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Updated: Jun 4, 2026
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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.
Bioscience, Biotechnology, and Biochemistry
|February 11, 2011
Summary
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.
