Site-Specific Radiofluorination of Biomolecules with 8-[18F]-Fluorooctanoic Acid Catalyzed by Lipoic Acid Ligase

被引:16
|
作者
Drake, Christopher R. [1 ]
Sevillano, Natalia [2 ]
Truillet, Charles [1 ]
Craik, Charles S. [2 ]
VanBrocklin, Henry F. [1 ]
Evans, Michael J. [1 ]
机构
[1] Univ Calif San Francisco, Dept Radiol & Biomed Imaging, Suite 350,185 Berry St, San Francisco, CA 94107 USA
[2] Univ Calif San Francisco, Dept Pharmaceut Chem, Genentech Hall,S-514,600 16th St, San Francisco, CA 94158 USA
关键词
ACTIVATOR RECEPTOR; LABELING PROTEINS; N-SUCCINIMIDYL; ANTIBODIES; PEPTIDES; STRATEGY; UPAR;
D O I
10.1021/acschembio.6b00172
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
New methodologies for site -specifically radio labeling proteins with F-18 are required to generate high quality radiotracerS for preclinical and clinical -applications with positron emission tomography. Herein, we report an approach by which we use lipoic a-cidligase (LplA) to conjugate [F-18]fluorooctanoic acid to an fragment bearing the peptide substrate of ITIA. The mild conditions 'of the reaction preserve antibodyimmunornactivity, and the efficiencyof LplA allows for >90% yield even with very small amounts of peptidic precursor (1-10 limo. These features advantageous compared to the current gold standard in the field: Moreover, the methodology introduces a new application for" an important "to-ol in chemical biology:
引用
收藏
页码:1587 / 1594
页数:8
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