Mechanism of cellular uptake and delivery of guanidinoglycosides

BIOL 130

Lev Elson-Schwab, lev@chem.ucsd.edu1, Pradip Chakarborty1, and Yitzhak Tor, ytor@ucsd.edu2. (1) Chemistry and Biochemistry, University of California, San Diego, 9500 Gilman Dr. Pacific Hall 6228, La Jolla, CA 92093, (2) Department of Chemistry and Biochemistry, University of California, San Diego, MC 0358, 9500 Gilman Drive, La Jolla, CA 92093
A major obstacle for the development of new therapeutic agents is drug delivery. Many drug candidates which show activity in vitro show greatly decreased activity in vivo because of sluggish organ/cellular uptake. We have discovered that guanidinoglycosides, a family of synthetic derivatives where all of the ammonium groups of aminoglycoside antibiotics have been converted into guanidinium groups, are efficiently taken up into eukaryotic cells. Here we will present our investigations into the proteoglycan dependence of guanidinoglycoside uptake. We will also provide evidence that guanidinoglycosides efficiently facilitate the uptake of very large bioactive cargo into cells.
 

Chemistry and Metabolism
4:30 PM-6:30 PM, Tuesday, 12 September 2006 Moscone Center -- Hall D, Poster

Division of Biological Chemistry

The 232nd ACS National Meeting, San Francisco, CA, September 10-14, 2006