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Page 1
NIBR-LTSi is a selective LATS kinase inhibitor activating YAP signaling and expanding tissue stem cells in vitro and in vivo.
Namoto K, Baader C, Orsini V, Landshammer A, Breuer E, Dinh KT, Ungricht R, Pikiolek M, Laurent S, Lu B, Aebi A, Schönberger K, Vangrevelinghe E, Evrova O, Sun T, Annunziato S, Lachal J, Redmond E, Wang L, Wetzel K, Capodieci P, Turner J, Schutzius G, Unterreiner V, Trunzer M, Buschmann N, Behnke D, Machauer R, Scheufler C, Parker CN, Ferro M, Grevot A, Beyerbach A, Lu WY, Forbes SJ, Wagner J, Bouwmeester T, Liu J, Sohal B, Sahambi S, Greenbaum LE, Lohmann F, Hoppe P, Cong F, Sailer AW, Ruffner H, Glatthar R, Humar B, Clavien PA, Dill MT, George E, Maibaum J, Liberali P, Tchorz JS. Namoto K, et al. Among authors: vangrevelinghe e. Cell Stem Cell. 2024 Apr 4;31(4):554-569.e17. doi: 10.1016/j.stem.2024.03.003. Cell Stem Cell. 2024. PMID: 38579685
An Activating Janus Kinase-3 Mutation Is Associated with Cytotoxic T Lymphocyte Antigen-4-Dependent Immune Dysregulation Syndrome.
Sic H, Speletas M, Cornacchione V, Seidl M, Beibel M, Linghu B, Yang F, Sevdali E, Germenis AE, Oakeley EJ, Vangrevelinghe E, Sailer AW, Traggiai E, Gram H, Eibel H. Sic H, et al. Among authors: vangrevelinghe e. Front Immunol. 2017 Dec 15;8:1824. doi: 10.3389/fimmu.2017.01824. eCollection 2017. Front Immunol. 2017. PMID: 29375547 Free PMC article.
Structure-Based Optimization of a Fragment-like TLR8 Binding Screening Hit to an In Vivo Efficacious TLR7/8 Antagonist.
Betschart C, Faller M, Zink F, Hemmig R, Blank J, Vangrevelinghe E, Bourrel M, Glatthar R, Behnke D, Barker K, Heizmann A, Angst D, Nimsgern P, Jacquier S, Junt T, Zipfel G, Ruzzante G, Loetscher P, Limonta S, Hawtin S, Andre CB, Boulay T, Feifel R, Knoepfel T. Betschart C, et al. Among authors: vangrevelinghe e. ACS Med Chem Lett. 2022 Mar 10;13(4):658-664. doi: 10.1021/acsmedchemlett.1c00696. eCollection 2022 Apr 14. ACS Med Chem Lett. 2022. PMID: 35450354 Free PMC article.
Target-Based Identification and Optimization of 5-Indazol-5-yl Pyridones as Toll-like Receptor 7 and 8 Antagonists Using a Biochemical TLR8 Antagonist Competition Assay.
Knoepfel T, Nimsgern P, Jacquier S, Bourrel M, Vangrevelinghe E, Glatthar R, Behnke D, Alper PB, Michellys PY, Deane J, Junt T, Zipfel G, Limonta S, Hawtin S, Andre C, Boulay T, Loetscher P, Faller M, Blank J, Feifel R, Betschart C. Knoepfel T, et al. Among authors: vangrevelinghe e. J Med Chem. 2020 Aug 13;63(15):8276-8295. doi: 10.1021/acs.jmedchem.0c00130. Epub 2020 Jul 30. J Med Chem. 2020. PMID: 32786235
A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore.
Ostermann N, Ruedisser S, Ehrhardt C, Breitenstein W, Marzinzik A, Jacoby E, Vangrevelinghe E, Ottl J, Klumpp M, Hartwieg JC, Cumin F, Hassiepen U, Trappe J, Sedrani R, Geisse S, Gerhartz B, Richert P, Francotte E, Wagner T, Krömer M, Kosaka T, Webb RL, Rigel DF, Maibaum J, Baeschlin DK. Ostermann N, et al. Among authors: vangrevelinghe e. J Med Chem. 2013 Mar 28;56(6):2196-206. doi: 10.1021/jm301706j. Epub 2013 Mar 15. J Med Chem. 2013. PMID: 23360239
Activity of the Type II JAK2 Inhibitor CHZ868 in B Cell Acute Lymphoblastic Leukemia.
Wu SC, Li LS, Kopp N, Montero J, Chapuy B, Yoda A, Christie AL, Liu H, Christodoulou A, van Bodegom D, van der Zwet J, Layer JV, Tivey T, Lane AA, Ryan JA, Ng SY, DeAngelo DJ, Stone RM, Steensma D, Wadleigh M, Harris M, Mandon E, Ebel N, Andraos R, Romanet V, Dölemeyer A, Sterker D, Zender M, Rodig SJ, Murakami M, Hofmann F, Kuo F, Eck MJ, Silverman LB, Sallan SE, Letai A, Baffert F, Vangrevelinghe E, Radimerski T, Gaul C, Weinstock DM. Wu SC, et al. Among authors: vangrevelinghe e. Cancer Cell. 2015 Jul 13;28(1):29-41. doi: 10.1016/j.ccell.2015.06.005. Cancer Cell. 2015. PMID: 26175414 Free PMC article.
Modulation of activation-loop phosphorylation by JAK inhibitors is binding mode dependent.
Andraos R, Qian Z, Bonenfant D, Rubert J, Vangrevelinghe E, Scheufler C, Marque F, Régnier CH, De Pover A, Ryckelynck H, Bhagwat N, Koppikar P, Goel A, Wyder L, Tavares G, Baffert F, Pissot-Soldermann C, Manley PW, Gaul C, Voshol H, Levine RL, Sellers WR, Hofmann F, Radimerski T. Andraos R, et al. Among authors: vangrevelinghe e. Cancer Discov. 2012 Jun;2(6):512-523. doi: 10.1158/2159-8290.CD-11-0324. Epub 2012 May 3. Cancer Discov. 2012. PMID: 22684457 Free PMC article.
Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805.
Baffert F, Régnier CH, De Pover A, Pissot-Soldermann C, Tavares GA, Blasco F, Brueggen J, Chène P, Drueckes P, Erdmann D, Furet P, Gerspacher M, Lang M, Ledieu D, Nolan L, Ruetz S, Trappe J, Vangrevelinghe E, Wartmann M, Wyder L, Hofmann F, Radimerski T. Baffert F, et al. Among authors: vangrevelinghe e. Mol Cancer Ther. 2010 Jul;9(7):1945-55. doi: 10.1158/1535-7163.MCT-10-0053. Epub 2010 Jun 29. Mol Cancer Ther. 2010. PMID: 20587663
29 results