960化工网
A two-step fluorinase enzyme mediated 18F labelling of an RGD peptide for positron emission tomography†
S. Thompson,M. Onega,S. Ashworth,I. N. Fleming,J. Passchier,D. O'Hagan
Chemical Communications Pub Date : 07/17/2015 00:00:00 , DOI:10.1039/C5CC05013H
Abstract

A two-step radiolabelling protocol of a cancer relevant cRGD peptide is described where the fluorinase enzyme is used to catalyse a transhalogenation reaction to generate [18F]-5′-fluoro-5′-deoxy-2-ethynyladenosine, [18F]FDEA, followed by a ‘click’ reaction to an azide tethered cRGD peptide. This protocol offers efficient radiolabelling of a biologically relevant peptide construct in water at pH 7.8, 37 °C in 2 hours, which was metabolically stable in rats and retained high affinity for αVβ3 integrin.

Graphical abstract: A two-step fluorinase enzyme mediated 18F labelling of an RGD peptide for positron emission tomography
平台客服
平台客服
平台在线客服