Biochemical and Biophysical Research Communications 2014-12-12

Improved tumor-targeting MRI contrast agents: Gd(DOTA) conjugates of a cycloalkane-based RGD peptide.

Ji-Ae Park, Yong Jin Lee, In Ok Ko, Tae-Jeong Kim, Yongmin Chang, Sang Moo Lim, Kyeong Min Kim, Jung Young Kim

Index: Biochem. Biophys. Res. Commun. 455(3-4) , 246-50, (2014)

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Abstract

Two new MRI contrast agents, Gd-DOTA-c(RGD-ACP-K) (1) and Gd-DOTA-c(RGD-ACH-K) (2), which were designed by incorporating aminocyclopentane (ACP)- or aminocyclohexane (ACH)-carboxylic acid into Gd-DOTA (gadolinium-tetraazacyclo dodecanetetraacetic acid) and cyclic RGDK peptides, were synthesized and evaluated for tumor-targeting ability in vitro and in vivo. Binding affinity studies showed that both 1 and 2 exhibited higher affinity for integrin receptors than cyclic RGDyK peptides, which were used as a reference. These complexes showed high relaxivity and good stability in human serum and have the potential to improve target-specific signal enhancement in vivo MR images. Copyright © 2014 Elsevier Inc. All rights reserved.