Synthesis of new 8(S)-HETE analogs and their biological evaluation as activators of the PPAR nuclear receptors

Autor: Erwan Ayral, Pierre Renard, Jean A. Boutin, Paul Mosset, Alain Ktorza, René Grée, Frédéric Caijo, Catherine Dacquet, Anne-Lise Girard, Valérie Audinot, Melanie Liutkus, Daniel H. Caignard

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry
Journal of Enzyme Inhibition and Medicinal Chemistry, Informa Healthcare, 2010, 25 (5), pp.653-72. ⟨10.3109/14756360903468171⟩
Journal of Enzyme Inhibition and Medicinal Chemistry, 2010, 25 (5), pp.653-72. ⟨10.3109/14756360903468171⟩

Structural modifications around 8-HETE (8-hydroxyeicosatetraenoic acid), a natural agonist of the PPAR (peroxisome proliferator-activated receptor) nuclear receptors have led previously to the identification of a promising analog, the quinoline S 706

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bb4bdbf3d3d5d3d2c0f5e73c1a47da28
https://pubmed.ncbi.nlm.nih.gov/20518620

Design, synthesis, and biological evaluation of 1,5-benzothiazepine-4-one derivatives targeting factor VIIa/tissue factor

Autor: Pierre Fulcrand, Philippe Gloanec, Philippe Mennecier, Jean Martinez, Gilbert Bergé, Jean-François Hernandez, Alain Rupin, Erwan Ayral, Tony Verbeuren, Guillaume De Nanteuil

Publikováno v: Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters, Elsevier, 2009, 19 (5), pp.1386-1391. ⟨10.1016/j.bmcl.2009.01.039⟩

414UR Times Cited:0 Cited References Count:43; The 1,5-benzothiazepine-4-one scaffold was earlier shown to provide efficient protease inhibitors. In this contribution, we describe its use in the design of factor VIIa/tissue factor inhibitors. A serie

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4920ba8c71c1daae63c453b41f9c7f68
https://hal.archives-ouvertes.fr/hal-00389293

JLK inhibitors: isocoumarin compounds as putative probes to selectively target the gamma-secretase pathway

Autor: Frédéric, Checler, Checler, Frédéric, Cristine, Alves da Costa, Alves da Costa, Cristine, Erwan, Ayral, Ayral, Erwan, David, Andrau, Andrau, David, Cécile, Dumanchin, Dumanchin, Cécile, Michael, Farzan, Farzan, Michael, Jean-François, Hernandez, Hernandez, Jean-François, J, Martinez, Solveig, Lefranc-Jullien, Lefranc-Jullien, Solveig, Philippe, Marambaud, Marambaud, Philippe, Andrea, Pasini, Pasini, Andrea, Agnès, Petit, Petit, Agnès, Christopher, Phiel, Phiel, Christopher, Philippe, Robert, Robert, Philippe, Peter, St George-Hyslop, St George-Hyslop, Peter, Sherwin, Wilk, Wilk, Sherwin

Publikováno v: Current Alzheimer research. 2(3)

Alzheimer's disease is characterized by the extracellular deposition of the amyloid beta-peptide that derives from its precursor betaAPP by sequential actions of beta- and gamma- secretases, respectively. Recent studies aimed at identifying these enz

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::99fd95cb86e641264dae08c4e81a399b
https://pubmed.ncbi.nlm.nih.gov/15974898

BACE1- and BACE2-expressing human cells: characterization of beta-amyloid precursor protein-derived catabolites, design of a novel fluorimetric assay, and identification of new in vitro inhibitors

Autor: David, Andrau, Cecile, Dumanchin-Njock, Erwan, Ayral, Jean, Vizzavona, Mike, Farzan, Michel, Boisbrun, Pierre, Fulcrand, Jean-Francois, Hernandez, Jean, Martinez, Solveig, Lefranc-Jullien, Frederic, Checler

Publikováno v: The Journal of biological chemistry. 278(28)

We have set up stably transfected HEK293 cells overexpressing the beta-secretases BACE1 and BACE2 either alone or in combination with wild-type beta-amyloid precursor protein (betaAPP). The characterization of the betaAPP-derived catabolites indicate

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::25bfaf75629d9531b2ec394720a5f3b2
https://pubmed.ncbi.nlm.nih.gov/12736275

JLK inhibitors: isocoumarin compounds as putative probes to selectively target the gamma-secretase pathway.

Autor: Checler F; Institut de Pharmacologie Moléculaire et Cellulaire, UMR6097 du CNRS, 660 route des Lucioles, Sophia-Antipolis, 06560 Valbonne, France. checler@ipmc.cnrs.fr., Alves da Costa C, Ayral E, Andrau D, Dumanchin C, Farzan M, Hernandez JF, Martinez J, Lefranc-Jullien S, Marambaud P, Pasini A, Petit A, Phiel C, Robert P, St George-Hyslop P, Wilk S

Publikováno v: Current Alzheimer research [Curr Alzheimer Res] 2005 Jul; Vol. 2 (3), pp. 327-34.