Synthesis of a novel bifunctional chelator AmBaSar based on sarcophagine for peptide conjugation and 64Cu radiolabelling

Hancheng Cai, John Fissekis, Peter S. Conti

Research output: Contribution to journalArticlepeer-review

69 Scopus citations

Abstract

Copper-64 shows promise as both a suitable PET imaging and therapeutic radionuclide due to its nuclear characteristics. Stable attachment of radioactive 64Cu2+ to targeted imaging probes requires the use of a bifunctional chelator. Sarcophagine (Sar) ligands coordinate the metal ion 64Cu2+ within the multiple macrocyclic rings comprising the cage structure, yielding extraordinarily stable complexes that are inert to dissociation of the metal ion in vivo. Several 64Cu labelled RGD derivatives have been applied in imaging of the ανβ3 integrin receptor expression during tumour angiogenesis. In order to design and develop novel molecular imaging probes containing RGD and Sar ligands, we designed a novel versatile Sar cage-like bifunctional chelator named AmBaSar, synthesized using a conventional synthetic strategy. Conjugation with the cyclic peptide RGD, and subsequent labelling with 64Cu, provided a new PET probe 64Cu- AmBaSar-RGD for imaging the ανβ3 integrin receptor.

Original languageEnglish (US)
Pages (from-to)5395-5400
Number of pages6
JournalDalton Transactions
Issue number27
DOIs
StatePublished - Aug 3 2009

ASJC Scopus subject areas

  • Inorganic Chemistry

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