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Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression.
Lama L, Adura C, Xie W, Tomita D, Kamei T, Kuryavyi V, Gogakos T, Steinberg JI, Miller M, Ramos-Espiritu L, Asano Y, Hashizume S, Aida J, Imaeda T, Okamoto R, Jennings AJ, Michino M, Kuroita T, Stamford A, Gao P, Meinke P, Glickman JF, Patel DJ, Tuschl T. Lama L, et al. Among authors: kuroita t. Nat Commun. 2019 May 21;10(1):2261. doi: 10.1038/s41467-019-08620-4. Nat Commun. 2019. PMID: 31113940 Free PMC article.
Whole Cell Active Inhibitors of Mycobacterial Lipoamide Dehydrogenase Afford Selectivity over the Human Enzyme through Tight Binding Interactions.
Ginn J, Jiang X, Sun S, Michino M, Huggins DJ, Mbambo Z, Jansen R, Rhee KY, Arango N, Lima CD, Liverton N, Imaeda T, Okamoto R, Kuroita T, Aso K, Stamford A, Foley M, Meinke PT, Nathan C, Bryk R. Ginn J, et al. Among authors: kuroita t. ACS Infect Dis. 2021 Feb 12;7(2):435-444. doi: 10.1021/acsinfecdis.0c00788. Epub 2021 Feb 2. ACS Infect Dis. 2021. PMID: 33527832 Free PMC article.
Novel approach of fragment-based lead discovery applied to renin inhibitors.
Tawada M, Suzuki S, Imaeda Y, Oki H, Snell G, Behnke CA, Kondo M, Tarui N, Tanaka T, Kuroita T, Tomimoto M. Tawada M, et al. Among authors: kuroita t. Bioorg Med Chem. 2016 Nov 15;24(22):6066-6074. doi: 10.1016/j.bmc.2016.09.065. Epub 2016 Sep 28. Bioorg Med Chem. 2016. PMID: 27720325
Soticlestat, a novel cholesterol 24-hydroxylase inhibitor shows a therapeutic potential for neural hyperexcitation in mice.
Nishi T, Kondo S, Miyamoto M, Watanabe S, Hasegawa S, Kondo S, Yano J, Watanabe E, Ishi T, Yoshikawa M, Ando HK, Farnaby W, Fujimoto S, Sunahara E, Ohori M, During MJ, Kuroita T, Koike T. Nishi T, et al. Among authors: kuroita t. Sci Rep. 2020 Oct 13;10(1):17081. doi: 10.1038/s41598-020-74036-6. Sci Rep. 2020. PMID: 33051477 Free PMC article.
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: kuroita t. 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.
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: kuroita t. 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 aryl-piperidine derivatives as potent and selective PET tracers for cholesterol 24-hydroxylase (CH24H).
Ikeda S, Kajita Y, Miyamoto M, Matsumiya K, Ishii T, Nishi T, Gay SC, Lane W, Constantinescu CC, Alagille D, Papin C, Tamagnan G, Kuroita T, Koike T. Ikeda S, et al. Among authors: kuroita t. Eur J Med Chem. 2022 Oct 5;240:114612. doi: 10.1016/j.ejmech.2022.114612. Epub 2022 Jul 14. Eur J Med Chem. 2022. PMID: 35863274 Free article.
47 results