Closo-dodecaborate(2-) as a linker for iodination of macromolecules: Aspects on conjugation chemistry and biodistribution

Closo-dodecaborate(2-) as a linker for iodination of macromolecules : Aspects on conjugation chemistry and biodistribution

Tolmachev, Vladimir (author): Uppsala universitet,Institutionen för onkologi, radiologi och klinisk immunologi,BMS

Koziorowski, Jacek (author): Uppsala universitet,Institutionen för onkologi, radiologi och klinisk immunologi,BMS

Sivaev, Igor (author): Uppsala universitet,Institutionen för onkologi, radiologi och klinisk immunologi,BMS

Lundqvist, Hans (author): Uppsala universitet,Institutionen för onkologi, radiologi och klinisk immunologi,BMS

Carlsson, Jörgen (author): Uppsala universitet,Institutionen för onkologi, radiologi och klinisk immunologi,BMS

Orlova, Anna (author): Uppsala universitet,Institutionen för onkologi, radiologi och klinisk immunologi,BMS

Gedda, Lars (author): Uppsala universitet,Institutionen för onkologi, radiologi och klinisk immunologi,BMS

Olsson, Pär (author): Uppsala universitet,Institutionen för onkologi, radiologi och klinisk immunologi,BMS

Sjöberg, Stefan (author)

Sundin, Anders (author): Uppsala universitet,Institutionen för onkologi, radiologi och klinisk immunologi,BMS

(creator_code:org_t)

1999-04-08
1999
English.
In: Bioconjugate chemistry. - : American Chemical Society (ACS). - 1043-1802 .- 1520-4812. ; 10:3, s. 338-45

Related links:: https://urn.kb.se/re...; show more...; https://doi.org/10.1...; show less...

Abstract Subject headings

Boron-containing compounds like closo-dodecaborate(2-) are in theory suitable for radioactive labeling with halogens. The boron-halogen bond is stronger than carbon-halogen bond and is not likely to be recognized by deiodinating enzymes in vivo. Peptides and proteins may be conjugated with various closo-dodecaborate(2-)-containing ligands, and thereafter, the conjugate can be iodinated. Since closo-dodecaborate(2-) is more avidly iodinated than tyrosine in moderately acidic media, such conjugates may be directly labeled on the boron part with radioisotopes of iodine using the standard Chloramine-T procedure. Mercapto-undecahydro-closo-dodecaborate(2-) (BSH) was reacted with the double bond of allyldextran to form a boronated dextran compound of the molecular size of about 70 kDa. This compound, in the text denoted as Dx-BS, and cesium dodecahydro-closo-dodecaborate(2-) were labeled using iodine-125. The two compounds were administered to rats in order to study their in vivo stability. The results indicate that iodinated Dx-BS is stable for about 20 h in vivo. The degradation rate, as indicated by thyroid uptake, was found low. [125I]Iodo-closo-dodecaborate(2-), which is a possible degradation product of [125I]Dx-BS-I, was rapidly excreted in urine without significant accumulation in any organ.

By the author/editor: Tolmachev, Vladi ...; Koziorowski, Jac ...; Sivaev, Igor; Lundqvist, Hans; Carlsson, Jörgen; Orlova, Anna; show more...; Gedda, Lars; Olsson, Pär; Sjöberg, Stefan; Sundin, Anders; show less...

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