Helene Munier-Lehmann

Helene Munier-Lehmann

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Helene Munier-Lehmann

Helene Munier-Lehmann

Publications by authors named "Helene Munier-Lehmann"

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1-(Piperidin-3-yl)thymine amides as inhibitors of thymidylate kinase.

J Enzyme Inhib Med Chem 2019 Dec;34(1):1730-1739

Laboratory for Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Ghent University, Ghent, Belgium.

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http://dx.doi.org/10.1080/14756366.2019.1662790DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6920704PMC
December 2019

First-in-class allosteric inhibitors of bacterial IMPDHs.

Eur J Med Chem 2019 Apr 2;167:124-132. Epub 2019 Feb 2.

Institut Pasteur, Unité de Chimie et Biocatalyse, Département de Biologie Structurale et Chimie, CNRS UMR3523, 28 rue du Dr Roux, F-75015, Paris, France. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2019.01.064DOI Listing
April 2019

Screening and evaluation of antiviral compounds against Equid alpha-herpesviruses using an impedance-based cellular assay.

Virology 2019 01 26;526:105-116. Epub 2018 Oct 26.

LABÉO Frank Duncombe, 14280 Saint-Contest, France; Normandie Univ, UNICAEN, BIOTARGEN EA7450, 14280 Saint-Contest, France; Normandie Univ, UNICAEN, ImpedanCELL core facility, SF 4206 ICORE, 14280 Saint-Contest, France. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S00426822183032
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http://dx.doi.org/10.1016/j.virol.2018.10.013DOI Listing
January 2019

Tetrahydro-2-furanyl-2,4(1H,3H)-pyrimidinedione derivatives as novel antibacterial compounds against .

Int J Mycobacteriol 2017 Jan-Mar;6(1):61-69

Department of Bioscience and Bioinformatics, Graduate School of Computer Science and Systems Engineering, Kyushu Institute of Technology, 680-4 Kawazu, Iizuka-shi, Fukuoka 820-8502, Japan; Biomedical Informatics Research and Development Center, Kyushu Institute of Technology, 680-4 Kawazu, Iizuka-shi, Fukuoka 820-8502, Japan.

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http://dx.doi.org/10.4103/2212-5531.201893DOI Listing
July 2018

Structure Guided Lead Generation toward Nonchiral M. tuberculosis Thymidylate Kinase Inhibitors.

J Med Chem 2018 04 15;61(7):2753-2775. Epub 2018 Mar 15.

Laboratory for Medicinal Chemistry (FFW) , Ghent University , Ottergemsesteenweg 460 , B-9000 Gent , Belgium.

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http://dx.doi.org/10.1021/acs.jmedchem.7b01570DOI Listing
April 2018

Synthesis of sulfamide analogues of deoxthymidine monophosphate as potential inhibitors of mycobacterial cell wall biosynthesis.

Carbohydr Res 2018 Mar 11;457:32-40. Epub 2018 Jan 11.

Department of Chemistry, University of Canterbury, Private Bag 4800, Christchurch, 8140, New Zealand; Biomolecular Interaction Centre, University of Canterbury, Private Bag 4800, Christchurch, 8140, New Zealand. Electronic address:

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http://dx.doi.org/10.1016/j.carres.2018.01.001DOI Listing
March 2018

Corrigenda to "Elaboration of a proprietary thymidylate kinase inhibitor motif towards anti-tuberculosis agents" [Bioorg Med Chem 24 (2016) 5172-5182].

Bioorg Med Chem 2017 10 18;25(20):5889. Epub 2017 Aug 18.

Laboratory for Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Ghent University, Ottergemsesteemweg 460, B-9000 Ghent, Belgium. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2017.08.023DOI Listing
October 2017

Elaboration of a proprietary thymidylate kinase inhibitor motif towards anti-tuberculosis agents.

Bioorg Med Chem 2016 11 24;24(21):5172-5182. Epub 2016 Aug 24.

Laboratory for Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Ghent University, Ottergemsesteemweg 460, B-9000 Ghent, Belgium. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2016.08.041DOI Listing
November 2016

Anti-mycobacterial activity of thymine derivatives bearing boron clusters.

Eur J Med Chem 2016 Oct 15;121:71-81. Epub 2016 May 15.

Screening Laboratory, Institute of Medical Biology PAS, 106 Lodowa St, 93-232 Lodz, Poland. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2016.05.030DOI Listing
October 2016

Respiratory syncytial virus infection in macaques is not suppressed by intranasal sprays of pyrimidine biosynthesis inhibitors.

Antiviral Res 2016 Jan 22;125:58-62. Epub 2015 Nov 22.

Institut Pasteur, Unité de Génomique Virale et Vaccination, Paris, France; CNRS, UMR3569, Paris, France. Electronic address:

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http://dx.doi.org/10.1016/j.antiviral.2015.11.006DOI Listing
January 2016

Two classes of bacterial IMPDHs according to their quaternary structures and catalytic properties.

PLoS One 2015 23;10(2):e0116578. Epub 2015 Feb 23.

Institut Pasteur, Unité de Chimie et Biocatalyse, Département de Biologie Structurale et Chimie, 28 rue du Dr Roux, F-75015, Paris, France; Centre Nationale de la Recherche Scientifique, Unité Mixte de Recherche 3523, F-75015, Paris, France.

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0116578PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4338043PMC
December 2015

The Toxicity of a Novel Antifungal Compound Is Modulated by Endoplasmic Reticulum-Associated Protein Degradation Components.

Antimicrob Agents Chemother 2015 Dec 14;60(3):1438-49. Epub 2015 Dec 14.

Institut Pasteur, Unité de Génétique des Interactions Macromoléculaires, Département Génomes et Génétique, Paris, France CNRS UMR3525, Paris, France

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http://aac.asm.org/content/60/3/1438.full.pdf
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http://aac.asm.org/lookup/doi/10.1128/AAC.02239-15
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http://dx.doi.org/10.1128/AAC.02239-15DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4775935PMC
December 2015

Crystallographic studies of two variants of Pseudomonas aeruginosa IMPDH with impaired allosteric regulation.

Acta Crystallogr D Biol Crystallogr 2015 Sep 25;71(Pt 9):1890-9. Epub 2015 Aug 25.

Unité de Chimie et Biocatalyse, Institut Pasteur, 75015 Paris, France.

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http://dx.doi.org/10.1107/S1399004715013115DOI Listing
September 2015

Original 2-(3-alkoxy-1H-pyrazol-1-yl)pyrimidine derivatives as inhibitors of human dihydroorotate dehydrogenase (DHODH).

J Med Chem 2015 Jan 6;58(2):860-77. Epub 2015 Jan 6.

Unité de Chimie et Biocatalyse, Département de Biologie Structurale et Chimie, Institut Pasteur , 28 Rue du Dr. Roux, 75724 Paris Cedex 15, France.

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http://pubs.acs.org/doi/10.1021/jm501446r
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http://dx.doi.org/10.1021/jm501446rDOI Listing
January 2015

[Stimulation of the antiviral innate immune response by pyrimidine biosynthesis inhibitors: a surprise of phenotypic screening].

Med Sci (Paris) 2015 Jan 6;31(1):98-104. Epub 2015 Feb 6.

Unité de chimie et biocatalyse, département de biologie structurale et chimie Institut Pasteur, CNRS UMR3523, 28, rue du Docteur Roux, 75724 Paris Cedex 15, France.

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http://dx.doi.org/10.1051/medsci/20153101019DOI Listing
January 2015

High-throughput screening for broad-spectrum chemical inhibitors of RNA viruses.

J Vis Exp 2014 May 5(87). Epub 2014 May 5.

Unité de Génomique Virale et Vaccination, Virology Department, Institut Pasteur, CNRS UMR3569;

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http://dx.doi.org/10.3791/51222DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4172263PMC
May 2014

Synergy of the antibiotic colistin with echinocandin antifungals in Candida species.

J Antimicrob Chemother 2013 Jun 1;68(6):1285-96. Epub 2013 Feb 1.

Institut Pasteur, Unité Biologie et Pathogénicité Fongiques, Département Génomes et Génétique, F-75015 Paris, France.

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http://dx.doi.org/10.1093/jac/dks538DOI Listing
June 2013

MgATP regulates allostery and fiber formation in IMPDHs.

Structure 2013 Jun 2;21(6):975-85. Epub 2013 May 2.

CNRS, UMR5048, Universités Montpellier 1 et 2; Centre de Biochimie Structurale, 29 rue de Navacelles, F-34090 Montpellier, France.

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http://dx.doi.org/10.1016/j.str.2013.03.011DOI Listing
June 2013

On dihydroorotate dehydrogenases and their inhibitors and uses.

J Med Chem 2013 Apr 20;56(8):3148-67. Epub 2013 Mar 20.

Institut Pasteur, Unité de Chimie et Biocatalyse, Département de Biologie Structurale et Chimie, 28 Rue du Dr. Roux, 75724 Paris Cedex 15, France.

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http://dx.doi.org/10.1021/jm301848wDOI Listing
April 2013

Synthesis and evaluation of 5'-modified thymidines and 5-hydroxymethyl-2'-deoxyuridines as Mycobacterium tuberculosis thymidylate kinase inhibitors.

Bioorg Med Chem 2013 Jan 5;21(1):257-68. Epub 2012 Nov 5.

Laboratory for Medicinal Chemistry, Faculty of Pharmaceutical Sciences (FFW), Ghent University, Harelbekestraat 72, 9000 Ghent, Belgium.

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http://dx.doi.org/10.1016/j.bmc.2012.10.018DOI Listing
January 2013

The composition of the culture medium influences the β-1,3-glucan metabolism of Aspergillus fumigatus and the antifungal activity of inhibitors of β-1,3-glucan synthesis.

Antimicrob Agents Chemother 2012 Jun 5;56(6):3428-31. Epub 2012 Mar 5.

Unité des Aspergillus and Unité de Chimie et Biocatalyse, Institut Pasteur, Paris, France.

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http://dx.doi.org/10.1128/AAC.05661-11DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3370737PMC
June 2012

Synthesis and inhibitory activity of thymidine analogues targeting Mycobacterium tuberculosis thymidine monophosphate kinase.

Bioorg Med Chem 2011 Dec 18;19(24):7603-11. Epub 2011 Oct 18.

Laboratory for Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Ghent University, Harelbekestraat 72, B-9000 Ghent, Belgium.

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http://dx.doi.org/10.1016/j.bmc.2011.10.021DOI Listing
December 2011

Structural and functional characterization of the Mycobacterium tuberculosis uridine monophosphate kinase: insights into the allosteric regulation.

Nucleic Acids Res 2011 Apr 10;39(8):3458-72. Epub 2010 Dec 10.

Atelier de Bio- et Chimie Informatique Structurale, CNRS, UMR5048, Centre de Biochimie Structurale, 29 rue de Navacelles, F-34090 Montpellier, France.

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http://dx.doi.org/10.1093/nar/gkq1250DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3082897PMC
April 2011

Metalloprotease vsm is the major determinant of toxicity for extracellular products of Vibrio splendidus.

Appl Environ Microbiol 2008 Dec 3;74(23):7108-17. Epub 2008 Oct 3.

Institut Pasteur, Unité Plasticité du Génome Bactérien, CNRS URA 2171, Paris, France.

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http://dx.doi.org/10.1128/AEM.01261-08DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2592927PMC
December 2008

Substituted benzyl-pyrimidines targeting thymidine monophosphate kinase of Mycobacterium tuberculosis: synthesis and in vitro anti-mycobacterial activity.

Bioorg Med Chem 2008 Jun 25;16(11):6075-85. Epub 2008 Apr 25.

Unité de Chimie Organique, CNRS, URA2128, Département Biologie Structurale et Chimie, Institut Pasteur, 28, rue du Dr Roux, 75724 Paris cedex 15, France.

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http://dx.doi.org/10.1016/j.bmc.2008.04.045DOI Listing
June 2008

Rational design of 5'-thiourea-substituted alpha-thymidine analogues as thymidine monophosphate kinase inhibitors capable of inhibiting mycobacterial growth.

J Med Chem 2007 Nov 2;50(22):5281-92. Epub 2007 Oct 2.

Laboratory for Medicinal Chemistry (FFW), University of Gent, Harelbekestraat 72, 9000 Ghent, Belgium.

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http://dx.doi.org/10.1021/jm0706158DOI Listing
November 2007

Structural and functional consequences of single amino acid substitutions in the pyrimidine base binding pocket of Escherichia coli CMP kinase.

FEBS J 2007 Jul 3;274(13):3363-73. Epub 2007 Jun 3.

Laboratory of Enzymology and Applied Microbiology, Cantacuzino Institute, Bucharest, Romania.

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http://dx.doi.org/10.1111/j.1742-4658.2007.05870.xDOI Listing
July 2007

Multiple microfermentor battery: a versatile tool for use with automated parallel cultures of microorganisms producing recombinant proteins and for optimization of cultivation protocols.

Appl Environ Microbiol 2006 Aug;72(8):5225-31

Plate-forme 5 Production de Protéines Recombinantes et d'Anticorps, Institut Pasteur, 25-28 rue du Dr. Roux, 75724 Paris cedex 15, France.

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http://dx.doi.org/10.1128/AEM.00239-06DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1538699PMC
August 2006

Unique GMP-binding site in Mycobacterium tuberculosis guanosine monophosphate kinase.

Proteins 2006 Feb;62(2):489-500

Laboratoire d'Enzymologie et Biochimie Structurales, CNRS, Gif sur Yvette, France.

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http://dx.doi.org/10.1002/prot.20662DOI Listing
February 2006

LEA3D: a computer-aided ligand design for structure-based drug design.

J Med Chem 2005 Apr;48(7):2457-68

Centre de Biochimie Structurale (CNRS UMR 5048, INSERM UMR U554), Faculté de Pharmacie, Université Montpellier I, 15, avenue Charles Flahault, 34060 Montpellier Cedex, France.

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http://dx.doi.org/10.1021/jm0492296DOI Listing
April 2005

The crystal structure of Mycobacterium tuberculosis thymidylate kinase in complex with 3'-azidodeoxythymidine monophosphate suggests a mechanism for competitive inhibition.

Biochemistry 2005 Jan;44(1):130-7

LCCP, UMR 5075, IBS-CEA/CNRS/UJF, 41 avenue Jules Horowitz, 38027 Grenoble Cedex 1, France.

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http://dx.doi.org/10.1021/bi0484163DOI Listing
January 2005

Discovery of bicyclic thymidine analogues as selective and high-affinity inhibitors of Mycobacterium tuberculosis thymidine monophosphate kinase.

J Med Chem 2004 Dec;47(25):6187-94

Laboratory for Medicinal Chemistry (FFW), Ghent University, Harelbekestraat 72, 9000 Ghent, Belgium.

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http://dx.doi.org/10.1021/jm040847wDOI Listing
December 2004

Insight into the activation mechanism of Bordetella pertussis adenylate cyclase by calmodulin using fluorescence spectroscopy.

Eur J Biochem 2004 Feb;271(4):821-33

Laboratoire pour l'Utilisation du Rayonnement Electromagnétique, UMR 130 du CNRS, Université Paris-Sud, Orsay, France.

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http://dx.doi.org/10.1111/j.1432-1033.2004.03987.xDOI Listing
February 2004

Structural and dynamic studies on ligand-free adenylate kinase from Mycobacterium tuberculosis revealed a closed conformation that can be related to the reduced catalytic activity.

Biochemistry 2004 Jan;43(1):67-77

Institut National de la Santé et de la Recherche Médicale U350 et Institut Curie-Recherche, Centre Universitaire, Bâtiments 110-112, F-91405 Orsay, France.

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http://dx.doi.org/10.1021/bi0355995DOI Listing
January 2004

Thymidine and thymidine-5'-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase.

Bioorg Med Chem Lett 2003 Sep;13(18):3045-8

Laboratory for Medicinal Chemistry (FFW), Ghent University, Harelbekestraat 72, B-9000 Gent, Belgium.

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http://dx.doi.org/10.1016/s0960-894x(03)00643-7DOI Listing
September 2003

Comparative study of purine and pyrimidine nucleoside analogues acting on the thymidylate kinases of Mycobacterium tuberculosis and of humans.

Chembiochem 2003 Aug;4(8):742-7

Institut Pasteur, Unité de Chimie Organique (URA CNRS 2128) 28, Rue du Dr Roux, 75724 Paris Cedex 15, France.

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http://doi.wiley.com/10.1002/cbic.200300608
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http://dx.doi.org/10.1002/cbic.200300608DOI Listing
August 2003

Reaction of human UMP-CMP kinase with natural and analog substrates.

Eur J Biochem 2003 Apr;270(8):1784-90

Unité de Régulation Enzymatique des Activités Cellulaires, CNRS URA 2185, Institut Pasteur, Paris, France.

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http://dx.doi.org/10.1046/j.1432-1033.2003.03537.xDOI Listing
April 2003

Enzymatic and structural analysis of inhibitors designed against Mycobacterium tuberculosis thymidylate kinase. New insights into the phosphoryl transfer mechanism.

J Biol Chem 2003 Feb 25;278(7):4963-71. Epub 2002 Nov 25.

Unité de Biochimie Structurale, URA 2185 du CNRS, Biologie Structurale et Agents Infectieux, Institut Pasteur, 25 rue du Dr Roux, 75015 Paris, France.

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http://dx.doi.org/10.1074/jbc.M209630200DOI Listing
February 2003

Synthesis and evaluation of thymidine-5'-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase.

Bioorg Med Chem Lett 2002 Oct;12(19):2695-8

Laboratory for Medicinal Chemistry (FFW), Ghent University, Harelbekestraat 72, B-9000 Gent, Belgium.

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http://dx.doi.org/10.1016/s0960-894x(02)00551-6DOI Listing
October 2002

Sugar specificity of bacterial CMP kinases as revealed by crystal structures and mutagenesis of Escherichia coli enzyme.

J Mol Biol 2002 Feb;315(5):1099-110

Laboratoire d'Enzymologie et de Biochimie Structurales, UPR 9063 du CNRS, Gif-sur-Yvette Cedex, 91198, France.

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http://dx.doi.org/10.1006/jmbi.2001.5286DOI Listing
February 2002

Nucleoside analogues as inhibitors of thymidylate kinases: possible therapeutic applications.

Chembiochem 2002 Jan;3(1):108-10

Institut Pasteur, Unite de Chimie Organique, 28, Rue du Dr Roux, 75724 Paris Cedex 15, France.

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http://dx.doi.org/10.1002/1439-7633(20020104)3:1<108::AID-CBIC108>3.0.CO;2-BDOI Listing
January 2002