Gd-DOTA Conjugate of RGD as a Potential Tumor-Targeting MRI Contrast Agent

Tumor recognition: Conjugation of 1,4,7,10‐tetraazacyclododecane‐1,4,7,10‐tetraacetic acid (DOTA) with the cyclic pentapeptide c(RGDYK) and subsequent complexation with GdCl3⋅6 H2O afforded Gd‐DOTA‐RGD, which, although a single molecular entity, is an efficient, target‐specific MRI contrast agent fo...

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Bibliographic Details
Published in:Chembiochem : a European journal of chemical biology 2008-11, Vol.9 (17), p.2811-2813
Main Authors: Park, Ji-Ae, Lee, Jae-Jun, Jung, Jae-Chang, Yu, Dae-Yeul, Oh, Chilhwan, Ha, Seunghan, Kim, Tae-Jeong, Chang, Yongmin
Format: Article
Language:English
Subjects:
Animals
Cell Line
Cell Survival - drug effects
Chickens
Contrast Media - chemical synthesis
Contrast Media - chemistry
Contrast Media - toxicity
Gd chelates
Genes, ras
Heterocyclic Compounds - chemistry
imaging agents
Integrin alphaVbeta3 - metabolism
Liver Neoplasms, Experimental - diagnosis
Liver Neoplasms, Experimental - metabolism
Liver Neoplasms, Experimental - pathology
Magnetic Resonance Imaging - methods
Mice
Mice, Transgenic
Neoplasm Transplantation
Oligopeptides - chemistry
Organometallic Compounds - chemistry
Protein Binding
receptors
relaxivity
tumor targeting
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Summary:Tumor recognition: Conjugation of 1,4,7,10‐tetraazacyclododecane‐1,4,7,10‐tetraacetic acid (DOTA) with the cyclic pentapeptide c(RGDYK) and subsequent complexation with GdCl3⋅6 H2O afforded Gd‐DOTA‐RGD, which, although a single molecular entity, is an efficient, target‐specific MRI contrast agent for the ανβ3 receptors in hepatocellular carcinoma in H‐ras12V transgenic mice. The compound displays very low cytotoxicity and might hence warrant further study for clinical usage.
ISSN:1439-4227
1439-7633
DOI:10.1002/cbic.200800529