Ehemalige Forschungsgruppen

Publikationen

2010
Haid S, Gentzsch J, Jannack B, Bailleul F, Davioud-Charvet E, Pietschmann T. Inhibition of hepatitis C virus entry by a plant-derived flavone.
J. Hepatol. Suppl. 1, 52:S293.

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. Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases: interaction with DNA.
J Med Chem. 2010; 53(8):3214-26.


2009
Chavain N, Davioud-Charvet E, Trivelli X, Mbeki L, Rottmann M, Brun R, Biot C.
Antimalarial Antimalarial activities of ferroquine conjugates with either glutathione reductase inhibitors or glutathione depletors via a hydrolyzable amide linker.
Bioorg. Med. Chem.2009; 17:8048--8059."


Wenzel IN, Wong PE, Maes L., Müller TJJ, Krauth-Siegel LR, Barrett M, Davioud-Charvet E. Antitrypanosomal unsaturated Mannich bases active against multidrug-resistant T. brucei brucei strains.
ChemMedChem. 2009; 4:339–51.

2008
Viry E, Battaglia E, Deborde V, Müller T, Réau R, Davioud-Charvet E, Bagrel D.
A sugar-modified phosphole gold complex with antiproliferative properties acting as a thioredoxin reductase inhibitor in MCF-7 cells.
ChemMedChem. 2008; 3:1667–70.

Müller T, Müller TJJ, Davioud-Charvet E.
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. 2008; 16:443–52.

Morin C, Besset T, Moutet JC, Fayolle M, Brückner M, Limosin D, Becker K, Davioud-Charvet E.
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. 2008; 6(15):2731–42.

Friebolin W, Jannack B, Wenzel N, Furrer J, Oeser T, Sanchez CP, Lanzer M, Yardley V, Becker K, Davioud-Charvet E. Antimalarial dual drugs based on potent inhibitors of glutathione reductase from Plasmodium falciparum.
J Med Chem. 2008; 51(5):1260–77.

2007
Kuntz, AN, Davioud-Charvet, E, Dessolin, J, Sayed, AA, Califf, LL, Arnér, ESJ, Williams DL
Schistosome redox balance and thioredoxin glutathione reductase: An essential parasite enzyme and novel drug target.
PLoS Med. 2007; 4(6):e206:1–16.


2006
Bauer H, Fritz-Wolf K, Winzer A, Kühner S, Little S, Yardley V, Vezin H, Palfey B, Schirmer H, Davioud-Charvet E.
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. 2006; 128:10784–94.

Andricopulo AD, Akoachere MB, Krogh R, Nickel C, McLeish MJ, Kenyon GL, Arscott LD, Williams Jr, H, Davioud-Charvet E, Becker K.
Specific inhibitors of Plasmodium falciparum thioredoxin reductase as potential antimalarial agents.
Bioorg. Med. Chem. Lett. 2006; 16:2283–92.

Urig S., Fritz-Wolf K., Réau R., Herold-Mende C., Tóth K., Davioud-Charvet E., Becker K.
Undressing of phosphine gold(I) complexes as irreversible inhibitors of human disulfide reductases.
Angew. Chem. Int. Ed. Engl. 2006; 45:1881–86.

2005
Krauth-Siegel RL, Davioud-Charvet E.
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. 2005, 867–76.

Koncarevic S, Deponte M, Fritz-Wolf K, Meyer M, Urig S, Fischer M, Réau R, Davioud-Charvet E, Becker K.
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. 2005, 325–30.

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.
Specific Inhibitors of Plasmodium falciparum thioredoxin reductase.
Flavins and Flavoproteins 2005 (Nishino T, Miura R, Tanokura M, Fukui K Ed.)
ArchiTect Inc Tokyo. 2005, 883–88.

Lee B, Bauer H, Melcher J, Ruppert T, Rattray L, Yardley V, Davioud-Charvet E, Krauth-Siegel RL Irreversible inhibition of trypanothione reductase by unsaturated Mannich bases: a divinylketone as key intermediate.
J. Med. Chem. 2005; 48:7400–10.

Millet R, Urig S, Jacob J, Gromer S, Moulinoux J-P, Becker K, Davioud-Charvet E.
Synthesis of 5-nitro-2-furancarbohydrazides and their cis-diamminedichloroplatinum complexes as irreversible inhibitors of human thioredoxin reductase.
J. Med. Chem. 2005; 48, 7024–39.

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.
Mechanistic studies of a novel, highly potent gold-phosphole inhibitor of human glutathione reductase.
J. Biol. Chem. 2005; 280, 20628–37.

2004
Biot C, Bauer H, Schirmer RH, Davioud-Charvet E.
5-Substituted tetrazoles as bioisosters of carboxylic acids. Bioisosterism and mechanistic studies on glutathione reductase inhibitors as antimalarials.
J. Med. Chem. 2004; 47:5972–583.

2003
Soulère L, Delplace P, Davioud-Charvet E, Py S, Sergheraert C, Hoffmann P, Périé J, Ricard I, Dive D.
Screening of P. falciparum iron superoxide dismutase inhibitors and accuracy of the SOD-assays.
Bioorg. Med. Chem. 2003; 11:4941–44.
Davioud-Charvet E, McLeish MJ, Veine D, Giegel D, Arscott LD, Andricopulo AD, Becker K, Müller S, Schirmer RH, Williams CH, Kenyon GL.
Mechanism-based inactivation of thioredoxin reductase from Plasmodium falciparum by Mannich bases. Implication for cytotoxicity.
Biochemistry 2003; 42:13319–30.

Biot C, Dessolin J, Grellier P, Davioud-Charvet E.
Double-drug development against antioxidant enzymes from Plasmodium falciparum.
Redox Report 2003; 8:280–83.

2002
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.
A novel mechanism for inhibition of HIV-1 reverse transcriptase.
Bioorg. Chem. 2002; 30:443–58.

Irmler A, Bechthold A, Davioud-Charvet E, Hofmann V, Réau R, Gromer S, Schirmer RH, Becker K.
Disulfide reductases – current developments.
Flavins and Flavoproteins 2002 (Chapman, S.K., Perham, R.N., Scrutton N.S., Eds.)
Agency for Scientific Publications Berlin. 2002, 803–15.

Davioud-Charvet E, McLeish MJ, Veine D, Giegel D, Andricopulo AD, Becker K, Müller S, Schirmer RH, Williams CH, Kenyon GL.
Mechanism-based inactivation of thioredoxin reductase from Plasmodium falciparum by Mannich bases. implications for drug design.
Flavins and Flavoproteins 2002 (Chapman, S.K., Perham, R.N., Scrutton N.S., Eds.)
Agency for Scientific Publications Berlin. 2002, 845–51

Millet, R., Maes, L., Landry, V., Sergheraert, C., Davioud-Charvet, E. (2002)
Antitrypanosomal activities and cytotoxicity of 5-nitro-2-furancarbohydrazides.
Bioorg. Med. Chem. Lett. 12, 3601–3604.

Vendeville S, Goossens F, Debreu-Fontaine MA, Landry V, Davioud-Charvet E, Grellier P, Scharpe S, Sergheraert C.
Comparison of the inhibition of human and Trypanosoma cruzi prolyl endopeptidases.
Bioorg. Med. Chem. 2002; 10:1719–29.

2001
Davioud-Charvet E, Delarue S, Biot C, Schwöbel B, Böhme CC, Müssigbrodt A, Maes L, Sergheraert C, Grellier P, Schirmer RH, Becker K.
A prodrug form of a Plasmodium falciparum glutathione reductase inhibitor conjugated with a 4-anilinoquinoline.
J. Med. Chem. 2001; 44:4268–76.

Grellier P, Vendeville S, Joyeau R, Bastos IM, Drobecq H, Frappier F, Teixeira AR, Schrevel J, Davioud-Charvet E, Sergheraert C, Santana JM
Trypanosoma cruzi prolyl oligopeptidase Tc80 is involved in nonphagocytic mammalian cell invasion by trypomastigotes.
J. Biol. Chem. 2001; 276:47078–86.

Dessolin J, Biot C, Davioud-Charvet E. Bromination studies of the 2,3-dimethylnaphthazarin core allowing easy access to naphthazarin derivatives.
J. Org. Chem. 2001; 66:5616–19.

Girault S, Grellier P, Berecibar A, Maes L, Lemière P, Mouray E, Davioud-Charvet E, Sergheraert C.
Antiplasmodial activity and cytotoxicity of bis- and triquinolines with linear or cyclic amino linkers.
J. Med. Chem. 2001; 44, 1658–65.

Girault S, Davioud-Charvet E, Maes L, Dubremetz J-F, Debreu M-A, Landry V, Sergheraert C.
Potent and specific inhibitors of trypanothione reductase from Trypanosoma cruzi: bis(2-aminodiphenylsulfides) for fluorescent labeling studies.
Bioorg. Med. Chem. 2001; 9:837–46.

Salmon-Chemin L, Buisine E, Yardley V, Kohler S, Debreu MA, Landry V, Sergheraert C, Croft SL, Krauth-Siegel LR, Davioud-Charvet E.
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. 2001; 44:548–65.

2000
Glineur C, Davioud-Charvet E, Vandenbunder B.
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. 2000; 352:583–91.

Girault S, Grellier P, Berecibar A, Maes L, Mouray E, Lemière P, Debreu MA, Davioud-Charvet E, Sergheraert C.
Antimalarial, antitrypanosomal, antileishmanial activities and cytotoxicity of bis(9-amino-6-chloro-2-methoxyacridines): influence of the linker.
J. Med. Chem. 2000; 43:2646–54.

Salmon-Chemin L, Lemaire A, De Freitas S, Deprez B, Sergheraert C, Davioud-Charvet E.
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. 2000; 10:631–35.

Bonnet B, Soullez D, Girault S, Maes L, Landry V, Davioud-Charvet E, Sergheraert C.
Trypanothione reductase inhibition / trypanocidal activity relationships in a 1,4-bis(3-aminopropyl)piperazine series.
Bioorg. Med. Chem. 2000; 8:95–103.

1999
Davioud-Charvet E, Berecibar A, Girault S, Landry V, Drobecq H, Sergheraert C.
Synthesis of polyamine derivatives for the preparation of affinity chromatography columns for the search of new Trypanosoma cruzi targets.
Bioorg. Med. Chem. Lett. 1999; 9:1567–72.

Vendeville S, Bourel L, Davioud-Charvet E, Grellier P, Deprez B, Sergheraert C.
Automated Parellel Synthesis of a tetrahydroisoquinolin-based library: potential prolyl endopeptidase inhibitors.
Bioorg. Med. Chem. Lett. 1999; 9:437–42.

Davioud-Charvet E, Becker K, Landry V, Gromer S, Loge C, Sergheraert C.
Synthesis of alternative substrates for trypanothione reductase and thioredoxin reductase: an inexpensive microtiter colorimetric assay for inhibitor screening.
Anal. Biochem. 1999; 268:1–8.

Montrichard F, Le Guen F, Laval-Martin DL, Davioud-Charvet E.
Evidence for the co-existence of glutathione reductase and trypanothione reductase in the nontrypanosomatid Euglenozoa: Euglena gracilis Z.
FEBS Lett. 1999; 442:29–33.