Explanipedia

Hunting for lubeluzole analogues as antimyotonic agents with reduced cardiac liability Open

Maria Maddalena Cavalluzzi, Roberta Gualdani, Alessandro Farinato, Concetta Altamura, Sabata Pierno , et al. · 2025

Lubeluzole is a neuroprotective agent displaying antimyotonic activity. Lubeluzole clinical development as an antiischemic drug was discontinued due to a lack of efficacy in human trials and possible cardiac toxicity. Since lubeluzole is a…

Conditional deletion of TRPC1 channel modulates synaptic plasticity, long term depression, and memory extinction in Fragile X syndrome mice Open

Farah Issa, Xavier Yerna, Thibaud Parpaite, Caren Jabbour, Olivier Schakman , et al. · 2025

Primary Cell Cultures in Neurobiology: Optimized Protocol for Culture of Mouse Fetal Hindbrain Neurons Open

Hadrien Glibert, Laure Bridoux, Maëlle Palate, Coralie Piget, Marie‐Thérèse Ahn , et al. · 2025

Primary cultures of neural cells are important key tools for basic and translational neuroscience research. These primary cell cultures are classically generated from the rodent brain hippocampus or cortex and optimized for enrichment in n…

Editorial: Chronic pain: what is the mechanism? Open

James D. Adams, Ching‐Liang Hsieh, Roberta Gualdani · 2024

TRPV1 corneal neuralgia mutation: Enhanced pH response, bradykinin sensitization, and capsaicin desensitization Open

Roberta Gualdani, Solène Barbeau, Jun‐Hui Yuan, Deborah S. Jacobs, Philippe Gailly , et al. · 2024

The factors that contribute to pain after nerve injury remain incompletely understood. Laser-assisted in situ keratomileusis (LASIK) and photorefractive keratectomy (PRK) are common surgical techniques to correct refractive errors. After L…

hERG stereoselective modulation by mexiletine‐derived ureas: Molecular docking study, synthesis, and biological evaluation Open

Gualtiero Milani, Roberta Budriesi, Elisa Tavazzani, Maria Maddalena Cavalluzzi, Laura Mattioli , et al. · 2023

Long QT syndrome (LQTS) is a disorder of cardiac electrophysiology resulting in life‐threatening arrhythmias; nowadays, only a few drugs are available for the management of LQTS. Focusing our attention on LQT2, one of the most common subty…

CCDC 2209758: Experimental Crystal Structure Determination Open

Gualtiero Milani, Roberta Budriesi, Elisa Tavazzani, Maria Maddalena Cavalluzzi, Laura Mattioli , et al. · 2023

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 …

CCDC 2209759: Experimental Crystal Structure Determination Open

Gualtiero Milani, Roberta Budriesi, Elisa Tavazzani, Maria Maddalena Cavalluzzi, Laura Mattioli , et al. · 2023

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 …

Conditional deletion of KCC2 impairs synaptic plasticity and both spatial and nonspatial memory Open

Anna Kreis, Farah Issa, Xavier Yerna, Caren Jabbour, Olivier Schakman , et al. · 2023

The postsynaptic inhibition through GABA A receptors (GABA A R) relies on two mechanisms, a shunting effect due to an increase in the postsynaptic membrane conductance and, in mature neurons, a hyperpolarization effect due to an entry of c…

Lipoyl-Based Antagonists of Transient Receptor Potential Cation A (TRPA1) Downregulate Osteosarcoma Cell Migration and Expression of Pro-Inflammatory Cytokines Open

Oscar Francesconi, Francisco Corzana, Georgia‐Ioanna Kontogianni, Giorgio Pesciullesi, Roberta Gualdani , et al. · 2022

Osteosarcoma is a heterogeneous tumor intimately linked to its microenvironment, which promotes its growth and spread. It is generally accompanied by cancer-induced bone pain (CIBP), whose main component is neuropathic pain. The TRPA1 ion …

A TRPM7 mutation linked to familial trigeminal neuralgia: Omega current and hyperexcitability of trigeminal ganglion neurons Open

Roberta Gualdani, Philippe Gailly, Jun‐Hui Yuan, Xavier Yerna, Giulia Di Stefano , et al. · 2022

Trigeminal neuralgia (TN) is a unique pain disorder characterized by intense paroxysmal facial pain within areas innervated by the trigeminal nerve. Although most cases of TN are sporadic, familial clusters of TN suggest that genetic facto…

Prdm12 modulates pain-related behavior by remodeling gene expression in mature nociceptors Open

Aurore Latragna, Alba Sabaté San José, Panagiotis Tsimpos, Simon Vermeiren, Roberta Gualdani , et al. · 2021

Prdm12 is a conserved epigenetic transcriptional regulator that displays restricted expression in nociceptors of the developing peripheral nervous system. In mice, Prdm12 is required for the development of the entire nociceptive lineage. I…

Overexpression of wild-type human amyloid precursor protein alters GABAergic transmission Open

Anna Kreis, Jana Desloovere, Núria Suelves, Nathalie Pierrot, Xavier Yerna , et al. · 2021

Trigeminal Neuralgia TRPM8 Mutation Open

Roberta Gualdani, Jun‐Hui Yuan, Philip R. Effraim, Giulia Di Stefano, Andrea Truini , et al. · 2021

We propose that Arg30Gln confers gain-of-function attributes on TRPM8, which contribute to pathogenesis of trigeminal neuralgia in patients carrying this mutation.

Lubeluzole: from anti-ischemic drug to preclinical antidiarrheal studies Open

Maria Maddalena Cavalluzzi, Roberta Budriesi, Maria Antonietta De Salvia, Laura Quintieri, Monica Piarulli , et al. · 2020

Mechanical activation of TRPV4 channels controls albumin reabsorption by proximal tubule cells Open

Roberta Gualdani, François Seghers, Xavier Yerna, Olivier Schakman, Nicolas Tajeddine , et al. · 2020

Fluid pressure in the proximal tubule activates TRPV4 to promote endocytosis and retention of albumin.

Correction: Gualdani, R.; et al. Store-Operated Calcium Entry Contributes to Cisplatin-Induced Cell Death in Non-Small Cell Lung Carcinoma. Cancers 2019, 11, 430 Open

Roberta Gualdani, Marie de Clippele, Ikram Ratbi, Philippe Gailly, Nicolas Tajeddine · 2020

The authors wish to make the following corrections to this paper [...]

How TRPC Channels Modulate Hippocampal Function Open

Roberta Gualdani, Philippe Gailly · 2020

Transient receptor potential canonical (TRPC) proteins constitute a group of receptor-operated calcium-permeable nonselective cationic membrane channels of the TRP superfamily. They are largely expressed in the hippocampus and are able to …

Amyloid Precursor Protein (APP) Controls the Expression of the Transcriptional Activator Neuronal PAS Domain Protein 4 (NPAS4) and Synaptic GABA Release Open

Rémi Opsomer, Sabrina Contino, Florian Perrin, Roberta Gualdani, Bernadette Tasiaux , et al. · 2020

The amyloid precursor protein (APP) has been extensively studied as the precursor of the β-amyloid (Aβ) peptide, the major component of the senile plaques found in the brain of Alzheimer’s disease (AD) patients. However, the function of AP…

Role of the TRPC1 Channel in Hippocampal Long-Term Depression and in Spatial Memory Extinction Open

Xavier Yerna, Olivier Schakman, Ikram Ratbi, Anna Kreis, Sophie Lepannetier , et al. · 2020

Group I metabotropic glutamate receptors (mGluR) are involved in various forms of synaptic plasticity that are believed to underlie declarative memory. We previously showed that mGluR5 specifically activates channels containing TRPC1, an i…

Store-Operated Calcium Entry Contributes to Cisplatin-Induced Cell Death in Non-Small Cell Lung Carcinoma Open

Roberta Gualdani, Marie de Clippele, Ikram Ratbi, Philippe Gailly, Nicolas Tajeddine · 2019

Cisplatin (CDDP) is one of the principal chemotherapeutic agents used for the first-line treatment of many malignancies, including non-small cell lung carcinoma (NSCLC). Despite its use for over 40 years, its mechanism of action is not yet…

Mechanical activation of TRPV4 channels controls albumin reabsorption by proximal tubule cells Open

Roberta Gualdani, François Seghers, Xavier Yerna, Olivier Schakman, Nicolas Tajeddine , et al. · 2019

The proximal tubule (PT) mediates the endocytosis of essential substances filtered through the glomerulus, including albumin and a large variety of low molecular weight proteins that would otherwise be lost in urine. Variations in the amou…

Activation of TRPC1 Channel by Metabotropic Glutamate Receptor mGluR5 Modulates Synaptic Plasticity and Spatial Working Memory Open

Sophie Lepannetier, Roberta Gualdani, Sabrina Tempesta, Olivier Schakman, François Seghers , et al. · 2018

Group I metabotropic glutamate receptors, in particular mGluR5, have been implicated in various forms of synaptic plasticity that are believed to underlie declarative memory. We observed that mGluR5 specifically activated a channel contain…

Drug Interactions With the Ca2+-ATPase From Sarco(Endo)Plasmic Reticulum (SERCA) Open

Francesco Tadini‐Buoninsegni, Serena Smeazzetto, Roberta Gualdani, Maria Rosa Moncelli · 2018

The sarco(endo)plasmic reticulum Ca²⁺-ATPase (SERCA) is an intracellular membrane transporter that utilizes the free energy provided by ATP hydrolysis for active transport of Ca²⁺ ions from the cytoplasm to the lumen …

Molecular Insights into hERG Potassium Channel Blockade by Lubeluzole Open

Roberta Gualdani, Maria M. Cavalluzzi, Francesco Tadini‐Buoninsegni, Marino Convertino, Philippe Gailly , et al. · 2018

Background/Aims: Lubeluzole is a benzothiazole derivative that has shown neuroprotective properties in preclinical models of ischemic stroke. However, clinical research on lubeluzole is now at a standstill, since lubeluzole seems to be ass…

Gating mechanisms of TRPC1 channel in hippocampal neurons. Open

Roberta Gualdani, Sophie Lepannetier, Anna Kreis, Olivier Schakman, Philippe Gailly · 2018

Event Abstract Back to Event Gating mechanisms of TRPC1 channel in hippocampal neurons. Roberta Gualdani1, Sophie Lepannetier1, Anna Kreis1, Olivier Schakman1 and Philippe Gailly1* 1 Université Catholique de Louvain, Belgium The canonical …

Supplementary Material for: Molecular Insights into hERG Potassium Channel Blockade by Lubeluzole Open

Roberta Gualdani, Maria Maddalena Cavalluzzi, Francesco Tadini‐Buoninsegni, Marino Convertino, Philippe Gailly , et al. · 2018

Background/Aims: Lubeluzole is a benzothiazole derivative that has shown neuroprotective properties in preclinical models of ischemic stroke. However, clinical research on lubeluzole is now at a standstill, since lubeluzole s…

Lipoyl-Homotaurine Derivative (ADM_12) Reverts Oxaliplatin-Induced Neuropathy and Reduces Cancer Cells Malignancy by Inhibiting Carbonic Anhydrase IX (CAIX) Open

Marco Fragai, Giuseppina Comito, Lorenzo Di Cesare Mannelli, Roberta Gualdani, V. Calderone , et al. · 2017

Oxaliplatin (OXA) is a valuable and largely used cancer drug which induces a serious and intractable neuropathy. The lipoyl-homotaurine derivative (ADM_12) reverts in vivo OXA-induced neuropathy, and it is an effective antagonist of the no…

The Chemistry and Pharmacology of Citrus Limonoids Open

Roberta Gualdani, Maria Maddalena Cavalluzzi, Giovanni Lentini, Solomon Habtemariam · 2016

Citrus limonoids (CLs) are a group of highly oxygenated terpenoid secondary metabolites found mostly in the seeds, fruits and peel tissues of citrus fruits such as lemons, limes, oranges, pumellos, grapefruits, bergamots, and mandarins. Re…

Assessing the in Vitro Cardiotoxicity of Superparamagnetic Ion Oxide Nanoparticles (SPIONs) Open

Roberta Gualdani, Andrea Guerrini, Elvira Fantechi, Claudio Sangregorio, Maria Rosa Moncelli · 2016

Roberta Gualdani YOU? Author Swipe