Anion as a Prosthetic Group for Labelling Proteins with Astatine

Anna Orlova1,2 , Ondrej Lebeda3, Vladimir Tolmachev1, 

Stefan Sjoberg2, Jorgen Carlsson1 and Hans Lundqvist1 

1 UNIT OF BIOMEDICAL RADIATION SCIENCES, UPPSALA UNIVERSITY, RUDBECK LABORATORY, SE-751 85 UPPSALA, SWEDEN 

3 NUCLEAR PHYSICS INSTITUTE, CZ-250 68 REZ NEAR PRAGUE, CZECH REPUBLIC 

Astatine-211 is a promising radionuclide for systemic therapy1 3 due to its decay properties with a half-life of 7.2 hours and an effective emission of one a-particle per decay. However, the weakness of the astatine-protein bond formed after direct astatination1 4 has so far limited its clinical use. To overcome these problems indirect labelling methods have been tried such as the use of ALsuccinimidyl-(trialkylstannyl) benzoate as an intermediate for the astatination of antibodies using conjugation procedures.5 8 

Anna Orlova Ondrej Lebeda, Vladimir Tolmachev  

Stefan Sjdberg, Jbrgen Carlsson and Hans Lundqvist  

The aim of this paper is to study the influence of different reaction parameters on the labelling yield in the astatination of and to evaluate the merits of this anion as a possible prosthetic group for astatination of protein. 

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Orlova, A., Lebeda, O., Tohnachev, V. et al. 2000a. C/o o-dodecaborate (2-) anion as a prosthetic group for labelling proteins with astatine. Spec. Publ. - R. Soc. Chem., 253, 144—7. 

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