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

Abstract:

:New methodologies for site-specifically radiolabeling proteins with (18)F 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 acid ligase (LplA) to conjugate [(18)F]-fluorooctanoic acid to an antibody fragment bearing the peptide substrate of LplA. The mild conditions of the reaction preserve antibody immunoreactivity, and the efficiency of LplA allows for >90% yield even with very small amounts of peptidic precursor (1-10 nmol). These features are advantageous compared to the current gold standard in the field. Moreover, the methodology introduces a new application for an important tool in chemical biology.

journal_name

ACS Chem Biol

journal_title

ACS chemical biology

authors

Drake CR,Sevillano N,Truillet C,Craik CS,VanBrocklin HF,Evans MJ

doi

10.1021/acschembio.6b00172

subject

Has Abstract

pub_date

2016-06-17 00:00:00

pages

1587-94

issue

6

eissn

1554-8929

issn

1554-8937

journal_volume

11

pub_type

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