2017
- Academic Unit
- Radiology; Radiation Oncology
- Record Identifier
- 9984313084302771
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