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Discovery of Potent and Centrally Active 6-Substituted 5-Fluoro-1,3-dihydro-oxazine β-Secretase (BACE1) Inhibitors via Active Conformation Stabilization.
Nakahara K, Fuchino K, Komano K, Asada N, Tadano G, Hasegawa T, Yamamoto T, Sako Y, Ogawa M, Unemura C, Hosono M, Ito H, Sakaguchi G, Ando S, Ohnishi S, Kido Y, Fukushima T, Dhuyvetter D, Borghys H, Gijsen HJM, Yamano Y, Iso Y, Kusakabe KI. Nakahara K, et al. Among authors: asada n. J Med Chem. 2018 Jul 12;61(13):5525-5546. doi: 10.1021/acs.jmedchem.8b00011. Epub 2018 Jun 14. J Med Chem. 2018. PMID: 29775538
Structure-Based Approaches to Improving Selectivity through Utilizing Explicit Water Molecules: Discovery of Selective β-Secretase (BACE1) Inhibitors over BACE2.
Fujimoto K, Yoshida S, Tadano G, Asada N, Fuchino K, Suzuki S, Matsuoka E, Yamamoto T, Yamamoto S, Ando S, Kanegawa N, Tonomura Y, Ito H, Moechars D, Rombouts FJR, Gijsen HJM, Kusakabe KI. Fujimoto K, et al. Among authors: asada n. J Med Chem. 2021 Mar 25;64(6):3075-3085. doi: 10.1021/acs.jmedchem.0c01858. Epub 2021 Mar 15. J Med Chem. 2021. PMID: 33719429
Discovery of Extremely Selective Fused Pyridine-Derived β-Site Amyloid Precursor Protein-Cleaving Enzyme (BACE1) Inhibitors with High In Vivo Efficacy through 10s Loop Interactions.
Ueno T, Matsuoka E, Asada N, Yamamoto S, Kanegawa N, Ito M, Ito H, Moechars D, Rombouts FJR, Gijsen HJM, Kusakabe KI. Ueno T, et al. Among authors: asada n. J Med Chem. 2021 Oct 14;64(19):14165-14174. doi: 10.1021/acs.jmedchem.1c00359. Epub 2021 Sep 23. J Med Chem. 2021. PMID: 34553947
Highly Potent and Oral Macrocyclic Peptides as a HIV-1 Protease Inhibitor: mRNA Display-Derived Hit-to-Lead Optimization.
Kusumoto Y, Hayashi K, Sato S, Yamada T, Kozono I, Nakata Z, Asada N, Mitsuki S, Watanabe A, Wakasa-Morimoto C, Uemura K, Arita S, Miki S, Mizutare T, Mikamiyama H. Kusumoto Y, et al. Among authors: asada n. ACS Med Chem Lett. 2022 Sep 1;13(10):1634-1641. doi: 10.1021/acsmedchemlett.2c00310. eCollection 2022 Oct 13. ACS Med Chem Lett. 2022. PMID: 36262395 Free PMC article.
Structure-Based Design of Selective β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitors: Targeting the Flap to Gain Selectivity over BACE2.
Fujimoto K, Matsuoka E, Asada N, Tadano G, Yamamoto T, Nakahara K, Fuchino K, Ito H, Kanegawa N, Moechars D, Gijsen HJM, Kusakabe KI. Fujimoto K, et al. Among authors: asada n. J Med Chem. 2019 May 23;62(10):5080-5095. doi: 10.1021/acs.jmedchem.9b00309. Epub 2019 May 13. J Med Chem. 2019. PMID: 31021626
Discovery of an Extremely Potent Thiazine-Based β-Secretase Inhibitor with Reduced Cardiovascular and Liver Toxicity at a Low Projected Human Dose.
Tadano G, Komano K, Yoshida S, Suzuki S, Nakahara K, Fuchino K, Fujimoto K, Matsuoka E, Yamamoto T, Asada N, Ito H, Sakaguchi G, Kanegawa N, Kido Y, Ando S, Fukushima T, Teisman A, Urmaliya V, Dhuyvetter D, Borghys H, Van Den Bergh A, Austin N, Gijsen HJM, Yamano Y, Iso Y, Kusakabe KI. Tadano G, et al. Among authors: asada n. J Med Chem. 2019 Oct 24;62(20):9331-9337. doi: 10.1021/acs.jmedchem.9b01140. Epub 2019 Oct 8. J Med Chem. 2019. PMID: 31549838
Discovery of Atabecestat (JNJ-54861911): A Thiazine-Based β-Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor Advanced to the Phase 2b/3 EARLY Clinical Trial.
Koriyama Y, Hori A, Ito H, Yonezawa S, Baba Y, Tanimoto N, Ueno T, Yamamoto S, Yamamoto T, Asada N, Morimoto K, Einaru S, Sakai K, Kanazu T, Matsuda A, Yamaguchi Y, Oguma T, Timmers M, Tritsmans L, Kusakabe KI, Kato A, Sakaguchi G. Koriyama Y, et al. Among authors: asada n. J Med Chem. 2021 Feb 25;64(4):1873-1888. doi: 10.1021/acs.jmedchem.0c01917. Epub 2021 Feb 15. J Med Chem. 2021. PMID: 33588527 Clinical Trial.
Origin of the kinetic HDAC2-selectivity of an HDAC inhibitor.
Mishima H, Itoh Y, Kurohara T, Suzuki T, Asada N, Kusakabe KI, Okamoto Y. Mishima H, et al. Among authors: asada n. J Comput Chem. 2023 Jul 5;44(18):1604-1609. doi: 10.1002/jcc.27111. Epub 2023 Apr 19. J Comput Chem. 2023. PMID: 37074817
225 results