Journal
NUCLEAR MEDICINE AND BIOLOGY
Volume 31, Issue 6, Pages 747-752Publisher
ELSEVIER SCIENCE INC
DOI: 10.1016/j.nucmedbio.2004.02.007
Keywords
annexin V; apoptosis; PET imaging; Ewing's sarcoma
Funding
- NCI NIH HHS [R01 CA088004, R01-CA88004, 1P30-CA-51008, R01 CA088004-08, R41-CA93105] Funding Source: Medline
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The clinical response to antitumor therapy is measured using imaging, such as CT or MRI, 6-12 weeks following chemotherapy treatment. The images at that time reflect both tumor cell death and new growth. Therefore, the amount of tumor cell death caused by chemotherapy cannot be efficiently quantified with current imaging modalities. A quantitative measurement of tumor cell death immediately following chemotherapy is needed to help validate both new agents and to optimize administration of existing therapies. Annexin V is a 36kD protein that binds to exposed phosphatidylserine (PS) on dying cells. In order to synthesize a probe that can detect cell death in vivo, the positron emitter F-18 was conjugated to annexin V via the compound N- succinimidyl-4-[F-18]fluorobenzoate, [F-18]SFB. The decay corrected radiochemical yield of F-18 labeled annexin V from F-18 fluoride was 17.6+/-5.6 % (n=4) in three hours. The stepwise radiochemical yield of the conjugation step with annexin V was as high as 70% when a protein concentration of 5 mg/ml was used. Cancer cells treated with the chemotherapeutic agent, etoposide, showed an 88% increase in the binding of F-18 labeled annexin V compared to untreated cells. We conclude that [F-18] labeled annexin V can be readily prepared by the conjugation of annexin V with [F-18]SFB and that the positron-emitting compound is biologically active in detecting apoptosis. (C) 2004 Elsevier Inc. All rights reserved.
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