Mu.Ta.Lig - COST ACTION CA15135


14 June 2016


General information

Name: LUC
Surname: DEMANGE
Cell phone number with international prefix: +33 6 33 31 33 36
Country: France
Affiliation: Université Paris Descartes and Institut de Chimie de Nice UMR CNRS 7272
Gender: F □ M X
Year of the PhD title: 2001
Personal web page: http://
Previous COST participation: No X Yes


List of 10 selected publications within last 5 years

1. Liu W.-Q., Borriello L., Allain B., Pavoni S., Hermine O., Garbay C., Raynaud F., Lepelletier Y., Demange L.* Int. J. Pept. Res. Ther., 2015, 21(1), 117-124. New peptides structurally-related to VEGF-A165 exon 7 and 8 encoded domains antagonize its binding to NRP-1 and VEGF-R1
2. Liu W.-Q., Megale V., Borriello L., Leforban B., Montès M., Goldwaser E., Gresh N., Piquemal J.-P., Hadj-Slimane R., Hermine O., Garbay C., Raynaud F., Lepelletier Y., Demange L.* Bioorg. Med. Chem. Lett., 2014, 24(17), 4254-4259. Synthesis and structure-activity relationship of non-peptidic antagonists of neuropilin-1 receptor.
3. Borriello L., Montès M., Lepelletier Y., Leforban B., Liu W.-Q., Demange L., Delhomme B., Pavoni S., Jarray R., Boucher J-L., Dufour S., Hermine O., Garbay C.; Hadj-Slimane R., Raynaud F. Cancer Lett., 2014, 349(2), 120-127. Structure-based discovery of a small non-peptidic neuropilins antagonist exerting in vitro and in vivo anti-tumor activity on breast cancer model.
4. Houzé S., Hoang, N.-T., Lozach, O., LeBras J., Meijer L., Galons H., Demange L.* Molecules, 2014, 19(9), 15237-15257. Several human cyclin-dependent kinase inhibitors, structurally related to (R)-roscovitine, as new anti-malarial agents.
5. Lautru S., Lijiang S., Demange L., Lombès T., Galons H., Challis G.L., Pernodet J.-L., Angewandte Chem., 2012, 51(30), 7454-7458. A sweet origin for the key congocidine precursor 4-acetamidopyrrole-2-carboxylate.
6. Demange L.*, Nait Abdellah F., Lozach O., Ferandin Y., Gresh N., Meijer L., Galons H. Bioorg. Med. Chem. Lett., 2013, 23(1), 125-131. Potent inhibitors of CDK5 derived from roscovitine: synthesis, biological evaluation and molecular modeling.
7. Oumata N., Bettayeb K., Ferandin Y., Demange L., Lopez-Giral A., Goddard M-L., Myrianthopoulos V., Mikros E., Flajolet M., Greengard P., Meijer L., Galons H. J. Med. Chem., 2008, 51 (17), 5229-5242. Roscovitine-derived, dual specificity inhibitors of cyclin-dependent kinases (CDKs) and casein kinase 1 (CK1)
8. Bettayeb K., Oumata N., Demange L., Meijer L., Galons H. WO2009034475 & WO2009034411. Perharidines as CDK inhibitors in the treatment of proliferative diseases. (2009)
9. Demange L., Boeglin D., Moulin A., Mousseaux D., Ryan J., Bergé G., Gagne D., Heitz A., Perrissoud D., Locatelli V., Torsello A., Galleyrand J-C., Fehrentz J-A., Martinez J. J. Med. Chem. 2007, 50(8), 1939-1957. Synthesis and pharmacological in vitro and in vivo evaluations of novel triazole derivatives as ligands of the ghrelin receptor. 1.
10. Martinez J., Fehrentz J.-A., Boeglin D., Demange L., Moulin A. EP1757290; WO2007020013; US2007037857. Novel triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors. (2007)


Main skills and expertise (up to 5)

1.      Organic synthesis, synthetic methodologies, medicinal chemistry, chemical biology
2.      Nucleic acids chemistry
3.      Fluorescence labelling
4.      Meeting management


Main equipment/facilities available in the participants’ lab (up to 5)

1.      NMR and MS platform
2.      UV/IR/DC/fluorescence/ITC
3.      Oligonucleotides synthesizer
4.      HPLC and HPLC-MS  systems
5.      Cell culture (P1)



Short personal activity proposal for the COST Action CA15135 (max 1000 characters)

I am currently involved in Nice in two research program devoted to the discovery of novel anti-angiogenic and anti-inflammatory compounds. One of the most advanced project is devoted to the search for new inhibitions of the VEGF-A/Neuropilin interaction, which is a validated target in angiogenesis. By a multi-step screening procedure, applied on a library of more than 300000 compounds, and involving structure-based virtual ligand screening (SB-VLS) then iterative cellular and molecular tests, we identified the first non peptidic inhibitors of this interaction. These compounds are active both in vitro and in vivo. In collaboration with oncologists in Nice and Monaco, we recently demonstrated that, in the case of the resistant kidney cancer, these molecules are 50 more potent than the drug currently administrated to patients. However, even if these drugs have been initially designed to specifically target the VEGF-A/Neuropilin interaction, cellular assays clearly established the existence of other molecular and cellular targets to be elucidated. The COST action 15135 might be the opportunity to identify these targets and to characterize the profile of action of these promising molecules.


In relation with these research activities and also with my technical skills, I would be also interested in new synthetic process devoted to the development of potential new multi-targeted molecules, and to the development of chemical databases.


Another aspect of my carrier is my involvement in the French Medicinal Chemistry Society (“Société de Chimie Thérapeutique, SCT”). In this society, I am chair for the Young Research Fellow Meeting (YRFM) since 2007. Even if the YRFM is a “low-cost” meeting (registration fees, housing, lunches, diner and gala cost less to 70 euros to the attendee), the science which is presented inside is not “low-cost”, as demonstrated by the support we received from (grants for students) from the EFMC (European Federation for Medicinal Chemistry), from two journals of the American Chemical Society (J. Med. Chem. and ACS Med. Chem. Lett.) and also from the Royal Chemical Society (RSC). I am also in charge of the joint award SCT – “Institut de Recherches Servier” entitled “Award for Young Researcher in Medicinal Chemistry”.  This concourse is devoted to European junior scientists, no older than 36 years. It awards the dawn of the laureate’s career, and considers globally his research contributions. This prize might be attributed to one, two… or more (!) young scientists.

Therefore, I will be interested in contributing to the organization of the COST scientific meetings and summer schools.




Work Group preference: score from 1 (preferred) to 4 (not preferred)

Work Group of the CA15135 COST Action Score
WG1: Development of new chemical entities 1
WG2: Selection of biological targets and assessment of biological data 3
WG3: Development of chemical databases 1
WG4: Development of Computational methods for multiple ligand design and discovery 4