Improved synthesis of [18F]FS-PTAD as a new tyrosine-specific prosthetic group for radiofluorination of biomolecules

被引：19

作者：

Al-Momani, Ehab ^{[1
]}

Israel, Ina ^{[1
]}

Buck, Andreas K. ^{[1
]}

Samnick, Samuel ^{[1
]}

机构：

[1] Univ Wurzburg, Dept Nucl Med, D-97080 Wurzburg, Germany

来源：

APPLIED RADIATION AND ISOTOPES | 2015年 / 104卷

关键词：

Prosthetic group; F-18]FS-PTAD; Radiofluorination; Ene-like reaction; Tyrosine conjugation; PET; PEPTIDES; AGENT; F-18; ACID; BIOCONJUGATION; RADIOSYNTHESIS; PROTEINS; TRACERS; GRADE;

D O I：

10.1016/j.apradiso.2015.06.021

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

A novel prosthetic group, 4-(p-([F-18]fluorosulfonyl)phenyl)-1,2,4-triazoline-3,5-dione ([F-18]FS-PTAD) for site-specific radiofluorination of tyrosine residue in small molecules is described. Coupling of [F-18]FS-PTAD with L-tyrosine, N-acetyl-L-tyrosine methyl amide and phenol as model compounds were achieved in buffered aqueous solution at room temperature, resulting in the corresponding fluorinated tyrosine and phenol derivatives. The total synthesis time including radiosynthesis, HPLC purification and formulation was less than 60 min (n=15) with >= 98% radio chemical purity. An initial in vitro evaluation of [F-18]FS-PTAD-tyrosine in glioma cell lines revealed moderate uptake. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：136 / 142

页数：7

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