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Gadopiclenol: A q = 2 Gadolinium-Based MRI Contrast Agent Combining High Stability and Efficacy.
Invest Radiol
October 2024
From the Research and Innovation Department, Guerbet, Roissy, France (I.M., M.-C.D.G., J.-F.M., A.D., Y.B., N.D., I.S., G.B., C.M., C.F., O.R., S.C.); General, Organic, and Biomedical Chemistry Unit, NMR and Molecular Imaging Laboratory, University of Mons, Mons, Belgium (C.H., S.L.); and Institute of Inorganic and Analytical Chemistry, University of Münster, Münster, Germany (C.K., T.J.M., U.K.).
Objectives: Gadopiclenol is a q = 2 pyclen gadolinium-based contrast agent (GBCA) recently approved by the Food and Drug Administration, European Medicines Agency, and other European countries. The aim of this report is to demonstrate its stability in multiple stressed in vitro conditions and in vivo, in rat kidney, while maintaining its higher relaxivity compared with conventional GBCAs on the market.
Materials And Methods: Both gadopiclenol and its chemical precursor Pi828-Gd were characterized and compared with q = 1 gadolinium (Gd) complexes.
Diazocines as Guests of Cucurbituril Macrocycles: Light-Responsive Binding and Supramolecular Catalysis of Thermal Isomerization.
J Am Chem Soc
December 2024
Laboratório Associado para a Química Verde (LAQV), Rede de Química e Tecnologia (REQUIMTE), Departamento de Química, Faculdade de Ciências e Tecnologia, Universidade NOVA de Lisboa, 2829-516 Caparica, Portugal.
The photoswitching of supramolecular host-guest complexes is the basis of numerous molecularly controlled macroscopic functions, such as sol-gel transition, photopharmacology, the active transport of ions or molecules, light-powered molecular machines, and much more. The most commonly used systems employ photoactive azobenzene guests and synthetic host molecules, which bind as the stable isomers and dissociate as the forms after exposure to UV light. We present a new, extraordinarily efficient cucurbit[7]uril (CB7)/diazocine host/guest complex with inverted stability that self-assembles under UV irradiation and dissociates in the dark.
View Article and Find Full Text PDFCell-Permeable Peptide Inhibitors of the p53-hDM2 Interaction via Foldamer Helix Mimicry and Bis-Thioether Stapling.
J Med Chem
December 2024
Univ. Bordeaux, CNRS, Bordeaux INP, CBMN, UMR 5248, IECB, F-33607 Pessac, France.
Combining helical foldamers with α-peptides can produce α-helix mimetics with a reduced peptide character and enhanced resistance to proteolysis. Previously, we engineered a hybrid peptide-oligourea sequence replicating the N-terminal α-helical domain of p53 to achieve high affinity binding to hDM2. Here, we further advance this strategy by combining the foldamer approach with side chain cross-linking to create more constrained cell-permeable inhibitors capable of effectively engaging the target within cells.
View Article and Find Full Text PDFMetal (M = Cr, Mo, W, Re) carbonyl complexes with porphyrin and carborane isocyanide ligands: light-induced oxidation and carbon oxide release for antitumor efficacy.
Biomater Sci
December 2024
A. N. Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, 28 Bld. 1 Vavilov Street, 119334 Moscow, Russian Federation.
The tetrapyrrolic macrocycle as a scaffold for various chemical modifications provides broad opportunities for the preparation of complex multifunctional conjugates suitable for binary antitumor therapies. Typically, illumination with monochromatic light triggers the photochemical generation of reactive oxygen species (ROS) (photodynamic effect). However, more therapeutically valuable effects can be achieved upon photoactivation of tetrapyrrole derivatives.
View Article and Find Full Text PDFThe Gadolinium Research and Education Committee (GREC) is a working group of the European Society for Magnetic Resonance in Medicine and Biology (ESMRMB), established in 2016. The aim of the committee is to monitor scientific evidence for a continuous quality and safety improvement of enhanced MRI using gadolinium-based contrast agents (GBCAs), and also assess potential alternatives. The scope of the present article is to describe the level of evidence concerning safety beyond the single patient (access to community and environmental impact), justification and optimization of the use of GBCAs beyond dosage (appropriateness and influence on clinical decision making), dose reduction with the use of AI (benefits and pitfalls), the advent of next-generation GBCAs (based on currently available data).
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