TY  - JOUR
AU  - Klika, Karel
AU  - Da Pieve, Chiara
AU  - Kopka, Klaus
AU  - Smith, Graham
AU  - Makarem, Ata
TI  - Synthesis and application of a thiol-reactive HBED-type chelator for development of easy-to-produce Ga-radiopharmaceutical kits and imaging probes.
JO  - Organic & biomolecular chemistry
VL  - 19
IS  - 8
SN  - 1477-0539
CY  - Cambridge
PB  - Royal Society of Chemistry
M1  - DKFZ-2021-00277
SP  - 1722-1726
PY  - 2021
N1  - #EA:A390#LA:E030# /Division of Radiopharmaceutical Chemistry,2021 Mar 4;19(8):1722-1726
AB  - In radiopharmaceutical syntheses, maleimide is commonly used for linking thiol-bearing bioactive molecules to metal-complexing ligands (chelators). However, due to instability of the resulting linkage, phenyloxadiazolyl methylsulfone (PODS) was developed as an alternative to maleimide. This coupling strategy has never been attempted with HBED which is a powerful chelator for gallium-radiolabeling especially at ambient temperature. Here we present HBED-CC-PODS as a bifunctional chelator scaffold for the site-selective conjugation of thiol-bearing vectors and [68Ga]Ga-radiolabeling.
LB  - PUB:(DE-HGF)16
C6  - pmid:33527964
DO  - DOI:10.1039/D0OB02513E
UR  - https://inrepo02.dkfz.de/record/167329
ER  -