Search Results - "Gelin, Muriel"
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Small-Molecule Inhibitors of Cyclophilins Block Opening of the Mitochondrial Permeability Transition Pore and Protect Mice From Hepatic Ischemia/Reperfusion Injury
Published in Gastroenterology (New York, N.Y. 1943) (01-11-2019)“…Hepatic ischemia/reperfusion injury is a complication of liver surgery that involves mitochondrial dysfunction resulting from mitochondrial permeability…”
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Fragment-based discovery of a new family of non-peptidic small-molecule cyclophilin inhibitors with potent antiviral activities
Published in Nature communications (22-09-2016)“…Cyclophilins are peptidyl-prolyl cis/trans isomerases (PPIase) that catalyse the interconversion of the peptide bond at proline residues. Several cyclophilins…”
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New Chemical Probe Targeting Bacterial NAD Kinase
Published in Molecules (Basel, Switzerland) (22-10-2020)“…Nicotinamide adenine dinucleotide (NAD) kinases are essential and ubiquitous enzymes involved in the tight regulation of NAD/nicotinamide adenine dinucleotide…”
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Toward the Design of Ligands Selective for the C-Terminal Domain of TEADs
Published in Journal of medicinal chemistry (28-04-2022)“…The Hippo signaling pathway plays a fundamental role in the control of organ growth, cell proliferation, and stem cell characters. TEADs are the main…”
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TOWARDS THE DESIGN OF LIGANDS OF THE INTERNAL POCKET TEADS C-TERMINAL DOMAIN
Published in European journal of medicinal chemistry (01-11-2024)Get full text
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Insight into the role of the Bateman domain at the molecular and physiological levels through engineered IMPDHs
Published in Protein science (20-06-2023)“…Inosine 5'-monophosphate dehydrogenase (IMPDH) is a^ ubiquitous enzyme that catalyzes the NAD+ -dependent oxidation of inosine 5'-monophosphate into xanthosine…”
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Crystal structure of human NADK2 reveals a dimeric organization and active site occlusion by lysine acetylation
Published in Molecular cell (01-09-2022)“…NAD kinases (NADKs) are metabolite kinases that phosphorylate NAD molecules to make NADP , a limiting substrate for the generation of reducing power NADPH…”
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w TSA-CRAFT : an open-access web server for rapid analysis of thermal shift assay experiments
Published in Bioinformatics advances (29-09-2023)“…The automated data processing provided by the tool enables now to reach high throughput speed analysis of thermal shift assays. While the software is powerful…”
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wTSA-CRAFT: an open-access web server for rapid analysis of thermal shift assay experiments
Published in Bioinformatics advances (2023)“…Abstract Motivation The automated data processing provided by the TSA-CRAFT tool enables now to reach high throughput speed analysis of thermal shift assays…”
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Insight into the role of the Bateman domain at the molecular and physiological levels through engineered IMP dehydrogenases
Published in Protein science (01-08-2023)“…Inosine 5′‐monophosphate (IMP) dehydrogenase (IMPDH) is an ubiquitous enzyme that catalyzes the NAD+‐dependent oxidation of inosine 5′‐monophosphate into…”
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Discovery of a cryptic site at the interface 2 of TEAD – Towards a new family of YAP/TAZ-TEAD inhibitors
Published in European journal of medicinal chemistry (15-12-2021)“…The Hippo pathway is involved in organ size control and tissue homeostasis by regulating cell growth, proliferation and apoptosis. It controls the…”
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Structure-Based and Knowledge-Informed Design of B-Raf Inhibitors Devoid of Deleterious PXR Binding
Published in Journal of medicinal chemistry (27-12-2021)Get full text
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Structure-Based and Knowledge-Informed Design of B‑Raf Inhibitors Devoid of Deleterious PXR Binding
Published in Journal of medicinal chemistry (27-01-2022)“…Dabrafenib is an anticancer drug currently used in the clinics, alone or in combination. However, dabrafenib was recently shown to potently activate the human…”
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Synthesis and structure-activity relationship studies of original cyclic diadenosine derivatives as nanomolar inhibitors of NAD kinase from pathogenic bacteria
Published in European journal of medicinal chemistry (15-01-2023)“…Nicotinamide adenine dinucleotide kinases (NAD kinases) are essential and ubiquitous enzymes involved in the production of NADP(H) which is an essential…”
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Dimerization of the Pragmin Pseudo-Kinase Regulates Protein Tyrosine Phosphorylation
Published in Structure (London) (03-04-2018)“…The pseudo-kinase and signaling protein Pragmin has been linked to cancer by regulating protein tyrosine phosphorylation via unknown mechanisms. Here we…”
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Development of LM-41 and AF-2112, two flufenamic acid-derived TEAD inhibitors obtained through the replacement of the trifluoromethyl group by aryl rings
Published in Bioorganic & medicinal chemistry letters (15-10-2023)“…[Display omitted] The Hippo pathway regulates organ size and tissue homeostasis by controlling cell proliferation and apoptosis. The YAP–TEAD transcription…”
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Structure-Based and Knowledge-Informed Design of B-Raf Inhibitors Devoid of Deleterious PXR Binding
Published in Journal of medicinal chemistry (27-01-2022)Get full text
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First-in-class allosteric inhibitors of bacterial IMPDHs
Published in European journal of medicinal chemistry (01-04-2019)“…Inosine-5‘-monophosphate dehydrogenase (IMPDH) is an essential enzyme in many bacterial pathogens and is considered as a potential drug target for the…”
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Structure‐based design, synthesis and biological evaluation of a NAD+ analogue targeting Pseudomonas aeruginosa NAD kinase
Published in The FEBS journal (01-01-2023)“…Multidrug resistance is a major public health problem that requires the urgent development of new antibiotics and therefore the identification of novel…”
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Crystallographic studies of two variants of Pseudomonas aeruginosa IMPDH with impaired allosteric regulation
Published in Acta crystallographica. Section D, Biological crystallography. (01-09-2015)“…Inosine‐5′‐monophosphate dehydrogenases (IMPDHs), which are the rate‐limiting enzymes in guanosine‐nucleotide biosynthesis, are important therapeutic targets…”
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