Literature DB >> 9468020

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

C F Foulon1, K L Alston, M R Zalutsky.   

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.

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Year:  1998        PMID： 9468020     DOI： 10.1016/s0969-8051(97)00166-2

Source DB:  PubMed          Journal:  Nucl Med Biol        ISSN： 0969-8051            Impact factor:   2.408


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