Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 4, Issue 2, Pages 216-219Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml3003499
Keywords
dual modality; SPECT/MR; RGD peptide; small molecule; tumor targeting
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Funding
- Programs of Development Research Center of PET Application Technology & The Programs of Clinical Application Research of Radiopharmaceuticals in the National Nuclear Technology Program, ROK
- Nuclear R&D Program through the National Research Foundation of Korea (NRF) [2009-0081817, 2012013722]
- MEST, ROK
- KNU
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The work describes the synthesis and in vivo application of [Gd(L)(H2O)]center dot xH(2)O, where L is a (I-125/I-127-RGD)- DOTA conjugate, as a tumor-targeting SPECT/MR bimodal imaging probe. Here, (I-125/I-127-RGD)-DOTA signifies a cocktail mixture of radioisotopic (1a, L = I-125-RGD-DOTA) and natural (1b, L = I-127-RGD-DOTA) Gd complexes. The two complexes are chemically equivalent as revealed by HPLC, and their cocktail mixture exhibits the integrin-specific tumor enhancement, demonstrating that they constitute essentially a single bimodal imaging probe. Employment of a cocktail mixture thus proves to be a sole and practical approach to overcome the sensitivity difference problem between MRI and SPECT.
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