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Page 1
Discovery of orally efficacious RORγt inverse agonists. Part 2: Design, synthesis, and biological evaluation of novel tetrahydroisoquinoline derivatives.
Kono M, Oda T, Tawada M, Imada T, Banno Y, Taya N, Kawamoto T, Tokuhara H, Tomata Y, Ishii N, Ochida A, Fukase Y, Yukawa T, Fukumoto S, Watanabe H, Uga K, Shibata A, Nakagawa H, Shirasaki M, Fujitani Y, Yamasaki M, Shirai J, Yamamoto S. Kono M, et al. Among authors: fukase y. Bioorg Med Chem. 2018 Jan 15;26(2):470-482. doi: 10.1016/j.bmc.2017.12.008. Epub 2017 Dec 11. Bioorg Med Chem. 2018. PMID: 29258712
Discovery of orally efficacious RORγt inverse agonists, part 1: Identification of novel phenylglycinamides as lead scaffolds.
Shirai J, Tomata Y, Kono M, Ochida A, Fukase Y, Sato A, Masada S, Kawamoto T, Yonemori K, Koyama R, Nakagawa H, Nakayama M, Uga K, Shibata A, Koga K, Okui T, Shirasaki M, Skene R, Sang B, Hoffman I, Lane W, Fujitani Y, Yamasaki M, Yamamoto S. Shirai J, et al. Among authors: fukase y. Bioorg Med Chem. 2018 Jan 15;26(2):483-500. doi: 10.1016/j.bmc.2017.12.006. Epub 2017 Dec 9. Bioorg Med Chem. 2018. PMID: 29262987
Identification of novel quinazolinedione derivatives as RORγt inverse agonist.
Fukase Y, Sato A, Tomata Y, Ochida A, Kono M, Yonemori K, Koga K, Okui T, Yamasaki M, Fujitani Y, Nakagawa H, Koyama R, Nakayama M, Skene R, Sang BC, Hoffman I, Shirai J, Yamamoto S. Fukase Y, et al. Bioorg Med Chem. 2018 Feb 1;26(3):721-736. doi: 10.1016/j.bmc.2017.12.039. Epub 2017 Dec 28. Bioorg Med Chem. 2018. PMID: 29342416
Discovery of [ cis-3-({(5 R)-5-[(7-Fluoro-1,1-dimethyl-2,3-dihydro-1 H-inden-5-yl)carbamoyl]-2-methoxy-7,8-dihydro-1,6-naphthyridin-6(5 H)-yl}carbonyl)cyclobutyl]acetic Acid (TAK-828F) as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse Agonist.
Kono M, Ochida A, Oda T, Imada T, Banno Y, Taya N, Masada S, Kawamoto T, Yonemori K, Nara Y, Fukase Y, Yukawa T, Tokuhara H, Skene R, Sang BC, Hoffman ID, Snell GP, Uga K, Shibata A, Igaki K, Nakamura Y, Nakagawa H, Tsuchimori N, Yamasaki M, Shirai J, Yamamoto S. Kono M, et al. Among authors: fukase y. J Med Chem. 2018 Apr 12;61(7):2973-2988. doi: 10.1021/acs.jmedchem.8b00061. Epub 2018 Mar 14. J Med Chem. 2018. PMID: 29510038
Discovery of benzimidazole derivatives as orally active renin inhibitors: Optimization of 3,5-disubstituted piperidine to improve pharmacokinetic profile.
Tokuhara H, Imaeda Y, Fukase Y, Iwanaga K, Taya N, Watanabe K, Kanagawa R, Matsuda K, Kajimoto Y, Kusumoto K, Kondo M, Snell G, Behnke CA, Kuroita T. Tokuhara H, et al. Among authors: fukase y. Bioorg Med Chem. 2018 Jul 23;26(12):3261-3286. doi: 10.1016/j.bmc.2018.04.051. Epub 2018 Apr 27. Bioorg Med Chem. 2018. PMID: 29754833
Design and Synthesis of Conformationally Constrained RORγt Inverse Agonists.
Sato A, Fukase Y, Kono M, Ochida A, Oda T, Sasaki Y, Ishii N, Tomata Y, Fukumoto S, Imai YN, Uga K, Shibata A, Yamasaki M, Nakagawa H, Shirasaki M, Skene R, Hoffman I, Sang BC, Snell G, Shirai J, Yamamoto S. Sato A, et al. Among authors: fukase y. ChemMedChem. 2019 Nov 20;14(22):1917-1932. doi: 10.1002/cmdc.201900416. Epub 2019 Nov 5. ChemMedChem. 2019. PMID: 31659845
Discovery of TAK-272: A Novel, Potent, and Orally Active Renin Inhibitor.
Imaeda Y, Tokuhara H, Fukase Y, Kanagawa R, Kajimoto Y, Kusumoto K, Kondo M, Snell G, Behnke CA, Kuroita T. Imaeda Y, et al. Among authors: fukase y. ACS Med Chem Lett. 2016 Sep 12;7(10):933-938. doi: 10.1021/acsmedchemlett.6b00251. eCollection 2016 Oct 13. ACS Med Chem Lett. 2016. PMID: 27774132 Free PMC article.
Deglycase-activity oriented screening to identify DJ-1 inhibitors.
Maksimovic I, Finkin-Groner E, Fukase Y, Zheng Q, Sun S, Michino M, Huggins DJ, Myers RW, David Y. Maksimovic I, et al. Among authors: fukase y. RSC Med Chem. 2021 Jun 2;12(7):1232-1238. doi: 10.1039/d1md00062d. eCollection 2021 Jul 21. RSC Med Chem. 2021. PMID: 34355187 Free PMC article.
Chemical structure-guided design of dynapyrazoles, cell-permeable dynein inhibitors with a unique mode of action.
Steinman JB, Santarossa CC, Miller RM, Yu LS, Serpinskaya AS, Furukawa H, Morimoto S, Tanaka Y, Nishitani M, Asano M, Zalyte R, Ondrus AE, Johnson AG, Ye F, Nachury MV, Fukase Y, Aso K, Foley MA, Gelfand VI, Chen JK, Carter AP, Kapoor TM. Steinman JB, et al. Among authors: fukase y. Elife. 2017 May 19;6:e25174. doi: 10.7554/eLife.25174. Elife. 2017. PMID: 28524820 Free PMC article.
89 results