A5085633496- Advanced biosensing and bioanalysis techniques
- DNA and Nucleic Acid Chemistry
- RNA Interference and Gene Delivery
- Click Chemistry and Applications
- RNA and protein synthesis mechanisms
- Cancer therapeutics and mechanisms
- Monoclonal and Polyclonal Antibodies Research
- HER2/EGFR in Cancer Research
- Molecular Junctions and Nanostructures
- RNA Research and Splicing
- Advanced Biosensing Techniques and Applications
Université de Bourgogne
2022-2025
Centre National de la Recherche Scientifique
2019-2025
Institut de Chimie Moléculaire de l'Université de Bourgogne
2022-2025
Institut de Chimie
2022-2025
Université de Toulouse
2019-2021
La Ligue Contre le Cancer
2020-2021
Université Toulouse III - Paul Sabatier
2020-2021
Institut de Pharmacologie et de Biologie Structurale
2019-2021
G-quadruplexes (G4) are non-canonical DNA structures found in the genome of most species including human. Small molecules stabilizing these structures, called G4 ligands, have been identified and, for some them, shown to induce cytotoxic double-strand breaks. Through use an unbiased genetic approach, we identify here topoisomerase 2α (TOP2A) as a major effector cytotoxicity induced by two clastogenic pyridostatin and CX-5461, latter molecule currently undergoing phase I/II clinical trials...
Guanine-rich DNA strands can fold into non-canonical four-stranded secondary structures named G-quadruplexes (G4). Experimental evidences suggest that G4-DNA surrounding transcription start sites act as cis-regulatory elements by either stimulating or inhibiting gene transcription. Therefore, proteins able to target and regulate specific G4 formation/unfolding are crucial for G4-mediated transcriptional control. Here we present data revealing CNBP acts in vitro a G4-unfolding protein over...
The existence and functional relevance of DNA RNA G-quadruplexes (G4s) in human cells is now beyond debate, but how did we reach such a level confidence? Thanks to panoply molecular tools techniques that are routinely implemented wet labs. Among them, G4 imaging ranks high because its reliability practical convenience, which makes cellular detection quick easy; also, this technique sensitive responsive any modulations cells, thus allows gaining precious insights into biology. Herein, briefly...
Real-time imaging of antibody-drug conjugates (ADCs) offers valuable insights for assessing tumor targeting specificity, monitoring therapeutic efficacy, and detecting off-target accumulation that may cause adverse effects. To enable precise tracking, we developed a versatile fluorescent platform based on an NIR-II emitting aza-BODIPY dye, which can be site-specifically grafted onto IgG1 antibody to generate well-defined ADCs. As proof concept, synthesized HER2-targeting trastuzumab...
Abstract G-quadruplexes (G4) are non-canonical secondary structures consisting in stacked tetrads of hydrogen-bonded guanines bases. An essential feature G4 is their intrinsic polymorphic nature, which characterized by the equilibrium between several conformations (also called topologies) and presence different types loops with variable lengths. In cells, functions rely on protein or enzymatic factors that recognize promote resolve these structures. order to characterize new G4-dependent...
Gold(<sc>iii</sc>) porphyrins have a square planar geometry and an extra positive charge, compatible with stronger electrostatic π-stacking interactions.
Interrogating G-quadruplex (G4) biology at its deepest roots in human cells relies on the design, synthesis, and use of ever smarter molecular tools. Here, we demonstrate versatility biomimetic G4 ligands referred to as TASQ (template assembled synthetic G-quartet) which a biotin handle was incorporated for G4-focused chemical investigations. We have rethought biotinylated design make it readily chemically accessible via an efficient click-chemistry-based strategy. The resulting...
Chemical biology hinges on multivalent molecular tools that can specifically interrogate and/or manipulate cellular circuitries from the inside. The success of many these approaches relies make it possible to visualize biological targets in cells and then isolate them for identification purposes. To this end, click chemistry has become just a few years vital tool offering practically convenient solutions address highly complicated questions. We report here two clickable tools, biomimetic...
Abstract Non-coding RNAs (ncRNAs) in human cells do not lead to protein synthesis and constitute a substantial portion of the transcriptome. Human long non-coding (lncRNAs) orchestrate critical cellular functions influencing development, differentiation, metabolism. Dysregulation lncRNAs has been correlated with several pathological conditions such as neurodegenerative autoimmune disorders, diabetes, cancer. Recent reports have suggested involvement G4s regulate colorectal cancer (CRC)...
Abstract G-quadruplexes (G4), non-canonical DNA structures, are involved in several essential processes. Stabilization of G4 structures by small compounds (G4 ligands) affects almost all transactions, including telomere maintenance and genomic stability. Here, thanks to a powerful unbiased genetic approach, we identify topoisomerase 2-alpha (TOP2A) as the main effector cell cytotoxicity induced CX5461, ligand currently undergoing phase I/II clinical trials. This approach also allowed new...
Abstract Transient melting of the duplex‐DNA (B‐DNA) during DNA transactions allows repeated sequences to fold into non‐B‐DNA structures, including junctions and G‐quadruplexes. These noncanonical structures can act as impediments polymerase progression along duplex, thereby triggering damage ultimately jeopardizing genomic stability. Their stabilization by ad hoc ligands is currently being explored a putative anticancer strategy since it might represent an efficient way inflict toxic...
Transient melting of the duplex-DNA (B-DNA) during DNA transactions allows repeated sequences to fold into non-B-DNA structures, including junctions and G-quadruplexes. These noncanonical structures can act as impediments polymerase progression along duplex, thereby triggering damage ultimately jeopardizing genomic stability. Their stabilization by ad hoc ligands is currently being explored a putative anticancer strategy since it might represent an efficient way inflict toxic specifically...
Abstract G-quadruplexes (G4) are non-canonical secondary structures consisting in stacked tetrads of hydrogen-bonded guanines bases. An essential feature G4 is their intrinsic polymorphic nature, which characterized by the equilibrium between several conformations (also called topologies) and presence different types loops with variable lengths. In cells, functions rely on protein or enzymatic factors that recognize promote resolve these structures. order to characterize new G4-dependent...
Abstract Chemical biology hinges on multivalent molecular tools that uniquely allow for interrogating and/or manipulating cellular circuitries from the inside. The success of many these approaches relies make it possible to visualize biological targets in cells and then isolate them identification purposes. To this end, click chemistry has become just a few years vital tool offering practically convenient solutions address highly complicated question. We report here two clickable tools,...