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Macrocyclic Peptides as a Novel Class of NNMT Inhibitors: A SAR Study Aimed at Inhibitory Activity in the Cell.
Hayashi K, Uehara S, Yamamoto S, Cary DR, Nishikawa J, Ueda T, Ozasa H, Mihara K, Yoshimura N, Kawai T, Ono T, Yamamoto S, Fumoto M, Mikamiyama H. Hayashi K, et al. Among authors: yamamoto s. ACS Med Chem Lett. 2021 Jun 2;12(7):1093-1101. doi: 10.1021/acsmedchemlett.1c00134. eCollection 2021 Jul 8. ACS Med Chem Lett. 2021. PMID: 34267879 Free PMC article.
Discovery of S-217622, a Noncovalent Oral SARS-CoV-2 3CL Protease Inhibitor Clinical Candidate for Treating COVID-19.
Unoh Y, Uehara S, Nakahara K, Nobori H, Yamatsu Y, Yamamoto S, Maruyama Y, Taoda Y, Kasamatsu K, Suto T, Kouki K, Nakahashi A, Kawashima S, Sanaki T, Toba S, Uemura K, Mizutare T, Ando S, Sasaki M, Orba Y, Sawa H, Sato A, Sato T, Kato T, Tachibana Y. Unoh Y, et al. Among authors: yamamoto s. J Med Chem. 2022 May 12;65(9):6499-6512. doi: 10.1021/acs.jmedchem.2c00117. Epub 2022 Mar 30. J Med Chem. 2022. PMID: 35352927 Free PMC article.
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: yamamoto t, yamamoto s. 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: yamamoto s. 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
Balancing potency and basicity by incorporating fluoropyridine moieties: Discovery of a 1-amino-3,4-dihydro-2,6-naphthyridine BACE1 inhibitor that affords robust and sustained central Aβ reduction.
Nakahara K, Mitsuoka Y, Kasuya S, Yamamoto T, Yamamoto S, Ito H, Kido Y, Kusakabe KI. Nakahara K, et al. Among authors: yamamoto t, yamamoto s. Eur J Med Chem. 2021 Apr 15;216:113270. doi: 10.1016/j.ejmech.2021.113270. Epub 2021 Feb 7. Eur J Med Chem. 2021. PMID: 33765486
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: yamamoto t, yamamoto s. 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.
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