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View article: TDMQ20 as A Drug Candidate for Wilson’s Disease: Comparison with D-Penicillamine, Trientine, and Tetrathiomolybdate In Vitro and In Mice
TDMQ20 as A Drug Candidate for Wilson’s Disease: Comparison with D-Penicillamine, Trientine, and Tetrathiomolybdate In Vitro and In Mice Open
Background/Objectives: The lifelong treatment of Wilson’s disease (WD) currently relies on copper chelators with relatively poor metal specificity, which frequently exhibit serious adverse effects. There is a real medical need for a specif…
View article: High specificity is a key parameter for copper ligands as future therapeutic agents for Alzheimer’s, Wilson’s, and cancer diseases
High specificity is a key parameter for copper ligands as future therapeutic agents for Alzheimer’s, Wilson’s, and cancer diseases Open
The loss of copper homeostasis is considered a characteristic feature of several major human diseases such as Alzheimer’s, Wilson’s, or cancer diseases. Consequently, the design of new efficient ligands targeting copper regulation is a maj…
View article: B3GALT6 mutations lead to compromised connective tissue biomechanics in Ehlers-Danlos syndrome
B3GALT6 mutations lead to compromised connective tissue biomechanics in Ehlers-Danlos syndrome Open
Ehlers-Danlos syndromes (EDS) comprise a genetically and clinically heterogenous group of rare diseases that cause severe, often fatal, damage to connective tissue. The molecular basis of EDS implicates defects in extracellular matrix comp…
View article: Correction: Embo-Ibouanga et al. Peptide-Alkoxyamine Drugs: An Innovative Approach to Fight Schistosomiasis: “Digging Their Graves with Their Forks”. Pathogens 2024, 13, 482
Correction: Embo-Ibouanga et al. Peptide-Alkoxyamine Drugs: An Innovative Approach to Fight Schistosomiasis: “Digging Their Graves with Their Forks”. Pathogens 2024, 13, 482 Open
There was an error in the original publication [...]
View article: Hybrid Molecules as Efficient Drugs against Multidrug‐Resistant Malaria Parasites
Hybrid Molecules as Efficient Drugs against Multidrug‐Resistant Malaria Parasites Open
This review is focused on hybrid molecules defined as chemical entities with two or more structural domains, as antimalarial drug‐candidates, over the past 25 years. Due to their different pharmacophores, such hybrids can interact with a s…
View article: Reductive Activation of Artefenomel (OZ439) by Fe(II)-Heme, Related to Its Antimalarial Activity
Reductive Activation of Artefenomel (OZ439) by Fe(II)-Heme, Related to Its Antimalarial Activity Open
The 1,2,4-trioxolane antimalarial drug, OZ439 (artefenomel), exhibits cross-resistance to artemisinins in vitro with similar survival rates of artemisinin-resistant parasites after dihydroartemisinin or OZ439 exposure, suggesting that this…
View article: Dynamic covalent bonding (DCB): the bond lability of alkoxyamines as drugs against <i>Schistosoma mansoni</i> and <i>Plasmodium falciparum</i>
Dynamic covalent bonding (DCB): the bond lability of alkoxyamines as drugs against <i>Schistosoma mansoni</i> and <i>Plasmodium falciparum</i> Open
To dig its grave with its fork : How feeding Plasmodium and Schistosoma with hybrid peptide-alkoxyamines that release reactive radicals in the presence of enzymatic activities leads to their death.
View article: <i>In vitro</i> evaluation of ganaplacide/lumefantrine combination against <i>Plasmodium falciparum</i> in a context of artemisinin resistance
<i>In vitro</i> evaluation of ganaplacide/lumefantrine combination against <i>Plasmodium falciparum</i> in a context of artemisinin resistance Open
Background Ganaplacide, also known as KAF156, is among the new antimalarial drug candidates that have successfully reached Phase III clinical trials, and is proposed in combination with lumefantrine. This combination could replace the curr…
View article: Peptide-Alkoxyamine Drugs: An Innovative Approach to Fight Schistosomiasis: “Digging Their Graves with Their Forks”
Peptide-Alkoxyamine Drugs: An Innovative Approach to Fight Schistosomiasis: “Digging Their Graves with Their Forks” Open
The expansion of drug resistant parasites sheds a serious concern on several neglected parasitic diseases. Our recent results on cancer led us to envision the use of peptide-alkoxyamines as a highly selective and efficient new drug against…
View article: Hybrid Peptide-Alkoxyamine Drugs: A Strategy for the Development of a New Family of Antiplasmodial Drugs
Hybrid Peptide-Alkoxyamine Drugs: A Strategy for the Development of a New Family of Antiplasmodial Drugs Open
The emergence and spread of drug-resistant Plasmodium falciparum parasites shed a serious concern on the worldwide control of malaria, the most important tropical disease in terms of mortality and morbidity. This situation has led us to co…
View article: Copper selective 8-aminoquinoline based tetradentate chelators as anticancer agents
Copper selective 8-aminoquinoline based tetradentate chelators as anticancer agents Open
The copper chelator TDMQ20 inhibits proliferation and migration of cancer cells. Its mechanism, maybe driven by the coordination chemistry of copper, involves intracellular production of reactive oxygen species and induction of tumor cell …
View article: Unprecedented linear products by a mechanochemically activated Biginelli reaction using lawsone
Unprecedented linear products by a mechanochemically activated Biginelli reaction using lawsone Open
The Biginelli reaction, a crucial multicomponent reaction, was investigated involving 2-hydroxy-1,4-naphthoquinone (lawsone), p -substituted benzaldehydes, and ureas.
View article: The Specific Copper(II) Chelator TDMQ20 Is Efficient for the Treatment of Wilson’s Disease in Mice
The Specific Copper(II) Chelator TDMQ20 Is Efficient for the Treatment of Wilson’s Disease in Mice Open
(1) Background: In patients with Wilson’s disease, the deficiency of the copper carrier ATP7B causes the accumulation of copper in the liver, brain and various other organs. Lifelong treatment is therefore mandatory, using copper chelators…
View article: Oxidation of TDMQ20, a Specific Copper Chelator as Potential Drug Against Alzheimer's Disease
Oxidation of TDMQ20, a Specific Copper Chelator as Potential Drug Against Alzheimer's Disease Open
Developed as a regulator of copper homeostasis in the brain of patients affected by Alzheimer's disease (AD), TDMQ20 is a specific copper(II) chelator able to restore short term memory in AD mice. To anticipate on metabolic studies of this…
View article: Hybrid molecules based on an emodin scaffold. Synthesis and activity against SARS-CoV-2 and <i>Plasmodium</i>
Hybrid molecules based on an emodin scaffold. Synthesis and activity against SARS-CoV-2 and <i>Plasmodium</i> Open
A series of hybrid emodin–polyamine or emodin–norchlorcyclizine molecules have been synthesized and evaluated as potential antiviral and antimalarial agents. ( R )-Emoxyzine-2 was as potent as remdesivir in inhibiting SARS-CoV-2 replicatio…
View article: Distribution in Rat Blood and Brain of TDMQ20, a Copper Chelator Designed as a Drug-Candidate for Alzheimer’s Disease
Distribution in Rat Blood and Brain of TDMQ20, a Copper Chelator Designed as a Drug-Candidate for Alzheimer’s Disease Open
(1) Background: TDMQ20 is a specific regulator of copper homeostasis in the brain, able to inhibit cognitive impairment in the early stages of Alzheimer’s disease (AD) in mouse models of AD. To promote the further development of this drug-…
View article: Proteomics Evidence of the Role of TDMQ20 in the Cholinergic System and Synaptic Transmission in a Mouse Model of Alzheimer’s Disease
Proteomics Evidence of the Role of TDMQ20 in the Cholinergic System and Synaptic Transmission in a Mouse Model of Alzheimer’s Disease Open
The interaction between copper ions and amyloid peptide Aβ has been reported to be involved in Alzheimer's disease (AD) pathology. Based on copper coordination biochemistry, we designed specific copper chelators [tetradentate monoquinoline…
View article: Design of Anti-infectious Agents from Lawsone in a Three-Component Reaction with Aldehydes and Isocyanides
Design of Anti-infectious Agents from Lawsone in a Three-Component Reaction with Aldehydes and Isocyanides Open
The first effective synthetic approach to naphthofuroquinones via a reaction involving lawsone, various aldehydes, and three isocyanides under microwave irradiation afforded derivatives in moderate to good yields. In addition, for less-rea…
View article: How to Define a Nanozyme
How to Define a Nanozyme Open
Over the past 15 years, many articles have considered "nanozymes" as ferromagnetic nanoparticles having an "intrinsic peroxidase-like activity" in the presence of hydrogen peroxide. However, the definition and the catalytic activity of the…
View article: Synthesis and Antimalarial Activities of New Hybrid Atokel Molecules
Synthesis and Antimalarial Activities of New Hybrid Atokel Molecules Open
The currently spreading resistance of the malaria parasite Plasmodium falciparum to artemisinin‐based combination therapies makes an urgent need for new efficient drugs. Aiming to kill artemisinin‐resistant Plasmodium , a series of novel h…
View article: Antimalarial Inhibitors Targeting Epigenetics or Mitochondria in Plasmodium falciparum: Recent Survey upon Synthesis and Biological Evaluation of Potential Drugs against Malaria
Antimalarial Inhibitors Targeting Epigenetics or Mitochondria in Plasmodium falciparum: Recent Survey upon Synthesis and Biological Evaluation of Potential Drugs against Malaria Open
Despite many efforts, malaria remains among the most problematic infectious diseases worldwide, mainly due to the development of drug resistance by P. falciparum. Over the past decade, new essential pathways have been emerged to fight agai…
View article: "Nanozymes" without catalytic activity should be renamed
"Nanozymes" without catalytic activity should be renamed Open
In the aftermath of the report by L. Gao, et al. (Nature Nanotechnol. 2007, 2, 577-583), ferromagnetic nanoparticles such as magnetite are considered by many authors as having an "intrinsic peroxidase-like activity" in the presence of hydr…
View article: TDMQ20, a Specific Copper Chelator, Reduces Memory Impairments in Alzheimer’s Disease Mouse Models
TDMQ20, a Specific Copper Chelator, Reduces Memory Impairments in Alzheimer’s Disease Mouse Models Open
Besides targeting amyloid or tau metabolisms, regulation of redox metal ions is a recognized therapeutic target for Alzheimer's disease (AD). Based on the bioinorganic chemistry of copper, we designed specific chelators of copper(II) (TDMQ…
View article: CCDC 1938657: Experimental Crystal Structure Determination
CCDC 1938657: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 1938691: Experimental Crystal Structure Determination
CCDC 1938691: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Alkoxyamines Designed as Potential Drugs against Plasmodium and Schistosoma Parasites
Alkoxyamines Designed as Potential Drugs against Plasmodium and Schistosoma Parasites Open
Malaria and schistosomiasis are major infectious causes of morbidity and mortality in the tropical and sub-tropical areas. Due to the widespread drug resistance of the parasites, the availability of new efficient and affordable drugs for t…
View article: Comment on “Free-Radical Formation by the Peroxidase-Like Catalytic Activity of MFe<sub>2</sub>O<sub>4</sub> (M = Fe, Ni, and Mn) Nanoparticles”
Comment on “Free-Radical Formation by the Peroxidase-Like Catalytic Activity of MFe<sub>2</sub>O<sub>4</sub> (M = Fe, Ni, and Mn) Nanoparticles” Open
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View article: Why Is Tetradentate Coordination Essential for Potential Copper Homeostasis Regulators in Alzheimer's Disease?
Why Is Tetradentate Coordination Essential for Potential Copper Homeostasis Regulators in Alzheimer's Disease? Open
Research of effective drugs against Alzheimer's disease (AD) is currently one of the most challenging topics in medicinal chemistry. Despite the documented detrimental effect of the disruption of copper ion homeostasis in AD, this potentia…
View article: Corrigendum: Preparation of Tetradentate Copper Chelators as Potential Anti‐Alzheimer Agents
Corrigendum: Preparation of Tetradentate Copper Chelators as Potential Anti‐Alzheimer Agents Open
In the caption of Figure 10, page 692, the words ‘absence’ and ‘presence’ were reversed. The caption should read as follows: “Production of H2O2 by copper complexes of TDMQ5, 19, 20 or 22, associated to ascorbate, in the absence (hashed ba…