Abstract
A novel annexin A5 derivative (cys-annexin A5) with a single cysteine residue at its C-terminal has been developed and successfully labeled in high labeling yield with 99mTc by a ligand exchange reaction. Like the 1st generation 99mTc-HYNIC-annexin A5, the novel 99mTc-cys-annexin A5 derivative shows in normal mice mainly renal and, to a lesser extent, hepatobiliary excretion. In rat models of hepatic apoptosis there was 283% increase in hepatic uptake of 99mTc-cys-annexin A5 as compared to normal mice. The results indicate that the novel 99mTc-cys-annexin A5 is a potential apoptosis imaging agent.
Highlights
Apoptosis or programmed cell death (PCD) plays an important role in physiology and in pathology [1,2]
Positron emission tomography (PET) with its higher sensitivity, better spatial resolution and the ability to better quantify the radiopharmaceutical uptake is superior to single photon emmission computed tomography (SPECT) imaging, and the low uptake of 18F-annexin A5 in the liver, spleen and kidney might represent an advantage over 99mTc-annexin
A5 [30], production of 18F-annexin A5 depends on the availability of an expensive on-site cyclotron for the production of fluorine-18 (t1/2 = 109.8 min). 68Ga has suitable physical properties for PET imaging
Summary
Apoptosis or programmed cell death (PCD) plays an important role in physiology and in pathology [1,2]. The anticoagulant activity is based on the high-affinity for PS These characteristics make a derivative of annexin A5 a suitable candidate for imaging of apoptosis. Professor Hua Zichun and his colleagues have developed a novel annexin A5 derivative (cys-annexin A5) with a single cysteine residue at C-terminal [25]. Their findings show that the the detection signal of fluorescein isothiocyanate (FITC)-cys-annexin A5 is greater than that of FITC-wild-type annexin A5. In mice tracer uptake was studied by ex vivo biodistribution experiments and the results were compared to those of the 1st-generation 99mTc-HYNIC-annexin A5. Apoptosis was confirmed in situ on liver slices using the terminal deoxynucleotidyl transferase (TdT) dUTP nick endlabeling (TUNEL) assay
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