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

MEDI 279

Lisa R. Jones, lisarj@stanford.edu, Department of Chemistry, Stanford University, Stanford, CA 94305-5080 and Paul A. Wender, wenderp@stanford.edu, Department of Chemistry, Department of Molecular Pharmacology, Stanford University, Stanford, CA 94305.
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.