TY - JOUR
T1 - Cyclization of RGD peptide sequences via the macrocyclic chelator DOTA for integrin imaging
AU - Hao, Guiyang
AU - Sun, Xiankai
AU - Do, Quyen N.
AU - Ocampo-García, Blanca
AU - Vilchis-Juárez, Andrea
AU - Ferro-Flores, Guillermina
AU - De León-Rodríguez, Luis M.
PY - 2012/12/14
Y1 - 2012/12/14
N2 - 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.
AB - 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.
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U2 - 10.1039/c2dt31493b
DO - 10.1039/c2dt31493b
M3 - Article
C2 - 23085681
AN - SCOPUS:84868650401
SN - 1477-9226
VL - 41
SP - 14051
EP - 14054
JO - Dalton Transactions
JF - Dalton Transactions
IS - 46
ER -