Synthesis and physicochemical characterization of Gd-C4-thyroxin-DTPA, a potential MRI contrast agent. Evaluation of its affinity for human serum albumin by proton relaxometry, NMR diffusometry and electrospray mass spectrometry.
[en] Gd-C4-thyroxin-DTPA, a potential MRI contrast agent, was synthesized from Gd-DTPA and thyroxine, which interacts strongly with human serum albumin (HSA). It was characterized in water by its relaxometric properties and its stability versus zinc transmetallation. The affinity of the complex for HSA was studied by three different methods: proton relaxometry, NMR diffusometry, and electrospray mass spectrometry. From the results it appears that Gd-C4-thyroxin-DTPA exhibits a relatively high relaxivity (r1 = 9.01 s-1 mM-1 at 1.5T and 310 K), a good stability versus zinc transmetallation, and a strong interaction with HSA (Ka ~ 10000 M-1 with 2 binding sites). The kinetics of the exchange between the bound and the free form of the complex was evaluated by the NMR diffusometry technique. Competition experiments have allowed the assignment of the chelate's binding site on HSA.
Disciplines :
Radiology, nuclear medicine & imaging Chemistry
Author, co-author :
Henoumont, Céline ; Université de Mons > Faculté de Médecine et de Pharmacie > Chimie générale, organique et biomédicale
Vander Elst, Luce ; Université de Mons > Faculté de Médecine et de Pharmacie > Chimie générale, organique et biomédicale
Laurent, Sophie ; Université de Mons > Faculté de Médecine et de Pharmacie > Chimie générale, organique et biomédicale
Muller, Robert ; Université de Mons > Faculté de Médecine et de Pharmacie > Chimie générale, organique et biomédicale
Language :
English
Title :
Synthesis and physicochemical characterization of Gd-C4-thyroxin-DTPA, a potential MRI contrast agent. Evaluation of its affinity for human serum albumin by proton relaxometry, NMR diffusometry and electrospray mass spectrometry.
Publication date :
01 January 2010
Journal title :
Journal of Physical Chemistry B
ISSN :
1520-6106
Publisher :
American Chemical Society, United States - District of Columbia
Volume :
114
Issue :
10
Pages :
3689-3697
Peer reviewed :
Peer Reviewed verified by ORBi
Research unit :
M108 - Chimie générale, organique et biomédicale
Research institute :
R550 - Institut des Sciences et Technologies de la Santé R100 - Institut des Biosciences
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