title: 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 Lu(3+) or Cu(2+) complexes of these compounds, c(DOTA-RGDf) and c(DOTA-RGD), showed a metal dependent affinity towards integrin α(v)β(3)in vitro and the (177)Lu(3+) or (64)Cu(2+) labelled derivatives showed specific tumour uptake in MCF7 and U87MG tumour bearing mice.
authors.affiliation: The University of Texas Southwestern Medical Center, 5323 Harry Hines Blvd, Dallas, TX 75390, USA.
authors.forename: Guiyang
authors.initials: G
authors.lastname: Hao
authors.forename: Xiankai
authors.initials: X
authors.lastname: Sun
authors.forename: Quyen N
authors.initials: QN
authors.lastname: Do
authors.forename: Blanca
authors.initials: B
authors.lastname: Ocampo-García
authors.forename: Andrea
authors.initials: A
authors.lastname: Vilchis-Juárez
authors.forename: Guillermina
authors.initials: G
authors.lastname: Ferro-Flores
authors.forename: Luis M
authors.initials: LM
authors.lastname: De León-Rodríguez
mesh_terms: D000818:Animals; D001692:Biological Transport; D045744:Cell Line, Tumor; D002614:Chelating Agents / Q000737:chemistry*; D003500:Cyclization; D006573:Heterocyclic Compounds, 1-Ring / Q000737:chemistry*; D006801:Humans; D039302:Integrin alphaVbeta3 / Q000378:metabolism*; D047028:Macrocyclic Compounds / Q000737:chemistry*; D051379:Mice; D057054:Molecular Imaging / Q000379:methods*; D009842:Oligopeptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism*
chemical_list: D002614:Chelating Agents; D006573:Heterocyclic Compounds, 1-Ring; D039302:Integrin alphaVbeta3; D047028:Macrocyclic Compounds; D009842:Oligopeptides; C071349:1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid; C047981:arginyl-glycyl-aspartic acid