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Closo ‐dodecaborate (2‐) anion as a potential prosthetic group for attachment of astatine to proteins. Aspects of the labelling chemistry with chloramine‐T
Author(s) -
Orlova Anna,
Lebeda Ondrej,
Tolmachev Vladimir,
Sjöberg Stefan,
Carlsson Jörgen,
Lundqvist Hans
Publication year - 2000
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/(sici)1099-1344(20000315)43:3<251::aid-jlcr311>3.0.co;2-z
Subject(s) - chemistry , labelling , chloramine t , yield (engineering) , chloramine , reagent , radiochemistry , radiolysis , ion , combinatorial chemistry , biochemistry , organic chemistry , chlorine , aqueous solution , metallurgy , materials science
Closo ‐dodecarborate (2−) was proposed as a prosthetic group for direct labelling of proteins with 211 At for radionuclide therapy. Astatination of closo ‐dodecarborate (2−) anion using Chloramine‐T was studied, and the influence of pH, reaction time, amount of substrate and oxidant was determined. A maximum labelling yield of 55–75% was found in the pH range 7–8. A spontaneous astatination of closo ‐dodecarborate (2−) in the absence of Chloramine‐T was also found, presumably due to generation of oxidising products from water radiolysis. Our results indicate that derivatives of closo ‐dodecarborate (2−) anion may be used as prosthetic groups for direct labelling of proteins. Copyright © 2000 John Wiley & Sons, Ltd.