Actual Area of Research
PEPTIDOMIMETICS INHIBITORS OF PROTEIN/PROTEIN INTERACTIONS INVOLVING ß-SHEETS
Amyloid proteins aggregation inhibition. ß amyloide peptide, Synuclein, protein tau : Interest in Neurodegenerative diseases. IAPP : interest in type II Diabetes.
Design of peptidomimetic aggregation inhibitors, synthesis, biophysicochemical evaluation (NMR, Fluorescence, EC, CD, SPR, TEM, IMS-MS, 19F NMR …), molecular modelling.
FLUORINATED AMINO ACIDS and PEPTIDES, METHODOLOGY OF SYNTHESIS : trifluoromethylated beta-aminoacides, acyclic, cyclopropanes, aminoaziridines, triazoles…
Various Activities
Since 2010 Co-DIRECTION (with Dr. B. Crousse) of the team FLUOPEPIT OF BIOCIS. https://www.biocis.universite-paris-saclay.fr/?-Molecules-fluorees-et-peptides-d-&lang=en. 2 Full Prof, 1 DR CNRS, 3 MCU, 1 IE, PhDs (5-10), Masters (2-3).
Since 2015 Deputy director of the Doctoral school “Therapeutic innovation” ED569. 300 PhD students. Organization of their multidisciplinary training (scientific and transferable skills). Recruitment management. Conflict management between PhD students and their supervisor. In charge of the International relations and programmes.
National Academic Collaborations (UMR 8612/UPSaclay, UMR 7203/Sorbonne Univ., LCP/UPSaclay…)
International Academic Collaborations (Germany, Italy, Israel, Spain, Switzerland, USA)
National, European and international funding, in particular in HORIZON 2020 programme.
Partner of ITN « TubInTrain » : https://www.tubintrain.eu/ (2019-2023)
Partner of FETOPEN « NoPest » : https://www.h2020nopest.org/ (2019-2024) https://eugloh-network.pageflow.io/no-pest
Industrial collaborations
Teaching Activities
Medicinal Chemistry : Students in Pharmacy, in M1 and M2 Master in Pharmaceutical Sciences, in L3 Biology-Chemistry (Faculty of Pharmacy and UFR Orsay)
Peptide Chemistry : M1 Master Students in Chemistry (UFR Orsay)
Contact
Disciplines
- Chimie13
- Chimie/Chimie thérapeutique12
- Chimie/Chimie organique7
- Sciences du Vivant [q-bio]/Biochimie, Biologie Moléculaire3
- Physique [physics]2
- Chimie/Cristallographie1
- Chimie/Chimie inorganique1
- Sciences du Vivant [q-bio]/Biochimie, Biologie Moléculaire/Biochimie [q-bio.BM]1
- Sciences du Vivant [q-bio]/Biochimie, Biologie Moléculaire/Biophysique1
- Sciences du Vivant [q-bio]/Biologie cellulaire1
- Sciences du Vivant [q-bio]/Neurosciences [q-bio.NC]/Neurobiologie1
- Sciences du Vivant [q-bio]1
- Sciences de l'ingénieur [physics]/Génie des procédés1
Mots-clefs
- Aggregation4
- Amyloid3
- Fluorine2
- Peptide2
- Peptidomimetic2
- Peptidomimetics2
- Type 2 diabetes2
- Aza-peptide1
- Beta-sheet1
- Capillary electrophoresis1
- Chaperone1
- Constrained amino acids1
- Coordination modes1
- Cyclopropanes1
- Dimerization inhibitors1
- Foldamer1
- HIAPP1
- HIV1
- Helix1
- Human amylin1
- Ion mobility mass spectrometry1
- Michael addition1
- N ligands1
- Palladium1
- Platinum1
- Protease1
- Protein-protein interaction1
- Tauopathies1
- Tauopathies peptide peptidomimetic protein-protein interaction chaperone1
- ThT fluorescence spectroscopy1
- Unnatural amino acid1
- Β-hairpin1
Auteurs
Ongeri Sandrine35
Kaffy Julia12
Soulier Jean-Louis12
Tonali Nicolo10
Lequin Olivier9
Taverna Myriam7
Crousse Benoit7
Milcent Thierry6
Crousse Benoît6
Correia Isabelle5
Halgand Frédéric5
Berardet Corentin4
Bernadat Guillaume4
Khemtémourian Lucie4
Lesma Jacopo4
Sicsic Sames4
Retailleau Pascal4
Ha-Duong Tâp4
Correia Isabelle4
Brinet Dimitri3
Dorgeret Bertrand3
Fanelli Roberto3
Kaffy Julia3
Ha-Duong Tap3
Lequin Olivier3
Arenas José Laxio2
Bizet Faustine2
Erba Emanuela2
Gelmi Maria Luisa2
Guitot Karine2
Hao Jing2
Kihal Nadjib2
Piarulli Umberto2
Ramamoorthy Ayyalusamy2
Reboud-Ravaux Michèle2
Shi Chenghui2
Vidu Anamaria2
Xu Yaochun2
van Heijenoort Carine2
Taverna Myriam2
van Heijenoort Carine2
van Der Rest Guillaume2
Brigaud Thierry2
Aitken David J1
Albinati Alberto1
Allsop David1
Bannwarth Ludovic1
Bernadat G.1
Berthouze Magali1
Bisi Nicolo1
Boggetto Nicole1
Cayrou Chloé1
Chassaing Gérard1
Chaume Grégory1
Collinet Bruno1
Crousse B.1
Crousse Benoit1
Desyergne Audrey1
Di Lorenzo Davide1
Dufau Laure1
Ennen Inga1
Fera Katia Fabiana1
Frutos Silvia1
Gallard Jean-François1
Garfagnini Irene1
Gautier Arnaud1
Giner Mireille1
Giralt Ernest1
Giraud Francois1
Giraud François1
Gonzalez Simon1
Gonçalves R.1
Hannappel Yvonne1
Hoffmann Anais1
Husson Henri-Philippe1
Iacone Yasmine1
Jamart-Grégoire Brigitte1
Keita Massaba1
Khemtemourian Lucie1
Kozelka Jiri1
Kyrko Dimitra1
Laxio Arenas José1
Leblanc Karine1
Lemoine Pascale1
Lezoualc'H Frank1
Maigret Bernard1
Mamone M.1
Mathieu Loïc1
Merabet Naïma1
Milcent T.1
Morgant Georges1
Nguyen-Huy Dung1
Noinville Sylvie1
Oliva Agostino1
Pannecouque Christophe1
Panzeri Silvia1
Pellegrino Sara1
Pruvost Alain1
Ramirez Lisa Marie1
Ranjan Sahoo Bikash1
Ravault Delphine1
Reboud-Ravaux Michele1
Ressad Fariza1
Ressurreicao Ana Sofia Marques1
Retailleau Pascal1
Rivail Lucie1
Rizzato Silvia1
Rodrigo Jordi1
Russo Olivier1
Sagan Sandrine1
Sahoo Bikash1
Saraç Murat1
Soloshonok Vadim1
Soloshonok Vadim A.1
Soulier Jean‐louis1
Taylor Mark1
Vahdati Leila1
Vahdati Leïla1
Vanderesse Régis1
Viossat Bernard1
de Bona Rocco1
van Baelinghem Laurence1
dos Santos Mickaël1
Rose Thierry1
Walrant Astrid1
Berque-Bestel Isabelle1
Legrand Baptiste1
Laxio Arenas José1
Ghermani Nour-Eddine1
Tonali Nicolo1
Mabondzo Aloise1
Zweckstetter Markus1
Dumond Julien1
Luo Jinghui1
Dodero Veronica1
Gelmi Maria Luisa1
Brandt Roland1
Bourguet Erika1
Gillet Jean-Michel1
Ha‐duong Tap1
Fischmeister Rodolphe1
Ongeri S.1
Chaume Grégory1
Maillard Ludovic1
Lensen Nathalie1
Giraud Francois1
Ciccone Lidia1
Sewald Norbert1
Bodero Lizeth1
Blanchard Fabian1
de Clercq Erik1
Auteurs de la structure
Revues
- European Journal of Medicinal Chemistry5
- Journal of Medicinal Chemistry5
- Chemistry - A European Journal3
- Organic & Biomolecular Chemistry3
- Chemical Communications2
- European Journal of Organic Chemistry2
- New Journal of Chemistry2
- Beilstein Journal of Organic Chemistry2
- Frontiers in Cell and Developmental Biology1
- Analytical and Bioanalytical Chemistry1
Année de production
Institutions
Laboratoires
Départements
Équipes de recherche
Articles dans une revue34 document
- Thierry Milcent, Pascal Retailleau, Benoit Crousse, Sandrine Ongeri. Synthesis of extended fluorinated tripeptides based on the tetrahydropyridazine scaffold. Beilstein Journal of Organic Chemistry, 2024, 20, pp.3174-3181. ⟨10.3762/bjoc.20.262⟩. ⟨hal-05142142⟩
- Dimitra Kyrko, Murat Saraç, Jing Hao, Pascal Retailleau, Sandrine Ongeri, et al.. Functionalized α‐Fluorinated Amines from Imines and Enol Ethers. Advanced Synthesis and Catalysis, 2024, 366 (16), pp.3460-3465. ⟨10.1002/adsc.202400517⟩. ⟨hal-04756974⟩
- José Laxio Arenas, Jacopo Lesma, Tap Ha‐duong, Bikash Ranjan Sahoo, Ayyalusamy Ramamoorthy, et al.. Composition and Conformation of Hetero‐ versus Homo‐Fluorinated Triazolamers Influence their Activity on Islet Amyloid Polypeptide Aggregation. Chemistry - A European Journal, 2024, 30 (28), pp.e202303887. ⟨10.1002/chem.202303887⟩. ⟨hal-04756674⟩
- Chloé Cayrou, Astrid Walrant, Delphine Ravault, Karine Guitot, Sylvie Noinville, et al.. Incorporation of CF 3 -pseudoprolines into polyproline type II foldamers confers promising biophysical features. Chemical Communications, In press, ⟨10.1039/D4CC02895C⟩. ⟨hal-04660873⟩
- Chenghui Shi, Julia Kaffy, Tâp Ha-Duong, Jean-François Gallard, Alain Pruvost, et al.. Proteolytically Stable Diaza-Peptide Foldamers Mimic Helical Hot Spots of Protein–Protein Interactions and Act as Natural Chaperones. Journal of Medicinal Chemistry, 2023, 66 (17), pp.12005-12017. ⟨10.1021/acs.jmedchem.3c00611⟩. ⟨hal-04458911⟩
- Chenghui Shi, Isabelle Correia, Nicolo Tonali, Sandrine Ongeri, Olivier Lequin. Two consecutive aza-amino acids in peptides promote stable β-turn formation in water. Organic & Biomolecular Chemistry, 2022, 20 (43), pp.8430-8437. ⟨10.1039/d2ob01225a⟩. ⟨hal-03955106⟩
- Lizeth Bodero, Karine Guitot, Nathalie Lensen, Olivier Lequin, Thierry Brigaud, et al.. Introducing the Chiral Constrained α‐Trifluoromethylalanine in Aib Foldamers to Control, Quantify and Assign the Helical Screw‐Sense**. Chemistry - A European Journal, 2022, 28 (8), pp.e202103887. ⟨10.1002/chem.202103887⟩. ⟨hal-03626224⟩
- José Laxio Arenas, Pascal Retailleau, Jean-Michel Gillet, Nour-Eddine Ghermani, Sandrine Ongeri, et al.. 5-Fluoro-1,2,3-triazole motif in peptides and its electronic properties. Organic & Biomolecular Chemistry, 2022, 20 (43), pp.8410-8414. ⟨10.1039/D2OB01716D⟩. ⟨hal-04249450⟩
- Jacopo Lesma, Faustine Bizet, Corentin Berardet, Nicolo Tonali, Sara Pellegrino, et al.. β-Hairpin Peptide Mimics Decrease Human Islet Amyloid Polypeptide (hIAPP) Aggregation. Frontiers in Cell and Developmental Biology, 2021, 9, ⟨10.3389/fcell.2021.729001⟩. ⟨hal-03367992⟩
- José Laxio Arenas, Yaochun Xu, Thierry Milcent, Carine van Heijenoort, Francois Giraud, et al.. Fluorinated Triazole Foldamers: folded or extended conformational preferences. ChemPlusChem, 2021, ⟨10.1002/cplu.202000791⟩. ⟨hal-03796604⟩
- Julia Kaffy, Corentin Berardet, Loïc Mathieu, Baptiste Legrand, Myriam Taverna, et al.. Helical γ‐Peptide Foldamers as Dual Inhibitors of Amyloid‐β Peptide and Islet Amyloid Polypeptide Oligomerization and Fibrillization. Chemistry - A European Journal, 2020, 26 (64), pp.14612-14622. ⟨10.1002/chem.202001716⟩. ⟨hal-03011765⟩
- Nicolo Tonali, Isabelle Correia, Jacopo Lesma, Guillaume Bernadat, Sandrine Ongeri, et al.. Introducing sequential aza--amino acids units induces repeated β--turns and helical conformations in peptides. Organic & Biomolecular Chemistry, 2020, 18, pp.3452-3458. ⟨10.1039/c9ob02654a⟩. ⟨hal-02888753⟩
- Corentin Berardet, Julia Kaffy, Frédéric Halgand, Guillaume van Der Rest, Sandrine Ongeri, et al.. Evidence for different in vitro oligomerization behaviors of synthetic hIAPP obtained from different sources. Analytical and Bioanalytical Chemistry, 2020, 412 (13), pp.3103-3111. ⟨10.1007/s00216-020-02560-5⟩. ⟨hal-03011853⟩
- Corentin Berardet, Julia Kaffy, Sandrine Ongeri, Myriam Taverna. A capillary zone electrophoresis method to investigate the oligomerization of the human Islet Amyloid Polypeptide involved in Type 2 Diabetes. Journal of Chromatography A, 2018, 1578, pp.83-90. ⟨10.1016/j.chroma.2018.10.006⟩. ⟨hal-04305493⟩
- Faustine Bizet, Nicolo Tonali, Jean-Louis Soulier, Agostino Oliva, Julia Kaffy, et al.. Towards a general synthesis of di-aza-amino acids containing peptides. New Journal of Chemistry, 2018, 42 (20), pp.17062-17072. ⟨10.1039/c8nj03635g⟩. ⟨hal-02347605⟩
- Benoît Crousse, Pascal Retailleau, Thierry Milcent, Sandrine Ongeri, Vadim A. Soloshonok. Synthesis of Trifluoromethylated Pyrrolidine and Piperidine Amino Acids. SYNFACTS, 2018, 14 (10), pp.1015. ⟨10.1055/s-0037-1610969⟩. ⟨hal-02347510⟩
- Jing Hao, Thierry Milcent, Pascal Retailleau, Vadim Soloshonok, Sandrine Ongeri, et al.. Asymmetric Synthesis of Cyclic Fluorinated Amino Acids. European Journal of Organic Chemistry, 2018, 2018 (27-28), pp.3688-3692. ⟨10.1002/ejoc.201800255⟩. ⟨hal-02347674⟩
- Nicolo Tonali, Julia Kaffy, Jean-Louis Soulier, Maria Luisa Gelmi, Emanuela Erba, et al.. Structure-activity relationships of β-hairpin mimics as modulators of amyloid β-peptide aggregation. European Journal of Medicinal Chemistry, 2018, 154, pp.280-293. ⟨10.1016/j.ejmech.2018.05.018⟩. ⟨hal-04305545⟩
- Nicolo Tonali, Julia Kaffy, Jean-Louis Soulier, Maria Luisa Gelmi, Emanuela Erba, et al.. Structure-activity relationships of β-hairpin mimics as modulators of amyloid β-peptide aggregation. European Journal of Medicinal Chemistry, 2018, 154, pp.280-293. ⟨10.1016/j.ejmech.2018.05.018⟩. ⟨hal-02392954⟩
- Yaochun Xu, Isabelle Correia, Tap Ha-Duong, Nadjib Kihal, Jean-Louis Soulier, et al.. The use of 4,4,4-trifluorothreonine to stabilize extended peptide structures and mimic β-strands. Beilstein Journal of Organic Chemistry, 2017, 13, pp.2842 - 2853. ⟨10.3762/bjoc.13.276⟩. ⟨hal-01700974⟩
- Leïla Vahdati, Julia Kaffy, Dimitri Brinet, Guillaume Bernadat, Isabelle Correia, et al.. Synthesis and Characterization of Hairpin Mimics that Modulate the Early Oligomerization and Fibrillization of Amyloid β-Peptide. European Journal of Organic Chemistry, 2017, 2017 (20), pp.2971-2980. ⟨10.1002/ejoc.201700010⟩. ⟨hal-02467878⟩
- M. Mamone, R. Gonçalves, Fabian Blanchard, G. Bernadat, S. Ongeri, et al.. N-Difluoromethyl-triazole as a constrained scaffold in peptidomimetics. Chemical Communications, 2017, 53 (36), pp.5024-5027. ⟨10.1039/c7cc01298e⟩. ⟨hal-02998189⟩
- Julia Kaffy, Dimitri Brinet, Jean-Louis Soulier, Isabelle Correia, Nicolo Tonali, et al.. Designed Glycopeptidomimetics Disrupt Protein–Protein Interactions Mediating Amyloid β-Peptide Aggregation and Restore Neuroblastoma Cell Viability. Journal of Medicinal Chemistry, 2016, 59 (5), pp.2025-2040. ⟨10.1021/acs.jmedchem.5b01629⟩. ⟨hal-02467871⟩
- Leila Vahdati, Roberto Fanelli, Guillaume Bernadat, Isabelle Correia, Olivier Lequin, et al.. Synthesis and conformational studies of a stable peptidomimetic beta-hairpin based on a bifunctional diketopiperazine turn inducer. New Journal of Chemistry, 2015, 39 (5), pp.3250-3258. ⟨10.1039/c4nj01437e⟩. ⟨hal-01366397⟩
- Julia Kaffy, Dimitri Brinet, Jean-Louis Soulier, Lucie Khemtémourian, Olivier Lequin, et al.. Structure-activity relationships of sugar-based peptidomimetics as modulators of amyloid β-peptide early oligomerization and fibrillization.. European Journal of Medicinal Chemistry, 2014, 86C, pp.752-758. ⟨10.1016/j.ejmech.2014.09.031⟩. ⟨hal-01067196⟩
- Massaba Keita, Rocco de Bona, Mickaël dos Santos, Olivier Lequin, Sandrine Ongeri, et al.. Access to novel amino trifluoromethyl cyclopropane carboxylic acid derivatives. Tetrahedron, 2013, 69 (15), pp.3308-3315. ⟨10.1016/j.tet.2013.02.012⟩. ⟨hal-01366842⟩
- Laure Dufau, Ana Sofia Marques Ressurreicao, Roberto Fanelli, Nadjib Kihal, Anamaria Vidu, et al.. Carbonylhydrazide-Based Molecular Tongs Inhibit Wild-Type and Mutated HIV-1 Protease Dimerization. Journal of Medicinal Chemistry, 2012, 55 (15), pp.6762-6775. ⟨10.1021/jm300181j⟩. ⟨hal-01544073⟩
- Bertrand Dorgeret, Lucie Khemtémourian, Isabelle Correia, Jean-Louis Soulier, Olivier Lequin, et al.. Sugar-based peptidomimetics inhibit amyloid β-peptide aggregation. European Journal of Medicinal Chemistry, 2011, 46 (12), pp.5959-5969. ⟨10.1016/j.ejmech.2011.10.008⟩. ⟨hal-02467773⟩
- Bertrand Dorgeret, Lucie Khemtémourian, Isabelle Correia, Jean-Louis Soulier, Olivier Lequin, et al.. Sugar-based peptidomimetics inhibit amyloid β-peptide aggregation.. European Journal of Medicinal Chemistry, 2011, 46 ((12)), pp.5959-69. ⟨10.1016/j.ejmech.2011.10.008⟩. ⟨hal-00692384⟩
- Erika Bourguet, Isabelle Correia, Bertrand Dorgeret, Gérard Chassaing, Sames Sicsic, et al.. Synthesis and conformational studies of pseudopeptides containing an unsymmetrical triazine scaffold. Journal of Peptide Science, 2008, 14 (5), pp.596-609. ⟨10.1002/psc.944⟩. ⟨hal-02465291⟩
- Ludovic Bannwarth, Thierry Rose, Silvia Frutos, Ernest Giralt, Régis Vanderesse, et al.. Peptidomimetic dimerization inhibitors of HIV-1 protease : further insights into structural and mechanism of action.. Antiviral Research, 2007, 74 (3), pp.A64. ⟨10.1016/j.antiviral.2007.01.098⟩. ⟨hal-00199087⟩
- David J Aitken, Alberto Albinati, Arnaud Gautier, Henri-Philippe Husson, Georges Morgant, et al.. Platinum(II) and palladium(II) complexes with N-aminoguanidine. European Journal of Inorganic Chemistry, 2007, pp.3327-3334. ⟨hal-00165303⟩
- Jean-Louis Soulier, Olivier Russo, Mireille Giner, Lucie Rivail, Magali Berthouze, et al.. Design and Synthesis of Specific Probes for Human 5-HT 4 Receptor Dimerization Studies. Journal of Medicinal Chemistry, 2005, 48 (20), pp.6220-6228. ⟨10.1021/jm050234z⟩. ⟨hal-03161404⟩
- Naïma Merabet, Julien Dumond, Bruno Collinet, Laurence van Baelinghem, Nicole Boggetto, et al.. New Constrained “Molecular Tongs” Designed To Dissociate HIV-1 Protease Dimer. Journal of Medicinal Chemistry, 2004, 47 (25), pp.6392-6400. ⟨10.1021/jm040833q⟩. ⟨hal-05022397⟩
Pré-publications, Documents de travail2 document
- Davide Di Lorenzo, Nicolo Bisi, Julia Kaffy, Lisa Marie Ramirez, Markus Zweckstetter, et al.. Synthetic chaperone based on Hsp90-Tau interaction inhibits pathological Tau aggregation and rescues physiological Tau-Microtubule interaction. 2025. ⟨hal-05047264⟩
- José Laxio Arenas, Jacopo Lesma, Tap Ha-Duong, Bikash Sahoo, Ayyalusamy Ramamoorthy, et al.. Relation between conformation and activity on islet amyloid polypeptide aggregation of fluorinated foldamers based on Ndifluoromethyl-1,4-triazole amino acids. 2023. ⟨hal-04273096⟩
Education/Career
- Since 2011 Full Professor in Medicinal Chemistry – BioCIS UMR 8076, Faculty of Pharmacy, Univ. Paris Saclay (ex Univ. Paris Sud)
- 2001-2011 Associate Professor in Medicinal Chemistry – BioCIS UMR 8076, Faculty of Pharmacy, Univ. Paris Sud.
- 1999/2001 Post-Doctoral researcher. Univ Milan (Italy). Pr. C. Gennari. European Grant
- 1995-1999 PhD in Organic Chemistry, Univ. Paris Descartes. Pr. H-P Husson
- 1995/1996 Dyson-Perrins Laboratory, Oxford (UK). Pr. Sir J. E. Baldwin
- 1994/1995 Master Degree in Organic Chemistry Univ. Paris 5.
One year Research training in Pharmaceutical Company (SERVIER Laboratories). - 1989-1995 Pharmacy Degree, Faculty of Pharmacy – Univ. Paris 5