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Review
. 2021 Apr;87(4):447-464.
doi: 10.1007/s00280-020-04218-6. Epub 2021 Jan 19.

The role of the glutamine transporter ASCT2 in antineoplastic therapy

Estefânia Teixeira  1 , Cláudia Silva  1   2 , Fátima Martel  3   4
Affiliations
Review

The role of the glutamine transporter ASCT2 in antineoplastic therapy

Estefânia Teixeira et al. Cancer Chemother Pharmacol. 2021 Apr.

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.

Keywords: ASCT2; Antineoplastic therapy; Glutamine uptake; Metabolic reprogramming.

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