High throughput in vivo phenotypic screening for drug repurposing: Discovery of MLR-1023 a novel insulin sensitizer and novel Lyn kinase activator with clinical proof of concept
作者: Christopher A. LipinskiAndrew G. Reaume
作者单位: 1Melior Discovery, Inc., 860 Springdale Drive, Exton, PA 19087, United States
刊名: Bioorganic & Medicinal Chemistry, 2020, Vol.28 (9)
来源数据库: Elsevier Journal
DOI: 10.1016/j.bmc.2020.115425
关键词: Phenotypic screenFragmentsDrug repurposingInsulin sensitizerAllosteric modulators
原始语种摘要: Abstract(#br)Drug discovery requires the combination of medicinal chemistry and biology. In this article Chris Lipinski, the medicinal chemist, describes the chemical origins at Pfizer of Tolimidone 1 the starting point for the repurposed MLR-1023 (Ochman et al., 2012). Andrew Reaume, the biologist, describes his motivation to develop a high quality (i.e. in vivo model) phenotypic screening platform as an ideal drug repositioning platform.
全文获取路径: Elsevier  (合作)
影响因子:2.903 (2012)

  • sensitizer 激活剂
  • screening 筛分
  • insulin 胰岛素
  • novel 长篇小说
  • phenotypic 表型的
  • kinase 激酶
  • clinical 临床的
  • activator 活化剂
  • proof 证明
  • throughput 吞吐量