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Updated: Nov 20, 2025

Glutamine Flux Imaging Using Genetically Encoded Sensors
Published on: July 31, 2014
The role of the glutamine transporter ASCT2 in antineoplastic therapy
Estefânia Teixeira1, Cláudia Silva1,2, Fátima Martel3,4
1Department of Biomedicine, Unit of Biochemistry, Faculty of Medicine, University of Porto, Al Prof. Hernâni Monteiro, 4200-319, Porto, Portugal.
Abstract:
Cancer cells are metabolically reprogrammed to support their high rates of proliferation, continuous growth, survival, invasion, metastasis, and resistance to cancer treatments. Among changes in cancer cell bioenergetics, the role of glutamine metabolism has been receiving increasing attention. Increased glutaminolysis in cancer cells is associated with increased expression of membrane transporters that mediate the cellular uptake of glutamine. ASCT2 (Alanine, Serine, Cysteine Transporter 2) is a Na+-dependent transmembrane transporter overexpressed in cancer cells and considered to be the primary transporter for glutamine in these cells. The possibility of inhibiting ASCT2 for antineoplastic therapy is currently under investigation. In this article, we will present the pharmacological agents currently known to act on ASCT2, which have been attracting attention in antineoplastic therapy research. We will also address the impact of ASCT2 inhibition on the prognosis of some cancers. We conclude that ASCT2 inhibition and combination of ASCT2 inhibitors with other anti-tumor therapies may be a promising antineoplastic strategy. However, more research is needed in this area.
Insights
Inhibiting the ASCT2 transporter, crucial for cancer cell glutamine uptake, shows promise for new cancer treatments. Targeting ASCT2, alone or with other therapies, may improve cancer prognosis.
Area of Science:
- Oncology
- Molecular Biology
- Biochemistry
Background:
- Cancer cells exhibit metabolic reprogramming to sustain rapid proliferation and survival.
- Glutamine metabolism is increasingly recognized as a key factor in cancer bioenergetics.
- The transmembrane transporter ASCT2 (Alanine, Serine, Cysteine Transporter 2) is overexpressed in cancer cells and facilitates glutamine uptake.
Purpose of the Study:
- To review pharmacological agents targeting ASCT2 for cancer therapy.
- To discuss the impact of ASCT2 inhibition on cancer prognosis.
- To evaluate ASCT2 inhibition as a potential antineoplastic strategy.
Main Methods:
- Literature review of pharmacological agents acting on ASCT2.
- Analysis of studies investigating ASCT2 inhibition in cancer models.
- Examination of clinical research on ASCT2 inhibitors.
Main Results:
- ASCT2 is a primary glutamine transporter in cancer cells.
- Pharmacological agents targeting ASCT2 are under investigation for antineoplastic therapy.
- ASCT2 inhibition demonstrates potential impact on cancer prognosis.
Conclusions:
- ASCT2 inhibition represents a promising antineoplastic strategy.
- Combining ASCT2 inhibitors with other anti-tumor therapies may enhance efficacy.
- Further research is necessary to fully establish ASCT2-targeted therapies.
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