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Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints.
Winneroski, Leonard L; Erickson, Jon A; Green, Steven J; Lopez, Jose E; Stout, Stephanie L; Porter, Warren J; Timm, David E; Audia, James E; Barberis, Mario; Beck, James P; Boggs, Leonard N; Borders, Anthony R; Boyer, Robert D; Brier, Richard A; Hembre, Erik J; Hendle, Jörg; Garcia-Losada, Pablo; Minguez, Jose Miguel; Mathes, Brian M; May, Patrick C; Monk, Scott A; Rankovic, Zoran; Shi, Yuan; Watson, Brian M; Yang, Zhixiang; Mergott, Dustin J.
Affiliation
  • Winneroski LL; Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
  • Erickson JA; Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
  • Green SJ; Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
  • Lopez JE; Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
  • Stout SL; Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
  • Audia JE; Constellation Pharmaceuticals, Cambridge, MA 02140, USA(2).
  • Barberis M; Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
  • Beck JP; Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
  • Borders AR; Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
  • Boyer RD; Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
  • Brier RA; Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
  • Hembre EJ; Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
  • Hendle J; Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Biotechnology Center, San Diego, CA 92121, USA.
  • Garcia-Losada P; Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
  • Minguez JM; Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
  • Mathes BM; Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
  • Monk SA; Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
  • Rankovic Z; Chemical Biology & Therapeutics St. Jude Children's Research Hospital, 262 Danny Thomas Place, Memphis, TN 38105, USA(2).
  • Shi Y; Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
  • Watson BM; Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
  • Yang Z; Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
  • Mergott DJ; Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA. Electronic address: mergottdu@lilly.com.
Bioorg Med Chem ; 28(1): 115194, 2020 01 01.
Article in En | MEDLINE | ID: mdl-31786008
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Full text: 1 Database: MEDLINE Main subject: Protease Inhibitors / Aspartic Acid Endopeptidases / Cyclopropanes / Amyloid Precursor Protein Secretases Limits: Humans Language: En Year: 2020 Type: Article
Fulltext
Print
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PubMed Links
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Full text: 1 Database: MEDLINE Main subject: Protease Inhibitors / Aspartic Acid Endopeptidases / Cyclopropanes / Amyloid Precursor Protein Secretases Limits: Humans Language: En Year: 2020 Type: Article