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Novel Fe 3+ ‐Based 1 H MRI β ‐Galactosidase Reporter Molecules

Novel Fe 3+ ‐Based 1 H MRI β ‐Galactosidase Reporter Molecules There is increasing interest in the development of reporter agents to reveal enzyme activity in vivo using imaging in small animals. We have previously demonstrated the feasibility of detecting lacZ gene activity using the commercially available 3,4‐cyclohexenoesculetin‐β‐D‐galactopyranoside (S‐Gal) as a 1H MRI reporter. Specifically, β‐galactosidase (β‐gal) releases the aglycone, which forms a magnetic resonance contrast‐inducing paramagnetic precipitate in the presence of Fe3+. Contrast was primarily T2‐weighted signal loss, but T1 effects were also observed. Since T1‐contrast generally provides signal enhancement as opposed to loss, it appeared attractive to explore whether analogues could be generated with enhanced characteristics. We now report the design and synthesis of novel analogues together with characterization of 1H MRI contrast based on both T1 and T2 response to β‐gal activity in vitro for the lead agent. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png ChemPlusChem Wiley

Novel Fe 3+ ‐Based 1 H MRI β ‐Galactosidase Reporter Molecules

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References (60)

Publisher
Wiley
Copyright
Copyright © 2012 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinheim
ISSN
2192-6506
eISSN
2192-6506
DOI
10.1002/cplu.201100072
Publisher site
See Article on Publisher Site

Abstract

There is increasing interest in the development of reporter agents to reveal enzyme activity in vivo using imaging in small animals. We have previously demonstrated the feasibility of detecting lacZ gene activity using the commercially available 3,4‐cyclohexenoesculetin‐β‐D‐galactopyranoside (S‐Gal) as a 1H MRI reporter. Specifically, β‐galactosidase (β‐gal) releases the aglycone, which forms a magnetic resonance contrast‐inducing paramagnetic precipitate in the presence of Fe3+. Contrast was primarily T2‐weighted signal loss, but T1 effects were also observed. Since T1‐contrast generally provides signal enhancement as opposed to loss, it appeared attractive to explore whether analogues could be generated with enhanced characteristics. We now report the design and synthesis of novel analogues together with characterization of 1H MRI contrast based on both T1 and T2 response to β‐gal activity in vitro for the lead agent.

Journal

ChemPlusChemWiley

Published: May 1, 2012

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