Search Results - "Dugué, Laurence"
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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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Crystal structure of the Trypanosoma cruzi EIF4E5 translation factor homologue in complex with mRNA cap-4
Published in Nucleic acids research (20-06-2019)“…Association of the initiation factor eIF4E with the mRNA cap structure is a key step for translation. Trypanosomatids present six eIF4E homologues, showing a…”
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Structural analysis of the Trypanosoma brucei EIF4E6/EIF4G5 complex reveals details of the interaction between unusual eIF4F subunits
Published in Scientific reports (25-01-2024)“…Recognition of the mRNA 5′ end is a critical step needed for translation initiation. This step is performed by the cap binding protein eIF4E, which joins the…”
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From Substrate to Fragments to Inhibitor Active In Vivo against Staphylococcus aureus
Published in ACS infectious diseases (13-03-2020)“…Antibiotic resistance is a worldwide threat due to the decreasing supply of new antimicrobials. Novel targets and innovative strategies are urgently needed to…”
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A convenient synthesis of 4(5)-(hetero)aryl-1H-imidazoles via microwave-assisted Suzuki–Miyaura cross-coupling reaction
Published in Tetrahedron letters (12-11-2014)“…[Display omitted] A simple and rapid access to a variety of 4(5)-arylated imidazoles via palladium-catalyzed Suzuki–Miyaura cross-coupling reaction is…”
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In Vivo Reshaping the Catalytic Site of Nucleoside 2′-Deoxyribosyltransferase for Dideoxy- and Didehydronucleosides via a Single Amino Acid Substitution
Published in The Journal of biological chemistry (18-07-2008)“…Nucleoside 2′-deoxyribosyltransferases catalyze the transfer of 2-deoxyribose between bases and have been widely used as biocatalysts to synthesize a variety…”
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Screening and In Situ Synthesis Using Crystals of a NAD Kinase Lead to a Potent Antistaphylococcal Compound
Published in Structure (London) (06-06-2012)“…Making new ligands for a given protein by in situ ligation of building blocks (or fragments) is an attractive method. However, it suffers from inherent…”
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Substrate specificity of vaccinia virus thymidylate kinase
Published in The FEBS journal (01-12-2005)“…Anti‐poxvirus therapies are currently limited to cidofovir [(S)‐1‐(3‐hydroxy‐2‐phosphonylmethoxypropyl)cytosine], but drug‐resistant strains have already been…”
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Nucleotide binding to human UMP‐CMP kinase using fluorescent derivatives − a screening based on affinity for the UMP‐CMP binding site
Published in The FEBS journal (01-07-2007)“…Methylanthraniloyl derivatives of ATP and CDP were used in vitro as fluorescent probes for the donor‐binding and acceptor‐binding sites of human UMP‐CMP…”
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Probing the Substrate Recognition Mechanism of the Human MTH1 Protein by Nucleotide Analogs
Published in Journal of molecular biology (27-02-2004)“…To examine the substrate recognition mechanism of the human MTH1 protein, which hydrolyzes 2-hydroxy-dATP, 8-hydroxy-dATP, and 8-hydroxy-dGTP, ten nucleotide…”
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Nucleoside Analogues as Inhibitors of Thymidylate Kinases: Possible Therapeutic Applications
Published in Chembiochem : a European journal of chemical biology (04-01-2002)“…Membrane‐permeable nonphosphorylated thymidine analogues (see structure) are active as competitive inhibitors of M. tuberculosis thymidylate kinase (TMPK) as…”
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Synthesis and recognition by DNA polymerases of a reactive nucleoside, 1-(2-deoxy-β-d-erythro-pentofuranosyl)-imidazole-4-hydrazide
Published in Nucleic acids research (01-05-2002)“…We report the synthesis of a new nucleoside, 1‐(2‐deoxy-β-d-erythro-pentofuranosyl)-imidazole-4-hydrazide (dYNH2) as a reactive monomer for DNA…”
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Looking for New Pyrimidine Acyclic Nucleotide Analogues Designed for Phosphorylation by Human Ump-Cmp Kinase
Published in Nucleosides, nucleotides & nucleic acids (01-01-2007)“…Human UMP-CMP kinase is involved in the phosphorylation of nucleic acid precursors and also in the activation of antiviral analogues including cidofovir, an…”
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3‘-C-Branched-Chain-Substituted Nucleosides and Nucleotides as Potent Inhibitors of Mycobacterium tuberculosis Thymidine Monophosphate Kinase
Published in Journal of medicinal chemistry (28-08-2003)“…Thymidine monophosphate kinase (TMPK) of Mycobacterium tuberculosis (TMPKmt) represents an attractive target for blocking the bacterial DNA synthesis. In an…”
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Recognition of Nucleotide Analogs Containing the 7,8-Dihydro-8-oxo Structure by the Human MTH1 Protein
Published in Journal of biochemistry (Tokyo) (01-12-2006)“…The MTH1 protein catalyzes hydrolysis of oxidatively damaged purine nucleotides including 8-hydroxy-dGTP to the monophosphates. The MTH1 protein seems to act…”
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Expedient and generic synthesis of imidazole nucleosides by enzymatic transglycosylation
Published in Organic & biomolecular chemistry (14-04-2016)“…A straightforward route to original imidazole-based nucleosides that makes use of an enzymatic N-transglycosylation step is reported in both the ribo- and…”
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Comparative Study of Purine and Pyrimidine Nucleoside Analogues Acting on the Thymidylate Kinases of Mycobacterium tuberculosis and of Humans
Published in Chembiochem : a European journal of chemical biology (04-08-2003)“…Thymidine monophosphate kinase (TMPK) from Mycobacterium tuberculosis (TMPKmt) is an attractive target for the design of specific inhibitors. This fact is the…”
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Substrate recognition by the human MTH1 protein
Published in Nucleic acids research (2002)“…A nucleotide pool sanitizing enzyme, the human MTH1 protein, hydrolyzes 2-hydroxy-dATP, 8-hydroxy-dATP, and 8-hydroxyd-GTP. To examine the substrate…”
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3‘-C-Branched-Chain-Substituted Nucleosides and Nucleotides as Potent Inhibitors of Mycobacterium t uberculosis Thymidine Monophosphate Kinase
Published in Journal of medicinal chemistry (28-08-2003)“…Thymidine monophosphate kinase (TMPK) of Mycobacterium tuberculosis (TMPKmt) represents an attractive target for blocking the bacterial DNA synthesis. In an…”
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