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Rational Design of Novel 1,3-Oxazine Based β-Secretase (BACE1) Inhibitors: Incorporation of a Double Bond To Reduce P-gp Efflux Leading to Robust Aβ Reduction in the Brain.
Fuchino K, Mitsuoka Y, Masui M, Kurose N, Yoshida S, Komano K, Yamamoto T, Ogawa M, Unemura C, Hosono M, Ito H, Sakaguchi G, Ando S, Ohnishi S, Kido Y, Fukushima T, Miyajima H, Hiroyama S, Koyabu K, Dhuyvetter D, Borghys H, Gijsen HJM, Yamano Y, Iso Y, Kusakabe KI. Fuchino K, et al. Among authors: komano k. J Med Chem. 2018 Jun 28;61(12):5122-5137. doi: 10.1021/acs.jmedchem.8b00002. Epub 2018 May 23. J Med Chem. 2018. PMID: 29733614
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: komano k. 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
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: komano k. 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 a Tricyclic β-Lactam as a Potent Antimicrobial Agent against Carbapenem-Resistant Enterobacterales, Including Strains with Reduced Membrane Permeability and Four-Amino Acid Insertion into Penicillin-Binding Protein 3: Structure-Activity-Relationships and In Vitro and In Vivo Activities.
Sato J, Kusano H, Aoki T, Shibuya S, Yokoo K, Komano K, Oguma T, Matsumoto S, Nakamura R, Sato T, Yamawaki K. Sato J, et al. Among authors: komano k. ACS Infect Dis. 2022 Mar 11;8(3):400-410. doi: 10.1021/acsinfecdis.1c00549. Epub 2022 Feb 3. ACS Infect Dis. 2022. PMID: 35112852
Close association between non-alcoholic fatty liver disease and ossification of the posterior longitudinal ligament of the spine.
Endo T, Koike Y, Miyoshi H, Hisada Y, Fujita R, Suzuki R, Tanaka M, Tsujimoto T, Shimamura Y, Hasegawa Y, Kanayama M, Hashimoto T, Oha F, Noro N, Komano K, Ishii M, Ito YM, Iwasaki N, Takahata M. Endo T, et al. Among authors: komano k. Sci Rep. 2021 Aug 31;11(1):17412. doi: 10.1038/s41598-021-96714-9. Sci Rep. 2021. PMID: 34465807 Free PMC article.
Discovery of 2-Sulfinyl-Diazabicyclooctane Derivatives, Potential Oral β-Lactamase Inhibitors for Infections Caused by Serine β-Lactamase-Producing Enterobacterales.
Fujiu M, Yokoo K, Sato J, Shibuya S, Komano K, Kusano H, Sato S, Aoki T, Kohira N, Kanazawa S, Watari R, Kawachi T, Hirakawa Y, Nagamatsu D, Kashiwagi E, Maki H, Yamawaki K. Fujiu M, et al. Among authors: komano k. J Med Chem. 2021 Jul 8;64(13):9496-9512. doi: 10.1021/acs.jmedchem.1c00799. Epub 2021 Jun 18. J Med Chem. 2021. PMID: 34143627
Introduction of a Thio Functional Group to Diazabicyclooctane: An Effective Modification to Potentiate the Activity of β-Lactams against Gram-Negative Bacteria Producing Class A, C, and D Serine β-Lactamases.
Fujiu M, Yokoo K, Sato J, Shibuya S, Komano K, Kusano H, Sato S, Aoki T, Kohira N, Miyagawa S, Kawachi T, Yamawaki K. Fujiu M, et al. Among authors: komano k. ACS Infect Dis. 2020 Nov 13;6(11):3034-3047. doi: 10.1021/acsinfecdis.0c00560. Epub 2020 Nov 4. ACS Infect Dis. 2020. PMID: 33147950
14 results