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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: kawada 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
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: kawada h. 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
Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.
Kinoshita K, Ono Y, Emura T, Asoh K, Furuichi N, Ito T, Kawada H, Tanaka S, Morikami K, Tsukaguchi T, Sakamoto H, Tsukuda T, Oikawa N. Kinoshita K, et al. Among authors: kawada h. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3788-93. doi: 10.1016/j.bmcl.2011.04.020. Epub 2011 Apr 22. Bioorg Med Chem Lett. 2011. PMID: 21561771
9-substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as highly selective and potent anaplastic lymphoma kinase inhibitors.
Kinoshita K, Kobayashi T, Asoh K, Furuichi N, Ito T, Kawada H, Hara S, Ohwada J, Hattori K, Miyagi T, Hong WS, Park MJ, Takanashi K, Tsukaguchi T, Sakamoto H, Tsukuda T, Oikawa N. Kinoshita K, et al. Among authors: kawada h. J Med Chem. 2011 Sep 22;54(18):6286-94. doi: 10.1021/jm200652u. Epub 2011 Aug 25. J Med Chem. 2011. PMID: 21823617
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: kawada 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
Optimization of the phenylurea moiety in a phosphoinositide 3-kinase (PI3K) inhibitor to improve water solubility and the PK profile by introducing a solubilizing group and ortho substituents.
Kawada H, Ebiike H, Tsukazaki M, Yamamoto S, Koyama K, Nakamura M, Morikami K, Yoshinari K, Yoshida M, Ogawa K, Shimma N, Tsukuda T, Ohwada J. Kawada H, et al. Bioorg Med Chem. 2016 Jul 1;24(13):2897-2906. doi: 10.1016/j.bmc.2016.04.060. Epub 2016 Apr 28. Bioorg Med Chem. 2016. PMID: 27189888
420 results