M Sylvain Broussy » Team : Medicinal chemistry and translational research

M Sylvain Broussy

Professor University Paris CitéCiTCoM
Tel :: Number

Biographical Info

Research:
  • Organic synthesis
  • Spectroscopy
  • Medicinal chemistry
  • Biochemical and biophysical assays
  • Molecular modeling
Activity:
  • Member of the laboratory council
Selected Publications :
  1. Wang, L, Liu, WQ, Broussy, S, Han, B, Fang, H(2023)Recent advances of anti-angiogenic inhibitors targeting VEGF/VEGFR axis. Front Pharmacol 14 :1307860.
  2. Ye, X, Gaucher, JF, Hu, H, Wang, L, Broussy, S(2023)Dimer Peptide Ligands of Vascular Endothelial Growth Factor: Optimizing Linker Length for High Affinity and Antiangiogenic Activity. J Med Chem 66 (14):9753-9765.
  3. Namjoo, M et al.(2023)A VEGFB-Based Peptidomimetic Inhibits VEGFR2-Mediated PI3K/Akt/mTOR and PLCγ/ERK Signaling and Elicits Apoptotic, Antiangiogenic, and Antitumor Activities. Pharmaceuticals (Basel) 16 (6):.
  4. Ye, F, Lin, M, Jin, J, Broussy, S(2022)Editorial: Computer-aided drug design: Drug discovery, computational modelling, and artificial intelligence. Front Chem 10 :968687.
  5. Gaucher, JF, Reille-Seroussi, M, Broussy, S(2022)Structural and ITC Characterization of Peptide-Protein Binding: Thermodynamic Consequences of Cyclization Constraints, a Case Study on Vascular Endothelial Growth Factor Ligands. Chemistry 28 (48):e202200465.
  6. Ye, X, Gaucher, JF, Vidal, M, Broussy, S(2021)A Structural Overview of Vascular Endothelial Growth Factors Pharmacological Ligands: From Macromolecules to Designed Peptidomimetics. Molecules 26 (22):.
  7. Wang, L et al.(2021)A Cyclic Peptide Epitope of an Under-Explored VEGF-B Loop 1 Demonstrated In Vivo Anti-Angiogenic and Anti-Tumor Activities. Front Pharmacol 12 :734544.
  8. Tiwari, VK, Powell, DR, Broussy, S, Berkowitz, DB(2021)Rapid Enantioselective and Diastereoconvergent Hybrid Organic/Biocatalytic Entry into the Oseltamivir Core. J Org Chem 86 (9):6494-6503.
  9. Laaroussi, H et al.(2020)Synthesis of indole inhibitors of silent information regulator 1 (SIRT1), and their evaluation as cytotoxic agents. Eur J Med Chem 202 :112561.
  10. Sadremomtaz, A et al.(2020)Molecular docking, synthesis and biological evaluation of Vascular Endothelial Growth Factor (VEGF) B based peptide as antiangiogenic agent targeting the second domain of the Vascular Endothelial Growth Factor Receptor 1 (VEGFR1D2) for anticancer application. Signal Transduct Target Ther 5 (1):76.
  11. Broussy, S, Laaroussi, H, Vidal, M(2020)Biochemical mechanism and biological effects of the inhibition of silent information regulator 1 (SIRT1) by EX-527 (SEN0014196 or selisistat). J Enzyme Inhib Med Chem 35 (1):1124-1136.
  12. Wang, L et al.(2019)Structural studies of the binding of an antagonistic cyclic peptide to the VEGFR1 domain 2. Eur J Med Chem 169 :65-75.
  13. Trapiella-Alfonso, L et al.(2018)Colorimetric immunoassays for the screening and specificity evaluation of molecules disturbing VEGFs/VEGFRs interactions. Anal Biochem 544 :114-120.
  14. Wang, L et al.(2018)Synthesis and characterization of water-soluble macrocyclic peptides stabilizing protein α-turn. Org Biomol Chem 16 (3):459-471.
  15. Wang, L et al.(2017)Identification of Peptidic Antagonists of Vascular Endothelial Growth Factor Receptor 1 by Scanning the Binding Epitopes of Its Ligands. J Med Chem 60 (15):6598-6606.
  16. Reille-Seroussi, M et al.(2017)VEGFR1 domain 2 covalent labeling with horseradish peroxidase: Development of a displacement assay on VEGF. Anal Biochem 530 :107-112.
  17. Gaucher, JF et al.(2016)Biophysical Studies of the Induced Dimerization of Human VEGF Receptor 1 Binding Domain by Divalent Metals Competing with VEGF-A. PLoS One 11 (12):e0167755.
  18. Cottet, K et al.(2016)Guttiferone A Aggregates Modulate Silent Information Regulator 1 (SIRT1) Activity. J Med Chem 59 (20):9560-9566.
  19. Karukurichi, KR et al.(2015)Mini-ISES identifies promising carbafructopyranose-based salens for asymmetric catalysis: Tuning ligand shape via the anomeric effect. Sci Adv 1 (6):.
  20. Reille-Seroussi, M et al.(2015)Vascular Endothelial Growth Factor Peptide Ligands Explored by Competition Assay and Isothermal Titration Calorimetry. Biochemistry 54 (33):5147-56.
  21. Wang, L et al.(2014)Design and synthesis of C-terminal modified cyclic peptides as VEGFR1 antagonists. Molecules 19 (10):15391-407.
  22. Friest, JA, Broussy, S, Chung, WJ, Berkowitz, DB(2011)Combinatorial catalysis employing a visible enzymatic beacon in real time: synthetically versatile (pseudo)halometalation/carbocyclizations. Angew Chem Int Ed Engl 50 (38):8895-9.
  23. Friest, JA, Maezato, Y, Broussy, S, Blum, P, Berkowitz, DB(2010)Use of a robust dehydrogenase from an archael hyperthermophile in asymmetric catalysis-dynamic reductive kinetic resolution entry into (S)-profens. J Am Chem Soc 132 (17):5930-1.
  24. Broussy, S, Cheloha, RW, Berkowitz, DB(2009)Enantioselective, ketoreductase-based entry into pharmaceutical building blocks: ethanol as tunable nicotinamide reductant. Org Lett 11 (2):305-8.
  25. Broussy, S, Waldmann, H(2007)Solid phase synthesis of highly substituted tetrahydropyrans by tandem ene-reaction/intramolecular Sakurai cyclization. J Comb Chem 9 (6):1138-43.
  26. Broussy, S, Bernardes-Génisson, V, Quémard, A, Meunier, B, Bernadou, J(2005)The first chemical synthesis of the core structure of the benzoylhydrazine-NAD adduct, a competitive inhibitor of the Mycobacterium tuberculosis enoyl reductase. J Org Chem 70 (25):10502-10.
  27. Kupan, A et al.(2006)Guanine oxidation by electron transfer: one- versus two-electron oxidation mechanism. Chembiochem 7 (1):125-33.
  28. Broussy, S et al.(2005)1H and 13C NMR characterization of pyridinium-type isoniazid-NAD adducts as possible inhibitors of InhA reductase of Mycobacterium tuberculosis. Org Biomol Chem 3 (4):670-3.
  29. Broussy, S, Bernardes-Génisson, V, Gornitzka, H, Bernadou, J, Meunier, B(2005)Studies on the 4-benzoylpyridine-3-carboxamide entity as a fragment model of the Isoniazid-NAD adduct. Org Biomol Chem 3 (4):666-9.
  30. Broussy, S, Coppel, Y, Nguyen, M, Bernadou, J, Meunier, B(2003)1H and 13C NMR characterization of hemiamidal isoniazid-NAD(H) adducts as possible inhibitors of InhA reductase of Mycobacterium tuberculosis. Chemistry 9 (9):2034-8.
  31. Nguyen, M, Quémard, A, Broussy, S, Bernadou, J, Meunier, B(2002)Mn(III) pyrophosphate as an efficient tool for studying the mode of action of isoniazid on the InhA protein of Mycobacterium tuberculosis. Antimicrob Agents Chemother 46 (7):2137-44.
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