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Evaluation of an 111In-DOTA–Rhenium Cyclized {alpha}-MSH Analog: A Novel Cyclic-Peptide Analog with Improved Tumor-Targeting Properties

JianQing Chen, Zhen Cheng, Nellie K. Owen, Timothy J. Hoffman, Yubin Miao, Silvia S. Jurisson and Thomas P. Quinn

Departments of Biochemistry, Radiology, and Chemistry, University of Missouri–Columbia, Columbia; and Harry S. Truman Memorial Veterans Hospital, Columbia, Missouri



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FIGURE 1. Structure of DOTA-ReCCMSH.

 


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FIGURE 2. Radioactivity uptake (%ID) in urine (A), intestines (B), and kidneys (C) for 111In-DOTA–ReCCMSH (ReCCMSH), DOTA-CCMSH (CCMSH), DOTA-CMSH (CMSH), and DOTA-NDP (NDP) in B16/F1 murine melanoma–bearing C57 mice at 0.5, 2, 4, and 24 h after injection (n = 5).

 


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FIGURE 3. Tumor retention of radioactivity and clearance of radioactivity from normal tissues for 111In-DOTA–ReCCMSH over time (%ID/g) (n = 5). Area under curve (AUC) and ratio of tumor AUC to tissue AUC for blood, lung, liver, and carcass are also listed.

 





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