Enzyme-Activated Gd3+ Magnetic Resonance Imaging Contrast Agents with a Prominent Receptor-Induced Magnetization Enhancement

Clinically relevant relaxivity enhancement of a magnetic resonance imaging (MRI) contrast agent has been achieved by using prodrug Gd3+ complexes (see picture, DTPA=diethylenetriaminepentaaceto). Enzymatic cleavage of lysine residues from the prodrug exposes a group that has a high affinity to human...

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Bibliographic Details
Published in:Angewandte Chemie International Edition 2001-08, Vol.40 (15), p.2903-2906
Main Authors: Nivorozhkin, Alexander L., Kolodziej, Andrew F., Caravan, Peter, Greenfield, Matthew T., Lauffer, Randall B., McMurry, Thomas J.
Format: Article
Language:English
Subjects:
chelates
inhibitors
lanthanides
MRI
peptides
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Summary:Clinically relevant relaxivity enhancement of a magnetic resonance imaging (MRI) contrast agent has been achieved by using prodrug Gd3+ complexes (see picture, DTPA=diethylenetriaminepentaaceto). Enzymatic cleavage of lysine residues from the prodrug exposes a group that has a high affinity to human serum albumin and promotes enhanced relaxivity, thus enabling the detection of targets at submicromolar concentrations.
ISSN:1433-7851
1521-3773
DOI:10.1002/1521-3773(20010803)40:15<2903::AID-ANIE2903>3.0.CO;2-N