Synthesis and evaluation of a 18F-labelled recombinant annexin-V derivative, for identification and quantification of apoptotic cells with PET.
In this report, we describe the synthesis of 4-[18F]-fluorobenzoyl-annexin V (4-[18F]FBA). In a four-step procedure, 4-[18F]FBA was synthesised with a microcomputer controlled, automated module within 90min. The radiochemical yield was in the range of 15-20% (corrected for decay) with a specific activity of more than 35GBq/micromol. The specific binding was confirmed by studies of 4-[18F]FBA with phosphatidylserine-containing liposomes. The biological activity of 4-[18F]FBA was verified by measuring its binding to Jurkat T-cell lymphoblasts after induction of apoptosis as compared to control cells without apoptosis. 4-[18F]FBA seems to be a suited tracer to measure apoptotic activity in vivo.
Zijlstra
S
S
Herz- und Diabeteszentrum Nordrhein-Westfalen, Universitätsklinik der Ruhr-Universität, Bochum, Bad Oeynhausen, Germany. szijlstra@hdz.nrw.de
Gunawan
J
J
Burchert
W
W
D017304:Annexin A5 / Q000737:chemistry / Q000378:metabolism; D017209:Apoptosis; D002452:Cell Count; D005462:Fluorine Radioisotopes; D006801:Humans; D019169:Jurkat Cells; D008081:Liposomes / Q000378:metabolism; D010718:Phosphatidylserines / Q000378:metabolism; D011485:Protein Binding; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D011994:Recombinant Proteins / Q000737:chemistry / Q000378:metabolism; D014055:Tomography, Emission-Computed / Q000379:methods*
D017304:Annexin A5; D005462:Fluorine Radioisotopes; D008081:Liposomes; D010718:Phosphatidylserines; D019275:Radiopharmaceuticals; D011994:Recombinant Proteins