title: Functional comparison of annexin V analogues labeled indirectly and directly with iodine-124.
abstract: We are interested in imaging cell death in vivo using annexin V radiolabeled with (124)I. In this study, [(124)I]4IB-annexin V and [(124)I]4IB-ovalbumin were made using [(124)I]N-hydroxysuccinimidyl-4-iodobenzoate prepared by iododestannylation of N-hydroxysuccinimidyl-4-(tributylstannyl)benzoate. [(124)I]4IB-annexin V binds to phosphatidylserine-coated microtiter plates and apoptotic Jurkat cells and accumulates in hepatic apoptotic lesions in mice treated with anti-Fas antibody, while [(124)I]4IB-ovalbumin does not. In comparison with (124)I-annexin V, [(124)I]4IB-annexin V has a higher rate of binding to phosphatidylserine in vitro, a higher kidney and urine uptake, a lower thyroid and stomach content uptake, greater plasma stability and a lower rate of plasma clearance. Binding of radioactivity to apoptotic cells relative to normal cells in vitro and in vivo appears to be lower for [(124)I]4IB-annexin V than for (124)I-annexin V.
authors.affiliation: CRUK/UMIST Department of Radiochemical Targeting and Imaging, Paterson Institute for Cancer Research, M20 4BX Manchester, UK. bdekker@picr.man.ac.uk
authors.forename: Bronwen
authors.initials: B
authors.lastname: Dekker
authors.forename: Heather
authors.initials: H
authors.lastname: Keen
authors.forename: David
authors.initials: D
authors.lastname: Shaw
authors.forename: Lynn
authors.initials: L
authors.lastname: Disley
authors.forename: David
authors.initials: D
authors.lastname: Hastings
authors.forename: John
authors.initials: J
authors.lastname: Hadfield
authors.forename: Andrew
authors.initials: A
authors.lastname: Reader
authors.forename: Donald
authors.initials: D
authors.lastname: Allan
authors.forename: Peter
authors.initials: P
authors.lastname: Julyan
authors.forename: Alastair
authors.initials: A
authors.lastname: Watson
authors.forename: Jamal
authors.initials: J
authors.lastname: Zweit
mesh_terms: D000818:Animals; D017304:Annexin A5 / Q000031:analogs & derivatives / Q000493:pharmacokinetics*; D017209:Apoptosis / Q000502:physiology*; D006801:Humans; D007457:Iodine Radioisotopes / Q000493:pharmacokinetics; D019169:Jurkat Cells; D008657:Metabolic Clearance Rate; D051379:Mice; D009928:Organ Specificity; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics; D014018:Tissue Distribution
chemical_list: D017304:Annexin A5; D007457:Iodine Radioisotopes; D019275:Radiopharmaceuticals