Synthesis and Relaxometric Characterization of a MRI Gd-Based Probe Responsive to Glutamic Acid Decarboxylase Enzymatic Activity
| Autor: | Markus Aswendt, Silvio Aime, Eliana Gianolio, Roberta Napolitano, Giorgio Pariani, Franco Fedeli, Zsolt Baranyai |
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| Rok vydání: | 2013 |
| Předmět: |
Magnetic Resonance Spectroscopy
Static Electricity Glutamate decarboxylase Contrast Media Gadolinium Endogeny Chemistry Techniques Synthetic 010402 general chemistry 01 natural sciences In vivo Drug Discovery medicine Neurons chemistry.chemical_classification biology medicine.diagnostic_test Glutamate Decarboxylase 010405 organic chemistry Magnetic resonance imaging Magnetic Resonance Imaging In vitro Enzyme assay 0104 chemical sciences Enzyme Biochemistry chemistry Molecular Probes biology.protein Molecular Medicine Macromolecule |
| Zdroj: | Journal of Medicinal Chemistry; Vol 56 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm301831f |
| Popis: | Novel contrast agent based systems, which selectively visualize specific cells, e.g., neurons in the brain, would be of substantial importance for the fast developing field of molecular magnetic resonance imaging (MRI). We report here the synthesis and in vitro validation of a Gd(III)-based contrast agent designed to act as an MRI responsive probe for imaging the activity of the enzyme glutamic acid decarboxylase (GAD) present in neurons. Upon the action of the enzyme, the Gd(III) complex increases its hydration sphere and takes on a residual positive charge that promotes its binding to endogenous macromolecules. Both effects contribute in a synergic way to generate a marked relaxation enhancement, which directly reports enzyme activity and will allow activity detection of GAD positive cells in vitro and in vivo selectively. |
| Databáze: | OpenAIRE |
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