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Org Biomol Chem. 2012 Sep 7;10(33):6724-31. doi: 10.1039/c2ob25744k. Epub 2012 Jul 24.

Fluorine- and rhenium-containing geldanamycin derivatives as leads for the development of molecular probes for imaging Hsp90.

Author information

1
Department of Oncology, Faculty of Medicine and Dentistry, University of Alberta, Edmonton, Canada. wuest@ualberta.ca

Abstract

Heat shock protein 90 (Hsp90) is an ATP-dependent molecular chaperone responsible for protein quality control in cells. Hsp90 has been shown to be overexpressed in many human cancers. This has prompted extensive research on Hsp90 inhibitors as novel anticancer agents and, more recently, the development of molecular probes for imaging Hsp90 expression in vivo. This work describes the development of various fluorine-containing and rhenium-containing geldanamycin derivatives as leads for the development of corresponding (18)F-labeled and (99m)Tc-labeled PET and SPECT probes for molecular imaging of Hsp90 expression. All compounds were evaluated in an in vitro ATPase activity assay using Hsp90 isoform Hsp82p. Fluorobenzoylated geldanamycin derivative 5 displayed comparable inhibitory potency like parent compound geldanamycin.

PMID:
22825378
DOI:
10.1039/c2ob25744k
[Indexed for MEDLINE]

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