Target intelligence / Profile preview

Neutral amino acid transporter B(0) (ASCT2) (ASCT2)

Target
ASCT2
Molecular classification
Transporter, Solute carrier family
01

Overview

Neutral amino acid transporter B(0), commonly known as ASCT2, is a sodium-dependent solute carrier protein encoded by the SLC1A5 gene (UniProt: P46459). It functions primarily as an obligatory exchanger of neutral amino acids, including glutamine, alanine, serine, and asparagine, across the plasma membrane (NCBI Gene: 6510). ASCT2 plays a pivotal role in maintaining amino acid homeostasis and supporting cellular metabolism, particularly in rapidly dividing cells (PubMed: 29403062). In the context of oncology, ASCT2 is frequently overexpressed in various malignancies, such as triple-negative breast cancer and non-small cell lung cancer, to facilitate "glutamine addiction" (PubMed: 26096102). This upregulation allows cancer cells to import sufficient glutamine to fuel the tricarboxylic acid (TCA) cycle and biosynthetic pathways. Consequently, ASCT2 has emerged as a significant therapeutic target, with several small molecule inhibitors like V-9302 and antibody-drug conjugates under investigation (PubMed: 29403062). Beyond its metabolic role, ASCT2 serves as the primary entry receptor for several retroviruses, including the RD114 virus (UniProt: P46459). Therapeutic strategies targeting ASCT2 aim to disrupt tumor nutrient supply, leading to metabolic crisis and cell death.

Other names
SLC1A5Solute carrier family 1 member 5Alanine/serine/cysteine/threonine transporter 2AAATATB(0)RDRC
02

Mechanism of action

Competitive inhibition of neutral amino acid transport and antibody-mediated targeted cytotoxicity (PubMed: 29403062).

03

Biological functions

Amino acid transport (UniProt: P46459)Glutamine homeostasis (PubMed: 26096102)Cell growth and proliferation (PubMed: 29403062)Metabolic reprogramming (PubMed: 26096102)
04

Disease associations

Cancer (e.g., Breast, Lung, Prostate) (PubMed: 29403062)Viral infection (e.g., RD114 retrovirus) (UniProt: P46459)
05

Safety considerations

Potential impairment of T-cell mediated immune responses (PubMed: 29403062)Gastrointestinal toxicity due to disruption of intestinal glutamine transport (UniProt: P46459)Potential impact on brain amino acid balance (PubMed: 16186101)
06

Interacting drugs

V-9302 (PubMed: 29403062)

4 more in the full profile.

07

Biomarkers

SLC1A5 protein expression (IHC) (PubMed: 26096102)18F-glutamine uptake (PET imaging) (PubMed: 28254790)

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