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Abstract #1898

Aminocyclopentane- And Aminocyclophexane-Carboxylic Acid Containing Cyclic RGD-DOTA-Gd Conjugates with High Specific Affinity for &[alpha] &[nu] &[beta]3 Integrin as MRI Contrast Agents

In Ok Ko1, Ji-Ae Park1, Jung Young Kim1, Wonho Lee1, Sang Moo Lim2, Kyeong Min Kim1

1Molecular Imaging Research Center, Korea Institute of Radiological & Medical Science, Seoul, Korea; 2Department of Nuclear Medicine, Korea Institute of Radiological & Medical Science, Seoul, Korea

We designed two integrin &[alpha] &[nu] &[beta]3-specific MRI contrast agents, which is an inserted aminocyclopentane (ACP) or amicocyclohexane (ACH)-carboxylic acid into c(RGDK) to improve the binding affinity, and evaluated their tumor targeting efficacy in U87MG tumor bearing mice. Substitution of ACP or ACH in the lead structure c(RGD-ACP-K)-DOTA and c(RGD-ACH-K)-DOTA exhibited much higher binding affinity for &[alpha] &[nu] &[beta]3 integrin than c(RGDyK). The in vivo MR images of mice obtained with c(RGD-ACP-K)-DOTA-Gd and c(RGD-ACH-K)-DOTA-Gd showed a significant enhancement in the tumor.

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Keywords

achieved acid additional affinities affinity agent agents assay attractive basis bearing binding blocking candidates capable cell cells coherent complex complexes condition confirmed conjugated conjugates conjugation containing contrast custom cyclic demonstrating described designed efficacy enhancement establish evaluated experimental explain expressed flank formation gadolinium generated improve in vivo initially injected injection injections inserted institute known mass material matrix medical medicine mice model modified molecular motion mouse nothing nuclear nude paramagnetic park partially peptide post potential prepared previously proton purification purity radiological receptor relatively respectively reveal sang science slice slower specifically spectroscopy strong structure subcutaneous subsequently synthesize synthesized tail taken targeting trio tumbling tumor tumors twice types various vein worth yields young