Marc Le Borgne - Professeur - Directeur de l'EA 4446

Marc Le Borgne

Tel.: +33 478 777 542 (Work)
Fax: +33 478 777 082 (Secretary)


Education and Experiences

2011 Director of the Research Team EA 4446 B2MC, UCBL.
2009 Student Exchange Correspondent with Canada and USA, Faculty of Pharmacy, UCBL.
2008 Recruitment as Professor in Medicinal Chemistry, Faculty of Pharmacy - University Lyon 1 (UCBL).
2007 Habilitation in Medicinal Chemistry, national examination - Paris.
2005/08 Vice-Dean in charge of general affairs, logistics and international cooperation, Faculty of Pharmacy - Nantes Atlantic University.
2003 Accreditation to supervise research (HDR diploma) in Medicinal Chemistry. Title: “Taylor-made molecules as aromatase inhibitors and antifungal agents” - Nantes Atlantic University.
2000 Research assistant (1997-1999) and Assistant Professor (2000-2008) in the Laboratory of Medicinal Chemistry, Faculty of Pharmacy - Nantes Atlantic University.
Lecturer within the framework of continuing education of Pharmacists - Association of Post University Higher Education in Pharmacy - Region Loire-Atlantique.
1998 Thesis award in physico-chemical sciences, awarded by the French Academy of Pharmacy.
1997 Pharmaco-chemistry Ph-D at the Nantes Atlantic University.
1994 PharmD at the Nantes Atlantic University.
1992 Practice of Pharmacy (POP) at the Welsh School of Pharmacy.

Research Interests

Drug Discovery, Ligand-Based Drug Design, Medicinal and pharmaceutical chemistry, Small molecules

Infectiology: imidazole and triazole-type inhibitors as antifungal and/or antileishmanial agents (CYP51, PLA2), meningococcal polysaccharide (serogroup C, Menactra®), site-directed conjugation (glycoconjugate vaccines), Zn-chelating agents.
Cancerology: indole-type compounds as enzyme inhibitors (CYP19, CYP26), naphthyridine-type compounds as kinase inhibitors (Aurora), indenoindole- and indole-type compounds as kinase inhibitors (CK2, Dyrks), design of allosteric and protein-protein interaction inhibitors.
Chemoresistances: peptidomimetics as modulators of ABC-type transporters, design of ABCG2 inhibitors.
Materials: synthetic clays, their preparation and complexation studies.
Studies on Active Pharmaceutical Ingredients: spironolactone, tetrabenazine, tramadol.

Scientific Expertise and Reviewing

- Member of the editorial boards of Current Bioactive Compounds and Pharmaceuticals.
- Associate Editor of J. Enz. Inhib. Med. Chem. (until 2009-2012).
- Reviewing for publication in J. Enz. Inhib. Med. Chem., ACS Med. Chem. Lett., Arch. Pharm. Med. Chem., Curr. Bioactiv. Compds, Bioorg. Med. Chem. Lett., Bioorg. Med. Chem., Eur. J. Med. Chem., Tetrahedron Lett., ChemMedChem.
- 15 supervisions of PhDs (4 with international label).
- Reviewing of Research Applications: National Research Agency (France), Regional Council of Hauts-de-France (France), French National Cancer League (France), Evaluator for The Czech Academy of Sciences (Czech Republic), Committee for Evaluation of Research (Italy).
- Management of industrial contracts: (i) Yang Ji Chemicals Co – South Korea (antifungals); (ii) Æterna Zentaris – Germany (kinase inhibitors); Sanofi Pasteur – Neuville-sur-Saône (glycoconjugate vaccines, conjugation chemistry).

Recent Peer-Reviewed Journal Articles

1. Jabor Gozzi G, Bouaziz Z, Winter E, Daflon-Yunes N, Aichele D, Nacereddine A, Marminon C, Valdameri G, Zeinyeh W, Bollacke A, Guillon J, Lacoudre A, Pinaud N, Cadena SM, Jose J, Le Borgne M, Di Pietro A. Converting Potent Indeno[1,2-b]indole Inhibitors of Protein Kinase CK2 into Selective Inhibitors of the Breast Cancer Resistance Protein ABCG2. J Med Chem. 2015 Jan 8;58(1):265-77.
2. Neyra C, Paladino J, Le Borgne M. Depolymerization of polysialic acid by hydrogen peroxide oxidation. Structural exploration of tetrasialic acid and its reaction products. Carbohydr Polym. 2015 Jan 22;115:494-501.
3. Bouaziz Z, Issa S, Gentili J, Gratz A, Bollacke A, Kassack M, Jose J, Herfindal L, Gausdal G, Døskeland SO, Mullié C, Sonnet P, Desgrouas C, Taudon N, Valdameri G, Di Pietro A, Baitiche M, Le Borgne M. Biologically active carbazole derivatives: focus on oxazinocarbazoles and related compounds. J Enzyme Inhib Med Chem. 2015 Apr;30(2):180-8.
4. Alchab, F.; Sibille, E.; Ettouati, L.; Bana, E.; Bouaziz, Z.; Mularoni, A.; Monniot, E.; Bagrel, D.; Jose, J.; Le Borgne, M.; Chaimbault, P. Screening of indeno[1,2-b]indoloquinones by MALDI-MS: a new set of potential CDC25 phosphatase inhibitors brought to light. J Enzyme Inhib Med Chem. 2016;31(sup3):25-32.
5. Haidar S, Bouaziz Z, Marminon C, Laitinen T, Poso A, Le Borgne M, Jose J. Development of pharmacophore model for indeno[1,2-b]indoles as human protein kinase CK2 inhibitors and database mining. Pharmaceuticals (Basel). 2017 Jan 9;10(1).
6. Bestgen, B.; Belaid-Choucair, Z.; Lomberget, T.; Le Borgne, M.; Filhol, O.; Cochet, C. In search of small molecule inhibitors targeting the flexible CK2 subunit interface. Pharmaceuticals (Basel). 2017 Feb 3;10(1).
7. Lamera, E.; Bouacida, S.; Le Borgne, M.; Bouaziz, Z.; Bouraiou, A. Sequential MCR/Fisher indolization strategy for the construction of polycyclic carbazole derivatives. Tetrahedron Lett. 2017 March 29;58(13):1305-07.
8. Bayart, C.; Peronin, S.; Jean, E.; Paladino, J.; Talaga, P.; Le Borgne, M. The combined use of analytical tools for exploring tetanus toxin and tetanus toxoid structures. J Chromatogr B Analyt Technol Biomed Life Sci. 2017 Jun 1;1054:80-92.
9. Enhancement of iodinin solubility by encapsulation into cyclodextrin nanoparticles. Prandina A, Herfindal L, Radix S, Rongved P, Døskeland SO, Le Borgne M, Perret F. J Enzyme Inhib Med Chem. 2018 Dec;33(1):370-375.
10. Self-Assembled Supramolecular Nanoparticles Improve the Cytotoxic Efficacy of CK2 Inhibitor THN7. Nacereddine A, Bollacke A, Róka E, Marminon C, Bouaziz Z, Fenyvesi F, Bácskay IK, Jose J, Perret F, Le Borgne M. Pharmaceuticals (Basel). 2018 Jan 26;11(1).

Recent Invited Lectures

1. Le Borgne M. Cancer drug design and discovery: focus on the design of small molecules. College of Pharmacy, California Northstate University, Pr. Anupam Bishayee. Sacramento (US), 2014 Dec 18.
2. Le Borgne M. At the crossroads of chemistry and biology: inhibiting protein kinase CK2 by heterocyclic small molecules. XVI International Conference on Heterocycles in Bioorganic Chemistry, Bioheterocycles 2015, University of Lorraine. Metz (FR), 2015 Jun 11.
3. Le Borgne M. Protein kinase CK2 is an attractive druggable target for anti-cancer drug design. Faculty of Pharmacy, University of Debrecen, Pr. Bácskay Ildikó. Debrecen (HU), 2015 Jul 16.
4. Le Borgne M. Polyheterocyclic systems: design and synthesis of anti-cancer agents and more… Scienze Farmaceutiche, Università degli Studi di Firenze, Pr. Claudiu Supuran. Firenze (IT), 2016 Jun 14.
5. Le Borgne M. The medicinal chemist's toolbox: how to use it to develop small molecule CK2 inhibitors. European Chemistry Congress, Holiday Inn Rome Aurelia. Rome (IT), 2016 Jun 16-18.
6. Le Borgne M. Indeno[1,2-b]indoles: a good scaffold for designing bioactive molecules. 5th International Conference on MedChem & CADD. Phoenix (US), 2016 Dec 5-7.
7. Le Borgne M. Recent developments to convert potent indeno[1,2-b]indole inhibitors of protein kinase CK2 into selective inhibitors of the breast cancer resistance protein ABCG2. Skaggs School of Pharmacy and Pharmaceutical Sciences, UC San Diego, Dr. Ruben Abagyan. San Diego (US), 2016 Dec 9.
8. Le Borgne M. Exploration of indenoindoles as promising bioactive agents: design, synthesis, 3D-QSAR study, ADME properties, biological activities. Franco-Brazilian Meeting on Pharmaceutical Sciences. Curitiba (BR), 2017 Feb 13-14.
9. Le Borgne M. An international MedChem toolbox for developing Drug Discovery projects. Department of Pharmacology and Pharmaceutical Sciences, USC School of Pharmacy, Pr. Vassilios Papadopoulos. Los Angeles (US), 2017 Jun 9.
10. Le Borgne M. Exploring protein kinase CK2 by designing heterocyclic compounds. 7th BBBB International Conference on Pharmaceutical Sciences. Balatonfüred (HU), 2017 Oct 5.