Issue 11, 2010

A paramagnetic chemical exchange-based MRI probe metabolized by cathepsin D: design, synthesis and cellular uptake studies

Abstract

Overexpression of the aspartyl protease cathepsin D is associated with certain cancers and Alzheimer’s disease; thus, it is a potentially useful imaging biomarker for disease. A dual fluorescence/MRI probe for the potential detection of localized cathepsin D activity has been synthesized. The probe design includes both MRI and optical reporter groups connected to a cell penetrating peptide by a cathepsin D cleavable sequence. This design results in the selective intracellular deposition (determined fluorimetrically) of the MRI and optical reporter groups in the presence of overexpressed cathepsin D. The probe also provided clearly detectable in vitro MRI contrast by the mechanism of paramagnetic chemical exchange effects (OPARACHEE).

Graphical abstract: A paramagnetic chemical exchange-based MRI probe metabolized by cathepsin D: design, synthesis and cellular uptake studies

Supplementary files

Article information

Article type
Paper
Submitted
22 Dec 2009
Accepted
09 Mar 2010
First published
26 Mar 2010

Org. Biomol. Chem., 2010,8, 2560-2566

A paramagnetic chemical exchange-based MRI probe metabolized by cathepsin D: design, synthesis and cellular uptake studies

M. Suchý, R. Ta, A. X. Li, F. Wojciechowski, S. H. Pasternak, R. Bartha and R. H. E. Hudson, Org. Biomol. Chem., 2010, 8, 2560 DOI: 10.1039/B926639A

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