A highly effective bifunctional ligand for radioimmunotherapy applications

Chem Commun (Camb). 2011 May 21;47(19):5584-6. doi: 10.1039/c0cc05707j. Epub 2011 Apr 5.

Abstract

A novel bifunctional ligand (3p-C-NETA) for antibody-targeted radioimmunotherapy (RIT) of β-emitting radioisotopes (90)Y and (177)Lu was efficiently synthesized via an unexpected regiospecific ring opening of an aziridinium ion. 3p-C-NETA instantly formed a very stable complex with (90)Y or (177)Lu. 3p-C-NETA is an excellent bifunctional ligand for RIT.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Beta Particles / therapeutic use
  • Cross-Linking Reagents / chemical synthesis
  • Cross-Linking Reagents / chemistry*
  • Heterocyclic Compounds / chemical synthesis
  • Heterocyclic Compounds / chemistry*
  • Ligands
  • Radioimmunotherapy*
  • Stereoisomerism
  • Substrate Specificity

Substances

  • (2-(4,7-biscarboxymethyl(1,4,7)triazacyclonona-1-yl-ethyl)carbonylmethylamino)acetic acid
  • Cross-Linking Reagents
  • Heterocyclic Compounds
  • Ligands