Christine Gravier-Pelletier
Senior Research Scientist, CNRS
Chemistry towards life sciences
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
2023
Transport of N-acetylchitooligosaccharides and fluorescent N-acetylchitooligosaccharide analogs into rat liver lysosomes
Y. Bouzidi, M. Bosco, H. Gao, S. Pradeau, L. Matheron, I. Chantret, P. Busca, S. Fort, C. Gravier-Pelletier, S.E.H. Moore*
Glycobiology 2023, cwad099, https://doi.org/10.1093/glycob/cwad099
2022
1) Recent advances in nanotechnology for eradicating bacterial biofilm
Sahli, C.; Moya, S.; Lomas, J. S.; Gravier-Pelletier, C.; Briandet, R.; Hémadi, M.*
Theranostics 2022; 12, 2383-2405. doi:10.7150/thno.67296.
2) A sub-micromolar MraYAA Inhibitor with an aminoribosyl uridine structure and a (S,S)-tartaric diamide: Synthesis, biological evaluation and molecular modeling
Oliver, M.; Le Corre, L.; Poinsot, M.; Bosco, M.; Wan, H.; Amoroso, A.; Joris, B.; Bouhss, A.; Calvet-Vitale*, S.; Gravier-Pelletier, C.*
Molecules 2022, 27, 1769. https://doi.org/10.3390/molecules27061769
3) Systemic bis‑phosphinic acid derivative restores chloride transport in Cystic Fibrosis mice.
Faria da Cunha, M.; Pranke, I.; Sassi, A.; Schreiweiss, C.; Moriceau, S.; Vidovic, D.; Hatton A.; Carlon, M.; Creste, G.; Berhal, F.; Prestat, G.; Freund, R.; Odolczyk, N.; Jais, J. P.; Gravier-Pelletier, C.; Zielenkiewicz, P.; Jullien, J.; Hinzpeter, A.; Oury, F.; Edelman, A. and Sermet-Gaudelus, I.
Sci. Rep. 2022, 12, doi: 10.1038/s41598-022-09678-9
4) New MraYAA Inhibitors with an Aminoribosyl Uridine Structure and an Oxadiazole
Wan, H.; Ben Othman, R.; Le Corre, L.; Poinsot, M.; Oliver, M.; Amoroso, A.; Joris, B.; Touzé, T.; Auger, R.; Calvet-Vitale, S.; Bosco, M.*; Gravier-Pelletier, C.*
Antibiotics 2022, 11, 1189. https://doi.org/10.3390/antibiotics11091189
2021
1) Bardin, E.; Pastor, A.; Semeraro, M.; Golec, A.; Hayes, K.; Chevalier, B.; Berhal, F.; Prestat, G.; Hinzpeter, A.; Gravier-Pelletier, C.; Pranke, I.; Sermet-Gaudelus, I. Modulators of CFTR. Updates on Clinical Development and Future Directions. Eur. J. Med. Chem. 2021, 113195 doi.org/10.1016/j.ejmech.2021.113195
2) New insights into structure and function of bis-phosphinic acid derivatives and implications for CFTR modulation
Bitam S.; Elbahnsi A.; Creste G.; Pranke I.; Chevalier B.; Berhal F.; Hoffmann B.; Servel N.; Tondelier D.; Hatton A.; Moquereau C.; Faria Da Cunha M.; Pastor A.; Hinzpeter A.; Mornon J.-P.; Prestat G.; Edelman A.; Callebaut I.*; Gravier-Pelletier C.*; Sermet-Gaudelus I.*
Sci. Rep. 2021, 11, 6842. https://doi.org/10.1038/s41598-021-83240-x.
3) Synthesis, biological evaluation and molecular modeling of urea-containing MraY inhibitors.
Oliver, M.; Le Corre, L.; Poinsot, M.; Corio, A.; Madegard, L.; Bosco, M.; Amoroso, A.; Joris, B.; Auger, R.; Touzé, T.; Bouhss, A.; Calvet-Vitale, S.*; Gravier-Pelletier, C.*
Org. Biomol. Chem. 2021, 19, 5844 – 5866. DOI: 10.1039/D1OB00710F
4) Regioselective functionalization of quinolines through C-H activation: A comprehensive review.
Corio, A.; Gravier-Pelletier, C.; Busca, P.*
Molecules 2021, 26, 5467. https://doi.org/10.3390/molecules26185467
2020
1) Michaël Bosco, Su-Jin Paik, Patricia Busca, Stuart Moore, Christine Gravier-Pelletier, Synthetic route to glycosyl β-1C-(phosphino)-phosphonates as unprecedented stable glycosyl diphosphate analogs and their preliminary biological evaluation. Molecules 2020, 25, 4969; doi:10.3390/molecules25214969
2) 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.
2019
1) 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.
2) 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.
2018
1) 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.
2) 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.
2017
1) 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.
2) 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.
Before
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- Le Merrer, Y.; Gravier-Pelletier, C.; Maton, W.; Numa, M.; Depezay, J. A Concise Route to Carbasugars. SYNLETT 1999, No. 8, 1322–1324.
- 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.