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Title | Discovery of Potent and Centrally Active 6-Substituted 5-Fluoro-1,3-dihydro-oxazine beta-Secretase (BACE1) Inhibitors via Active Conformation Stabilization |
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Journal, issue, pages | J. Med. Chem., Vol. 61, Page 5525-5546, Year 2018 |
Publish date | Sep 27, 2017 (structure data deposition date) |
Authors | Nakahara, K. / Fuchino, K. / Komano, K. / Asada, N. / Tadano, G. / Hasegawa, T. / Yamamoto, T. / Sako, Y. / Ogawa, M. / Unemura, C. ...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, H.J.M. / Yamano, Y. / Iso, Y. / Kusakabe, K.I. |
External links | J. Med. Chem. / PubMed:29775538 |
Methods | X-ray diffraction |
Resolution | 2.2 Å |
Structure data | PDB-5ygx: |
Chemicals | ChemComp-IOD: ChemComp-GOL: ChemComp-DMS: ChemComp-0B5: ChemComp-HOH: |
Source |
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Keywords | HYDROLASE/INHIBITOR / beta secretase / HYDROLASE-INHIBITOR complex |