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Page 1
Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition.
Weigert O, Lane AA, Bird L, Kopp N, Chapuy B, van Bodegom D, Toms AV, Marubayashi S, Christie AL, McKeown M, Paranal RM, Bradner JE, Yoda A, Gaul C, Vangrevelinghe E, Romanet V, Murakami M, Tiedt R, Ebel N, Evrot E, De Pover A, Régnier CH, Erdmann D, Hofmann F, Eck MJ, Sallan SE, Levine RL, Kung AL, Baffert F, Radimerski T, Weinstock DM. Weigert O, et al. Among authors: vangrevelinghe e. J Exp Med. 2012 Feb 13;209(2):259-73. doi: 10.1084/jem.20111694. Epub 2012 Jan 23. J Exp Med. 2012. PMID: 22271575 Free PMC article.
A small-molecule dengue virus entry inhibitor.
Wang QY, Patel SJ, Vangrevelinghe E, Xu HY, Rao R, Jaber D, Schul W, Gu F, Heudi O, Ma NL, Poh MK, Phong WY, Keller TH, Jacoby E, Vasudevan SG. Wang QY, et al. Among authors: vangrevelinghe e. Antimicrob Agents Chemother. 2009 May;53(5):1823-31. doi: 10.1128/AAC.01148-08. Epub 2009 Feb 17. Antimicrob Agents Chemother. 2009. PMID: 19223625 Free PMC article.
2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors.
Gerspacher M, Furet P, Pissot-Soldermann C, Gaul C, Holzer P, Vangrevelinghe E, Lang M, Erdmann D, Radimerski T, Regnier CH, Chene P, De Pover A, Hofmann F, Baffert F, Buhl T, Aichholz R, Blasco F, Endres R, Trappe J, Drueckes P. Gerspacher M, et al. Among authors: vangrevelinghe e. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1724-7. doi: 10.1016/j.bmcl.2010.01.069. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20138510
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
Syk inhibitors with high potency in presence of blood.
Thoma G, Blanz J, Bühlmayer P, Drückes P, Kittelmann M, Smith AB, van Eis M, Vangrevelinghe E, Zerwes HG, Che JJ, He X, Jin Y, Lee CC, Michellys PY, Uno T, Liu H. Thoma G, et al. Among authors: vangrevelinghe e. Bioorg Med Chem Lett. 2014 May 15;24(10):2278-82. doi: 10.1016/j.bmcl.2014.03.075. Epub 2014 Apr 3. Bioorg Med Chem Lett. 2014. PMID: 24726806
Discovery and profiling of a selective and efficacious Syk inhibitor.
Thoma G, Smith AB, van Eis MJ, Vangrevelinghe E, Blanz J, Aichholz R, Littlewood-Evans A, Lee CC, Liu H, Zerwes HG. Thoma G, et al. Among authors: vangrevelinghe e. J Med Chem. 2015 Feb 26;58(4):1950-63. doi: 10.1021/jm5018863. Epub 2015 Feb 9. J Med Chem. 2015. PMID: 25633741
Orally bioavailable Syk inhibitors with activity in a rat PK/PD model.
Thoma G, Veenstra S, Strang R, Blanz J, Vangrevelinghe E, Berghausen J, Lee CC, Zerwes HG. Thoma G, et al. Among authors: vangrevelinghe e. Bioorg Med Chem Lett. 2015 Oct 15;25(20):4642-7. doi: 10.1016/j.bmcl.2015.08.037. Epub 2015 Aug 18. Bioorg Med Chem Lett. 2015. PMID: 26320624
31 results