Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Laurent F. Hennequin"'
Autor:
Romain Pierre, Anne Brethon, Sylvain A. Jacques, Aurélie Blond, Sandrine Chambon, Sandrine Talano, Catherine Raffin, Branislav Musicki, Claire Bouix-Peter, Loic Tomas, Gilles Ouvry, Rémy Morgentin, Laurent F. Hennequin, Craig S. Harris
Publikováno v:
Beilstein Journal of Organic Chemistry, Vol 17, Iss 1, Pp 156-165 (2021)
In our hands, efficient access to the 4-amino-3-carboxamide disubstituted pyridine-2(1H)-one kinase hinge-binder motif proved to be more challenging than anticipated requiring a significant investment in route scouting and optimization. This full pap
Externí odkaz:
https://doaj.org/article/2acdd653d9364f4c95c1ad7741ba07ae
Autor:
Severine H. Collet, Patrick Poulin, Claire E. Wilson, Nicolas Atrux-Tallau, Laurent F. Hennequin, Jean-Michel Linget
Publikováno v:
Journal of Pharmaceutical Sciences. 108:603-619
The minipig continues to build a reputation as a viable alternative large animal model to predict humans in dermatology and toxicology studies. Therefore, it is essential to describe and predict the pharmacokinetics in that species to speed up the cl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::994838e6c747b92246b183caf1ccbfd4
https://doi.org/10.1016/j.xphs.2018.09.001
https://doi.org/10.1016/j.xphs.2018.09.001
Autor:
Corinne Millois, Loïc Tomas, Catherine Comino, Laurence Dumais, Sandrine Talano, Kevin Reverse, Céline Mathieu, Craig S. Harris, Nicolas Vanthuyne, Grégoire Mouis, Anne-Laurence Ghilini, Laurent F. Hennequin, Claire Bouix-Peter, Vincent Rodeschini, Ghizlane El-Bazbouz, Laurence Clary, Sandrine Chambon, Romain Pierre, Jean-François Fournier, Anne Brethon
Publikováno v:
Tetrahedron
Tetrahedron, Elsevier, 2018, 74 (37), pp.4805-4822. ⟨10.1016/j.tet.2018.07.029⟩
Tetrahedron, 2018, 74 (37), pp.4805-4822. ⟨10.1016/j.tet.2018.07.029⟩
Tetrahedron, Elsevier, 2018, 74 (37), pp.4805-4822. ⟨10.1016/j.tet.2018.07.029⟩
Tetrahedron, 2018, 74 (37), pp.4805-4822. ⟨10.1016/j.tet.2018.07.029⟩
International audience; During our search for topically-active Caspase-1 inhibitors, we identified a novel class of potent in-hibitors based on a 1,3,5-trisubstituted uracil motif equipped with an L-aspartate semi-aldehyde derived warhead. In the lit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6fec40dca9ff1ebf6ef20f7e1e77cb56
https://doi.org/10.1016/j.tet.2018.07.029
https://doi.org/10.1016/j.tet.2018.07.029
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:
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:
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:
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:
Sandra Hubert, Martin Guilliams, Carlos G. Briseño, Benoit Malleret, Lai Guan Ng, Baptiste Janela, Mai Chan Lau, Josephine Lum, Kenneth M. Murphy, Philippe Musette, Yannick Simoni, Leen Vanhoutte, Bernard Malissen, Laurent F. Hennequin, Christian Wohn, Wan Ting Kong, Amit Patel, Michael G. Fehlings, Michael Poidinger, Rasha Msallam, Florent Ginhoux, Ansuman T. Satpathy, Emmanuel Vial, Jinmiao Chen, Chi Ching Goh, Francesca Zolezzi, Feriel Hacini-Rachinel, Evan W. Newell, Alexander A. Maini, Simon Yona
Publikováno v:
Immunity
Immunity, Elsevier, 2019, 50 (4), pp.1069-1083. ⟨10.1016/j.immuni.2019.03.001⟩
Immunity, 2019, 50 (4), pp.1069-1083. ⟨10.1016/j.immuni.2019.03.001⟩
IMMUNITY
IMMUNITY, 2019, 50 (4), pp.1069-1083. ⟨10.1016/j.immuni.2019.03.001⟩
Immunity, Elsevier, 2019, 50 (4), pp.1069-1083. ⟨10.1016/j.immuni.2019.03.001⟩
Immunity, 2019, 50 (4), pp.1069-1083. ⟨10.1016/j.immuni.2019.03.001⟩
IMMUNITY
IMMUNITY, 2019, 50 (4), pp.1069-1083. ⟨10.1016/j.immuni.2019.03.001⟩
Skin conventional dendritic cells (cDCs) exist as two distinct subsets, cDC1s and cDC2s, which maintain the balance of immunity to pathogens and tolerance to self and microbiota. Here, we examined the roles of dermal cDC1s and cDC2s during bacterial
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4ea848e9dc854a3bae780908b4528c00
https://hal.archives-ouvertes.fr/hal-02359448
https://hal.archives-ouvertes.fr/hal-02359448
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