Issue 46, 2012
From the journal:

Dalton Transactions

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

Guiyang Hao,a   Xiankai Sun,*a   Quyen N. Do,a   Blanca Ocampo-García,b   Andrea Vilchis-Juárez,b   Guillermina Ferro-Floresb  and  Luis M. De León-Rodríguez*c  

* Corresponding authors

a The University of Texas Southwestern Medical Center, 5323 Harry Hines Blvd, Dallas, TX 75390, USA
E-mail: xiankai.sun@utsouthwestern.edu
Fax: +1 214-645-2885
Tel: +1 214-645-5978

b Instituto Nacional de Investigaciones Nucleares, Carretera México-Toluca S/N, La Marquesa, Ocoyoacac, Estado de México, México
E-mail: guillermina.ferro@inin.gob.mx
Fax: +52 555-329-7306
Tel: +52 555-329-7200

c Universidad de Guanajuato, Cerro de la Venada S/N, Guanajuato, México
E-mail: lmdeleon@ugto.mx
Fax: +52 473-732-6252

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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Article information

DOI
https://doi.org/10.1039/C2DT31493B
Article type
Communication
Submitted
08 Jul 2012
Accepted
01 Oct 2012
First published
22 Oct 2012

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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