Abstract In the pursuit of CuII-responsive MRI contrast agents with enhanced CuII affinity, we report the synthesis and characterization of two LnIII-DO3A-C3AmpicGH complexes (LnIII = GdIII, EuIII), featuring a tetradentate CuII-binding moiety, along with the corresponding mononuclear CuII-C3AmpicG…
Abstract α-N-Pyridylthiosemicarbazones (PTSC) are anticancer agents that can induce oxidative stress in cells, likely through interactions with metal ions. Redox-active Cu and Fe bind strongly to PTSC, forming complexes Cu-PTSC and Fe-PTSC2. These complexes have been proposed to directly catalyze…
Abstract The intricate interplay between brain iron homeostasis and pathological α-Synuclein (αSyn) in Parkinson's Disease (PD) is still unclear. αSyn is the primary protein involved in disease progression and promotes cytotoxicity by impairing dopamine synthesis, mitochondrial dysfunction and…
Abstract The failure of the therapeutic administration of superoxide dismutase (SOD) and catalase (CAT) enzymes to prevent oxidative stress has fostered the development of metal complexes that are capable of mimicking their activity. In the present work, two new pyridine azacyclophane ligands…
Abstract The cell plasma membrane acts as a semi-permeable barrier essential for cellular protection and function, posing a challenge for therapeutic molecule delivery. Conventional techniques for crossing this barrier, including biophysical and biochemical methods, often exhibit limitations such…
Abstract Overproduction of reactive oxygen species (ROS) is involved in several diseases. Copper can be an efficient catalysts for ROS generation, as it was suggested for Cu bound to aberrant sites. Determination of rates and type of ROS production in more complex biological media is challenging…
Abstract Alzheimer's disease (AD) is a complex neurodegenerative disorder characterized by progressive decline of cognitive functions, yet its underlying aetiology remains elusive. While amyloid-β (Aβ) and tau pathologies have been extensively studied, emerging evidence suggests that metal and…
Abstract Imaging extracellular Cu2+ in vivo is important due to its role in physiological and pathological processes. Magnetic resonance imaging is a promising modality for this purpose but developing contrast agents selective for Cu2+ over abundant Zn2+ ions remains a challenge. We synthesized and…
Abstract Selective chemical modifications of biomolecules are in high demand for the development and implementation of chemical biology strategies. Methods involving radicals have emerged as powerful options yet potentially generate side reactivities when involving harsh reaction conditions. We…
Abstract We report the design and synthesis of ratiometric 19F-ATCUN (Xxx-Zzz-His) peptide probes for the selective and reversible detection of Ni2⁺ and Cu2⁺ by 19F NMR spectroscopy. In contrast to fluorescence-based approaches, 19F NMR enables background-free detection in biological media, due to…
Abstract Promising results in preclinical diagnosis based on 89Zr-immunoPET have fostered the development of efficient chelators for this tetravalent metal. Leads in this area are octadentate ligands obtained by extension of the desferrioxamine B trihydroxamic acid DFO with a fourth bidentate…
Abstract Ru complexes are widely studied in photodynamic therapy. The type I mechanism of action is based on a photoinduced electron transfer from the complex to O2 and needs an electron donor to be catalytic. Little is known about electron donors among physiologically relevant compounds. Hence, we…
Abstract Cu(II) coordination complexes are emerging as promising anticancer agents due to their ability to induce oxidative stress through reactive oxygen species (ROS) generation. In this study, we synthesized and characterized two novel Cu(II) metallopeptide systems, 1/Cu(II) and 2/Cu(II),…
Abstract Imaging extracellular Cu2+ in vivo is of paramount interest due to its biological importance in both physiological and pathological states. Magnetic resonance imaging (MRI) is a powerful technique to do so. However, the development of efficient MRI contrast agents selective for Cu2+,…
Abstract Several copper-ligands, including 1,10-phenanthroline (Phen), have been investigated for anticancer purposes based on their capacity to bind excess copper (Cu) in cancer tissues and form redox active complexes able to catalyse the formation of reactive oxygen species (ROS), ultimately…
Abstract CPPs, or Cell-Penetrating Peptides, offer invaluable utility in disease treatment due to their ability to transport various therapeutic molecules across cellular membranes. Their unique characteristics, such as biocompatibility and low immunogenicity, make them ideal candidates for…
Abstract Metal ion-catalysed overproduction of reactive oxygen species (ROS) are believed to contribute significantly to oxidative stress and be involved in several biological processes, from immune defence to development of diseases. Among the essential metal ions, copper is one of the most…
Abstract Cu-thiosemicarbazones have been intensively investigated for their application in cancer therapy or as antimicrobials. Copper(II)-di-2-pyridylketone-4,4-dimethyl-thiosemicarbazone (CuII-Dp44mT) showed anticancer activity in the submicromolar concentration range in cell culture. The…
Abstract The chelator diacetyl-bis(N4-methylthiosemicarbazone) (ATSM) and its complexes with CuII and ZnII are becoming increasingly investigated for medical applications such as PET imaging for anti-tumour therapy and the treatment of amyotrophic lateral sclerosis. However, the solubility in water…
Abstract Cu chelation in biological systems is of interest as a tool to study the metabolism of this essential metal or for applications in the case of diseases with a systemic or local Cu overload, such as Wilson's or Alzheimer's disease. The choice of the chelating agent must meet several…
