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Distribution of 16alpha-[18F]fluoro-estradiol-3,17beta-disulfamate (FESDS) in rats, tumour-bearing mice and piglets

Brust, P.; Rodig, H.; Römer, J.; Kasch, H.; Bergmann, R.; Füchtner, F.; Zips, D.; Baumann, M.; Steinbach, J.; Johannsen, B.

Based on a high affinity to the enzyme estrone sulfatase (ES) 16alpha-[18F]fluoroestradiol-3,17beta-disulfamate ([18F]FESDS) has been suggested as a potential PET tracer for imaging steroid-dependent breast tumours. The distribution of [18F]FESDS was studied in rats, tumour-bearing nude mice and piglets. In all species evidence for tracer binding to a second target, the enzyme carbonic anhydrase (CA), was obtained. ES and CA inhibitors significantly reduced the radiotracer uptake in various organs but not in tumours. It is concluded that [18F]FESDS binds to ES and CA in vivo but this binding is not strong enough to allow tumour imaging with positron emission tomography (PET)..

Keywords: estradiol; disulfamate; estrone sulfatase; carbonic anhydrase; positron emission tomography; tumour

  • Applied Radiation and Isotopes 57 (2002) 687-695

Permalink: https://www.hzdr.de/publications/Publ-4057
Publ.-Id: 4057