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Issue 46, 2012
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Cyclization of RGD peptide sequences via the macrocyclic chelator DOTA for integrin imaging

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Abstract

Two bicyclic compounds containing Arg-Gly-Asp (RGD) motifs (RGDf and RGD) were synthesized by cyclizing the peptide sequence across the macrocyclic ring of DOTA via two non-adjacent carboxylate pendent arms. The Lu3+ or Cu2+ complexes of these compounds, c(DOTA-RGDf) and c(DOTA-RGD), showed a metal dependent affinity towards integrin αvβ3in vitro and the 177Lu3+ or 64Cu2+ labelled derivatives showed specific tumour uptake in MCF7 and U87MG tumour bearing mice.

Graphical abstract: Cyclization of RGD peptide sequences via the macrocyclic chelator DOTA for integrin imaging

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Publication details

The article was received on 08 Jul 2012, accepted on 01 Oct 2012 and first published on 22 Oct 2012


Article type: Communication
DOI: 10.1039/C2DT31493B
Citation: Dalton Trans., 2012,41, 14051-14054
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    Cyclization of RGD peptide sequences via the macrocyclic chelator DOTA for integrin imaging

    G. Hao, X. Sun, Q. N. Do, B. Ocampo-García, A. Vilchis-Juárez, G. Ferro-Flores and L. M. De León-Rodríguez, Dalton Trans., 2012, 41, 14051
    DOI: 10.1039/C2DT31493B

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