Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Jorge Kirilovsky"'
Autor:
Alain Claude-Marie Daugan, Francois Hyafil, Jorge Kirilovsky, Hervé Coste, Anne-Charlotte de Gouville, Cécile Ruault, Richard Frederic Labaudiniere, Pascal Grondin
Publikováno v:
Journal of Medicinal Chemistry. 46:4525-4532
Starting from ethyl beta-carboline-3-carboxylate (beta-CCE), 1, a modest inhibitor of type 5 phosphodiesterase (PDE5), a series of functionalized tetrahydro-beta-carboline derivatives has been identified as a novel chemical class of potent and select
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fefc764d9520b29015f394c2c2648146
https://doi.org/10.1021/jm030056e
https://doi.org/10.1021/jm030056e
Publikováno v:
British Journal of Pharmacology. 128:206-212
1. Natriuretic peptide receptors have been found in different heart preparations. However, the role of natriuretic peptides in the regulation of cardiac contractility remains largely elusive and was, therefore, studied here. 2. The rate of relaxation
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::996c48189d903113bc32df500fa480ea
https://doi.org/10.1038/sj.bjp.0702766
https://doi.org/10.1038/sj.bjp.0702766
Autor:
Anne Marie Jeanne Bouillot, Frédéric Donche, Olivier Mirguet, Rab K. Prinjha, Gael Krysa, Edwige Nicodeme, Ann Louise Walker, Chun-wa Chung, Laurie J. Gordon, Kevin Lee, Soren Beinke, David Matthew Wilson, Inma Rioja, Toni Lewis, Leanne Cutler, Dave Lugo, Jonathan Thomas Seal, Jason Witherington, Paul Bamborough, Yann Lamotte, Scott McCleary, Jorge Kirilovsky, Françoise Gellibert
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(8)
A novel series of quinoline isoxazole BET family bromodomain inhibitors are discussed. Crystallography is used to illustrate binding modes and rationalize their SAR. One member, I-BET151 (GSK1210151A), shows good oral bioavailability in both the rat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::efda9004d594274ddcec17c62b1aae4d
https://pubmed.ncbi.nlm.nih.gov/22437115
https://pubmed.ncbi.nlm.nih.gov/22437115
Autor:
Delphine Delannée, Agnès Costaz, Jonathan Thomas Seal, Lionel Trottet, Rémi Tellier, Jean-Marie Brusq, Olivier Mirguet, Anne Marie Jeanne Bouillot, Sandrine Martin, Gael Krysa, Anne-Benedicte Boullay, Jorge Kirilovsky, Eric Boursier, Jérôme Toum, Yann Dudit, Van-Loc Nguyen, Edwige Nicodeme, Françoise Gellibert, Alizon M. Riou, Pascal Huet, Romain Luc Marie Gosmini, Yann Lamotte, Florence Blandel, Frédéric Donche
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(8)
The discovery, synthesis and biological evaluation of a novel series of 7-isoxazoloquinolines is described. Several analogs are shown to increase ApoA1 expression within the nanomolar range in the human hepatic cell line HepG2.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::30974817f673615f23351a44033e69cf
https://pubmed.ncbi.nlm.nih.gov/22386529
https://pubmed.ncbi.nlm.nih.gov/22386529
Autor:
Rab K. Prinjha, Helen R. Flynn, Stephen A. Hughes, Jérôme Toum, Rachel Grimley, Chun-wa Chung, Sandrine Martin, Jean-Marie Brusq, Hervé Coste, Kevin Lee, Chris J. Delves, Alizon M. Riou, Romain Luc Marie Gosmini, Catherine A. Clément, Edwige Nicodeme, Anne Marie Jeanne Bouillot, Eric Boursier, Robert Woodward, Anne-Benedicte Boullay, Olivier Mirguet, Jorge Kirilovsky, Paul Homes, Jonathan I. Wilde, Paul Bamborough, Iain Uings, Julia H. White, Françoise Gellibert, Emma J. Jones, Florence Blandel, Sylvie M. Magny
Publikováno v:
Journal of medicinal chemistry. 54(11)
Epigenetic mechanisms of gene regulation have a profound role in normal development and disease processes. An integral part of this mechanism occurs through lysine acetylation of histone tails which are recognized by bromodomains. While the biologica
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0f90740093b6de29cdf1e487246ae0c9
https://pubmed.ncbi.nlm.nih.gov/21568322
https://pubmed.ncbi.nlm.nih.gov/21568322
Autor:
Julia H. White, Charles M. Rice, Rab K. Prinjha, Scott Dewell, Alexander Tarakhovsky, Chun-wa Chung, Jose M. Lora, Edwige Nicodeme, Paul A. Wilson, Kate L. Jeffrey, Kevin Lee, Hervé Coste, Uwe Schaefer, Jorge Kirilovsky, Rohit Chandwani, Ivan Marazzi, Soren Beinke
Interaction of pathogens with cells of the immune system results in activation of inflammatory gene expression. This response, although vital for immune defence, is frequently deleterious to the host due to the exaggerated production of inflammatory
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d36b5d8b7a2823a5891d224401ebd732
https://europepmc.org/articles/PMC5415086/
https://europepmc.org/articles/PMC5415086/
Autor:
Anne-Charlotte de Gouville, Pascal Grondin, Cécile Ruault, Jean Michel Linget, Francois Hyafil, Richard Frederic Labaudiniere, Alain Claude-Marie Daugan, Jorge Kirilovsky, Hervé Coste
Publikováno v:
Journal of medicinal chemistry. 46(21)
Modification of the hydantoin ring in the previously described lead compound 2a has led to the discovery of compound 12a, tadalafil, a highly potent and highly selective PDE5 inhibitor. The replacement of the hydantoin in compound 2a by a piperazined
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fa7f3a8a7236df75151a560bbf5d9d73
https://pubmed.ncbi.nlm.nih.gov/14521415
https://pubmed.ncbi.nlm.nih.gov/14521415
Autor:
Richard H. Wagner, Beverly Paigen, Stephen Harris, Edwige Nicodeme, Pierre L. Roubertoux, Christina Petros, Isabelle Le Roy, Xiaosong Wang, Ariel Darvasi, Gary A. Churchill, Jorge Kirilovsky, Renhua Li
Mapping quantitative trait loci (QTLs)with high resolution facilitates identification and positional cloning of the underlying genes. The novel approach of advanced intercross lines (AILs) generates many more recombination events and thus can potenti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::17764d651503e851c78e30baf7d0ffdd
https://europepmc.org/articles/PMC403739/
https://europepmc.org/articles/PMC403739/
Publikováno v:
FEBS letters. 183(1)
The role of lipids in the interaction of the β-adrenergic receptor (R) with the regulatory protein (G s ) was investigated. Solubilized preparations of R and of G s from turkey erythrocytes were delipidated by gel filtration. They were subsequently
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b90268f64dfe7594ac682778cbe4a2af
https://pubmed.ncbi.nlm.nih.gov/2984050
https://pubmed.ncbi.nlm.nih.gov/2984050
Publikováno v:
European journal of biochemistry. 166(1)
Detergent-solubilized preparations of the beta-adrenergic receptor (R) and of the guanyl nucleotide binding proteins (Gs) were extensively treated to remove phospholipids and cholesterol. Reconstitution of an R-Gs system was subsequently performed in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56de1c615cd89276edf6d2fbc4e0aa03
https://pubmed.ncbi.nlm.nih.gov/3036521
https://pubmed.ncbi.nlm.nih.gov/3036521