Mélanie ETHEVE-QUELQUEJEU

Professor

Laboratoire de Chimie et Biochimie pharmacologiques et toxicologiques (LCBPT) – CNRS UMR 8601
Université Paris Descartes
45 Rue des Saints Pères
75270 Paris Cedex 06
France

Curriculum Vitae

2012 – Professor of chemistry (section 32) – Université Paris Descartes

2009 – Habilitation à diriger des recherches, Université Pierre & marie Curie – ” Porphyrines, Carbohydrates and Nucleosides chemistry for synthesis of Biomolecules”.

2009 – Assistant Professor – Université Pierre et Marie Curie Paris VI – UMR 7201-IPCM – Team “Glycochimie Organique, Biologique et Supramoléculaire”, Pr. Matthieu Sollogoub

2000 – Assistant Professor – Université Pierre et Marie Curie Paris VI – UMR 7613, Team “Chimie des Glucides”, Pr. Jean-Marc Valéry

1998-99 – ATER-Université Pierre et Marie Curie Paris VI – UMR 7613, Team “Chimie des Glucides”, Pr. Jean-Marc Valéry

1998 – Post-Doctoral fellow -University of California, Santa Barbara, USA, Laboratoire du Pr. Bruce Lipshutz

1997- Post-Doctoral fellow- Stanford University, California, USA, Laboratoire du Pr. Jim Collman

1997 – Ph.D : “Etude de l’atropoisomérisation des tétrakis(o-nitrophényl) porphyrines et synthèses de modèles d’hémoproteines”.- Dr Eric Rose, Université Pierre et Marie Curie Paris VI

Publications

 C. Kitoun, M. Fonvielle, F. Djago, N. Sakkas, M. Lefresne, Q. Blancart Remaury, P. Poinot, M. Arthur, M. Etheve-Quelquejeu, L. Iannazzo, Phosphine-Mediated Bioconjugation of 3’-end of RNA, Org. Lett., 2020, DOI:10.1021/acs.orglett.0c02982.

 Li Bo; Li, Yongliang; Tomkiewicz-Raulet, C. ; Dao, P. ; Lietha, D.; Yen-Pon, E.; Du, Z.; Coumoul, X.;  Garbay, C.; Etheve-Quelquejeu, M.; Chen, H., Design, synthesis and biological evaluations of covalent inhibitors of Focal Adhesion Kinase (FAK) against human malignant glioblastoma, 2020, J. Med. Chem., just accepted.

C. Atdjian, D. Coelho, L. Iannazzo, M. Ethève-Quelquejeu, E. Braud, Synthesis of triazole-linked SAM-adenosine conjugates: functionalization of adenosine at N1 or N6 position without protecting groups, Molecules, 2020, 25, 3241.

Y.Luo, Y. Xiao, D. Onidas, I. Kherbouche, S. Mahouche, T. Brulé, N. Félidj, L. Iannazzo, M. Ethève-Quelquejeu, F. Gazeau, C. Mangeney Raman Reporters Derived From Aryl Diazonium Salts for SERS Encoded-Nanoparticles2020Chem. Commjust accepted

Flavie Bouchet, Heiner Atze, Matthieu Fonvielle, Zainab Edoo, Michel Arthur, Mélanie Ethève-Quelquejeu, Laura Iannazzo Diazabicyclooctane functionalization for inhibition of β-lactamases from enterobacteria, Journal of Medicinal Chemistry,  2020, 63, 10, 5257–5273  https://doi.org/10.1021/acs.jmedchem.9b02125

B. Mégarbane, Ca. Gamblin, O. Roussel1,  El. Bouaziz-Amar1, L. Chevillard, J. Callebert, H. Chen, G. Morineau, J-L. Laplanche, M. Etheve-Quelquejeu, M. E. Liechti, N. Benturquia, The neurobehavioral effects of the designer drug naphyrone – an experimental investigation with pharmacokinetics and concentration/effect relationship in mice, 2020, Psychopharmacology, https://doi.org/10.1007/s00213-020-05510-2.

Triboulet, S.; Edoo, Z.; Compain, F.; Ourghanlian, C.; Dupuis, A.; Dubee, V.; Sutterlin, L.; Atze, H.; Etheve-Quelquejeu, M.; Hugonnet, J.-E.; et al. Tryptophan Fluorescence Quenching in Beta-Lactam-Interacting Proteins Is Modulated by the Structure of Intermediates and Final Products of the Acylation Reaction. ACS Infect. Dis. 2019, 5 (7), 1169–1176. https://doi.org/10.1021/acsinfecdis.9b00023.

Oerum, S.; Catala, M.; Atdjian, C.; Brachet, F.; Ponchon, L.; Barraud, P.; Iannazzo, L.; Droogmans, L.; Braud, E.; Etheve-Quelquejeu, M.; et al. Bisubstrate Analogues as Structural Tools to Investigate m(6)A Methyltransferase Active Sites. RNA Biol. 2019, 16 (6), 798–808. https://doi.org/10.1080/15476286.2019.1589360.

Bhattacharje, N.; Triboulet, S.; Dubee, V.; Fonvielle, M.; Edoo, Z.; Hugonnet, J.-E.; Etheve-Quelquejeu, M.; Simorre, J.-P.; Field, M. J.; Arthur, M.; et al. Negative Impact of Carbapenem Methylation on the Reactivity of Beta-Lactams for Cysteine Acylation as Revealed by Quantum Calculations and Kinetic Analyses. Antimicrob. AGENTS Chemother. 2019, 63 (4). https://doi.org/10.1128/AAC.02039-18.

Benturquia, N.; Chevillard, L.; Poire, C.; Roussel, O.; Cohier, C.; Decleves, X.; Laplanche, J.-L.; Etheve-Quelquejeu, M.; Chen, H.; Megarbane, B. Is the 3,4-Methylendioxypyrovalerone/Mephedrone Combination Responsible for Enhanced Stimulant Effects? A Rat Study with Investigation of the Effect/Concentration Relationships. Psychopharmacology (Berl.) 2019, 236 (3), 891–901. https://doi.org/10.1007/s00213-018-4962-0.

Atehortua-Martinez, L. A.; Masniere, C.; Campolongo, P.; Chasseigneaux, S.; Callebert, J.; Zwergel, C.; Mai, A.; Laplanche, J.-L.; Chen, H.; Etheve-Quelquejeu, M.; et al. Acute and Chronic Neurobehavioral Effects of the Designer Drug and Bath Salt Constituent 3,4-Methylenedioxypyrovalerone in the Rat. J. Psychopharmacol. (Oxf.) 2019, 33 (3), 392–405. https://doi.org/10.1177/0269881118822151.

Yen-Pon, E.; Li, B.; Acebron-Garcia-de-Eulate, M.; Tomkiewicz-Raulet, C.; Dawson, J.; Lietha, D.; Frame, M. C.; Coumoul, X.; Garbay, C.; Etheve-Quelquejeu, M.; et al. Structure-Based Design, Synthesis, and Characterization of the First Irreversible Inhibitor of Focal Adhesion Kinase. ACS Chem. Biol. 2018, 13 (8), 2067–2073. https://doi.org/10.1021/acschembio.8b00250.

Ngadjeua, F.; Braud, E.; Saidjalolov, S.; Iannazzo, L.; Schnappinger, D.; Ehrt, S.; Hugonnet, J.-E.; Mengin-Lecreulx, D.; Patin, D.; Etheve-Quelquejeu, M.; et al. Critical Impact of Peptidoglycan Precursor Amidation on the Activity of L,D-Transpeptidases from Enterococcus Faecium and Mycobacterium Tuberculosis. Chem.- Eur. J. 2018, 24 (22), 5743–5747. https://doi.org/10.1002/chem.201706082.

Iannazzo, L.; Fonvielle, M.; Braud, E.; Hrebabecky, H.; Prochazkova, E.; Nencka, R.; Mathe, C.; Arthur, M.; Etheve-Quelquejeu, M. Synthesis of TRNA Analogues Containing a Terminal Ribose Locked in the South Conformation to Study TRNA-Dependent Enzymes. Org. Biomol. Chem. 2018, 16 (11), 1903–1911. https://doi.org/10.1039/c8ob00019k.

Fonvielle, M.; Bouhss, A.; Hoareau, C.; Patin, D.; Mengin-Lecreulx, D.; Iannazzo, L.; Sakkas, N.; El Sagheer, A.; Brown, T.; Etheve-Quelquejeu, M.; et al. Synthesis of Lipid-Carbohydrate-Peptidyl-RNA Conjugates to Explore the Limits Imposed by the Substrate Specificity of Cell Wall Enzymes on the Acquisition of Drug Resistance. Chem.- Eur. J. 2018, 24 (56), 14911–14915. https://doi.org/10.1002/chem.201802360.

Edoo, Z.; Iannazzo, L.; Compain, F.; Gallay, I. L. de la S.; van Tilbeurgh, H.; Fonvielle, M.; Bouchet, F.; Le Run, E.; Mainardi, J.-L.; Arthur, M.; et al. Synthesis of Avibactam Derivatives and Activity on Beta-Lactamases and Peptidoglycan Biosynthesis Enzymes of Mycobacteria. Chem.- Eur. J. 2018, 24 (32), 8081–8086. https://doi.org/10.1002/chem.201800923.

Atdjian, C.; Iannazzo, L.; Braud, E.; Etheve-Quelquejeu, M. Synthesis of SAM-Adenosine Conjugates for the Study of m(6)A-RNA Methyltransferases. Eur. J. Org. Chem. 2018, No. 32, 4411–4425. https://doi.org/10.1002/ejoc.201800798.

Sarkis, M.; Miteva, M. A.; Lang, M. C. D.; Jaouen, M.; Sari, M.-A.; Galcera, M.-O.; Etheve-Quelquejeu, M.; Garbay, C.; Bertho, G.; Braud, E. Insights into the Interaction of High Potency Inhibitor IRC-083864 with Phosphatase CDC25. PROTEINS-Struct. Funct. Bioinforma. 2017, 85 (4), 593–601. https://doi.org/10.1002/prot.25236.

Dao, P.; Lietha, D.; Etheve-Quelquejeu, M.; Garbay, C.; Chen, H. Synthesis of Novel 1,2,4-Triazine Scaffold as FAK Inhibitors with Antitumor Activity. Bioorg. Med. Chem. Lett. 2017, 27 (8), 1727–1730. https://doi.org/10.1016/j.bmcl.2017.02.072.

(14)        Le Corre, L.; Lang, M. C. D.; Garbay, C.; Gravier-Pelletier, C.; Busca, P.; Etheve-Quelquejeu, M.; Braud, E. Synthesis of Multifunctionalized 2-Iminothiazolidin-4-Ones and Their 2-Arylimino Derivatives. Synth.-Stuttg. 2016, 48 (24), 4569–4579. https://doi.org/10.1055/s-0035-1562521.

Iannazzo, L.; Soroka, D.; Triboulet, S.; Fonvielle, M.; Compain, F.; Dubee, V.; Mainardi, J.-L.; Hugonnet, J.-E.; Braud, E.; Arthur, M.; et al. Routes of Synthesis of Carbapenems for Optimizing Both the Inactivation of L,D-Transpeptidase Ldt(Mt1) of Mycobacterium Tuberculosis and the Stability toward Hydrolysis by Beta-Lactamase BlaC. J. Med. Chem. 2016, 59 (7), 3427–3438. https://doi.org/10.1021/acs.jmedchem.6b00096.

Fonvielle, M.; Sakkas, N.; Iannazzo, L.; Le Fournis, C.; Patin, D.; Mengin-Lecreulx, D.; El-Sagheer, A.; Braud, E.; Cardon, S.; Brown, T.; et al. Electrophilic RNA for Peptidyl-RNA Synthesis and Site-Specific Cross-Linking with TRNA-Binding Enzymes. Angew. Chem.-Int. Ed. 2016, 55 (43), 13553–13557. https://doi.org/10.1002/anie.201606843.

Smith, N.; Etheve-Quelquejeu, M.; Herbeuval, J.-P. Transformation of Plasmacytoid Dendritic Cells into Giant Multinuclear Cells by HIV-1. AIDS Res. Hum. RETROVIRUSES 2015, 31 (10), 959–960. https://doi.org/10.1089/aid.2015.0082.

annazzo, L.; Laisne, G.; Fonvielle, M.; Braud, E.; Herbeuval, J.-P.; Arthur, M.; Etheve-Quelquejeu, M. Synthesis of 3 `-Fluoro-TRNA Analogues for Exploring Non-Ribosomal Peptide Synthesis in Bacteria. CHEMBIOCHEM 2015, 16 (3), 477–486. https://doi.org/10.1002/cbic.201402523.

Iannazzo, L.; Benedetti, E.; Catala, M.; Etheve-Quelquejeu, M.; Tisne, C.; Micouin, L. Monitoring of Reversible Boronic Acid-Diol Interactions by Fluorine NMR Spectroscopy in Aqueous Media. Org. Biomol. Chem. 2015, 13 (33), 8817–8821. https://doi.org/10.1039/c5ob01362c.

Xu, B.; Unione, L.; Sardinha, J.; Wu, S.; Etheve-Quelquejeu, M.; Rauter, A. P.; Bleriot, Y.; Zhang, Y.; Martin-Santamaria, S.; Diaz, D.; et al. Gem-Difluorocarbadisaccharides: Restoring the Exo-Anomeric Effect. Angew. Chem.-Int. Ed. 2014, 53 (36), 9597–9602. https://doi.org/10.1002/anie.201405008.

Smith, N.; Etheve-Quelquejeu, M.; Herbeuval, J.-P. CD4 and Tumor Necrosis Factor-Related Apoptosis Ligand (TRAIL) Localization in HIV-Stimulated Plasmacytoid Dendritic Cells by Three-Dimensional Microscopy. AIDS Res. Hum. RETROVIRUSES 2014, 30 (12), 1158–1159. https://doi.org/10.1089/aid.2014.0125.

Santarem, M.; Fonvielle, M.; Sakkas, N.; Laisne, G.; Chemama, M.; Herbeuval, J.-P.; Braud, E.; Arthur, M.; Etheve-Quelquejeu, M. Synthesis of 3 `-Triazoyl-Dinucleotides as Precursors of Stable Phe-TRNA(Phe) and Leu-TRNA(Leu) Analogues. Bioorg. Med. Chem. Lett. 2014, 24 (15), 3231–3233. https://doi.org/10.1016/j.bmcl.2014.06.027.

Triboulet, S.; Dubee, V.; Lecoq, L.; Bougault, C.; Mainardi, J.-L.; Rice, L. B.; Etheve-Quelquejeu, M.; Gutmann, L.; Marie, A.; Dubost, L.; et al. Kinetic Features of L,D-Transpeptidase Inactivation Critical for Beta-Lactam Antibacterial Activity. PLOS ONE 2013, 8 (7). https://doi.org/10.1371/journal.pone.0067831.

Mellal, D.; Fonvielle, M.; Santarem, M.; Chemama, M.; Schneider, Y.; Iannazzo, L.; Braud, E.; Arthur, M.; Etheve-Quelquejeu, M. Synthesis and Biological Evaluation of Non-Isomerizable Analogues of Ala-TRNA(Ala). Org. Biomol. Chem. 2013, 11 (36), 6161–6169. https://doi.org/10.1039/c3ob41206g.

Leclerc, E.; Pannecoucke, X.; Etheve-Quelquejeu, M.; Sollogoub, M. Fluoro-C-Glycosides and Fluoro-Carbasugars, Hydrolytically Stable and Synthetically Challenging Glycomimetics. Chem. Soc. Rev. 2013, 42 (10), 4270–4283. https://doi.org/10.1039/c2cs35403a.

Fonvielle, M.; Mellal, D.; Patin, D.; Lecerf, M.; Blanot, D.; Bouhss, A.; Santarem, M.; Mengin-Lecreulx, D.; Sollogoub, M.; Arthur, M.; et al. Efficient Access to Peptidyl-RNA Conjugates for Picomolar Inhibition of Non-Ribosomal FemXWv Aminoacyl Transferase. Chem.- Eur. J. 2013, 19 (4), 1357–1363. https://doi.org/10.1002/chem.201201999.

Fonvielle, M.; de La Sierra-Gallay, I. L.; El-Sagheer, A. H.; Lecerf, M.; Patin, D.; Mellal, D.; Mayer, C.; Blanot, D.; Gale, N.; Brown, T.; et al. The Structure of FemX(Wv) in Complex with a Peptidyl-RNA Conjugate: Mechanism of Aminoacyl Transfer from Ala-TRNA(Ala) to Peptidoglycan Precursors. Angew. Chem.-Int. Ed. 2013, 52 (28), 7278–7281. https://doi.org/10.1002/anie.201301411.

Rose, E.; Raoul, N.; Etheve-Quelquejeu, M.; Gallo, E.; Boitrel, B.; Pecaut, J.; Dubois, L. Crystal Structure of a Chiral Binaphthyl Porphyrin. J. Porphyr. PHTHALOCYANINES 2012, 16 (3), 324–330. https://doi.org/10.1142/S1088424612500393.

Dubee, V.; Triboulet, S.; Mainardi, J.-L.; Etheve-Quelquejeu, M.; Gutmann, L.; Marie, A.; Dubost, L.; Hugonnet, J.-E.; Arthur, M. Inactivation of Mycobacterium Tuberculosis L,D-Transpeptidase Ldt(Mt1) by Carbapenems and Cephalosporins. Antimicrob. AGENTS Chemother. 2012, 56 (8), 4189–4195. https://doi.org/10.1128/AAC.00665-12.

Dubee, V.; Arthur, M.; Fief, H.; Triboulet, S.; Mainardi, J.-L.; Gutmann, L.; Sollogoub, M.; Rice, L. B.; Etheve-Quelquejeu, M.; Hugonnet, J.-E. Kinetic Analysis of Enterococcus Faecium L,D-Transpeptidase Inactivation by Carbapenems. Antimicrob. AGENTS Chemother. 2012, 56 (6), 3409–3412. https://doi.org/10.1128/AAC.06398-11.

Fonvielle, M.; Chemama, M.; Lecerf, M.; Villet, R.; Busca, P.; Bouhss, A.; Etheve-Quelquejeu, M.; Arthur, M. Decoding the Logic of the TRNA Regiospecificity of Nonribosomal FemX(Wv) Aminoacyl Transferase. Angew. Chem.-Int. Ed. 2010, 49 (30), 5115–5119. https://doi.org/10.1002/anie.201001473.

Fonvielle, M.; Chemama, M.; Villet, R.; Lecerf, M.; Bouhss, A.; Valery, J.-M.; Etheve-Quelquejeu, M.; Arthur, M. Aminoacyl-TRNA Recognition by the FemX(Wv) Transferase for Bacterial Cell Wall Synthesis. NUCLEIC ACIDS Res. 2009, 37 (5), 1589–1601. https://doi.org/10.1093/nar/gkn1039.

Chemama, M.; Fonvielle, M.; Arthur, M.; Valery, J.-M.; Etheve-Quelquejeu, M. Synthesis of Stable Aminoacyl-TRNA Analogues Containing Triazole as a Bioisoster of Esters. Chem.- Eur. J. 2009, 15 (8), 1929–1938. https://doi.org/10.1002/chem.200801563.

Chemama, M.; Fonvielle, M.; Villet, R.; Arthur, M.; Valery, J.-M.; Etheve-Quelquejeu, M. Stable Analogues of Aminoacyl-TRNA for Inhibition of an Essential Step of Bacterial Cell-Wall Synthesis (Vol 129, Pg 12642, 2007). J. Am. Chem. Soc. 2008, 130 (12), 4203. https://doi.org/10.1021/ja710232g.

Villet, R.; Fonvielle, M.; Busca, P.; Chemama, M.; Maillard, A. P.; Hugonnet, J.-E.; Dubost, L.; Marie, A.; Josseaume, N.; Mesnage, S.; et al. Idiosyncratic Features in TRNAs Participating in Bacterial Cell Wall Synthesis. NUCLEIC ACIDS Res. 2007, 35 (20), 6870–6883. https://doi.org/10.1093/nar/gkm778.

Etheve-Quelquejeu, M.; Tranchier, J.-P.; Rose-Munch, F.; Rose, E.; Naesens, L.; De Clercq, E. Eta(6)-(Arene)Tricarbonylehromium and Manganese Complexes Linked to 2 `-Deoxyuridine. ORGANOMETALLICS 2007, 26 (23), 5727–5730. https://doi.org/10.1021/om700674v.

Chemama, M.; Fonvielle, M.; Villet, R.; Arthur, M.; Valery, J.-M.; Etheve-Quelquejeu, M. Stable Analogues of Aminoacyl-TRNA for Inhibition of an Essential Step of Bacterial Cell-Wall Synthesis. J. Am. Chem. Soc. 2007, 129 (42), 12642+. https://doi.org/10.1021/ja0749946.