Design, synthesis, and characterization of a dual modality positron emission tomography and fluorescence imaging agent for monoclonal antibody tumor-targeted imaging

Academic Article

Abstract

  • A novel lysine-based trifunctional chelate 3 was designed, synthesized, and characterized and bears both a chelating moiety (CHX-A″) for sequestering radiometals (86Y or 111In) and the near-infrared dye Cy5.5 for dual modality PET (or SPECT) and fluorescence imaging, respectively. Successful conjugation of 3 to the monoclonal antibody trastuzumab (Herceptin) was achieved by efficient thiol-maleimide chemistry, thereby yielding immunoconjugate 2. Analysis of 2 by flow cytometry and competitive binding assay demonstrates that immunoconjugate 2 binds to SKOV3 tumor cells comparably to native trastuzumab and, thus, may be used as a tumor-targeted monoclonal antibody probe for multimodality imaging.
  • Authors

    Published In

    Digital Object Identifier (doi)

    Author List

  • Xu H; Baidoo K; Gunn AJ; Boswell CA; Milenic DE; Choyke PL; Brechbiel MW
  • Start Page

  • 4759
  • End Page

  • 4765
  • Volume

  • 50
  • Issue

  • 19