Preparation of F-18 labeled annexin V: A potential PET radiopharmaceutical for imaging cell death

J. Toretsky, A. Levenson, I. N. Weinberg, J. F. Tait, A. Üren, Ronnie Mease

Research output: Contribution to journalArticle

Abstract

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-[ 18F]fluorobenzoate, [18F]SFB. The decay corrected radiochemical yield of F-18 labeled annexin V from 18F 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 [18F] labeled annexin V can be readily prepared by the conjugation of annexin V with [ 18F]SFB and that the positron-emitting compound is biologically active in detecting apoptosis.

Original languageEnglish (US)
Pages (from-to)747-752
Number of pages6
JournalNuclear Medicine and Biology
Volume31
Issue number6
DOIs
StatePublished - Aug 2004
Externally publishedYes

Fingerprint

Radiopharmaceuticals
Annexin A5
Cell Death
Drug Therapy
Neoplasms
Electrons
Phosphatidylserines
Etoposide
Fluorides
Proteins
Therapeutics
Apoptosis
Growth
N-succinimidyl-4-fluorobenzoate

Keywords

  • Annexin V
  • Apoptosis
  • Ewing's Sarcoma
  • PET imaging

ASJC Scopus subject areas

  • Cancer Research
  • Molecular Medicine
  • Radiology Nuclear Medicine and imaging

Cite this

Preparation of F-18 labeled annexin V : A potential PET radiopharmaceutical for imaging cell death. / Toretsky, J.; Levenson, A.; Weinberg, I. N.; Tait, J. F.; Üren, A.; Mease, Ronnie.

In: Nuclear Medicine and Biology, Vol. 31, No. 6, 08.2004, p. 747-752.

Research output: Contribution to journalArticle

Toretsky, J. ; Levenson, A. ; Weinberg, I. N. ; Tait, J. F. ; Üren, A. ; Mease, Ronnie. / Preparation of F-18 labeled annexin V : A potential PET radiopharmaceutical for imaging cell death. In: Nuclear Medicine and Biology. 2004 ; Vol. 31, No. 6. pp. 747-752.
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