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Synthesis of DOTA-conjugated multivalent cyclic-RGD peptide dendrimers via 1,3-dipolar cycloaddition and their biological evaluation: implications for tumor targeting and tumor imaging purposes.

来自 Semantic Scholar

阅读量：

57

作者：

I Dijkgraaf，AY Rijnders，A Soede，AC Dechesne，GWV Esse，AJ Brouwer，FHM Corstens，OC Boerman，DTS Rijkers，RMJ Liskamp

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摘要：

This report describes the design and synthesis of a series of αVβ3integrin-directed monomeric, dimeric and tetramericcyclo[Arg-Gly-Asp-d-Phe-Lys] dendrimers using "click chemistry". It was found that the unprotectedN--azido derivative ofcyclo[Arg-Gly-Asp-d-Phe-Lys] underwent a highly chemoselective conjugation to amino acid-based dendrimers bearing terminal alkynes using a microwave-assisted Cu(i)-catalyzed 1,3-dipolar cycloaddition. The αVβ3binding characteristics of the dendrimers were determinedin vitroand theirin vivoαVβ3targeting properties were assessed in nude mice with subcutaneously growing human SK-RC-52 tumors. The multivalent RGD-dendrimers were found to have enhanced affinity toward the αVβ3integrin receptor as compared to the monomeric derivative as determined in anin vitrobinding assay. In case of the DOTA-conjugated111In-labeled RGD-dendrimers, it was found that the radiolabeled multimeric dendrimers showed specifically enhanced uptake in αVβ3integrin expressing tumorsin vivo.These studies showed that the tetrameric RGD-dendrimer had better tumor targeting properties than its dimeric and monomeric congeners.

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关键词：

nucleoside synthesis serine protease mimic DNA scaffold 2 ' modification

DOI：

10.1039/b615940k

被引量：

307

年份：

2007

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