title: Gallium labeled NOTA-based conjugates for peptide receptor-mediated medical imaging.
abstract: We report a straightforward and efficient synthetic strategy for the synthesis of three model glycine-arginine-glycine-aspartic acid-glycine (GRGDG) conjugates based on derivatives of NOTA and of their Ga(III) complexes targeted to the integrin α(ν)β(3) receptor. (71)Ga NMR spectroscopy showed that the Ga(III)-labeled conjugates are highly stable in aqueous solution. The (67)Ga-labeled conjugates proved to have high kinetic stability and showed a weak but specific binding to the receptors in a U87MG-glioblastoma cell line.
authors.affiliation: Centro de Química, Campus de Gualtar, Universidade do Minho, Braga, Portugal.
authors.forename: Arsénio
authors.initials: A
authors.lastname: de Sá
authors.forename: Aurea A
authors.initials: AA
authors.lastname: Matias
authors.forename: M Isabel M
authors.initials: MI
authors.lastname: Prata
authors.forename: Carlos F G C
authors.initials: CF
authors.lastname: Geraldes
authors.forename: P M T
authors.initials: PM
authors.lastname: Ferreira
authors.forename: João P
authors.initials: JP
authors.lastname: André
mesh_terms: D000595:Amino Acid Sequence; D045744:Cell Line, Tumor; D003287:Contrast Media / Q000138:chemical synthesis / Q000737:chemistry*; D056831:Coordination Complexes / Q000138:chemical synthesis / Q000737:chemistry*; D005708:Gallium / Q000737:chemistry*; D006571:Heterocyclic Compounds / Q000737:chemistry*; D006573:Heterocyclic Compounds, 1-Ring; D006801:Humans; D039302:Integrin alphaVbeta3 / Q000737:chemistry / Q000378:metabolism; D010455:Peptides / Q000737:chemistry*
chemical_list: D003287:Contrast Media; D056831:Coordination Complexes; D006571:Heterocyclic Compounds; D006573:Heterocyclic Compounds, 1-Ring; D039302:Integrin alphaVbeta3; D010455:Peptides; C048993:1,4,7-triazacyclononane-N,N',N''-triacetic acid; D005708:Gallium