Novel NanoLuc-type substrates with various C-6 substitutions

Bioorg Med Chem Lett. 2020 May 1;30(9):127085. doi: 10.1016/j.bmcl.2020.127085. Epub 2020 Mar 4.

Abstract

NanoLuc (NLuc)-furimazine bioluminescence system offers several advantages over established systems, including improved stability, smaller size, and >150-fold enhancement in bioluminescence. Herein, we designed and synthesized a series of bioluminescent substrates with varying at the C-6 position of furimazine for NLuc-furimazine bioluminescence system. Among all derivatives, compounds A6 and A11 provided excellent bioluminescence characteristics compared with furimazine in vitro and in vivo. We believe that these new NLuc substrates can broaden the application of NLuc bioluminescence techniques, especially in vivo bioluminescent imaging.

Keywords: Bioluminescence; Bioluminescent imaging; Bioluminescent substrates; Furimazine; NanoLuc.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • A549 Cells
  • Animals
  • Drug Design*
  • Furans / chemistry*
  • Gene Expression Regulation, Enzymologic
  • Humans
  • Imidazoles / chemistry*
  • Luciferases / chemical synthesis
  • Luciferases / chemistry
  • Luciferases / metabolism*
  • Luminescent Measurements / methods*
  • Mice
  • Mice, Nude
  • Nanotechnology / methods
  • Neoplasms, Experimental
  • Pyrazines / chemistry*

Substances

  • Furans
  • Imidazoles
  • Pyrazines
  • furimazine
  • Luciferases