Mu.Ta.Lig - COST ACTION CA15135

Prof. Vincent LISOWSKI

14 June 2016


General information

Surname: Vincent
Cell phone number with international prefix: +33670542856
Country: FRANCE
Affiliation: Montpellier University
Gender: F □ M
Year of the PhD title: 2002
Personal web page:     here  
Previous COST participation: No Yes


List of 10 selected publications within last 5 years

1. Vezenkov, L.; Sanchez, C; Bellet, V.; Martin, V.; Maynadier, M.; Bettache, N.; Lisowski, V.; Martinez, J.; Garcia, M.; Amblard,M.; Hernandez, J.-F. Structure–Activity Relationships of JMV4463, a Vectorized Cathepsin D Inhibitor with Antiproliferative Properties : The Unique Role of the AMPA-Based Vector. ChemMedChem 2016, 11, 302-308.
2. Mathieu, L.; Bonnel, C.; Masurier, N.; Maillard, L. T.; Martinez, J.; Lisowski, V. Cross-Claisen Condensation of N-Fmoc-Amino Acids – A Short Route to Heterocyclic gamma-Amino Acids. European Journal of Organic Chemistry 2015, 2262-2270.
3. Denoyelle, S.; Tambutet, G.; Masurier, N.; Maillard, L. T.; Martinez, J.; Lisowski, V. Synthesis of Thieno[3,2-e][1,4]diazepin-2-ones: Application of an Uncatalysed Pictet-Spengler Reaction. European Journal of Organic Chemistry 2015, 7146-7153.
4. Arama, D. P.; Soualmia, F.; Lisowski, V.; Longevial, J.-F.; Bosc, E.; Maillard, L. T.; Martinez, J.; Masurier, N.; El Amri, C. Pyrido-imidazodiazepinones as a new class of reversible inhibitors of human kallikrein 7. European Journal of Medicinal Chemistry 2015, 93, 202-213.
5. Malcor, J.-D.; Brouillette, Y.; Graffion, J.; Spielmann, K.; Masurier, N.; Maillard, L. T.; Martinez, J.; Lisowski, V. Synthesis and reactivity of pyrrolo[3,2-d][1,3]oxazine-2,4-dione. Access to new pyrrolo[3,2-e][1,4]diazepine-2,5-diones. Tetrahedron 2014, 70, 4631-4639.
6. Legrand, B.; Mathieu, L.; Lebrun, A.; Andriamanarivo, S.; Lisowski, V.; Masurier, N.; Zirah, S.; Kang, Y. K.; Martinez, J.; Maillard, L. T. Thiazole-Based gamma-Building Blocks as Reverse-Turn Mimetic to Design a Gramicidin S Analogue: Conformational and Biological Evaluation. Chemistry-a European Journal 2014, 20, 6713-6720.
7. Gallud, A.; Vaillant, O.; Maillard, L. T.; Arama, D. P.; Dubois, J.; Maynadier, M.; Lisowski, V.; Garcia, M.; Martinez, J.; Masurier, N. Imidazopyridine-fused [1,3]-diazepinones: Synthesis and antiproliferative activity. European Journal of Medicinal Chemistry 2014, 75, 382-390.
8. Mathieu, L.; Legrand, B.; Deng, C.; Vezenkov, L.; Wenger, E.; Didierjean, C.; Amblard, M.; Averlant-Petit, M.-C.; Masurier, N.; Lisowski, V.; Maillard, L. T. Helical Oligomers of Thiazole-Based -Amino Acids: Synthesis and Structural Studies. Angewandte Chemie-International Edition 2013, 52, 6006-6010.
9. Malcor, J.-D.; Payrot, N.; David, M.; Faucon, A.; Abouzid, K.; Jacquot, G.; Floquet, N.; Debarbieux, F.; Rougon, G.; Martinez, J.; Khrestchatisky, M.; Vlieghe, P.; Lisowski, V. Chemical Optimization of New Ligands of the Low-Density Lipoprotein Receptor as Potential Vectors for Central Nervous System Targeting. Journal of Medicinal Chemistry 2012, 55, 2227-2241.
10. Vlieghe, P.; Lisowski, V.; Martinez, J.; Khrestchatisky, M. Synthetic therapeutic peptides: science and market. Drug Discovery Today 2010, 15, 40-56.


Main skills and expertise (up to 5)

1. Medicinal chemistry (enzyme inhibition, peptide-based drug delivery system, foldamer)
2. organic chemistry : Peptide and heterocyclic chemistry
3. Solid phase chemistry (SPPS and SPOS)
4. Chemical biology  (ADC design)
5. Hit to Lead optimization, drug design


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

1. SynBio3 platform for SPPS facilities
2. Mass spectrometry platform (MS, LC-MS, GC-MS) (ESI, MALDI)
3. NMR facilities (300, 400, 600MHz, HR-MAS)
4. Liberty® peptide synthesizer
5. Internal chemical library



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

I am professor in pharmaceutical & medicinal chemistry (Pharm D & PhD) and hospital practitioner with an expertise in drug chemistry and pharmacology.  I do my research in the Institute of Biomolecules Max-Mousseron (IBMM – CNRS5247) in Montpellier (France, ). The research activities in IBMM concentrate on essential biomolecules such as lipids, nucleosides, nucleotides and nucleic acids, peptides and proteins, glycosides, biopolymers, prebiotic molecules and fluorinated molecules. The research programmes conducted on biomolecules concern their design, their synthesis and their pharmacology. In our group “solid-phase chemistry, peptides and heterocycles” research programs are mainly devoted to the design and the synthesis of RCPG ligands, enzyme inhibitors in the fields of cancerology, infectiology and neurosciences. We also develop technological innovations in the field of peptide engineering, foldamers, drug delivery systems and peptide-based materials. We have strong skills in heterocyclic, peptidic and foldamer chemistry. From a personal point of view I am currently involved in projects dedicated to the design of peptide-based vectors and the development of innovative antibody-drug conjugates (ADC). As peptides (and heterocycles) are potential useful tools in multi-target ligand approach, we offer facilities to develop peptide-based (or heterocycle-based) focused libraries by combinatorial approaches using SPPS or SPOS technology with a potential access to purification and analytical LC/MS platforms. The diversity of molecules in the internal library of IBMM is also an opportunity to gain new chemical entities.

I am also in the scientific council of the French Medicinal Chemistry Society (Société de Chimie Thérapeutique – SCT). As an active member of SCT, I contributed to the organization of several international meetings in the field of medicinal chemistry & chemical biology (Young Research Fellow Meeting (2014 in Montpellier) and the joint meeting SCT/GDCh Frontiers in Medicinal Chemistry (2016 in Bonn). This background in the organization of MedChem meetings and my position in SCT could be an opportunity to facilitate the development of European network for Cost Action15135 and to contribute to future 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 3
WG4: Development of Computational methods for multiple ligand design and discovery 4