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Updated: Jun 4, 2026
A Fluorescence-based Lymphocyte Assay Suitable for High-throughput Screening of Small Molecules
Published on: March 10, 2017
A new, convenient cell-based screening method for small-molecule glycolytic inhibitors
Mitsuhiro Kitagawa1, Mayuko Misawa, Seiichiro Ogawa
1Department of Biosciences and Informatics, Faculty of Science and Technology, Keio University, Yokohama, Kanagawa, Japan.
Abstract:
To counteract active glycolysis in tumors, we developed a new, convenient cell-based screening system to identify an inhibitor of glycolysis. Using this system, we searched for an inhibitor in the synthetic Carbasugar library and found two candidates. It was found that both inhibited glycolysis by suppressing the glucose uptake step in tumor cells.
Insights
Researchers developed a novel screening system to find glycolysis inhibitors for cancer. Two synthetic Carbasugar compounds were identified, effectively blocking glucose uptake in tumor cells to counteract tumor glycolysis.
Area of Science:
- Oncology
- Biochemistry
- Drug Discovery
Background:
- Tumors exhibit enhanced glycolysis, a metabolic hallmark supporting rapid proliferation.
- Targeting tumor glycolysis is a promising strategy for cancer therapy.
Purpose of the Study:
- To develop a convenient cell-based screening system for identifying glycolysis inhibitors.
- To discover novel inhibitors of glycolysis from a synthetic Carbasugar library.
Main Methods:
- Established a cell-based screening system to detect glycolysis inhibition.
- Screened a synthetic Carbasugar library using the developed system.
- Validated the inhibitory mechanism of candidate compounds on glucose uptake.
Main Results:
- Identified two synthetic Carbasugar compounds as potent inhibitors of glycolysis.
- Demonstrated that both compounds suppress glucose uptake in tumor cells.
- Confirmed the cell-based screening system's efficacy in identifying glycolysis inhibitors.
Conclusions:
- The developed screening system is effective for discovering glycolysis inhibitors.
- Synthetic Carbasugars show potential as therapeutic agents by inhibiting tumor glycolysis via glucose uptake suppression.
