38527-79-6Relevant academic research and scientific papers
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, Yuji,Hori, Akihiro,Ito, Hisanori,Yonezawa, Shuji,Baba, Yoshiyasu,Tanimoto, Norihiko,Ueno, Tatsuhiko,Yamamoto, Shiho,Yamamoto, Takahiko,Asada, Naoya,Morimoto, Kenji,Einaru, Shunsuke,Sakai, Katsunori,Kanazu, Takushi,Matsuda, Akihiro,Yamaguchi, Yoshitaka,Oguma, Takuya,Timmers, Maarten,Tritsmans, Luc,Kusakabe, Ken-Ichi,Kato, Akira,Sakaguchi, Gaku
supporting information, p. 1873 - 1888 (2021/03/01)
Accumulation of amyloid β peptides (Aβ) is thought to be one of the causal factors of Alzheimer's disease (AD). The aspartyl protease β-site amyloid precursor protein cleaving enzyme 1 (BACE1) is the rate-limiting protease for Aβ production, and therefore
Trifluoromethyl Dihydrothiazine-Based β-Secretase (BACE1) Inhibitors with Robust Central β-Amyloid Reduction and Minimal Covalent Binding Burden
Anan, Kosuke,Iso, Yasuyoshi,Oguma, Takuya,Nakahara, Kenji,Suzuki, Shinji,Yamamoto, Takahiko,Matsuoka, Eriko,Ito, Hisanori,Sakaguchi, Gaku,Ando, Shigeru,Morimoto, Kenji,Kanegawa, Naoki,Kido, Yasuto,Kawachi, Tomoyuki,Fukushima, Tamio,Teisman, Ard,Urmaliya, Vijay,Dhuyvetter, Deborah,Borghys, Herman,Austin, Nigel,Van Den Bergh, An,Verboven, Peter,Bischoff, Francois,Gijsen, Harrie J. M.,Yamano, Yoshinori,Kusakabe, Kenichi
supporting information, p. 1894 - 1910 (2019/11/22)
The β-site amyloid precursor protein cleaving enzyme 1 (BACE1, also known as β-secretase) is a promising target for the treatment of Alzheimer's disease. A pKa lowering approach over the initial leads was adopted to mitigate hERG inhibition and
