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

Guiyang Hao; Xiankai Sun; Quyen N. Do; Blanca Ocampo-García; Andrea Vilchis-Juárez; Guillermina Ferro-Flores; Luis M. De León-Rodríguez

doi:10.1039/C2DT31493B

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Dalton Transactions

Issue 46, 2012

The international journal for inorganic, organometallic and bioinorganic chemistry

Impact Factor 3.838 48 Issues per Year Indexed in MEDLINE

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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-Flores^b and Luis M. De León-Rodríguez*^c

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

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

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

Dalton Trans., 2012,41, 14051-14054

DOI: 10.1039/C2DT31493B
Received 08 Jul 2012, Accepted 01 Oct 2012
First published online 22 Oct 2012

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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 α_vβ₃in vitro and the ¹⁷⁷Lu³⁺ or ⁶⁴Cu²⁺ labelled derivatives showed specific tumour uptake in MCF7 and U87MG tumour bearing mice.

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Guiyang Hao
Xiankai Sun
Quyen N. Do
Blanca Ocampo-García
Andrea Vilchis-Juárez
Guillermina Ferro-Flores
Luis M. De León-Rodríguez

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

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

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