J. Am. Chem. Soc., 128 (20), 6526 -6527, 2006. 10.1021/ja0586283 S0002-7863(05)08628-2
Web Release Date: April 25, 2006

Copyright © 2006 American Chemical Society

Releasable Luciferin-Transporter Conjugates: Tools for the Real-Time Analysis of Cellular Uptake and Release

Lisa R. Jones, Elena A. Goun, Rajesh Shinde, Jonathan B. Rothbard, Christopher H. Contag, and Paul A. Wender*#

Departments of Chemistry, Molecular Pharmacology, and Pediatrics, Stanford University, Stanford, California 94305-5080

wenderp@stanford.edu

Received January 9, 2006

Abstract:

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.


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