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个人简介
Funded by a government fellowship (MENRT), he earned a Ph.D. in organic chemistry in 2002 in the laboratory of Prof. Jean-Louis Kraus (Marseille). Involved in an Alzherimer’s disease program in collaboration with Trophos (Start-up located in Marseille), he notably contributed to report the first protease inhibitor able to prevent Υ-secretase-mediated production of Aβ40/42 whithout affecting Notch cleavage (Nature Cell Biology, 2001).
Funded by both “Fondation pour la Recherche Médicale” and “France Alzheimer” fellowships, he spent one year and a half of post-doctoral studies at Harvard Medical School in the laboratory of Prof. Michael S. Wolfe (Boston, MA, USA). Dealing with solid phase peptide synthesis, he reported the discovery of subnanomolar helical D-tridecapeptide inhibitor of gamma-secretase, intramembrane protease involved in Alzheimer’s disease (J. Med. Chem., 2004). After a training in biochemistry, he was involved in a biochemical program using photoaffinity probes, providing strong evidences of the presence of an initial substrate-binding site of gamma-secretase on presenilin, near the active site (PNAS, 2005).
In 2004, he moved to Strasbourg (France) where he joined the medicinal chemistry laboratory of Dr. Jean-Jacques Bourguignon as a post-doc, before earning a permanent position as associate research professor (CNRS) in 2005.
His research interests deal with discovery, design and development of new pharmacological tools and therapeutic agents targeting mainly receptors (GPCRs) for the treatment of diseases or dysfunctions of central nervous system (e.g. pain, inflammation, psychiatric diseases…). He was more particularly involved in the development of new ligands of the RFamide receptors (GPCRs including NPFFR1, NPFFR2, GPR10, GPR54, and GPR103). He developed the first orally-active antagonist of the NPFF recptors for the prevention of opioid-induced hyperalgesia (Patent, 2012 and several articles). More recently, he is also involved in other fields such as cancer or the neglected diseases.
From a chemical point of view, one of his interests is focused on heterocyclic chemistry (synthesis of new heterocyclic scaffold, innovation in cross-coupling reaction, cycloisomerisation, etc). Since 2013, he is developing with Martine Schmitt a green chemistry approach, with the development of metal-catalyzed cross-coupling reactions (Ullmann, Suzuki, Sonogashira, Buchwald..) under micellar conditions (Green Chem, 2014).
Working on GPCRs recognizing neuropeptides, he is also interested by peptide synthesis. Using his knowledge in metal-catalysis applied to heterocyclic chemistry, he developed new peptidomimetics using metal-catalyzed reactions (patent 2014; OBC, 2015).
Both heterocyclic chemistry and peptidomimetic synthesis afford interesting scaffolds for medicinal chemistry and drug design.
研究兴趣
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Arthur Laure, Chloe Royet,Frederic Bihel,Blandine Baratte,Stephane Bach,Marion Peyressatre,May C. Morris
ACS PHARMACOLOGY & TRANSLATIONAL SCIENCEno. 5 (2024): 1377-1385
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Proceedings of the 36th European and the 12th International Peptide Symposium (2022)
Aline Bamia,Maha Sinane,Rima Naït-Saïdi,Jamila Dhiab,Marc Keruzoré,Phu Hai Nguyen, Agathe Bertho,Flavie Soubigou,Sophie Halliez,Marc Blondel,Capucine Trollet,Martine Simonelig,
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