Synthesis, Structure−Activity Relationship, and Receptor Pharmacology of a New Series of Quinoline Derivatives Acting as Selective, Noncompetitive mGlu1 Antagonists

Autor: Dominique Jean-Pierre Mabire, Alain Philippe Poncelet, Anne Simone Josephine Lesage, Ludy van Beijsterveldt, François Paul Bischoff, Ria Wouters, Christophe Adelinet, Yvan Rene Simonnet, Sophie Coupa, Marc Venet

Publikováno v: Journal of Medicinal Chemistry. 48:2134-2153

We describe the discovery and the structure-activity relationship of a new series of quinoline derivatives acting as selective and highly potent noncompetitive mGlu1 antagonists. We first identified cis-10 as a fairly potent mGlu1 antagonist (IC(50)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0f7727d62ed8ca5b6fa5eb08621ef93b
https://doi.org/10.1021/jm049499o

MK-801 alters RGS2 levels and adenylyl cyclase sensitivity in the rat striatum

Autor: Xavier Langlois, Jean-Marc Taymans, Josée E. Leysen, Anne Simone Josephine Lesage, Catarina Cruz

Publikováno v: Neuroreport, 16(2), 159-162. Lippincott Williams and Wilkins Ltd.
Taymans, J M, Cruz, C, Lesage, A S, Leysen, J E M F & Langlois, X 2005, ' MK-801 alters RGS2 levels and adenylyl cyclase sensitivity in the rat striatum ', Neuroreport, vol. 16, no. 2, pp. 159-162 . https://doi.org/10.1097/00001756-200502080-00018

The present report examines the eiects of acute NMDA antagonism on Regulator of G Protein Signaling 2 (RGS2) expression and adenylyl cyclase sensitivity in the rat striatum. MK- 801and phencyclidine rapidly down-regulate RGS2 mRNA. The down-regulatio

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d88c7e6cccfa795f055f9a7eaf0863e9
https://doi.org/10.1097/00001756-200502080-00018

Internalization of Human 5-HT4a and 5-HT4b Receptors is Splice Variant Dependent

Autor: Mirek R. Jurzak, Paul Van Gompel, Anne Simone Josephine Lesage, Katty Josson, Josée E. Leysen, Armelle Pindon, Geert Van Hecke

Publikováno v: Bioscience Reports. 24:215-223

The family of 5-HT4 receptors comprises 16 putative splice variants. We have previously shown that there are differences in signal transduction of the h5-HT4a and h5-HT4b receptors. In the present study, the internalization of these two splice varian

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4d6977989380ca83496ab646f545cfb5
https://doi.org/10.1007/s10540-005-2582-5

Neurotrophic and antileukemic daphnane diterpenoids from Synaptolepis kirkii

Autor: Luc Van Puyvelde, Simon G. Mathenge, Miroslav Cik, Francis P. Mudida, Josée E. Leysen, Wouters Walter Boudewijn Leopo, Jacky Van Dun, Ilse Van der Lindin, Anne Simone Josephine Lesage, Giovanni Appendino, Norbert De Kimpe, Weidong He

Publikováno v: Bioorganic & Medicinal Chemistry. 10:3245-3255

Biological assay guided fractionation of a dichloromethane extract of Synaptolepis kirkii led to the isolation of four new and five known daphnane-type diterpene orthoesters, whose structure was established by spectroscopic data. Full spectroscopic d

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9aa7db602da998f88d0a94f8fe21ac49
https://doi.org/10.1016/s0968-0896(02)00163-3

Binding of GDNF and Neurturin to Human GDNF Family Receptor α 1 and 2

Autor: Paul Van Gompel, Ilse Van der Linden, Stefan Masure, Miroslav Cik, Anne Simone Josephine Lesage, Robert Gordon, Josée E. Leysen, Menelas N. Pangalos

Publikováno v: Journal of Biological Chemistry. 275:27505-27512

The members of the glial cell line-derived neurotrophic factor (GDNF) family signal via binding to the glycosyl phosphatidylinositol-anchored membrane proteins, the GDNF family receptors α (GFRα), and activation of cRET. We performed a detailed ana

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::2f8761de3674ad22c644d16132725c56
https://doi.org/10.1074/jbc.m000306200