Introduction of five potentially metabolizable linking groups between 111In-cyclohexyl EDTA derivatives and F(ab')2 fragments of anti-carcinoembryonic antigen antibody--I. A new reproducible synthetic method

Nucl Med Biol. 1993 Aug;20(6):755-62. doi: 10.1016/0969-8051(93)90162-n.

Abstract

The purpose of this study was to synthesize new bifunctional linker-chelating agents for the modification of the in vivo distribution of 111In-labeled antibodies. A general simple synthetic method of preparing cyclohexyl EDTA (CDTA) derivatives containing a linker/spacer group is described. Linkers prepared included a diester, a six carbon aliphatic chain, two thioethers and a disulfide group. The CDTA-linker compounds were coupled to F(Ab')2 fragments of anti-carcinoembryonic antigen monoclonal antibody and labeled with 111In with good retention of immunoreactivity.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Carcinoembryonic Antigen / immunology*
  • Chelating Agents / chemical synthesis*
  • Chelating Agents / metabolism
  • Chromatography, High Pressure Liquid
  • Cross-Linking Reagents / chemical synthesis*
  • Cross-Linking Reagents / metabolism
  • Drug Stability
  • Edetic Acid / analogs & derivatives*
  • Edetic Acid / chemistry
  • Edetic Acid / metabolism
  • Immunoglobulin Fragments / chemistry*
  • Immunoglobulin Fragments / metabolism
  • Indium Radioisotopes / chemistry
  • Isotope Labeling / methods
  • Mice
  • Reproducibility of Results

Substances

  • Carcinoembryonic Antigen
  • Chelating Agents
  • Cross-Linking Reagents
  • Immunoglobulin Fragments
  • Indium Radioisotopes
  • CDTA
  • Edetic Acid