Gallium labeled NOTA-based conjugates for peptide receptor-mediated medical imaging

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7345-8. doi: 10.1016/j.bmcl.2010.10.059. Epub 2010 Oct 20.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Cell Line, Tumor
  • Contrast Media / chemical synthesis
  • Contrast Media / chemistry*
  • Coordination Complexes / chemical synthesis
  • Coordination Complexes / chemistry*
  • Gallium / chemistry*
  • Heterocyclic Compounds / chemistry*
  • Heterocyclic Compounds, 1-Ring
  • Humans
  • Integrin alphaVbeta3 / chemistry
  • Integrin alphaVbeta3 / metabolism
  • Peptides / chemistry*

Substances

  • Contrast Media
  • Coordination Complexes
  • Heterocyclic Compounds
  • Heterocyclic Compounds, 1-Ring
  • Integrin alphaVbeta3
  • Peptides
  • 1,4,7-triazacyclononane-N,N',N''-triacetic acid
  • Gallium