An erythroid-to-myeloid cell fate conversion is elicited by LSD1 inactivation

Autor: Sharon A. Singh, Yu Wang, Lei Yu, Takashi Moriguchi, Chia Jui Ku, Julien Pedron, Masayuki Yamamoto, Michael G. Rosenfeld, John H. Bushweller, Greggory Myers, Natee Jearawiriyapaisarn, James Douglas Engel, Rami Khoriaty, Andrew White, Kim-Chew Lim, Emily Schneider

Publikováno v: Blood. 138:1691-1704

Histone H3 lysine 4 methylation (H3K4Me) is most often associated with chromatin activation, and removing H3K4 methyl groups has been shown to be coincident with gene repression. H3K4Me demethylase KDM1a/LSD1 is a therapeutic target for multiple dise

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::507aceaec274169cd30b2d883fad808b
https://doi.org/10.1182/blood.2021011682

The epigenetic eraser LSD1 lies at the apex of a reversible erythroid to myeloid cell fate decision

Autor: Emily Schneider, Andrew White, Yv Wang, Takashi Moriguchi, Kim-Chew Lim, James Douglas Engel, John H. Bushweller, Chia Jui Ku, Julien Pedron, Michael G. Rosenfeld, Natee Jearawiriyapaisarn, Sharon A. Singh, Lei Yu, Greggory Myers, Masayuki Yamamoto, Rami Khoriaty

Histone H3 lysine 4 methylation (H3K4Me) is proximally associated with chromatin activation, and therefore removing H3K4 methyl groups is normally coincident with gene repression. H3K4Me demethylase KDM1a/LSD1 is a potential therapeutic target for mu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ceb36d58223d2124967452c4d6031439
https://doi.org/10.1101/2021.01.13.426552

Antikinetoplastid SAR study in 3-nitroimidazopyridine series: Identification of a novel non-genotoxic and potent anti-T. b. brucei hit-compound with improved pharmacokinetic properties

Autor: Alexis Valentin, Pierre Verhaeghe, Patrice Vanelle, Sophie Corvaisier, Damián Muruzabal, Caroline Castera-Ducros, Nadine Azas, Sébastien Hutter, Emilie Pinault, Alexandre Destere, Alan H. Fairlamb, Clotilde Boudot, Cyril Fersing, Pascal Rathelot, Susan Wyllie, Sandra Bourgeade-Delmas, Alix Sournia-Saquet, Aurélie Malzert-Fréon, Julien Pedron, Bertrand Courtioux, Amaya Azqueta, Marc Since, Jean Luc Stigliani, Nicolas Primas, Carole Di Giorgio, Youssef Kabri, Romain Paoli-Lombardo

Publikováno v: European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry, Elsevier, 2020, 206, pp.112668. ⟨10.1016/j.ejmech.2020.112668⟩

International audience; To study the antikinetoplastid 3-nitroimidazo[1,2-a]pyridine pharmacophore, a structure-activity relationship study was conducted through the synthesis of 26 original derivatives and their in vitro evaluation on both Leishmani

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8da65e5f41670c644ea019b322c91450
https://hal.archives-ouvertes.fr/hal-02920293

Antitrypanosomatid Pharmacomodulation at Position 3 of the 8-Nitroquinolin-2(1 H)-one Scaffold Using Palladium-Catalysed Cross-Coupling Reactions

Autor: Pierre Verhaeghe, Maryam Rastegari, Susan Wyllie, Clotilde Boudot, Alexis Valentin, Bertrand Courtioux, Colin Bonduelle, Hussein El-Kashef, Julien Pedron, Sandra Bourgeade-Delmas, Geneviève Pratviel, Lucie Paloque, Mansour Abdoulaye, Alix Sournia-Saquet, Alan H. Fairlamb

Publikováno v: ChemMedChem
ChemMedChem, 2018, 13 (20), pp.2217-2228. ⟨10.1002/cmdc.201800456⟩
ChemMedChem, Wiley-VCH Verlag, 2018, 13 (20), pp.2217-2228. ⟨10.1002/cmdc.201800456⟩

International audience; An antikinetoplastid pharmacomodulation study at position 3 of the recently described hit molecule 3-bromo-8-nitroquinolin-2(1H)-one was conducted. Twenty-four derivatives were synthesised using the Suzuki-Miyaura cross-coupli

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b94268e9a14d0dba7883701d5887e134
https://hal-unilim.archives-ouvertes.fr/hal-01888530

Novel 8-nitroquinolin-2(1 H )-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study

Autor: Susan Wyllie, Julien Pedron, Alain Moreau, Alix Sournia-Saquet, Pierre Verhaeghe, Bertrand Courtioux, Sébastien Hutter, Michèle Laget, Emmanuelle Mothes, Lucie Paloque, Clotilde Boudot, Alan H. Fairlamb, Sandra Bourgeade-Delmas, Laure Vendier, Geneviève Pratviel, Alexis Valentin, Elisa Boutet-Robinet, Nadine Azas, Jean-Luc Stigliani

Publikováno v: European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry, Elsevier, 2018, 155, pp.135-152. ⟨10.1016/j.ejmech.2018.06.001⟩
European Journal of Medicinal Chemistry, 2018, 155, pp.135-152. ⟨10.1016/j.ejmech.2018.06.001⟩

International audience; To study the antiparasitic 8-nitroquinolin-2(1H)-one pharmacophore, a series of 31 derivatives was synthesized in 1-5 steps and evaluated in vitro against both Leishmania infantum and Trypanosoma brucei brucei. In parallel, th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fd8cc004e3b57da170eaea9cfc484a16
https://hal-unilim.archives-ouvertes.fr/hal-01888465