Preliminary in vivo evaluation of a novel 99mTc-labeled HYNIC-cys-annexin A5 as an apoptosis imaging agent

Bioorg Med Chem Lett. 2008 Jul 1;18(13):3794-8. doi: 10.1016/j.bmcl.2008.05.044. Epub 2008 May 16.

Abstract

A novel cys-annexin A5 with a single cysteine-residue at its concave side has been developed by site-directed mutagenesis to allow conjugation through thiol-chemistry without affecting its apoptotic cell binding properties and was derivatized with HYNIC in a 1:1 stoichiometry. Similar to that of the 1st generation 99mTc-HYNIC-annexin A5, the novel 99mTc-HYNIC-cys-annexin A5 derivative shows in normal mice mainly renal and, to a lesser extent, hepatobiliary excretion. In murine models of hepatic apoptosis there was 257% increase in hepatic uptake of 99mTc-HYNIC-cys-annexin A5 as compared to normal mice. Using the novel tracer agent, acute reperfused myocardial infarction in rabbits was unequivocally delineated at 7h post-injection by muSPECT. The results indicate that the novel 99mTc-HYNIC-cys-annexin A5 shows similar apoptosis avidity as the 1st generation 99mTc-HYNIC-annexin A5.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Annexin A5 / chemistry*
  • Annexin A5 / pharmacology
  • Apoptosis*
  • Chemistry, Pharmaceutical / methods
  • Cysteine / analogs & derivatives*
  • Cysteine / chemistry
  • Cysteine / pharmacology
  • Drug Design
  • Liver / metabolism
  • Mice
  • Models, Chemical
  • Myocardial Infarction / metabolism
  • Organotechnetium Compounds / pharmacology*
  • Rabbits
  • Sulfhydryl Compounds / chemistry
  • Tomography, Emission-Computed, Single-Photon / methods

Substances

  • Annexin A5
  • Organotechnetium Compounds
  • Sulfhydryl Compounds
  • technetium 99m cysteine
  • technetium Tc 99m HYNIC annexin V
  • Cysteine