Fast Indirect Fluorine-18 Labeling of Protein/peptide Using the Useful 6-fluoronicotinic Acid-2,3,5,6-tetrafluorophenyl Prosthetic Group: A Method Comparable to Direct Fluorination

Overview

Journal J Labelled Comp Radiopharm

Specialties Nuclear Medicine
Pharmacology
Pharmacy
Radiology

Date 2016 Dec 20

PMID 27990672

Citations 18

Authors

Falguni Basuli

Xiang Zhang

Carolyn C Woodroofe

Elaine M Jagoda

Peter L Choyke

Rolf E Swenson

Affiliations

Soon will be listed here.

Abstract

Fluorine-18 labeling of biomolecules is mostly performed by an indirect labeling method using a prosthetic group. Fluorine-18 labeled 6-fluoronicotinic acid-2,3,5,6-tetrafluorophenyl ester is a useful prosthetic group to radiolabel a protein. Recently, we reported an improved preparation of this prosthetic group. To test the conjugation efficiency of the labeled ester prepared by this method, we have performed conjugation reactions with a peptide, a protein, and a small molecule. Prostate-specific membrane antigen targeting small molecule [ F]DCFPyL, αvβ3 integrin receptors targeting peptide [ F]c(RGDfK) and [ F]albumin were prepared in good radiochemical yields. The conjugation reactions were completed at 40°C to 50°C in 10 minutes. The overall radiochemical yield was 25% to 43% in 30 to 45 minutes.

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