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Gadolinium Complex of I-125/I-127-RGD-DOTA Conjugate as a Tumor-Targeting SPECT/MR Bimodal Imaging Probe

  作者 PARK JIAE; KIM JUNG YOUNG; LEE YONG JIN; LEE WONHO; LIM SANG MOO; KIM TAEJEONG; YOO JEONGSOO; CHANG YONGMIN; KIM KYEONG MIN  
  选自 期刊  ACS Medicinal Chemistry Letters;  卷期  2013年4-2;  页码  216-219  
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[摘要]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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