Astatine-211-labeled biotin conjugates resistant to biotinidase for use in pretargeted radioimmunotherapy.
Journal Article
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.
Full Text
Duke Authors
Cited Authors
- Foulon, CF; Alston, KL; Zalutsky, MR
Published Date
- February 1998
Published In
Volume / Issue
- 25 / 2
Start / End Page
- 81 - 88
PubMed ID
- 9468020
Pubmed Central ID
- 9468020
International Standard Serial Number (ISSN)
- 0969-8051
Digital Object Identifier (DOI)
- 10.1016/s0969-8051(97)00166-2
Language
- eng
Conference Location
- United States