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

Marc Le Borgne

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

Email: marc.le-borgne[at]

Education and Experiences

2011 Director of the Research Team EA 4446 B2C, UCBL.
2009 Student Exchange Correspondent with Canada, 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.
2006 General secretary of the association of Pharmacochemistry Grouping of the Atlantic Arc (GP2A) and Member of the editorial board of Journal of Enzyme Inhibition and Medicinal Chemistry.
2003 Accreditation to supervise research (HDR diploma) in Medicinal Chemistry. Title: “Taylor-made molecules as aromatase inhibitors and antifungal agents” - Nantes Atlantic University.
2000 Lecturer in the Group of Pr. G. Le Baut, at the Department 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 - Loire-Atlantique.
1997-1999 Research assistant in the Department of Medicinal Chemistry, Faculty of Pharmacy - Nantes Atlantic University.
1998 Thesis award in physico-chemical sciences, awarded by Académie Nationale de Pharmacie.
1997 Pharmaco-chemistry Ph-D at the Nantes Atlantic University.
1994 PharmD at the Nantes Atlantic University.

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 conjugaison, 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.
Studies on Active Pharmaceutical Ingredients: spironolactone, tetrabenazine, tramadol.

Scientific Expertise and Reviewing

- Associate Editor of J. Enz. Inhib. Med. Chem. (until 2009-2012).
- Member of the editorial board of Current Bioactive Compounds and Pharmaceuticals.
- 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.
- 14 supervisions of PhDs (5 with international label).
- Reviewing of Research Applications: National Research Agency (France), Structural & Regional Research Projects from Picardie and Lille (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 Corea (antifungals); (ii) Æterna Zentaris – Germany (kinase inhibitors); Sanofi Pasteur – Neuville-sur-Saône (glycoconjugate vaccines).

Recent Peer-Reviewed Journal Articles

1. Bourezg Z, Cartiser N, Ettouati L, Guillon J, Lacoudre A, Pinaud N, Le Borgne M, Fessi H. Structural elucidation of two photolytic degradation products of tetrabenazine. J Pharm Biomed Anal. 2014 Mar;91:138-43.
2. Defaux J, Antoine M, Logé C, Le Borgne M, Schuster T, Seipelt I, Aicher B, Teifel M, Günther E, Gerlach M, Marchand P. Discovery of (7-aryl-1,5-naphthyridin-2-yl)ureas as dual inhibitors of ERK2 and Aurora B kinases with antiproliferative activity against cancer cells. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3748-52.
3. 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.
4. 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.
5. de Ravel MR, Alameh G, Melikian M, Mahiout Z, Emptoz-Bonneton A, Matera EL, Lomberget T, Barret R, Rocheblave L, Walchshofer N, Beltran S, El Jawad L, Mappus E, Grenot C, Pugeat M, Dumontet C, Le Borgne M, Cuilleron CY. Synthesis of new steroidal inhibitors of p-glycoprotein-mediated multidrug resistance and biological evaluation on k562/r7 erythroleukemia cells. J Med Chem. 2015 Feb 26;58(4):1832-45.
6. 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.
7. Gratz A, Bollacke A, Stephan S, Nienberg C, Le Borgne M, Götz C, Jose J. Functional display of heterotetrameric human protein kinase CK2 on Escherichia coli: a novel tool for drug discovery. Microb Cell Fact. 2015 Jun 3;14:74.
8. Gozzi GJ, Bouaziz Z, Winter E, Daflon-Yunes N, Honorat M, Guragossian N, Marminon C, Valdameri G, Bollacke A, Guillon J, Pinaud N, Marchivie M, Cadena SM, Jose J, Le Borgne M, Di Pietro A. Phenolic indeno[1,2-b]indoles as ABCG2-selective potent and non-toxic inhibitors stimulating basal ATPase activity. Drug Des Devel Ther. 2015 Jul 3;9:3481-95.
9. Lecerf-Schmidt F, Haudecoeur R, Peres B, Ferreira Queiroz MM, Marcourt L, Challal S, Ferreira Queiroz E, Sotoing Taiwe G, Lomberget T, Le Borgne M, Wolfender JL, De Waard M, Robins RJ, Boumendjel A. Biomimetic synthesis of Tramadol. Chem Commun (Camb). 2015 Oct 4;51(77):14451-3.
10. Bollacke A, Nienberg C, Le Borgne M, Jose J. Toward selective CK2alpha and CK2alpha' inhibitors: Development of a novel whole-cell kinase assay by Autodisplay of catalytic CK2alpha'. J Pharm Biomed Anal. 2016 Mar 20;121:253-60.

Recent Invited Lectures

1. Le Borgne M. The indole scaffold and Drug Design. Centre for Pharmacy, University of Bergen, Med. Chem. Seminar, Pr. Bengt E. Haug. Bergen (NO), December 7 2010.
2. Le Borgne M., Bouaziz, Z. An overview on Casein Kinase 2. Translasjonell Signaleringsgruppe, Institute of Biomedicine, University of Bergen, Med. Chem. Seminar, Dr. Stein O. Døskeland. Bergen (NO), December 7 2010.
3. Le Borgne M. La Chimie à l’heure du développement durable : développement d’une « chimie durable » dans l’industrie pharmaceutique. Les Mercredis de la Science, Centre Culturel Français de l’Ambassade de France, Dr. Jean-Claude Duclos. Oslo (NO), December 8 2010.
4. Le Borgne M. Design and synthesis of small molecules as potential therapeutic agents. School of Pharmacy, University of Oslo, Med. Chem. Seminar, Pr. Trond V. Hansen. Oslo (NO), December 9 2010.
5. Le Borgne M. The pharmacist, a (bio)polytechnician of health: chemical sciences versus biological sciences. Campus Rockefeller, University Claude Bernard Lyon 1, 10th Conference of CIDPharmef, Lyon, May 31 2011.
6. Le Borgne M. (Aza)heterocycles and peptidomimetics as templates in Drug Design. Institut für Pharmazeutische und Medizinische Chemie, Universität des Saarlandes, Deutsch-Französischer Diskurs, Pr. Rolf W. Hartmann. Saarbruecken (DE), July 12 2011.
7. Le Borgne M. Development of small molecules as chemical probes and therapeutic agents. Bergen Hospital, Universitetet i Bergen, Dr. Stein O. Døskeland. Bergen (NO), October 31 2012.
8. Le Borgne M. From target to drug: development of bioactive small molecules as CK2 inhibitors and reversing agents. Faculty of Health Sciences, UiT The Arctic University of Norway, Drug Discovery Seminar, Pr. Ingebrigt Sylte. Tromsø (NO), November 2 2012.
9. Le Borgne M. A collaborative project in a European network in the search for new regulators of cancer cell development: indeno[1,2-b]indoles as a novel template for design of CK2 Inhibitors. Norwegian Pharmaceutical Society, Farmasidagene 2012, i Oslo Kongressenter Folkets Hus. Oslo (NO), November 7-9 2012.
10. Le Borgne M. Structure, function and inhibition of human protein kinase CK2. 27èmes Journées Franco-Belges (JFB) de Pharmacochimie and 21st Conference of the Groupement des Pharmacochimistes de l’Arc Atlantique (GP2A), University of Lille 2. Lille (FR), June 5-7 2013.
11. Le Borgne M. An international multidisciplinary approach to target protein kinase CK2. Biocenter 2, University of Helsinki, Pr. Jari Yli-Kauhaluoma. Helsinki (FI), November 27 2014.
12. Le Borgne M. Protein kinase CK2 is an attractive druggable target for anti-cancer drug design. Biocenter Oulu, University of Oulu, Pr. Lari Lehtiö. Oulu (FI), November 28 2014.
13. 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 (USA), December 18 2014.
14. 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), June 11 2015.
15. 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), July 16 2015.

Perspectives 2016, 2017…

Development of a new project: Zinc chelation by small molecule adjuvants potentiates meropenem activity.
Scientific leadership for a new Master “ Conception et Optimisation des Produits de Santé” (COPS).
Preparation of a Summer School on Innovation and Drug Discovery, University of Claude Bernard Lyon 1 (FR).
Management of the network “ChemBioInteractions” (FR, DE, NO, FI…).