Releasable luciferin-transporter conjugates: tools for the real-time analysis of cellular uptake and release

J Am Chem Soc. 2006 May 24;128(20):6526-7. doi: 10.1021/ja0586283.


The design, synthesis, and evaluation of conjugates of arginine-rich transporters and luciferin are described that release luciferin only after entry into cells that are stably transfected with luciferase. Each molecule of free luciferin that is released after entry generates a photon that can be measured allowing for real-time quantification of uptake and release in cells. The process provides a method to assay uptake and release of free luciferin as a function of variations in the releasable linker and in the transporter.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • 2,2'-Dipyridyl / analogs & derivatives
  • 2,2'-Dipyridyl / chemistry
  • Animals
  • Biological Transport / physiology*
  • Cell Line, Tumor
  • Cells / metabolism
  • Disulfides / chemistry
  • Disulfides / metabolism
  • Firefly Luciferin / analogs & derivatives*
  • Luciferases / metabolism
  • Luminescent Measurements
  • Male
  • Prostatic Neoplasms / metabolism
  • Transfection


  • Disulfides
  • 2,2'-dipyridyl disulfide
  • 2,2'-Dipyridyl
  • Firefly Luciferin
  • Luciferases