Astatine-211-labeled biotin conjugates resistant to biotinidase for use in pretargeted radioimmunotherapy

Nucl Med Biol. 1998 Feb;25(2):81-8. doi: 10.1016/s0969-8051(97)00166-2.

Abstract

We report herein the preparation and biological evaluation of two radioastatinated biotin conjugates, (3-[211At]astatobenzoyl)norbiotinamide and ((5-[211At]astato-3-pyridinyl)carbonyl)norbiotinamide. Both conjugates were stable in the presence of human serum and cerebrospinal fluid as well as murine serum, indicating a resistance to degradation to biotinidase. The normal tissue clearance of (3-[211At]astatobenzoyl)norbiotinamide and ((5-[211At]astato-3-pyridinyl)carbonyl)norbiotinamide was rapid, as observed previously with their iodo analogues. Also reported are the first syntheses of N-succinimidyl 5-[211At]astato-3-pyridinecarboxylate and 3-[211At]astatoaniline, two reagents of potential utility for labeling proteins and peptides with 211At.

Publication types

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

MeSH terms

  • Amidohydrolases / cerebrospinal fluid
  • Amidohydrolases / chemistry*
  • Animals
  • Astatine*
  • Biotin / analogs & derivatives*
  • Biotin / cerebrospinal fluid
  • Biotin / chemical synthesis
  • Biotin / chemistry*
  • Biotinidase
  • Humans
  • Mice
  • Mice, Inbred BALB C
  • Radioimmunotherapy*
  • Radioisotopes
  • Radiopharmaceuticals / cerebrospinal fluid
  • Radiopharmaceuticals / chemistry*
  • Streptavidin / chemistry
  • Tissue Distribution

Substances

  • ((5-astato-3-pyridinyl)carbonyl)norbiotinamide
  • (3-astatobenzoyl)norbiotinamide
  • Radioisotopes
  • Radiopharmaceuticals
  • Biotin
  • Streptavidin
  • Amidohydrolases
  • Biotinidase
  • Astatine