WARF: P08069US

High Throughput Assay for Sugar-Mediated Drug Transport


Jon Thorson, John Fitzgibbon

The Wisconsin Alumni Research Foundation (WARF) is seeking commercial partners interested in developing a systematic platform for rapidly assessing the impact of different sugars on sugar-mediated uptake into various cell types.
OVERVIEWBecause many anti-cancer drugs cause adverse side effects, molecular targeting techniques have been developed to specifically target drugs to tumor sites, minimizing their effects on healthy tissue. These techniques work by conjugating a small molecule or macromolecule to a cancer therapeutic. The small molecule or macromolecule then directs the therapeutic to the target site.

Molecular targeting techniques offer a broadly applicable platform for modulating the selectivity, specificity and other characteristics of a wide range of anti-cancer agents. However, an extensive array of small molecules and macromolecules is needed to provide specificity on an intracellular compartment, cell type or even organ level.

Because a fundamental characteristic of cancer cells is their increased uptake of glucose, sugar molecules may be an option. Glucose surrogates, such as the fluorescent molecule fluorodeoxyglucose (FDG), and glucose conjugates have been used successfully in cancer imaging and treatment. However, only a small set of “typical” sugars have been investigated for use in molecular targeting thus far.
THE INVENTIONUW-Madison researchers have developed a systematic platform for rapidly assessing the ability of a diverse range of sugars to enhance the uptake and selectivity of sugar conjugates. This invention may lead to the discovery of sugar molecules that improve the delivery of cancer therapeutics.

First, glycorandomization (see WARF reference numbers P04020US and P04455US) is used to generate a library of molecules that differ only by the sugars attached. Then each of these glycosylated molecules is contacted with cells, and their uptake into the cells is assessed relative to that of a corresponding molecule without the attached sugars. To determine selectivity, these sugar conjugates can be contacted with cells from different cell lines and their uptake compared to see if it is elevated in cells from a particular line.

Using this strategy, the researchers found that slight changes in sugar structure can lead to drastic changes in in vitro cellular uptake. They identified sugars that impart up to an eight-fold increase in selective uptake by tumor, rather than normal, cell lines. They also identified sugars that provide greater than a 10-fold increase in uptake as compared to the conventional sugars glucose, 2-deoxyglucose or FDG.
  • Determining how different sugars affect sugar-mediated uptake into cells
  • Discovering new sugars that may improve cancer treatment
  • Provides a rapid, quantitative assay to directly assess the impact of different sugars on sugar-mediated uptake into various cell types
  • Extends well beyond the standard small set of sugars used in typical sugar transport studies
  • Enables the discovery of atypical sugars that provide enhanced intracellular uptake and specificity of cancer therapeutics as compared to glucose, 2-deoxyglucose or FDG
  • Provides a non-radioactive means of studying sugar transport in cells
  • Library can be screened using any cell type.
  • Glycorandomization enables the rapid synthesis of large libraries of sugar conjugates by eliminating most of the tedious steps associated with conventional glycosylation strategies.
Contact Information
For current licensing status, please contact Rafael Diaz at or 608-960-9847.
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UW–Madison has the integrative capabilities to complete many key components of the drug development cycle, from discovery through clinical trials. As one of the top research universities in the world, and one of the two best-funded universities for research in the country, UW–Madison offers state-of-the-art facilities unmatched by most public universities.

These include the Small Molecule Screening Facility at the UW Comprehensive Cancer Center; the Zeeh Pharmaceutical Experiment Station, which provides consulting and laboratory services for developing formulations and studying solubility, stability and more; the Waisman Clinical Biomanufacturing Facility; the Wisconsin Institute for Medical Research, which provides UW–Madison with a complete translational research facility; and the innovative, interdisciplinary Wisconsin Institutes for Discovery, home to the private, nonprofit Morgridge Institute for Research and its public twin, WID, part of the university's graduate school. The highly qualified experts at these facilities are ready to work with you to create a library of candidates for drug development.