ChemBioScreen
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ÉQUIPES


Biochimie et Criblage



Directeur d’équipe


Hélène Munier-Lehmann

Laboratoire de rattachement


Unité de Chimie et Biocatalyse

Directeur du laboratoire


Sylvie Pochet

Affiliation


Institut Pasteur et CNRS UMR3523

Thèmes principaux


Maladies infectieuses
Enzymes du métabolisme des nucléotides


Plateformes associées


Brevets / Publications / Communications


Publications (2011-2016) :

1          Adamska, A., Rumijowska-Galewicz, A., Ruszczynska, A., Studzinska, M., Jablonska, A., Paradowska, E., Bulska, E., Munier-Lehmann, H., Dziadek, J., Lesnikowski, Z. J. and Olejniczak, A. B. (2016) Anti-mycobacterial activity of thymine derivatives bearing boron clusters. Eur. J. Med. Chem. 121, 71-81

2          Grandin, C., Hourani, M. L., Janin, Y. L., Dauzonne, D., Munier-Lehmann, H., Paturet, A., Taborik, F., Vabret, A., Contamin, H., Tangy, F. and Vidalain, P. O. (2016) Respiratory syncytial virus infection in macaques is not suppressed by intranasal sprays of pyrimidine biosynthesis inhibitors. Antiviral Research. 125, 58-62

3          Laskaris, P., Atrouni, A., Calera, J. A., d'Enfert, C., Munier-Lehmann, H., Cavaillon, J. M., Latge, J. P. and Ibrahim-Granet, O. (2016) Administration of zinc chelators improves survival of mice infected with Aspergillus fumigatus both in monotherapy and in combination with caspofungin. Antimicrobial Agents and Chemotherapy 60, 5631-5639

4          Raj, S., Krishnan, K., Askew, D. S., Helynck, O., Suzanne, P., Lesnard, A., Rault, S., Zeidler, U., d'Enfert, C., Latge, J. P., Munier-Lehmann, H. and Saveanu, C. (2016) The Toxicity of a Novel Antifungal Compound Is Modulated by Endoplasmic Reticulum-Associated Protein Degradation Components. Antimicrobial Agents and Chemotherapy 60, 1438-1449

5          Song, L., Risseeuw, M. D., Froeyen, M., Karalic, I., Goeman, J., Cappoen, D., Van der Eycken, J., Cos, P., Munier-Lehmann, H. and Van Calenbergh, S. (2016) Elaboration of a proprietary thymidylate kinase inhibitor motif towards anti-tuberculosis agents. Bioorganic & Medicinal Chemistry 24, 5172-5182

6          Alexandre, T., Raynal, B. and Munier-Lehmann, H. (2015) Two classes of bacterial IMPDHs according to their quaternary structures and catalytic properties PloS one. 10, e0116578

7          Labesse, G., Alexandre, T., Gelin, M., Haouz, A. and Munier-Lehmann, H. (2015) Crystallographic studies of two variants of Pseudomonas aeruginosa IMPDH with impaired allosteric regulation. Acta Crystallogr. D Biol. Crystallogr. 71, 1890-1899

8          Lucas-Hourani, M., Munier-Lehmann, H., El Mazouni, F., Malmquist, N. A., Harpon, J., Coutant, E. P., Guillou, S., Helynck, O., Noel, A., Scherf, A., Phillips, M. A., Tangy, F., Vidalain, P. O. and Janin, Y. L. (2015) Original 2-(3-Alkoxy-1H-pyrazol-1-yl)azines Inhibitors of Human Dihydroorotate Dehydrogenase (DHODH). J. Med. Chem. 58, 5579-5598

9          Munier-Lehmann, H., Lucas-Hourani, M., Guillou, S., Helynck, O., Zanghi, G., Noel, A., Tangy, F., Vidalain, P. O. and Janin, Y. L. (2015) Original 2-(3-Alkoxy-1H-pyrazol-1-yl)pyrimidine Derivatives as Inhibitors of Human Dihydroorotate Dehydrogenase (DHODH). J. Med. Chem. 58, 860-877

10        Vidalain, P. O., Lucas-Hourani, M., Helynck, O., Tangy, F. and Munier-Lehmann, H. (2015) [Stimulation of the antiviral innate immune response by pyrimidine biosynthesis inhibitors: a surprise of phenotypic screening]. Medecine sciences : M/S. 31, 98-104

11        Lucas-Hourani, M., Munier-Lehmann, H., Helynck, O., Komarova, A., Despres, P., Tangy, F. and Vidalain, P. O. (2014) High-throughput Screening for Broad-spectrum Chemical Inhibitors of RNA Viruses. J. Vis. Exp. 87, e51222

12        Aulner, N., Danckaert, A., Rouault-Hardoin, E., Desrivot, J., Helynck, O., Commere, P. H., Munier-Lehmann, H., Spaeth, G. F., Shorte, S. L., Milon, G. and Prina, E. (2013) High Content Analysis of Primary Macrophages Hosting Proliferating Amastigotes: Application to Anti-leishmanial Drug Discovery. PLoS Negl. Trop. Dis. 7, e2154

13        Carre, C., Jacquier, C., Bouge, A. L., de Chaumont, F., Besnard-Guerin, C., Thomassin, H., Pidoux, J., Da Silva, B., Chalatsi, E., Zahra, S., Olivo-Marin, J. C., Munier-Lehmann, H. and Antoniewski, C. (2013) AutomiG, a Biosensor to Detect Alterations in miRNA Biogenesis and in Small RNA Silencing Guided by Perfect Target Complementarity. PloS one. 8, e74296

14        Labesse, G., Alexandre, T., Vaupre, L., Salard-Arnaud, I., Him, J. L., Raynal, B., Bron, P. and Munier-Lehmann, H. (2013) MgATP Regulates Allostery and Fiber Formation in IMPDHs. Structure. 21, 975-985

15        Lucas-Hourani, M., Dauzonne, D., Jorda, P., Cousin, G., Lupan, A., Helynck, O., Caignard, G., Janvier, G., Andre-Leroux, G., Khiar, S., Escriou, N., Despres, P., Jacob, Y., Tangy, F., Munier-Lehmann, H. and Vidalain, P. O. (2013) Inhibition of Pyrimidine Biosynthesis Pathway Suppresses Viral Growth through Innate Immunity. PLoS Pathog. 9, e1003678

16        Lucas-Hourani, M., Lupan, A., Desprès, P., Thoret, S., Pamlard, O., Dubois, J., Guillou, C., Tangy, F., Vidalain, P. O. and Munier-Lehmann, H. (2013) A phenotypic assay to identify chikungunya virus inhibitors targeting the non-structural protein nsP2. Journal of Biomolecular Screening. 18, 172-179

17       Munier-Lehmann, H., Vidalain, P. O., Tangy, F. and Janin, Y. L. (2013) On dihydroorotate dehydrogenases and their inhibitors and uses. J. Med. Chem. 56, 3148-3167

18        Toti, K. S., Verbeke, F., Risseeuw, M. D., Frecer, V., Munier-Lehmann, H. and Van Calenbergh, S. (2013) Synthesis and evaluation of 5'-modified thymidines and 5-hydroxymethyl-2'-deoxyuridines as Mycobacterium tuberculosis thymidylate kinase inhibitors. Bioorganic & Medicinal Chemistry. 21, 257-268

19        Zeidler, U., Bougnoux, M. E., Lupan, A., Helynck, O., Doyen, A., Garcia, Z., Sertour, N., Clavaud, C., Saveanu, C., Munier-Lehmann, H. and d'Enfert, C. (2013) Synergy of the antibiotic colistin with echinocandin antifungals in Candida species. J. Antimicrob. Chemother. 68, 1285-1296

20        Clavaud, C., Beauvais, A., Barbin, L., Munier-Lehmann, H. and Latgé, J.-P. (2012) 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 tested. Antimicrobial Agents and Chemotherapy. 56, 3428-3431

21        Kogler, M., Busson, R., De Jonghe, S., Rozenski, J., Van Belle, K., Louat, T., Munier-Lehmann, H. and Herdewijn, P. (2012) Synthesis and Evaluation of 6-Aza-2'-deoxyuridine Monophosphate Analogs as Inhibitors of Thymidylate Synthases, and as Substrates or Inhibitors of Thymidine Monophosphate Kinase in Mycobacterium tuberculosis. Chemistry & Biodiversity. 9, 536-556

22        Van Calenbergh, S., Pochet, S. and Munier-Lehmann, H. (2012) Drug design and identification of potent leads against Mycobacterium tuberculosis thymidine monophosphate kinase. Current Topics in Medicinal Chemistry. 12, 694-705

23        Labesse, G., Benkali, K., Salard-Arnaud, I., Gilles, A. M. and Munier-Lehmann, H. (2011) Structural and functional characterization of the Mycobacterium tuberculosis uridine monophosphate kinase: insights into the allosteric regulation. Nucleic Acids Research. 39, 3458-3472

24        Van Poecke, S., Munier-Lehmann, H., Helynck, O., Froeyen, M. and Van Calenbergh, S. (2011) Synthesis and inhibitory activity of thymidine analogues targeting Mycobacterium tuberculosis thymidine monophosphate kinase. Bioorganic & Medicinal Chemistry. 19, 7603-7611


Brevet (2011-2016)

1          Janin, Y. L., Guillou, S., Lucas-Hourani, M., Munier-Lehmann, H., Noel, A., Salanouve, E., Tangy, F. and Vidalain, P. O. (2014) Pyrazole derivatives as dihydroorotate dehydrogenase (DHODH) inhibitors. EP14 305 516.8.