دورية أكاديمية

Self‐Immolative Activation of β‐Galactosidase‐Responsive Probes for In Vivo MR Imaging in Mouse Models.

التفاصيل البيبلوغرافية
العنوان: Self‐Immolative Activation of β‐Galactosidase‐Responsive Probes for In Vivo MR Imaging in Mouse Models.
المؤلفون: Lilley, Laura M., Kamper, Sarah, Caldwell, Michael, Chia, Zer Keen, Ballweg, David, Vistain, Luke, Krimmel, Jeffrey, Mills, Teresa Anne, MacRenaris, Keith, Lee, Paul, Waters, Emily Alexandria, Meade, Thomas J.
المصدر: Angewandte Chemie International Edition; 1/2/2020, Vol. 59 Issue 1, p388-394, 7p
مصطلحات موضوعية: GALACTOSIDASES, MAGNETIC resonance imaging, STRUCTURAL isomers, MICE, CARBOXYLATES, STRUCTURAL design, MAGNETIC resonance
مستخلص: Our lab has developed a new series of self‐immolative MR agents for the rapid detection of enzyme activity in mouse models expressing β‐galactosidase (β‐gal). We investigated two molecular architectures to create agents that detect β‐gal activity by modulating the coordination of water to GdIII. The first is an intermolecular approach, wherein we designed several structural isomers to maximize coordination of endogenous carbonate ions. The second involves an intramolecular mechanism for q modulation. We incorporated a pendant coordinating carboxylate ligand with a 2, 4, 6, or 8 carbon linker to saturate ligand coordination to the GdIII ion. This renders the agent ineffective. We show that one agent in particular (6‐C pendant carboxylate) is an extremely effective MR reporter for the detection of enzyme activity in a mouse model expressing β‐gal. [ABSTRACT FROM AUTHOR]
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قاعدة البيانات: Complementary Index
الوصف
تدمد:14337851
DOI:10.1002/anie.201909933