Work

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

Year: 2016

Type: article

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 [18F]DCFPyL, αvβ3 integrin receptors targeting peptide [18F]c(RGDfK) and [18F]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.

Source: Journal of Labelled Compounds and Radiopharmaceuticals

DOI: 10.1002/jlcr.3487

Authors: Falguni Basuli, Xiang Zhang, Carolyn C. Woodroofe, Elaine M. Jagoda, Peter L. Choyke, Rolf E. Swenson

Institutions: National Institutes of Health, National Heart, Lung, and Blood Institute, National Cancer Institute

Language: English

Topic: Radiopharmaceutical Chemistry and Applications

Subfield: Radiology, Nuclear Medicine and Imaging

Field: Medicine

Domain: Health Sciences

Open Access status: green

Funders: National Institutes of Health, National Cancer Institute

Awards: G386607036, G4705346009, G5888954722