Synthesis of Gd and (68) Ga Complexes in Conjugation with a Conformationally Optimized RGD Sequence as Potential MRI and PET Tumor-Imaging Probes (Articolo in rivista)

Type
Label
  • Synthesis of Gd and (68) Ga Complexes in Conjugation with a Conformationally Optimized RGD Sequence as Potential MRI and PET Tumor-Imaging Probes (Articolo in rivista) (literal)
Anno
  • 2012-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1002/cmdc.201200043 (literal)
Alternative label
  • Manzoni L; Belvisi L; Arosio D; Bartolomeo MP; Bianchi A; Brioschi C; Buonsanti F; Cabella C; Casagrande C; Civera M; De Matteo M; Fugazza L; Lattuada L; Maisano F; Miragoli L; Neira C; Pilkington-Miksa M; Scolastico C. (2012)
    Synthesis of Gd and (68) Ga Complexes in Conjugation with a Conformationally Optimized RGD Sequence as Potential MRI and PET Tumor-Imaging Probes
    in ChemMedChem (Print)
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Manzoni L; Belvisi L; Arosio D; Bartolomeo MP; Bianchi A; Brioschi C; Buonsanti F; Cabella C; Casagrande C; Civera M; De Matteo M; Fugazza L; Lattuada L; Maisano F; Miragoli L; Neira C; Pilkington-Miksa M; Scolastico C. (literal)
Rivista
Note
  • ISI Web of Science (WOS) (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • Manzoni L; Arosio D; Istituto di Scienze e Tecnologie Molecolari, Consiglio Nazionale delle Ricerche, Via Fantoli 16/15, I-20138 Milano, Italy Belvisi L; Scolastico C; Università di Milano, Dipartimento di Chimica Organica e Industriale, Via Venezian 21, I-20133 Milan, Italy and Univ Milan, Ctr Interdipartimentale Studi Biomol & Applicaz I, I-20138 Milan, Italy Bianchi A; Casagrande C; Civera M; De Matteo M; Pilkington-Miksa M; Univ Milan, Ctr Interdipartimentale Studi Biomol & Applicaz I, I-20138 Milan, Italy Bartolomeo MP; Brioschi C; Buonsanti F; Cabella C; Lattuada L; Maisano F; Miragoli L; Neira C; Bracco Imaging SpA, Bracco Res Ctr, I-10010 Colleretto Giacosa, TO, Italy Fugazza L; Adv Accelerator Applicat, I-10010 Colleretto Giacosa, TO, Italy (literal)
Titolo
  • Synthesis of Gd and (68) Ga Complexes in Conjugation with a Conformationally Optimized RGD Sequence as Potential MRI and PET Tumor-Imaging Probes (literal)
Abstract
  • We report the synthesis of novel chelates of Gd and 68Ga with DPTA, DOTA, HP-DOA3, as well as with AAZTA, a novel chelating agent developed by our research group. These chelating agents were appropriately conjugated, prior to metal complexation, with DB58, an RGD peptidomimetic, conformationally constrained on an azabicycloalkane scaffold and endowed with high affinity for integrin alpavbeta3. Because alphavbeta3 is involved in neo-angiogenesis in solid tumors and is also directly expressed in cancer cells (e.g. glioblastomas, melanomas) and ovarian, breast, and prostate cancers, these constructs could prove useful as molecular imaging probes in cancer diagnosis by MRI or PET techniques. Molecular modeling, integrin binding assays, and relaxivity assessments allowed the selection of compounds suitable for multiple expression on dendrimeric or nanoparticulate structures. These results also led us to an exploratory investigation of 68Ga complexation for the promising 68Ga-PET technique; the AAZTA complex 15(68Ga) exhibited uptake in a xenograft model of glioblastoma, suggesting potentially useful developments with new probes with improved affinity. (literal)
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