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

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8 Scopus citations

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 αvβ 3in vitro and the 177Lu3+ or 64Cu2+ labelled derivatives showed specific tumour uptake in MCF7 and U87MG tumour bearing mice.

Original languageEnglish (US)
Pages (from-to)14051-14054
Number of pages4
JournalDalton Transactions
Volume41
Issue number46
DOIs
StatePublished - Dec 14 2012

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ASJC Scopus subject areas

  • Inorganic Chemistry

Cite this

Hao, G., Sun, X., Do, Q. N., Ocampo-García, B., Vilchis-Juárez, A., Ferro-Flores, G., & De León-Rodríguez, L. M. (2012). Cyclization of RGD peptide sequences via the macrocyclic chelator DOTA for integrin imaging. Dalton Transactions, 41(46), 14051-14054. https://doi.org/10.1039/c2dt31493b