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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: harada 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: harada 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
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: harada 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: harada 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.
Molecular targeting of HER2-overexpressing biliary tract cancer cells with trastuzumab emtansine, an antibody-cytotoxic drug conjugate.
Yamashita-Kashima Y, Yoshimura Y, Fujimura T, Shu S, Yanagisawa M, Yorozu K, Furugaki K, Higuchi R, Shoda J, Harada N. Yamashita-Kashima Y, et al. Among authors: harada n. Cancer Chemother Pharmacol. 2019 Apr;83(4):659-671. doi: 10.1007/s00280-019-03768-8. Epub 2019 Jan 18. Cancer Chemother Pharmacol. 2019. PMID: 30659304
2,437 results