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Page 1
Enhanced inhibition of ERK signaling by a novel allosteric MEK inhibitor, CH5126766, that suppresses feedback reactivation of RAF activity.
Ishii N, Harada N, Joseph EW, Ohara K, Miura T, Sakamoto H, Matsuda Y, Tomii Y, Tachibana-Kondo Y, Iikura H, Aoki T, Shimma N, Arisawa M, Sowa Y, Poulikakos PI, Rosen N, Aoki Y, Sakai T. Ishii N, et al. Among authors: shimma n. Cancer Res. 2013 Jul 1;73(13):4050-4060. doi: 10.1158/0008-5472.CAN-12-3937. Epub 2013 May 10. Cancer Res. 2013. PMID: 23667175 Free PMC article.
The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors.
Aoki T, Hyohdoh I, Furuichi N, Ozawa S, Watanabe F, Matsushita M, Sakaitani M, Ori K, Takanashi K, Harada N, Tomii Y, Tabo M, Yoshinari K, Aoki Y, Shimma N, Iikura H. Aoki T, et al. Among authors: shimma n. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6223-7. doi: 10.1016/j.bmcl.2013.10.001. Epub 2013 Oct 9. Bioorg Med Chem Lett. 2013. PMID: 24157370
Design and synthesis of novel allosteric MEK inhibitor CH4987655 as an orally available anticancer agent.
Isshiki Y, Kohchi Y, Iikura H, Matsubara Y, Asoh K, Murata T, Kohchi M, Mizuguchi E, Tsujii S, Hattori K, Miura T, Yoshimura Y, Aida S, Miwa M, Saitoh R, Murao N, Okabe H, Belunis C, Janson C, Lukacs C, Schück V, Shimma N. Isshiki Y, et al. Among authors: shimma n. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1795-801. doi: 10.1016/j.bmcl.2011.01.062. Epub 2011 Jan 21. Bioorg Med Chem Lett. 2011. PMID: 21316218
Fluorine Scanning by Nonselective Fluorination: Enhancing Raf/MEK Inhibition while Keeping Physicochemical Properties.
Hyohdoh I, Furuichi N, Aoki T, Itezono Y, Shirai H, Ozawa S, Watanabe F, Matsushita M, Sakaitani M, Ho PS, Takanashi K, Harada N, Tomii Y, Yoshinari K, Ori K, Tabo M, Aoki Y, Shimma N, Iikura H. Hyohdoh I, et al. Among authors: shimma n. ACS Med Chem Lett. 2013 Sep 22;4(11):1059-63. doi: 10.1021/ml4002419. eCollection 2013 Nov 14. ACS Med Chem Lett. 2013. PMID: 24900605 Free PMC article.
Optimizing the Physicochemical Properties of Raf/MEK Inhibitors by Nitrogen Scanning.
Aoki T, Hyohdoh I, Furuichi N, Ozawa S, Watanabe F, Matsushita M, Sakaitani M, Morikami K, Takanashi K, Harada N, Tomii Y, Shiraki K, Furumoto K, Tabo M, Yoshinari K, Ori K, Aoki Y, Shimma N, Iikura H. Aoki T, et al. Among authors: shimma n. ACS Med Chem Lett. 2014 Jan 22;5(4):309-14. doi: 10.1021/ml400379x. eCollection 2014 Apr 10. ACS Med Chem Lett. 2014. PMID: 24900832 Free PMC article.
Host sphingolipid biosynthesis as a target for hepatitis C virus therapy.
Sakamoto H, Okamoto K, Aoki M, Kato H, Katsume A, Ohta A, Tsukuda T, Shimma N, Aoki Y, Arisawa M, Kohara M, Sudoh M. Sakamoto H, et al. Among authors: shimma n. Nat Chem Biol. 2005 Nov;1(6):333-7. doi: 10.1038/nchembio742. Epub 2005 Oct 16. Nat Chem Biol. 2005. PMID: 16408072
Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799.
Ohwada J, Ebiike H, Kawada H, Tsukazaki M, Nakamura M, Miyazaki T, Morikami K, Yoshinari K, Yoshida M, Kondoh O, Kuramoto S, Ogawa K, Aoki Y, Shimma N. Ohwada J, et al. Among authors: shimma n. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1767-72. doi: 10.1016/j.bmcl.2011.01.065. Epub 2011 Jan 22. Bioorg Med Chem Lett. 2011. PMID: 21316229
57 results