Specificity and Mechanism of Action of EHT 1864, a Novel Small Molecule Inhibitor of Rac Family Small GTPases
Shutes, Adam, Onesto, Cercina, Picard, Virginie, Leblond, Bertrand, Schweighoffer, Fabien, Der, Channing J.
Published in The Journal of biological chemistry (07.12.2007)
Published in The Journal of biological chemistry (07.12.2007)
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A novel DYRK1A (Dual specificity tyrosine phosphorylation‐regulated kinase 1A) inhibitor for the treatment of Alzheimer's disease: effect on Tau and amyloid pathologies in vitro
Coutadeur, Séverine, Benyamine, Hélène, Delalonde, Laurence, Oliveira, Catherine, Leblond, Bertrand, Foucourt, Alicia, Besson, Thierry, Casagrande, Anne‐Sophie, Taverne, Thierry, Girard, Angélique, Pando, Matthew P., Désiré, Laurent
Published in Journal of neurochemistry (01.05.2015)
Published in Journal of neurochemistry (01.05.2015)
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DYRK1A controls the transition from proliferation to quiescence during lymphoid development by destabilizing Cyclin D3
Thompson, Benjamin J, Bhansali, Rahul, Diebold, Lauren, Cook, Daniel E, Stolzenburg, Lindsay, Casagrande, Anne-Sophie, Besson, Thierry, Leblond, Bertrand, Désiré, Laurent, Malinge, Sébastien, Crispino, John D
Published in The Journal of experimental medicine (01.06.2015)
Published in The Journal of experimental medicine (01.06.2015)
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Journal Article
Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part I
Foucourt, Alicia, Hédou, Damien, Dubouilh-Benard, Carole, Désiré, Laurent, Casagrande, Anne-Sophie, Leblond, Bertrand, Loäec, Nadège, Meijer, Laurent, Besson, Thierry
Published in Molecules (Basel, Switzerland) (29.09.2014)
Published in Molecules (Basel, Switzerland) (29.09.2014)
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Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part II
Foucourt, Alicia, Hédou, Damien, Dubouilh-Benard, Carole, Girard, Angélique, Taverne, Thierry, Casagrande, Anne-Sophie, Désiré, Laurent, Leblond, Bertrand, Besson, Thierry
Published in Molecules (Basel, Switzerland) (26.09.2014)
Published in Molecules (Basel, Switzerland) (26.09.2014)
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Journal Article
2-Substituted Estradiol Bis-sulfamates, Multitargeted Antitumor Agents: Synthesis, In Vitro SAR, Protein Crystallography, and In Vivo Activity
Leese, Mathew P, Leblond, Bertrand, Smith, Andrew, Newman, Simon P, Di Fiore, Anna, De Simone, Giuseppina, Supuran, Claudiu T, Purohit, Atul, Reed, Michael J, Potter, Barry V. L
Published in Journal of medicinal chemistry (28.12.2006)
Published in Journal of medicinal chemistry (28.12.2006)
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Synthesis, biological evaluation, and stability studies of raloxifene mono- and bis-sulfamates as dual-targeting agents
Zaraei, Seyed-Omar, Dohle, Wolfgang, Anbar, Hanan S., El-Gamal, Randa, Leblond, Bertrand, Foster, Paul A., Al-Tel, Taleb H., Potter, Barry V.L., El-Gamal, Mohammed I.
Published in Bioorganic & medicinal chemistry (01.03.2024)
Published in Bioorganic & medicinal chemistry (01.03.2024)
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Journal Article
Rap1-Rac1 Circuits Potentiate Platelet Activation
Stefanini, Lucia, Boulaftali, Yacine, Ouellette, Timothy D, Holinstat, Michael, Désiré, Laurent, Leblond, Bertrand, Andre, Patrick, Conley, Pamela B, Bergmeier, Wolfgang
Published in Arteriosclerosis, thrombosis, and vascular biology (01.02.2012)
Published in Arteriosclerosis, thrombosis, and vascular biology (01.02.2012)
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Journal Article
An Unusual Binding Model of the Methyl 9‑Anilinothiazolo[5,4‑f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases
Chaikuad, Apirat, Diharce, Julien, Schröder, Martin, Foucourt, Alicia, Leblond, Bertrand, Casagrande, Anne-Sophie, Désiré, Laurent, Bonnet, Pascal, Knapp, Stefan, Besson, Thierry
Published in Journal of medicinal chemistry (23.11.2016)
Published in Journal of medicinal chemistry (23.11.2016)
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Journal Article
Therapeutic sensitivity to Rac GTPase inhibition requires consequential suppression of mTORC1, AKT, and MEK signaling in breast cancer
Hampsch, Riley A, Shee, Kevin, Bates, Darcy, Lewis, Lionel D, Désiré, Laurent, Leblond, Bertrand, Demidenko, Eugene, Stefan, Kurtis, Huang, Yina H, Miller, Todd W
Published in Oncotarget (28.03.2017)
Published in Oncotarget (28.03.2017)
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Journal Article
Microwave-accelerated Dimroth rearrangement for the synthesis of 4-anilino-6-nitroquinazolines. Application to an efficient synthesis of a microtubule destabilizing agent
Foucourt, Alicia, Dubouilh-Benard, Carole, Chosson, Elizabeth, Corbière, Cécile, Buquet, Catherine, Iannelli, Mauro, Leblond, Bertrand, Marsais, Francis, Besson, Thierry
Published in Tetrahedron (19.06.2010)
Published in Tetrahedron (19.06.2010)
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Journal Article
Abstract 2620: 3D multicellular pancreatic cancer spheroids as drug screening tool for pharmacological evaluation of EHT 5372 and other Mirk/DYRK1B inhibitors
CASAGRANDE, Anne-Sophie, BACHELOT, Florence, THROO, Emeline, MAHE, Florence, LEBLOND, Bertrand, BESSON, Thierry, PANDO, Matthew, DESIRE, Laurent
Published in Cancer research (Chicago, Ill.) (01.10.2014)
Published in Cancer research (Chicago, Ill.) (01.10.2014)
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Journal Article
DYRK1A controls the transition from proliferation to quiescence during lymphoid development by destabilizing Cyclin D3
Thompson, Benjamin J., Bhansali, Rahul, Diebold, Lauren, Cook, Daniel E., Stolzenburg, Lindsay, Casagrande, Anne-Sophie, Besson, Thierry, Leblond, Bertrand, Désiré, Laurent, Malinge, Sébastien, Crispino, John D.
Published in The Journal of cell biology (08.06.2015)
Published in The Journal of cell biology (08.06.2015)
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Journal Article
Abstract 2165: Structure activity relationship of a novel chemical class of Dyrk inhibitors
Casagrande, Anne-Sophie, Bachelot, Florence, Coutadeur, Séverine, Leblond, Bertrand, Besson, Thierry, Pando, Matthew P., Désiré, Laurent
Published in Cancer research (Chicago, Ill.) (15.04.2013)
Published in Cancer research (Chicago, Ill.) (15.04.2013)
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Journal Article
RAC1 Inhibition Targets Amyloid Precursor Protein Processing by γ-Secretase and Decreases Aβ Production in Vitro and in Vivo
Désiré, Laurent, Bourdin, Jérôme, Loiseau, Nadia, Peillon, Hélène, Picard, Virginie, De Oliveira, Catherine, Bachelot, Florence, Leblond, Bertrand, Taverne, Thierry, Beausoleil, Eric, Lacombe, Sandrine, Drouin, Dominique, Schweighoffer, Fabien
Published in The Journal of biological chemistry (11.11.2005)
Published in The Journal of biological chemistry (11.11.2005)
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Journal Article
Abstract 2164: Mirk/dyrk1B kinase inhibitor reduces the viability of patient-derived ovarian cancer ascites cells and the size of murine tumor xenografts
Deng, Xiaobing, Hu, Jing, Cunningham, Mary, Leblond, Bertrand, Besson, Thierry, Casagrande, Anne-Sophie, Désiré, Laurent, Friedman, Eileen A.
Published in Cancer research (Chicago, Ill.) (15.04.2013)
Published in Cancer research (Chicago, Ill.) (15.04.2013)
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Journal Article
The Chromosome 21 Kinase DYRK1A Controls Cell Cycle Exit and Survival During Lymphoid Development and Is a Novel Therapeutic Target In Acute Lymphoblastic Leukemia
Thompson, Benjamin J., Diebold, Lauren, Malinge, Sebastien, Leblond, Bertrand, Casagrande, Anne-Sophie, Désiré, Laurent, Foucourt, Alicia, Besson, Thierry, Hijiya, Nobuko, Crispino, John D.
Published in Blood (15.11.2013)
Published in Blood (15.11.2013)
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Journal Article
Rapl-Racl Circuits Potentiate Platelet Activation
STEFANINI, Lucia, BOULAFTALI, Yacine, OUELLETTE, Timothy D, HOLINSTAT, Michael, DESIRE, Laurent, LEBLOND, Bertrand, ANDRE, Patrick, CONLEY, Pamela B, BERGMEIER, Wolfgang
Published in Arteriosclerosis, thrombosis, and vascular biology (2012)
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Published in Arteriosclerosis, thrombosis, and vascular biology (2012)
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