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

Christine Gravier-Pelletier

Senior Research Scientist, CNRS

 

 

 

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

2019-… : Co-responsable de l’équipe Chemistry towards Life Sciences

2019-… : Responsable du groupe thématique Synthèse Organique pour la Recherche Biomédicale

2012 – 2018 Deputy Director of “INTERDISCIPLINARY CENTER FOR CHEMISTRY BIOLOGY-PARIS” CICB – Paris

2011 – 2018 Head of the team “ORGANIC SYNTHESIS FOR BIOMEDICAL RESEARCH ”

2006 – … CNRS Director of Research (DR2)

1998 : Habilitation à Diriger des Recherches, Université René Descartes, Synthèse de composés d’intérêt biologique à partir du D-mannitol et des acides L-ascorbique et D-isoascorbique.

1992 Chargée de Recherches CNRS (CR1)

1988 Chargée de Recherches CNRS (CR2)

1987 Post-doctoral fellow in Biochemistry with Nobel laureate Pr B. Samüelsson, “Purification of a human polymorphonuclear 5-lipoxygenase co-factor » Karolinska Institute, Stockholm, Sweden.

1986 PhD thesis in Organic Synthesis, Director: Pr J. –C. Depezay “Synthesis of Leukotriene(+)-LTB4 and of an analog from D-Mannitol” Université Pierre & Marie Curie.

Membre de la Société Chimique de France

Membre de la Société de Chimie Thérapeutique

Publications

 

  1. Fichez, J.; Soulie, C.; Corre, L. L.; Sayon, S.; Priet, S.; Alvarez, K.; Delelis, O.; Gizzi, P.; Prestat, G.; Gravier-Pelletier, C.; Marcelin, A.-G.; Calvez, V.; Busca, P. Discovery, SAR Study and ADME Properties of Methyl 4-Amino-3-Cyano-1-(2-Benzyloxyphenyl)-1H-Pyrazole-5-Carboxylate as an HIV-1 Replication Inhibitor. RSC Med. Chem. 2020. asap doi.org:10.1039/D0MD00025F.
  2. Massarweh, A.; Bosco, M.; Chantret, I.; Leger, T.; Jamal, L.; Roper, D. I.; Dowson, C. G.; Busca, P.; Bouhss, A.; Gravier-Pelletier, C.; et al. Bacterial Lipid II Analogs: Novel In Vitro Substrates for Mammalian Oligosaccharyl Diphosphodolichol Diphosphatase (DLODP) Activities. MOLECULES 2019, 24 (11). https://doi.org/10.3390/molecules24112135.
  3. Ashraf, U.; Tengo, L.; Le Corre, L.; Fournier, G.; Busca, P.; McCarthy, A. A.; Rameix-Welti, M.-A.; Gravier-Pelletier, C.; Ruigrok, R. W. H.; Jacob, Y.; et al. Destabilization of the Human RED-SMU1 Splicing Complex as a Basis for Host-Directed Antiinfluenza Strategy. Proc. Natl. Acad. Sci. U. S. A. 2019, 116 (22), 10968–10977. https://doi.org/10.1073/pnas.1901214116.
  4. Morlot, C.; Straume, D.; Peters, K.; Hegnar, O. A.; Simon, N.; Villard, A.-M.; Contreras-Martel, C.; Leisico, F.; Breukink, E.; Gravier-Pelletier, C.; et al. Structure of the Essential Peptidoglycan Amidotransferase MurT/GatD Complex from Streptococcus Pneumoniae. Nat. Commun. 2018, 9. https://doi.org/10.1038/s41467-018-05602-w.
  5. Fer, M. J.; Le Corre, L.; Pietrancosta, N.; Evrard-Todeschi, N.; Olatunji, S.; Bouhss, A.; Calvet-Vitale, S.; Gravier-Pelletier, C. Bacterial Transferase MraY, a Source of Inspiration towards New Antibiotics. Curr. Med. Chem. 2018, 25 (42), 6013–6029. https://doi.org/10.2174/0929867325666180330095154.
  6. Bosco, M.; Massarweh, A.; Iatmanen-Harbi, S.; Bouhss, A.; Chantret, I.; Busca, P.; Moore, S. E. H.; Gravier-Pelletier, C. Synthesis and Biological Evaluation of Chemical Tools for the Study of Dolichol Linked Oligosaccharide Diphosphatase (DLODP). Eur. J. Med. Chem. 2017, 125, 952–964. https://doi.org/10.1016/j.ejmech.2016.10.013.
  7. Ben Othman, R.; Fer, M. J.; Le Corre, L.; Calvet-Vitale, S.; Gravier-Pelletier, C. Effect of Uridine Protecting Groups on the Diastereoselectivity of Uridine-Derived Aldehyde 5’-Alkynylation. BEILSTEIN J. Org. Chem. 2017, 13, 1533–1541. https://doi.org/10.3762/bjoc.13.153.
  8. Massarweh, A.; Bosco, M.; Iatmanen-Harbi, S.; Tessier, C.; Auberger, N.; Busca, P.; Chantret, I.; Gravier-Pelletier, C.; Moore, S. E. H. Demonstration of an Oligosaccharide-Diphosphodolichol Diphosphatase Activity Whose Subcellular Localization Is Different than Those of Dolichyl-Phosphate-Dependent Enzymes of the Dolichol Cycle. J. LIPID Res. 2016, 57 (6), 1029–1042. https://doi.org/10.1194/jlr.M067330.
  9. Massarweh, A.; Bosco, M.; Iatmanen-Harbi, S.; Tessier, C.; Amana, L.; Busca, P.; Chantret, I.; Gravier-Pelletier, C.; Moore, S. E. H. Brefeldin A Promotes the Appearance of Oligosaccharyl Phosphates Derived from Glc(3)Man(9)GlcNAc(2)-PP-Dolichol within the Endomembrane System of HepG2 Cells. J. LIPID Res. 2016, 57 (8), 1477–1491. https://doi.org/10.1194/jlr.M068551.
  10. 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.
  11. Gayral, M.; Frlan, R.; Mravljak, J.; Gravier-Pelletier, C. Nucleophilic Opening of an Epoxide by a Masked Glycine Anion Equivalent: A Route to C-Glycosyl Amino Acids. SYNLETT 2016, 27 (10), 1551–1556. https://doi.org/10.1055/s-0035-1561987.
  12. Le Corre, L.; Tak-Tak, L.; Guillard, A.; Prestat, G.; Gravier-Pelletier, C.; Busca, P. Microwave-Assisted Preparation of 4-Amino-3-Cyano-5-Methoxycarbonyl-N-Arylpyrazoles as Building Blocks for the Diversity-Oriented Synthesis of Pyrazole-Based Polycyclic Scaffolds. Org. Biomol. Chem. 2015, 13 (2), 409–423. https://doi.org/10.1039/c4ob01951b.
  13. Fer, M. J.; Bouhss, A.; Patrao, M.; Le Corre, L.; Pietrancosta, N.; Amoroso, A.; Joris, B.; Mengin-Lecreulx, D.; Calvet-Vitale, S.; Gravier-Pelletier, C. 5 `-Methylene-Triazole-Substituted-Aminoribosyl Uridines as MraY Inhibitors: Synthesis, Biological Evaluation and Molecular Modeling. Org. Biomol. Chem. 2015, 13 (26), 7193–7222. https://doi.org/10.1039/c5ob00707k.
  14. Fer, M. J.; Olatunji, S.; Bouhss, A.; Calvet-Vitale, S.; Gravier-Pelletier, C. Toward Analogues of MraY Natural Inhibitors: Synthesis of 5 `-Triazole-Substituted-Aminoribosyl Uridines Through a Cu-Catalyzed Azide-Alkyne Cycloaddition. J. Org. Chem. 2013, 78 (20), 10088–10105. https://doi.org/10.1021/jo4014035.
  15. Mravljak, J.; Monasson, O.; Al-Dabbagh, B.; Crouvoisier, M.; Bouhss, A.; Gravier-Pelletier, C.; Le Merrer, Y. Synthesis and Biological Evaluation of a Diazepanone-Based Library of Liposidomycins Analogs as MraY Inhibitors. Eur. J. Med. Chem. 2011, 46 (5), 1582–1592. https://doi.org/10.1016/j.ejmech.2011.02.006.
  16. Lecercle, D.; Clouet, A.; Al-Dabbagh, B.; Crouvoisier, M.; Bouhss, A.; Gravier-Pelletier, C.; Le Merrer, Y. Bacterial Transferase MraY Inhibitors: Synthesis and Biological Evaluation. Bioorg. Med. Chem. 2010, 18 (12), 4560–4569. https://doi.org/10.1016/j.bmc.2010.04.023.
  17. Monasson, O.; Ginisty, M.; Mravljak, J.; Bertho, G.; Gravier-Pelletier, C.; Le Merrer, Y. Synthetic Studies towards Diazepanone Scaffolds. TETRAHEDRON-ASYMMETRY 2009, 20 (20), 2320–2330. https://doi.org/10.1016/j.tetasy.2009.09.022.
  18. Auberger, N.; Gravier-Pelletier, C.; Le Merrer, Y. Synthesis of a Beta-Ketophosphonate Bioisostere of UDP-N-Acetylglucosamine. Eur. J. Org. Chem. 2009, No. 20, 3323–3326. https://doi.org/10.1002/ejoc.200900399.
  19. Ciouet, A.; Gravier-Pelletier, C.; Al-Dabbag, B.; Bouhss, A.; Le Merrer, Y. Efficient Synthesis of a Bacterial Translocase MraY Inhibitor. TETRAHEDRON-ASYMMETRY 2008, 19 (4), 397–400. https://doi.org/10.1016/j.tetasy.2008.01.037.
  20. Babic, A.; Gobec, S.; Gravier-Pelletier, C.; Le Merrer, Y.; Pecar, S. Synthesis of 1-C-Linked Diphosphate Analogues of UDP-N-Ac-Glucosamine and UDP-N-Ac-Muramic Acid. TETRAHEDRON 2008, 64 (38), 9093–9100. https://doi.org/10.1016/j.tet.2008.07.009.
  21. Monasson, O.; Ginisty, M.; Bertho, G.; Gravier-Pelletier, C.; Le Merrer, Y. Efficient Synthesis of Polyfunctionalised Enantiopure Diazepanone Scaffolds. TETRAHEDRON Lett. 2007, 48 (46), 8149–8152. https://doi.org/10.1016/j.tetlet.2007.09.098.
  22. Le Corre, L.; Gravier-Pelletier, C.; Le Merrer, Y. Towards New MraY Inhibitors: A Serine Template for Uracil and 5-Amino-5-Deoxyribosyl Scaffolding. Eur. J. Org. Chem. 2007, No. 32, 5386–5394. https://doi.org/10.1002/ejoc.200700527.
  23. Khaled, A.; Gravier-Pelletier, C.; Le Merrer, Y. Synthesis of Bis-(2,3,4,6-Tetra-O-Acetyl-Alpha-D-Mannopyranosyl)-L- Serinyl Phosphate, as a Prodrug of Mannose-1-Phosphate. TETRAHEDRON-ASYMMETRY 2007, 18 (18), 2121–2124. https://doi.org/10.1016/j.tetasy.2007.09.023.
  24. Hardre, R.; Khaled, A.; Willemetz, A.; Dupre, T.; Moore, S.; Gravier-Pelletier, C.; Le Merrer, Y. Mono, Di and Tri-Mannopyranosyl Phosphates as Mannose-1-Phosphate Prodrugs for Potential CDG-Ia Therapy. Bioorg. Med. Chem. Lett. 2007, 17 (1), 152–155. https://doi.org/10.1016/j.bmcl.2006.09.074.
  25. Gravier-Pelletier, C.; Le Merrer, Y. Synthesis of Scaffolds with Glycomimetic Structures. Curr. Org. Synth. 2007, 4 (1), 1–13. https://doi.org/10.2174/157017907779981624.
  26. Ginisty, M.; Gravier-Pelletier, C.; Le Merrer, Y. Chemical Investigations in the Synthesis of O-Serinyl Aminoribosides. TETRAHEDRON-ASYMMETRY 2006, 17 (1), 142–150. https://doi.org/10.1016/j.tetasy.2005.11.019.
  27. Andriuzzi, O.; Gravier-Pelletier, C.; Bertho, G.; Prange, T.; Le Merrer, Y. Synthesis and Glycosidase Inhibitory Activity of New Hexa-Substituted C8-Glycomimetics. BEILSTEIN J. Org. Chem. 2005, 1. https://doi.org/10.1186/1860-5397-1-12.
  28. Andriuzzi, O.; Gravier-Pelletier, C.; Vogel, P.; Le Merrer, Y. Synthesis and Glycosidase Inhibitory Activity of New Penta-Substituted C8-Glycomimetics. TETRAHEDRON 2005, 61 (30), 7094–7104. https://doi.org/10.1016/j.tet.2005.05.066.
  29. Tite, T.; Lallemand, M.; Poupon, E.; Kunesch, N.; Tillequin, F.; Gravier-Pelletier, C.; Le Merrer, Y.; Husson, H. Synthesis of Polyhydroxylated Piperidines and Evaluation as Glycosidase Inhibitors. Bioorg. Med. Chem. 2004, 12 (19), 5091–5097. https://doi.org/10.1016/j.bmc.2004.07.039.
  30. Gravier-Pelletier, C.; Ginisty, M.; Le Merrer, Y. A Versatile Scaffold for a Library of Liposidomycins Analogues: A Crucial and Potent Glycosylation Step. TETRAHEDRON-ASYMMETRY 2004, 15 (2), 189–193. https://doi.org/10.1016/j.tetasy.2003.10.017.
  31. Andriuzzi, O.; Gravier-Pelletier, C.; Le Merrer, Y. Synthesis of C8-Glycomimetics as Potential Glycosidases Inhibitors. TETRAHEDRON Lett. 2004, 45 (43), 8043–8046. https://doi.org/10.1016/j.tetlet.2004.08.172.
  32. Gravier-Pelletier, C.; Maton, W.; Le Merrer, Y. A Straightforward Route to Indolizidine and Quinolizidine Analogs as New Potential Antidiabetics. SYNLETT 2003, No. 3, 333–336.
  33. Gravier-Pelletier, C.; Maton, W.; Dintinger, T.; Tellier, C.; Le Merrer, Y. Synthesis and Glycosidase Inhibitory Activity of Aminocyclitols with a C6-or a C7-Ring. TETRAHEDRON 2003, 59 (44), 8705–8720. https://doi.org/10.1016/j.tet.2003.09.049.
  34. Gravier-Pelletier, C.; Maton, W.; Le Merrer, Y. New Azadisaccharide Analogs as Potential Antidiabetics. TETRAHEDRON Lett. 2002, 43 (46), 8285–8288. https://doi.org/10.1016/S0040-4039(02)02016-6.
  35. Gravier-Pelletier, C.; Andriuzzi, O.; Le Merrer, Y. Efficient Route to Optically Pure Polyfunctionalized Cyclooctanes. TETRAHEDRON Lett. 2002, 43 (2), 245–248. https://doi.org/10.1016/S0040-4039(01)02126-8.
  36. Gravier-Pelletier, C.; Milla, M.; Le Merrer, Y.; Depezay, J. Liposidomycins – Synthetic Studies towards the Ribosyldiazepanone Moiety. Eur. J. Org. Chem. 2001, No. 16, 3089–3096.
  37. Gravier-Pelletier, C.; Maton, W.; Lecourt, T.; Le Merrer, Y. Efficient Access to Azadisaccharide Analogues. TETRAHEDRON Lett. 2001, 42 (27), 4475–4478. https://doi.org/10.1016/S0040-4039(01)00756-0.
  38. Le Merrer, Y.; Gauzy, L.; Gravier-Pelletier, C.; Depezay, J. Synthesis of C-2-Symmetric Guanidino-Sugars as Potent Inhibitors of Glycosidases. Bioorg. Med. Chem. 2000, 8 (2), 307–320. https://doi.org/10.1016/S0968-0896(99)00294-1.
  39. Le Merrer, Y.; Gravier-Pelletier, C.; Maton, W.; Numa, M.; Depezay, J. A Concise Route to Carbasugars. SYNLETT 1999, No. 8, 1322–1324.
  40. Le Merrer, Y.; Gravier-Pelletier, C.; Gerrouache, M.; Depezay, J. Access to Enantiopure Ribosyl-Diazepanone Core of Liposidomycins. TETRAHEDRON Lett. 1998, 39 (5–6), 385–388. https://doi.org/10.1016/S0040-4039(97)10597-4.