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Page 1
Validation of a New Methodology to Create Oral Drugs beyond the Rule of 5 for Intracellular Tough Targets.
Ohta A, Tanada M, Shinohara S, Morita Y, Nakano K, Yamagishi Y, Takano R, Kariyuki S, Iida T, Matsuo A, Ozeki K, Emura T, Sakurai Y, Takano K, Higashida A, Kojima M, Muraoka T, Takeyama R, Kato T, Kimura K, Ogawa K, Ohara K, Tanaka S, Kikuchi Y, Hisada N, Hayashi R, Nishimura Y, Nomura K, Tachibana T, Irie M, Kawada H, Torizawa T, Murao N, Kotake T, Tanaka M, Ishikawa S, Miyake T, Tamiya M, Arai M, Chiyoda A, Akai S, Sase H, Kuramoto S, Ito T, Shiraishi T, Kojima T, Iikura H. Ohta A, et al. Among authors: iikura h. J Am Chem Soc. 2023 Nov 8;145(44):24035-24051. doi: 10.1021/jacs.3c07145. Epub 2023 Oct 24. J Am Chem Soc. 2023. PMID: 37874670
Development of Orally Bioavailable Peptides Targeting an Intracellular Protein: From a Hit to a Clinical KRAS Inhibitor.
Tanada M, Tamiya M, Matsuo A, Chiyoda A, Takano K, Ito T, Irie M, Kotake T, Takeyama R, Kawada H, Hayashi R, Ishikawa S, Nomura K, Furuichi N, Morita Y, Kage M, Hashimoto S, Nii K, Sase H, Ohara K, Ohta A, Kuramoto S, Nishimura Y, Iikura H, Shiraishi T. Tanada M, et al. Among authors: iikura h. J Am Chem Soc. 2023 Aug 2;145(30):16610-16620. doi: 10.1021/jacs.3c03886. Epub 2023 Jul 18. J Am Chem Soc. 2023. PMID: 37463267
The energy-resolved neutron imaging system, RADEN.
Shinohara T, Kai T, Oikawa K, Nakatani T, Segawa M, Hiroi K, Su Y, Ooi M, Harada M, Iikura H, Hayashida H, Parker JD, Matsumoto Y, Kamiyama T, Sato H, Kiyanagi Y. Shinohara T, et al. Among authors: iikura h. Rev Sci Instrum. 2020 Apr 1;91(4):043302. doi: 10.1063/1.5136034. Rev Sci Instrum. 2020. PMID: 32357693
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: iikura h. 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.
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: iikura h. 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.
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: iikura h. 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
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: iikura h. 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.
23 results