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Groupleader: Elisabeth Davioud-Charvet
Elisabeth Davioud-Charvet
Synthesis and mechanism of cytotoxic and antiparasitic drugs that act by perturbing the redox equilibrium of their target cells
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Born in 1961
Academic Training and Positions
1979-1984 Pharmacy School, Lille II University, France
1985 Approbation in Pharmacochemistry
1988 PhD degree in Pharmacochemistry, Paris XI University, France
1989 - 1990 Postdoctoral Fellow in Biochemistry, Paris 6 University, France
1990 - 1994 Junior scientist at CNRS CR2, Laboratory of Biological Chemistry, Paris 6 University
1995 - 2001 Senior scientist at CNRS CR1, Laboratory of Chemistry of Biomolecules
co-group leader of the Team “Antiparasitic drugs”
1997 Habilitation, Lille II University, France
2001 - 2002 Visiting Research Scientist, Ann Arbor, Michigan University, USA,
College of Pharmacy (Prof. Dr. G. Kenyon) and Medical School (Prof. Dr. C. Williams Jr)
since 2001 Research Director DR2 at CNRS
since 2002 Junior Group Leader at the Heidelberg University Biochemistry Center (BZH)
since 2005 Group Leader (project B14) in the collaborative research center
Sonderforschungsbereich 544 entitled "Control of tropical infectious diseases”,
Heidelberg University
since 2008 Group Leader of the bioorganic & medicinal chemistry Team, in the research unit
UMR7509 CNRS-UdS, European School of Chemistry of Polymers and Materials
(ECPM), Strasbourg University, in double affiliation with Heidelberg University at
Biochemie-Zentrum Heidelberg (BZH).
since 2008 French representative of the COST Action CM0801 “New drugs for neglected
diseases” of the EU.
Research
New drugs against parasitic and cancer diseases are urgently and continuously needed. The aim of our interdisciplinary research is to substantiate disulfide reductase inhibitors as antiparasitic and cytostatic agents. Such compounds are active per se but, in addition, they can reverse thiol-based resistance against other drugs in parasites and tumour cells. Our strategy is based on the synthesis of mechanism-based inhibitors and subversive substrates of the selected targets, namely the glutathione reductases (GR) of the malarial parasite Plasmodium falciparum and man, the thioredoxin reductases (TrxR) of P. falciparum and man, and trypanothione reductase (TR) from Trypanosoma cruzi. The preparation of focused chemical libraries are developed in order to introduce structural diversity and to optimize the most potent inhibitors of the respective enzymes, using both classical medicinal chemistry and parallel synthesis. With the expectation of synergistic effect, double-headed prodrugs are prepared by linking bioreversibly (or not) a disulfide reductase inhibitor to a drug that is known to be directed to a specific subcellular compartment. Their effects on malarial parasites and on human cancer cell lines will be studied, with special emphasis on strains and cell lines that are resistant towards commonly used drugs in chemotherapy, i.e. the antimalarial chloroquine and the anticancer agent cis-dichlorodiamminoplatinum. These inhibitors might become of interest as antimalarial and/or as anticancer agents. The lead compounds will be produced by chemical bulk procedures and serve as candidates for in vivo experiments using mouse models. Validation of the selected targets will be achieved by correlating the molecular mode of action and the in vivo activities of the drug candidates, in particular by studying the modifications of enzyme structure and function exerted by the novel lead compounds. New compounds will be selected as potential antiparasitic or cytostatic drug candidates by the following criteria: high antiparasitic or antineoplastic activity, low toxicity against normal human cells, decrease of intracellular glutathione, thioredoxin or trypanothione levels, reversal of drug resistance, and tolerance by blood cells of persons with G6PD deficiency.
Download BZH Report Davioud-Charvet 2008-2010.
Publications
A plant-derived flavonoid inhibits entry of all HCV genotypes into human hepatocytes. Gastroenterology. 143(1):213-222.Haid S, Novodomská A, Gentzsch J, Grethe C, Geuenich S, Bankwitz D, Chhatwal P, Jannack B, Hennebelle T, Bailleul F, Keppler OT, Poenisch M, Bartenschlager R, Hernandez C, Lemasson M, Rosenberg AR, Wong-Staal F, Davioud-Charvet E, Pietschmann T. (2012)
Exploring the trifluoromenadione core as a template to design antimalarial redox-active agents interacting with glutathione reductase. Org Biomol Chem. 10(24):4795-806.Lanfranchi DA, Belorgey D, Müller T, Vezin H, Lanzer M, Davioud-Charvet E. (2012)
Glutathione reductase-catalyzed cascade of redox reactions to bioactivate potent antimalarial 1,4-naphthoquinones--a new strategy to combat malarial parasites. J Am Chem Soc. 133(30):11557-71.Müller T, Johann L, Jannack B, Brückner M, Lanfranchi DA, Bauer H, Sanchez C, Yardley V, Deregnaucourt C, Schrével J, Lanzer M, Schirmer RH, Davioud-Charvet E (2011)
Subversive substrates of glutathione reductases from Plasmodium falciparum-infected red blood cells as antimalarial agents. In: Apicomplexan parasites – Molecular approaches toward targeted drug development (Ed.: K. Becker), volume 2, 2011, from the series Drug Discovery in Infectious Diseases, (Ed.: P. M. Selzer), Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim, ISBN 978-3-527-32731-7. Davioud-Charvet E, Lanfranchi DA. (2011)
Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases: interaction with DNA. J Med Chem. 53(8):3214-26.Wenzel NI, Chavain N, Wang Y, Friebolin W, Maes L, Pradines B, Lanzer M, Yardley V, Brun R, Herold-Mende C, Biot C, Tóth K, Davioud-Charvet E. (2010)
Inhibition of hepatitis C virus entry by a plant-derived flavone. J. Hepatol. Suppl. 1, 52:S293.Haid S, Gentzsch J, Jannack B, Bailleul F, Davioud-Charvet E, Pietschmann T. (2010)
Antimalarial Antimalarial activities of ferroquine conjugates with either glutathione reductase inhibitors or glutathione depletors via a hydrolyzable amide linker. Bioorg. Med. Chem. 17:8048--8059."Chavain N, Davioud-Charvet E, Trivelli X, Mbeki L, Rottmann M, Brun R, Biot C. (2009)
Unsaturated Mannich bases active against multidrug-resistant Trypanosoma brucei brucei strains. ChemMedChem, 4(3), 339–351. https://doi.org/10.1002/cmdc.200800360Wenzel, I. N., Wong, P. E., Maes, L., Müller, T. J., Krauth-Siegel, R. L., Barrett, M. P., & Davioud-Charvet, E. (2009)
A sugar-modified phosphole gold complex with antiproliferative properties acting as a thioredoxin reductase inhibitor in MCF-7 cells. ChemMedChem. 3:1667–70.Viry E, Battaglia E, Deborde V, Müller T, Réau R, Davioud-Charvet E, Bagrel D. (2008)
Antimalarial dual drugs based on potent inhibitors of glutathione reductase from Plasmodium falciparum. J Med Chem. 51(5):1260–77.Friebolin W, Jannack B, Wenzel N, Furrer J, Oeser T, Sanchez CP, Lanzer M, Yardley V, Becker K, Davioud-Charvet E. (2008)
Synthesis of photo-reactive naphthoquinones for photoaffinity labeling of glutathione reductases. Flavins and Flavoproteins 2008 (Frago S, Gómez-Moreno C, Medina M eds) Prensas Universitarias Zaragoza. 16:443–52.Müller T, Müller TJJ, Davioud-Charvet E. (2008)
The aza-analogues of 1,4-naphthoquinones are potent substrates and inhibitors of plasmodial thioredoxin and glutathione reductases and of human erythrocyte glutathione reductase. Org. Biomol. Chem. 6(15):2731–42.Morin C, Besset T, Moutet JC, Fayolle M, Brückner M, Limosin D, Becker K, Davioud-Charvet E. (2008)
Schistosome redox balance and thioredoxin glutathione reductase: An essential parasite enzyme and novel drug target. PLoS Med. 4(6):e206:1–16.Kuntz, AN, Davioud-Charvet, E, Dessolin, J, Sayed, AA, Califf, LL, Arnér, ESJ, Williams DL. (2007)
A fluoro analogue of the menadione derivative 6-[2’-(3’-Methyl)-1’,4’-naphthoquinolyl]hexanoic acid is a suicide substrate of glutathione reductase. Crystal structure of the alkylated human enzyme. J. Am. Chem. Soc. 128:10784–94.Bauer H, Fritz-Wolf K, Winzer A, Kühner S, Little S, Yardley V, Vezin H, Palfey B, Schirmer H, Davioud-Charvet E. (2006)
Specific inhibitors of Plasmodium falciparum thioredoxin reductase as potential antimalarial agents. Bioorg. Med. Chem. Lett. 16:2283–92.Andricopulo AD, Akoachere MB, Krogh R, Nickel C, McLeish MJ, Kenyon GL, Arscott LD, Williams Jr, H, Davioud-Charvet E, Becker K. (2006)
Undressing of phosphine gold(I) complexes as irreversible inhibitors of human disulfide reductases. Angew. Chem. Int. Ed. Engl. 45:1881–86.Urig S., Fritz-Wolf K., Réau R., Herold-Mende C., Tóth K., Davioud-Charvet E., Becker K. (2006)
Irreversible inactivation of trypanothione reductase by unsaturated mannich bases: a divinyl ketone as key intermediate. J Med Chem. 48(23):7400-10.Lee B, Bauer H, Melchers J, Ruppert T, Rattray L, Yardley V, Davioud-Charvet E, Krauth-Siegel RL. (2005)
Mass Spectrometric analysis of human glutathione reductase modified by a gold-phosphole inhibitor. Flavins and Flavoproteins 2005 (Nishino T, Miura R, Tanokura M, Fukui K Ed.) ArchiTect Inc Tokyo. 325–30.Koncarevic S, Deponte M, Fritz-Wolf K, Meyer M, Urig S, Fischer M, Réau R, Davioud-Charvet E, Becker K. (2005)
Mechanistic studies of a novel, highly potent gold-phosphole inhibitor of human glutathione reductase. J. Biol. Chem. 280, 20628–37.Deponte M, Urig S, Arscott LD, Fritz-Wolf K, Réau R, Herold-Mende C, Koncarevic S, Meyer M, Davioud-Charvet E, Ballou DP, Williams CH, Becker K. (2005)
Specific Inhibitors of Plasmodium falciparum thioredoxin reductase. Flavins and Flavoproteins 2005 (Nishino T, Miura R, Tanokura M, Fukui K Ed.) ArchiTect Inc Tokyo. 883–88.Andricopulo, A. D., Akoachere, M. B., Krogh, R., Nickel, C., McLeish, M. J., Davioud-Charvet, E., Kenyon, G. L., Arscott, L. D., Williams, Jr., C. H., Becker, K. (2005)
Synthesis of 5-nitro-2-furancarbohydrazides and their cis-diamminedichloroplatinum complexes as bitopic and irreversible human thioredoxin reductase inhibitors. J Med Chem. 48(22):7024-39.Millet, R., Urig, S., Jacob, J., Amtmann, E., Moulinoux, J. P., Gromer, S., Becker, K., & Davioud-Charvet, E. (2005)
Trypanothione reductase and other flavoenzymes as targets of antiparasitic drugs. Flavins and Flavoproteins 2005 (Nishino T, Miura R, Tanokura M, Fukui K Ed.) ArchiTect Inc Tokyo. 867–76.Krauth-Siegel RL, Davioud-Charvet E. (2005)
5-substituted tetrazoles as bioisosteres of carboxylic acids. Bioisosterism and mechanistic studies on glutathione reductase inhibitors as antimalarials. J Med Chem. 47(24):5972-83.Biot C, Bauer H, Schirmer RH, Davioud-Charvet E. (2004)
Double-drug development against antioxidant enzymes from Plasmodium falciparum. Redox Report 8:280–83.Biot C, Dessolin J, Grellier P, Davioud-Charvet E. (2003)
Mechanism-based inactivation of thioredoxin reductase from Plasmodium falciparum by Mannich bases. Implications for cytotoxicity. Biochemistry 42(45):13319-13330.Davioud-Charvet E, McLeish MJ, Veine DM, Giegel D, Arscott LD, Andricopulo AD, Becker K, Müller S, Schirmer RH, Williams CH Jr, Kenyon GL. (2003)
Screening of P. falciparum iron superoxide dismutase inhibitors and accuracy of the SOD-assays. Bioorg. Med. Chem. 11:4941–44.Soulère L, Delplace P, Davioud-Charvet E, Py S, Sergheraert C, Hoffmann P, Périé J, Ricard I, Dive D. (2003)
A novel mechanism for inhibition of HIV-1 reverse transcriptase. Bioorg. Chem. 30:443–58.Skillman AG, Maurer KW, Roe DC, Stauber MJ, Eargle D, Ewing TJ, Muscate A, Davioud-Charvet E, Medaglia MV, Fisher RJ, Arnold E, Gao HQ, Buckheit R, Boyer PL, Hughes SH, Kuntz ID, Kenyon GL. (2002)
Antitrypanosomal activities and cytotoxicity of 5-nitro-2-furancarbohydrazides. Bioorg. Med. Chem. Lett. 12, 3601–3604.Millet, R., Maes, L., Landry, V., Sergheraert, C., Davioud-Charvet, E. (2002)
Comparison of the inhibition of human and Trypanosoma cruzi prolyl endopeptidases. Bioorg. Med. Chem. 10:1719–29.Vendeville S, Goossens F, Debreu-Fontaine MA, Landry V, Davioud-Charvet E, Grellier P, Scharpe S, Sergheraert C. (2002)
Disulfide reductases – current developments. Flavins and Flavoproteins 2002 (Chapman, S.K., Perham, R.N., Scrutton N.S., Eds.) Agency for Scientific Publications Berlin. 803–15.Irmler A, Bechthold A, Davioud-Charvet E, Hofmann V, Réau R, Gromer S, Schirmer RH, Becker K. (2002)
2- and 3-substituted-1,4-naphthoquinone derivatives as subversive substrates of trypanothione reductase and lipoamide dehydrogenase from Trypanosoma cruzi: synthesis and correlation between redox-cycling activities and in vitro cytotoxicity. J. Med. Chem. 44:548–65.Salmon-Chemin L, Buisine E, Yardley V, Kohler S, Debreu MA, Landry V, Sergheraert C, Croft SL, Krauth-Siegel LR, Davioud-Charvet E. (2001)
A prodrug form of a Plasmodium falciparum glutathione reductase inhibitor conjugated with a 4-anilinoquinoline. J. Med. Chem. 44:4268–76.Davioud-Charvet E, Delarue S, Biot C, Schwöbel B, Böhme CC, Müssigbrodt A, Maes L, Sergheraert C, Grellier P, Schirmer RH, Becker K. (2001)
Antiplasmodial activity and cytotoxicity of bis- and triquinolines with linear or cyclic amino linkers. J. Med. Chem. 44, 1658–65.Girault S, Grellier P, Berecibar A, Maes L, Lemière P, Mouray E, Davioud-Charvet E, Sergheraert C. (2001)
Bromination studies of the 2,3-dimethylnaphthazarin core allowing easy access to naphthazarin derivatives. J. Org. Chem. 66:5616–19.Dessolin J, Biot C, Davioud-Charvet E. (2001)
Potent and specific inhibitors of trypanothione reductase from Trypanosoma cruzi: bis(2-aminodiphenylsulfides) for fluorescent labeling studies. Bioorg. Med. Chem. 9:837–46.Girault S, Davioud-Charvet E, Maes L, Dubremetz J-F, Debreu M-A, Landry V, Sergheraert C. (2001)
Trypanosoma cruzi prolyl oligopeptidase Tc80 is involved in nonphagocytic mammalian cell invasion by trypomastigotes. J. Biol. Chem. 276:47078–86.Grellier P, Vendeville S, Joyeau R, Bastos IM, Drobecq H, Frappier F, Teixeira AR, Schrevel J, Davioud-Charvet E, Sergheraert C, Santana JM. (2001)
Antimalarial, antitrypanosomal, antileishmanial activities and cytotoxicity of bis(9-amino-6-chloro-2-methoxyacridines): influence of the linker. J. Med. Chem. 43:2646–54.Girault S, Grellier P, Berecibar A, Maes L, Mouray E, Lemière P, Debreu MA, Davioud-Charvet E, Sergheraert C. (2000)
Parallel synthesis of a library of 1,4–naphthoquinones and automated screening of potential inhibitors of trypanothione reductase from Trypanosoma cruzi. Bioorg. Med. Chem. Lett. 10:631–35.Salmon-Chemin L, Lemaire A, De Freitas S, Deprez B, Sergheraert C, Davioud-Charvet E. (2000)
The conserved redox-sensitive cysteine of the DNA-binding region in the c-Rel protein is involved in the regulation of the phosphorylation of the protein. Biochem. J. 352:583–91.Glineur C, Davioud-Charvet E, Vandenbunder B. (2000)
Trypanothione reductase inhibition / trypanocidal activity relationships in a 1,4-bis(3-aminopropyl)piperazine series. Bioorg. Med. Chem. 8:95–103.Bonnet B, Soullez D, Girault S, Maes L, Landry V, Davioud-Charvet E, Sergheraert C. (2000)
Automated Parellel Synthesis of a tetrahydroisoquinolin-based library: potential prolyl endopeptidase inhibitors. Bioorg. Med. Chem. Lett. 9:437–42.Vendeville S, Bourel L, Davioud-Charvet E, Grellier P, Deprez B, Sergheraert C. (1999)
Evidence for the co-existence of glutathione reductase and trypanothione reductase in the nontrypanosomatid Euglenozoa: Euglena gracilis Z. FEBS Lett. 442:29–33.Montrichard F, Le Guen F, Laval-Martin DL, Davioud-Charvet E. (1999)
Synthesis of alternative substrates for trypanothione reductase and thioredoxin reductase: an inexpensive microtiter colorimetric assay for inhibitor screening. Anal. Biochem. 268:1–8.Davioud-Charvet E, Becker K, Landry V, Gromer S, Loge C, Sergheraert C. (1999)
Synthesis of polyamine derivatives for the preparation of affinity chromatography columns for the search of new Trypanosoma cruzi targets. Bioorg. Med. Chem. Lett. 9:1567–72.Davioud-Charvet E, Berecibar A, Girault S, Landry V, Drobecq H, Sergheraert C. (1999)
Exploring the trifluoromenadione core as a template to design antimalarial redox-active agents interacting with glutathione reductase. Org Biomol Chem. 10(24):4795-806.Lanfranchi DA, Belorgey D, Müller T, Vezin H, Lanzer M, Davioud-Charvet E. (2012)
Glutathione reductase-catalyzed cascade of redox reactions to bioactivate potent antimalarial 1,4-naphthoquinones--a new strategy to combat malarial parasites. J Am Chem Soc. 133(30):11557-71.Müller T, Johann L, Jannack B, Brückner M, Lanfranchi DA, Bauer H, Sanchez C, Yardley V, Deregnaucourt C, Schrével J, Lanzer M, Schirmer RH, Davioud-Charvet E (2011)
Subversive substrates of glutathione reductases from Plasmodium falciparum-infected red blood cells as antimalarial agents. In: Apicomplexan parasites – Molecular approaches toward targeted drug development (Ed.: K. Becker), volume 2, 2011, from the series Drug Discovery in Infectious Diseases, (Ed.: P. M. Selzer), Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim, ISBN 978-3-527-32731-7. Davioud-Charvet E, Lanfranchi DA. (2011)
Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases: interaction with DNA. J Med Chem. 53(8):3214-26.Wenzel NI, Chavain N, Wang Y, Friebolin W, Maes L, Pradines B, Lanzer M, Yardley V, Brun R, Herold-Mende C, Biot C, Tóth K, Davioud-Charvet E. (2010)
Inhibition of hepatitis C virus entry by a plant-derived flavone. J. Hepatol. Suppl. 1, 52:S293.Haid S, Gentzsch J, Jannack B, Bailleul F, Davioud-Charvet E, Pietschmann T. (2010)
Antimalarial Antimalarial activities of ferroquine conjugates with either glutathione reductase inhibitors or glutathione depletors via a hydrolyzable amide linker. Bioorg. Med. Chem. 17:8048--8059."Chavain N, Davioud-Charvet E, Trivelli X, Mbeki L, Rottmann M, Brun R, Biot C. (2009)
Unsaturated Mannich bases active against multidrug-resistant Trypanosoma brucei brucei strains. ChemMedChem, 4(3), 339–351. https://doi.org/10.1002/cmdc.200800360Wenzel, I. N., Wong, P. E., Maes, L., Müller, T. J., Krauth-Siegel, R. L., Barrett, M. P., & Davioud-Charvet, E. (2009)
A sugar-modified phosphole gold complex with antiproliferative properties acting as a thioredoxin reductase inhibitor in MCF-7 cells. ChemMedChem. 3:1667–70.Viry E, Battaglia E, Deborde V, Müller T, Réau R, Davioud-Charvet E, Bagrel D. (2008)
Antimalarial dual drugs based on potent inhibitors of glutathione reductase from Plasmodium falciparum. J Med Chem. 51(5):1260–77.Friebolin W, Jannack B, Wenzel N, Furrer J, Oeser T, Sanchez CP, Lanzer M, Yardley V, Becker K, Davioud-Charvet E. (2008)
Synthesis of photo-reactive naphthoquinones for photoaffinity labeling of glutathione reductases. Flavins and Flavoproteins 2008 (Frago S, Gómez-Moreno C, Medina M eds) Prensas Universitarias Zaragoza. 16:443–52.Müller T, Müller TJJ, Davioud-Charvet E. (2008)
The aza-analogues of 1,4-naphthoquinones are potent substrates and inhibitors of plasmodial thioredoxin and glutathione reductases and of human erythrocyte glutathione reductase. Org. Biomol. Chem. 6(15):2731–42.Morin C, Besset T, Moutet JC, Fayolle M, Brückner M, Limosin D, Becker K, Davioud-Charvet E. (2008)
Schistosome redox balance and thioredoxin glutathione reductase: An essential parasite enzyme and novel drug target. PLoS Med. 4(6):e206:1–16.Kuntz, AN, Davioud-Charvet, E, Dessolin, J, Sayed, AA, Califf, LL, Arnér, ESJ, Williams DL. (2007)
A fluoro analogue of the menadione derivative 6-[2’-(3’-Methyl)-1’,4’-naphthoquinolyl]hexanoic acid is a suicide substrate of glutathione reductase. Crystal structure of the alkylated human enzyme. J. Am. Chem. Soc. 128:10784–94.Bauer H, Fritz-Wolf K, Winzer A, Kühner S, Little S, Yardley V, Vezin H, Palfey B, Schirmer H, Davioud-Charvet E. (2006)
Specific inhibitors of Plasmodium falciparum thioredoxin reductase as potential antimalarial agents. Bioorg. Med. Chem. Lett. 16:2283–92.Andricopulo AD, Akoachere MB, Krogh R, Nickel C, McLeish MJ, Kenyon GL, Arscott LD, Williams Jr, H, Davioud-Charvet E, Becker K. (2006)
Undressing of phosphine gold(I) complexes as irreversible inhibitors of human disulfide reductases. Angew. Chem. Int. Ed. Engl. 45:1881–86.Urig S., Fritz-Wolf K., Réau R., Herold-Mende C., Tóth K., Davioud-Charvet E., Becker K. (2006)
Irreversible inactivation of trypanothione reductase by unsaturated mannich bases: a divinyl ketone as key intermediate. J Med Chem. 48(23):7400-10.Lee B, Bauer H, Melchers J, Ruppert T, Rattray L, Yardley V, Davioud-Charvet E, Krauth-Siegel RL. (2005)
Mass Spectrometric analysis of human glutathione reductase modified by a gold-phosphole inhibitor. Flavins and Flavoproteins 2005 (Nishino T, Miura R, Tanokura M, Fukui K Ed.) ArchiTect Inc Tokyo. 325–30.Koncarevic S, Deponte M, Fritz-Wolf K, Meyer M, Urig S, Fischer M, Réau R, Davioud-Charvet E, Becker K. (2005)
Mechanistic studies of a novel, highly potent gold-phosphole inhibitor of human glutathione reductase. J. Biol. Chem. 280, 20628–37.Deponte M, Urig S, Arscott LD, Fritz-Wolf K, Réau R, Herold-Mende C, Koncarevic S, Meyer M, Davioud-Charvet E, Ballou DP, Williams CH, Becker K. (2005)
Specific Inhibitors of Plasmodium falciparum thioredoxin reductase. Flavins and Flavoproteins 2005 (Nishino T, Miura R, Tanokura M, Fukui K Ed.) ArchiTect Inc Tokyo. 883–88.Andricopulo, A. D., Akoachere, M. B., Krogh, R., Nickel, C., McLeish, M. J., Davioud-Charvet, E., Kenyon, G. L., Arscott, L. D., Williams, Jr., C. H., Becker, K. (2005)
Synthesis of 5-nitro-2-furancarbohydrazides and their cis-diamminedichloroplatinum complexes as bitopic and irreversible human thioredoxin reductase inhibitors. J Med Chem. 48(22):7024-39.Millet, R., Urig, S., Jacob, J., Amtmann, E., Moulinoux, J. P., Gromer, S., Becker, K., & Davioud-Charvet, E. (2005)
Trypanothione reductase and other flavoenzymes as targets of antiparasitic drugs. Flavins and Flavoproteins 2005 (Nishino T, Miura R, Tanokura M, Fukui K Ed.) ArchiTect Inc Tokyo. 867–76.Krauth-Siegel RL, Davioud-Charvet E. (2005)
5-substituted tetrazoles as bioisosteres of carboxylic acids. Bioisosterism and mechanistic studies on glutathione reductase inhibitors as antimalarials. J Med Chem. 47(24):5972-83.Biot C, Bauer H, Schirmer RH, Davioud-Charvet E. (2004)
Double-drug development against antioxidant enzymes from Plasmodium falciparum. Redox Report 8:280–83.Biot C, Dessolin J, Grellier P, Davioud-Charvet E. (2003)
Mechanism-based inactivation of thioredoxin reductase from Plasmodium falciparum by Mannich bases. Implications for cytotoxicity. Biochemistry 42(45):13319-13330.Davioud-Charvet E, McLeish MJ, Veine DM, Giegel D, Arscott LD, Andricopulo AD, Becker K, Müller S, Schirmer RH, Williams CH Jr, Kenyon GL. (2003)
Screening of P. falciparum iron superoxide dismutase inhibitors and accuracy of the SOD-assays. Bioorg. Med. Chem. 11:4941–44.Soulère L, Delplace P, Davioud-Charvet E, Py S, Sergheraert C, Hoffmann P, Périé J, Ricard I, Dive D. (2003)
A novel mechanism for inhibition of HIV-1 reverse transcriptase. Bioorg. Chem. 30:443–58.Skillman AG, Maurer KW, Roe DC, Stauber MJ, Eargle D, Ewing TJ, Muscate A, Davioud-Charvet E, Medaglia MV, Fisher RJ, Arnold E, Gao HQ, Buckheit R, Boyer PL, Hughes SH, Kuntz ID, Kenyon GL. (2002)
Antitrypanosomal activities and cytotoxicity of 5-nitro-2-furancarbohydrazides. Bioorg. Med. Chem. Lett. 12, 3601–3604.Millet, R., Maes, L., Landry, V., Sergheraert, C., Davioud-Charvet, E. (2002)
Comparison of the inhibition of human and Trypanosoma cruzi prolyl endopeptidases. Bioorg. Med. Chem. 10:1719–29.Vendeville S, Goossens F, Debreu-Fontaine MA, Landry V, Davioud-Charvet E, Grellier P, Scharpe S, Sergheraert C. (2002)
Disulfide reductases – current developments. Flavins and Flavoproteins 2002 (Chapman, S.K., Perham, R.N., Scrutton N.S., Eds.) Agency for Scientific Publications Berlin. 803–15.Irmler A, Bechthold A, Davioud-Charvet E, Hofmann V, Réau R, Gromer S, Schirmer RH, Becker K. (2002)
2- and 3-substituted-1,4-naphthoquinone derivatives as subversive substrates of trypanothione reductase and lipoamide dehydrogenase from Trypanosoma cruzi: synthesis and correlation between redox-cycling activities and in vitro cytotoxicity. J. Med. Chem. 44:548–65.Salmon-Chemin L, Buisine E, Yardley V, Kohler S, Debreu MA, Landry V, Sergheraert C, Croft SL, Krauth-Siegel LR, Davioud-Charvet E. (2001)
A prodrug form of a Plasmodium falciparum glutathione reductase inhibitor conjugated with a 4-anilinoquinoline. J. Med. Chem. 44:4268–76.Davioud-Charvet E, Delarue S, Biot C, Schwöbel B, Böhme CC, Müssigbrodt A, Maes L, Sergheraert C, Grellier P, Schirmer RH, Becker K. (2001)
Antiplasmodial activity and cytotoxicity of bis- and triquinolines with linear or cyclic amino linkers. J. Med. Chem. 44, 1658–65.Girault S, Grellier P, Berecibar A, Maes L, Lemière P, Mouray E, Davioud-Charvet E, Sergheraert C. (2001)
Bromination studies of the 2,3-dimethylnaphthazarin core allowing easy access to naphthazarin derivatives. J. Org. Chem. 66:5616–19.Dessolin J, Biot C, Davioud-Charvet E. (2001)
Potent and specific inhibitors of trypanothione reductase from Trypanosoma cruzi: bis(2-aminodiphenylsulfides) for fluorescent labeling studies. Bioorg. Med. Chem. 9:837–46.Girault S, Davioud-Charvet E, Maes L, Dubremetz J-F, Debreu M-A, Landry V, Sergheraert C. (2001)
Trypanosoma cruzi prolyl oligopeptidase Tc80 is involved in nonphagocytic mammalian cell invasion by trypomastigotes. J. Biol. Chem. 276:47078–86.Grellier P, Vendeville S, Joyeau R, Bastos IM, Drobecq H, Frappier F, Teixeira AR, Schrevel J, Davioud-Charvet E, Sergheraert C, Santana JM. (2001)
Antimalarial, antitrypanosomal, antileishmanial activities and cytotoxicity of bis(9-amino-6-chloro-2-methoxyacridines): influence of the linker. J. Med. Chem. 43:2646–54.Girault S, Grellier P, Berecibar A, Maes L, Mouray E, Lemière P, Debreu MA, Davioud-Charvet E, Sergheraert C. (2000)
Parallel synthesis of a library of 1,4–naphthoquinones and automated screening of potential inhibitors of trypanothione reductase from Trypanosoma cruzi. Bioorg. Med. Chem. Lett. 10:631–35.Salmon-Chemin L, Lemaire A, De Freitas S, Deprez B, Sergheraert C, Davioud-Charvet E. (2000)
The conserved redox-sensitive cysteine of the DNA-binding region in the c-Rel protein is involved in the regulation of the phosphorylation of the protein. Biochem. J. 352:583–91.Glineur C, Davioud-Charvet E, Vandenbunder B. (2000)
Trypanothione reductase inhibition / trypanocidal activity relationships in a 1,4-bis(3-aminopropyl)piperazine series. Bioorg. Med. Chem. 8:95–103.Bonnet B, Soullez D, Girault S, Maes L, Landry V, Davioud-Charvet E, Sergheraert C. (2000)
Automated Parellel Synthesis of a tetrahydroisoquinolin-based library: potential prolyl endopeptidase inhibitors. Bioorg. Med. Chem. Lett. 9:437–42.Vendeville S, Bourel L, Davioud-Charvet E, Grellier P, Deprez B, Sergheraert C. (1999)
Evidence for the co-existence of glutathione reductase and trypanothione reductase in the nontrypanosomatid Euglenozoa: Euglena gracilis Z. FEBS Lett. 442:29–33.Montrichard F, Le Guen F, Laval-Martin DL, Davioud-Charvet E. (1999)
Synthesis of alternative substrates for trypanothione reductase and thioredoxin reductase: an inexpensive microtiter colorimetric assay for inhibitor screening. Anal. Biochem. 268:1–8.Davioud-Charvet E, Becker K, Landry V, Gromer S, Loge C, Sergheraert C. (1999)
Synthesis of polyamine derivatives for the preparation of affinity chromatography columns for the search of new Trypanosoma cruzi targets. Bioorg. Med. Chem. Lett. 9:1567–72.Davioud-Charvet E, Berecibar A, Girault S, Landry V, Drobecq H, Sergheraert C. (1999)
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Biochemie-Zentrum
der Universität Heidelberg (BZH)
Im Neuenheimer Feld 328
69120 Heidelberg
der Universität Heidelberg (BZH)
Im Neuenheimer Feld 328
69120 Heidelberg
E-Mail:
elisabeth.davioud@unistra.fr