AI Article Synopsis
- The study focused on the role of carboxy group density in the effectiveness of peptide-based radiopharmaceuticals for targeting bones.
- Higher carboxy group densities were identified in oligo-γ-carboxy glutamic acid peptides (Gla), which were compared to other peptides like oligo-glutamic acid (Glu) and oligo-aspartic acid (Asp).
- Results demonstrated that the Gla-based radiopharmaceutical showed enhanced bone affinity, accumulation, and better imaging capabilities, indicating their potential as superior agents for bone imaging.
Article Abstract
We investigated the importance of the carboxy group density in bone affinity during the development of peptide-based bone-seeking radiopharmaceuticals and carriers. Oligo-γ-carboxy glutamic acid peptides [(Gla)] with higher carboxy group density than oligo-glutamic acid peptides [(Glu)] and oligo-aspartic acid peptides [(Asp)] were chosen. Using the radiogallium chelator -bis-[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine--diacetic acid (HBED-CC), we synthesized [Ga]Ga-HBED-CC-(Gla) ( = 1, 2, 5, 8, 11, or 14) with high yields. Hydroxyapatite-binding assays, biodistribution, and SPECT imaging showed higher affinity and bone accumulation for [Ga]Ga-HBED-CC-(Gla) compared to [Ga]Ga-HBED-CC-(Glu). Notably, [Ga]Ga-HBED-CC-(Gla) and [Ga]Ga-HBED-CC-(Gla) exhibited superior bone accumulation and rapid blood clearance. SPECT/CT imaging with [Ga]Ga-HBED-CC-(Gla) exclusively visualized the bone tissue. These findings support the potential use of [Ga]Ga-HBED-CC-(Gla) as excellent bone-imaging PET probes, suggesting (Gla) peptides are superior bone-seeking carriers.
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| http://dx.doi.org/10.1021/acs.molpharmaceut.3c01156 | DOI Listing |
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