Journal Article

DKFZ-2021-00277

http://join2-wiki.gsi.de/foswiki/pub/Main/Artwork/join2_logo100x88.png Synthesis and application of a thiol-reactive HBED-type chelator for development of easy-to-produce Ga-radiopharmaceutical kits and imaging probes.

Klika, K. (First author)DKFZ* ; Da Pieve, C. ; Kopka, K. ; Smith, G. ; Makarem, A. (Last author)DKFZ*

2021
Royal Society of Chemistry Cambridge

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Please use a persistent id in citations: doi:10.1039/D0OB02513E

Abstract: 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.

Note: #EA:A390#LA:E030# /Division of Radiopharmaceutical Chemistry,2021 Mar 4;19(8):1722-1726

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Contributing Institute(s):

1. AG Wirkstoffforschung (A390)
2. Radiopharmazeutische Chemie (E030)

Research Program(s):

1. 315 - Bildgebung und Radioonkologie (POF4-315) (POF4-315)

Appears in the scientific report 2021

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Database coverage:
; Allianz-Lizenz / DFG ; Chemical Reactions ; Clarivate Analytics Master Journal List ; Current Contents - Life Sciences ; Current Contents - Physical, Chemical and Earth Sciences ; Essential Science Indicators ; IF < 5 ; Index Chemicus ; JCR ; National-Konsortium ; Nationallizenz ; SCOPUS ; Science Citation Index Expanded ; Web of Science Core Collection

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