Issue 46, 2012

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

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

Supplementary files

Article information

Article type
Communication
Submitted
08 Jul 2012
Accepted
01 Oct 2012
First published
22 Oct 2012

Dalton Trans., 2012,41, 14051-14054

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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