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Page 1
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.
Targeting allostery in the Dynein motor domain with small molecule inhibitors.
Santarossa CC, Mickolajczyk KJ, Steinman JB, Urnavicius L, Chen N, Hirata Y, Fukase Y, Coudray N, Ekiert DC, Bhabha G, Kapoor TM. Santarossa CC, et al. Among authors: fukase y. Cell Chem Biol. 2021 Oct 21;28(10):1460-1473.e15. doi: 10.1016/j.chembiol.2021.04.024. Epub 2021 May 19. Cell Chem Biol. 2021. PMID: 34015309 Free PMC article.
Novel Pure αVβ3 Integrin Antagonists That Do Not Induce Receptor Extension, Prime the Receptor, or Enhance Angiogenesis at Low Concentrations.
Li J, Fukase Y, Shang Y, Zou W, Muñoz-Félix JM, Buitrago L, van Agthoven J, Zhang Y, Hara R, Tanaka Y, Okamoto R, Yasui T, Nakahata T, Imaeda T, Aso K, Zhou Y, Locuson C, Nesic D, Duggan M, Takagi J, Vaughan RD, Walz T, Hodivala-Dilke K, Teitelbaum SL, Arnaout MA, Filizola M, Foley MA, Coller BS. Li J, et al. Among authors: fukase y. ACS Pharmacol Transl Sci. 2019 Aug 2;2(6):387-401. doi: 10.1021/acsptsci.9b00041. eCollection 2019 Dec 13. ACS Pharmacol Transl Sci. 2019. PMID: 32259072 Free PMC article.
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 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
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
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 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.
88 results