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Discovery of a potent, metabolically stabilized resorcylic lactone as an anti-inflammatory lead.
Du H, Matsushima T, Spyvee M, Goto M, Shirota H, Gusovsky F, Chiba K, Kotake M, Yoneda N, Eguchi Y, DiPietro L, Harmange JC, Gilbert S, Li XY, Davis H, Jiang Y, Zhang Z, Pelletier R, Wong N, Sakurai H, Yang H, Ito-Igarashi H, Kimura A, Kuboi Y, Mizui Y, Tanaka I, Ikemori-Kawada M, Kawakami Y, Inoue A, Kawai T, Kishi Y, Wang Y. Du H, et al. Among authors: gusovsky f. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6196-9. doi: 10.1016/j.bmcl.2009.08.096. Epub 2009 Sep 3. Bioorg Med Chem Lett. 2009. PMID: 19783437
Discovery of anti-inflammatory clinical candidate E6201, inspired from resorcylic lactone LL-Z1640-2, III.
Shen Y, Boivin R, Yoneda N, Du H, Schiller S, Matsushima T, Goto M, Shirota H, Gusovsky F, Lemelin C, Jiang Y, Zhang Z, Pelletier R, Ikemori-Kawada M, Kawakami Y, Inoue A, Schnaderbeck M, Wang Y. Shen Y, et al. Among authors: gusovsky f. Bioorg Med Chem Lett. 2010 May 15;20(10):3155-7. doi: 10.1016/j.bmcl.2010.03.087. Epub 2010 Mar 30. Bioorg Med Chem Lett. 2010. PMID: 20399648
Discovery of an in vitro and in vivo potent resorcylic lactone analog of LL-Z1640-2 as anti-inflammatory lead, II.
Shen Y, Du H, Kotake M, Matsushima T, Goto M, Shirota H, Gusovsky F, Li X, Jiang Y, Schiller S, Spyvee M, Davis H, Zhang Z, Pelletier R, Ikemori-Kawada M, Kawakami Y, Inoue A, Wang Y. Shen Y, et al. Among authors: gusovsky f. Bioorg Med Chem Lett. 2010 May 15;20(10):3047-9. doi: 10.1016/j.bmcl.2010.03.119. Epub 2010 Apr 9. Bioorg Med Chem Lett. 2010. PMID: 20427182
E6201 [(3S,4R,5Z,8S,9S,11E)-14-(ethylamino)-8, 9,16-trihydroxy-3,4-dimethyl-3,4,9,19-tetrahydro-1H-2-benzoxacyclotetradecine-1,7(8H)-dione], a novel kinase inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase (MEK)-1 and MEK kinase-1: in vitro characterization of its anti-inflammatory and antihyperproliferative activities.
Goto M, Chow J, Muramoto K, Chiba K, Yamamoto S, Fujita M, Obaishi H, Tai K, Mizui Y, Tanaka I, Young D, Yang H, Wang YJ, Shirota H, Gusovsky F. Goto M, et al. Among authors: gusovsky f. J Pharmacol Exp Ther. 2009 Nov;331(2):485-95. doi: 10.1124/jpet.109.156554. Epub 2009 Aug 14. J Pharmacol Exp Ther. 2009. PMID: 19684251
E6201, a novel kinase inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase-1 and mitogen-activated protein kinase/extracellular signal-regulated kinase kinase kinase-1: in vivo effects on cutaneous inflammatory responses by topical administration.
Muramoto K, Goto M, Inoue Y, Ishii N, Chiba K, Kuboi Y, Omae T, Wang YJ, Gusovsky F, Shirota H. Muramoto K, et al. Among authors: gusovsky f. J Pharmacol Exp Ther. 2010 Oct;335(1):23-31. doi: 10.1124/jpet.110.168583. Epub 2010 Jul 13. J Pharmacol Exp Ther. 2010. PMID: 20627998
A novel antagonist of the prostaglandin E(2) EP(4) receptor inhibits Th1 differentiation and Th17 expansion and is orally active in arthritis models.
Chen Q, Muramoto K, Masaaki N, Ding Y, Yang H, Mackey M, Li W, Inoue Y, Ackermann K, Shirota H, Matsumoto I, Spyvee M, Schiller S, Sumida T, Gusovsky F, Lamphier M. Chen Q, et al. Among authors: gusovsky f. Br J Pharmacol. 2010 May;160(2):292-310. doi: 10.1111/j.1476-5381.2010.00647.x. Br J Pharmacol. 2010. PMID: 20423341 Free PMC article.
Novel small molecule inhibitors of TLR7 and TLR9: mechanism of action and efficacy in vivo.
Lamphier M, Zheng W, Latz E, Spyvee M, Hansen H, Rose J, Genest M, Yang H, Shaffer C, Zhao Y, Shen Y, Liu C, Liu D, Mempel TR, Rowbottom C, Chow J, Twine NC, Yu M, Gusovsky F, Ishizaka ST. Lamphier M, et al. Among authors: gusovsky f. Mol Pharmacol. 2014 Mar;85(3):429-40. doi: 10.1124/mol.113.089821. Epub 2013 Dec 16. Mol Pharmacol. 2014. PMID: 24342772
100 results