Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Jonathan Pascau"'
Autor:
Catherine Soulet, Laurent F. Hennequin, Nicolas Fleury-Brégeot, Craig S. Harris, Blanche Gauthier, Gwenaëlle Duvert, Etienne Thoreau, Laurent Chantalat, Karine Grisendi, Jean-François Fournier, Jerome Aubert, Michèle Aurelly, Rémy Morgentin, Claire Bouix-Peter, Bénédicte Drean, Guillaume Lafitte, Yushma Bhurruth-Alcor, Florence Joly, Jonathan Pascau, Branislav Musicki, Yves Rival, David Piwnica, Karinne Bouquet, Marion Delorme, T. Isabet, Corinne Millois, Loïc Tomas
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:2985-2992
A series of squaramide-based hydroxamic acids were designed, synthesized and evaluated against human HDAC enzyme. Squaramides were found to be potent in the Hut78 cell line, but initially suffered from low solubility. Leads with improved solubility a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cf8fc3308da8740d4b656640fc1c579f
https://doi.org/10.1016/j.bmcl.2018.06.029
https://doi.org/10.1016/j.bmcl.2018.06.029
Autor:
Laurence Dumais, Gilles Ouvry, Laurent Chantalat, Angélique Feret, Sandrine Chambon, Thibaud Portal, Sandrine Talano, Gwenaëlle Duvert, Catherine Soulet, Jean-Marie Arlabosse, Samuel Tabet, Sebastien Daver, Jonathan Pascau, Nicolas Rodeville, Catherine Raffin, Claire Bouix-Peter, Etienne Thoreau
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:1736-1741
Retinoids have a dominant role in topical acne therapy and to date, only RARβ and RARγ dual agonists have reached the market. Given the tissue distribution of RAR isoforms, it was hypothesized that developing RARγ -selective agonists could yield a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::517fb0a7d7837968887d3b3cc6a2c9bc
https://doi.org/10.1016/j.bmcl.2018.04.036
https://doi.org/10.1016/j.bmcl.2018.04.036
Autor:
Didier M. Roche, Danielle Orfila, Ghizlane El-Bazbouz, Laurence Dumais, Laurent F. Hennequin, Céline Mathieu, Michèle Aurelly, Jerome Aubert, Claude Lardy, Etienne Thoreau, Anne-Pascale Luzy, Claire Bouix-Peter, Kenny Mebrouk, T. Isabet, Jean-François Fournier, Kevin Reverse, Catherine Comino, Corinne Millois, Anne-Laurence Ghilini, Jonathan Pascau, Sandrine Talano, Anne Brethon, Craig S. Harris, Romain Pierre, Sandrine Chambon, Laurence Clary, Olivier Christin, Laurent Chantalat, Vincent Rodeschini
Publikováno v:
Journal of Medicinal Chemistry. 61:4030-4051
The use of an interleukin β antibody is currently being investigated in the clinic for the treatment of acne, a dermatological disorder affecting 650M persons globally. Inhibiting the protease responsible for the cleavage of inactive pro-IL1β into
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ec019288b4b7ac46663d3c2d49c71c93
https://doi.org/10.1021/acs.jmedchem.8b00067
https://doi.org/10.1021/acs.jmedchem.8b00067
Autor:
Craig S. Harris, Isabelle Cardinaud, Feriel Hacini-Rachinel, Nicolas Rodeville, Audrey Beillard, Arnaud Reitz, Marilyne Bourotte, Benoit Deprez, Laetitia Bonnary, Catherine Comino, Corinne Millois, Delphine Spiesse, Claire Bouix-Peter, Denis Duvert, Jean-Guy Boiteau, Jean-Marie Arlabosse, Yushma Bhurruth-Alcor, Anne-Pascale Luzy, Laurent F. Hennequin, Gaëlle Polge, Emmanuel Vial, Loïc Tomas, Samuel Tabet, Kevin Reverse, Arnaud Mathieu, Artur Pinto, Angélique Feret, Karine Bouquet, Gilles Ouvry, Stéphanie Astri, Nicolas Orsini, Jonathan Pascau, Nathalie Taquet, David Piwnica, Patricia Rossio
Publikováno v:
Bioorganic & Medicinal Chemistry. 26:945-956
Targeting the TNFα pathway is a validated approach to the treatment of psoriasis. In this pathway, TACE stands out as a druggable target and has been the focus of in-house research programs. In this article, we present the discovery of clinical cand
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4758b7574647be3dbf23c8335599b665
https://doi.org/10.1016/j.bmc.2017.07.054
https://doi.org/10.1016/j.bmc.2017.07.054
Autor:
Marcus Gastreich, Laurence Clary, Jonathan Pascau, Anne Brethon, Laurent Chantalat, Olivier Christin, Etienne Thoreau, Jean-François Fournier, Craig S. Harris, Didier Roche, T. Isabet, Vincent Rodeschini
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:5373-5377
Virtual fragmentation of a library of 12,000 compounds inspired by natural products led to a dataset of 153,000 fragments that was used as a source to identify effective P2-P3 scaffold replacement solutions for peptidic Caspase-1 inhibitors. Our stra
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d881a80c1d0784a009d2dfbeb9d39136
https://doi.org/10.1016/j.bmcl.2017.11.015
https://doi.org/10.1016/j.bmcl.2017.11.015
Autor:
Arnaud Reitz, Corinne Millois, Marilyne Bourotte, Feriel Hacini-Rachinel, Carine Rosignoli, Arnaud Mathieu, Sandrine Chambon, Denis Duvert, Anne-Pascale Luzy, Laetitia Bonnary, Gwenaëlle Duvert, Gilles Ouvry, Jonathan Pascau, Craig S. Harris, Benoit Deprez, Laurent F. Hennequin, Catherine Comino, Yushma Bhurruth-Alcor, Yaël Berton, Nathalie Taquet, Claire Bouix-Peter, Gaëlle Polge, Kevin Reverse, Artur Pinto, Karine Bouquet
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:1848-1853
Targeting the Tumor Necrosis Factor α signalling with antibodies has led to a revolution in the treatment of psoriasis. Locally inhibiting Tumor Necrosis Factor α Converting Enzyme (TACE or ADAM17) could potentially mimic those effects and help tre
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fb6d576b781466f2d73bb18129c36d97
https://doi.org/10.1016/j.bmcl.2017.02.035
https://doi.org/10.1016/j.bmcl.2017.02.035
Autor:
Romain Pierre, Etienne Thoreau, Catherine Raffin, Claire Bouix-Peter, Laurent Chantalat, Gaëlle Polge, Jonathan Pascau, Gilles Ouvry, Nathalie Taquet, Catherine Comino, Denis Duvert, Danielle Orfila, Agnès Perrin, Yves Rival, Laurent Francois Andre Hennequin, Laurent Lamy, Christophe Feret, Branislav Musicki, Veronique Parnet, Anne-Pascale Luzy, Olivier Christin, Fabrice Ciesielski, Craig S. Harris
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:5802-5808
Targeting the IL17 pathway and more specifically the nuclear receptor RORγ is thought to be beneficial in multiple skin disorders. The Letter describes the discovery of phenoxyindazoles and thiophenoxy indazoles as potent RORγ inverse agonists. Opt
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::af63284f22f668869fc68a5936ba38ec
https://doi.org/10.1016/j.bmcl.2016.10.023
https://doi.org/10.1016/j.bmcl.2016.10.023
Autor:
Etienne Thoreau, Loïc Tomas, T. Isabet, Laurent Chantalat, Craig S. Harris, Sophie Deret, Alessandro Taddei, Emmanuel Vial, Emeric Varvier, Emilie Borde, Laurent Lamy, Claire Defoin-Platel, Catherine Soulet, Nathalie Taquet, Laetitia Bonnary, Anne-Pascale Luzy, Michèle Aurelly, Laurence Clary, Claire Bouix-Peter, Gilles Ouvry, Laurent F. Hennequin, Mathieu Forissier, Jonathan Pascau
Publikováno v:
ACS Med Chem Lett
[Image: see text] Minor structural modifications—sometimes single atom changes—can have a dramatic impact on the properties of compounds. This is illustrated here on structures related to known mTOR inhibitor Sapanisertib. Subtle changes in the h
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a5530bad5fdbd9b7c5e242653b3983aa
https://pubmed.ncbi.nlm.nih.gov/31749911
https://pubmed.ncbi.nlm.nih.gov/31749911
Autor:
Etienne Thoreau, Craig S. Harris, David Froude, Franck Bihl, Gilles Ouvry, Delphine Spiesse, Patricia Rossio, Christophe Feret, Emmanuel Vial, Laurent F. Hennequin, Jonathan Pascau, Coralie Pascau, Romain Pierre, Claire Defoin-Platel, Nathalie Taquet, Catherine Hervouet, Veronique Parnet, Olivier Christin, Guillaume Lafitte, Sophie Deret, Catherine Raffin, Claire Bouix-Peter, Anne-Pascale Luzy, Feriel Hacini-Rachinel, Branislav Musicki, Danielle Orfila, Rodolphe Vatinel
Publikováno v:
Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters, 2018, 28 (8), pp.1269-1273. ⟨10.1016/j.bmcl.2018.03.041⟩
Bioorganic and Medicinal Chemistry Letters, Elsevier, 2018, 28 (8), pp.1269-1273. ⟨10.1016/j.bmcl.2018.03.041⟩
Bioorganic and Medicinal Chemistry Letters, 2018, 28 (8), pp.1269-1273. ⟨10.1016/j.bmcl.2018.03.041⟩
Bioorganic and Medicinal Chemistry Letters, Elsevier, 2018, 28 (8), pp.1269-1273. ⟨10.1016/j.bmcl.2018.03.041⟩
Progress in the identification of suitable RORγ inverse agonists as clinical candidates has been hampered by the high lipophilicity that seems required for high potency on this nuclear receptor. In this context, we decided to focus on the replacemen
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::00fa57781e16cd4033a4b4d8d851561b
https://hal.science/hal-02526180
https://hal.science/hal-02526180
Autor:
Coralie Pascau, Nicolas Atrux-Tallau, Laurent F. Hennequin, Christophe Feret, Gilles Ouvry, Feriel Hacini-Rachinel, Craig S. Harris, Claire Defoin-Platel, Nathalie Taquet, Sophie Deret, Mathieu Forissier, Hélène Huguet, Etienne Thoreau, Benjamin Ozello, Olivier Christin, Emmanuel Vial, Guillaume Lafitte, Danielle Orfila, Isabelle Carlavan, Franck Bihl, David Froude, Jean-François Fournier, Denis Duvert, Anne-Pascale Luzy, Delphine Spiesse, Patricia Rossio, Marie-Josée Cuadrado, Jonathan Pascau, Catherine Raffin, Aline Bondu, Claire Bouix-Peter, Catherine Hervouet, Guillaume Peluchon, Veronique Parnet, David Piwnica, Branislav Musicki, Rodolphe Vatinel, Romain Pierre
Publikováno v:
ChemMedChem
ChemMedChem, 2018, 13 (4), pp.321-337. ⟨10.1002/cmdc.201700758⟩
ChemMedChem, Wiley-VCH Verlag, 2018, 13 (4), pp.321-337. ⟨10.1002/cmdc.201700758⟩
ChemMedChem, 2018, 13 (4), pp.321-337. ⟨10.1002/cmdc.201700758⟩
ChemMedChem, Wiley-VCH Verlag, 2018, 13 (4), pp.321-337. ⟨10.1002/cmdc.201700758⟩
With possible implications in multiple autoimmune diseases, the retinoic acid receptor-related orphan receptor RORγ has become a sought-after target in the pharmaceutical industry. Herein are described the efforts to identify a potent RORγ inverse
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ad689ccdeaf5f01fb20f8a6ff41d3b4a
https://hal.science/hal-02526191
https://hal.science/hal-02526191