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Amino acid transporter (Peptide transporter for peptide-specific families) (Often abbreviated as AAT for amino acid transporter, PepT for peptide transporter, and SLC followed by family number for specific genes (e.g., SLC1A5 for ASCT2))

Target
Often abbreviated as AAT for amino acid transporter, PepT for peptide transporter, and SLC followed by family number for specific genes (e.g., SLC1A5 for ASCT2)
Molecular classification
Transporter, Solute carrier (SLC) protein, Membrane protein, Secondary active transporter, Facilitated transporter
01

Overview

Amino acid and peptide transporters are membrane proteins critical for moving amino acids (single units) and peptides (short chains) across cell membranes. They belong primarily to the solute carrier (SLC) families and facilitate transport through active (energy-dependent) or passive (facilitated) mechanisms. These transporters are widely expressed in tissues such as the intestine, kidney, brain, and immune cells, playing a central role in nutrient absorption, control of neurotransmitter levels, immune cell function, and cellular metabolism. Multiple transporter subtypes exist, each with distinct substrate specificities (neutral, basic, acidic amino acids, or peptides). Dysregulation or mutation in these transporters can contribute to various diseases, and several are therapeutic targets, especially in cancer, neurology, and metabolism

Other names
Solute carrier family (SLC family)Neutral amino acid transporter (e.g., ASCT2)Cationic amino acid transporter (e.g., CAT)Proton-coupled oligopeptide transporter (e.g., PepT1, PepT2)System A, System L, System N transporterSodium-coupled amino acid transporterLAT1, ASCT1, ASCT2, GAT-1
02

Mechanism of action

Competitive inhibition of substrate binding, Substrate mimetic transport blockers, Modulation of transport activity (allosteric regulation), Transport-mediated prodrug uptake and activation

03

Biological functions

Nutrient uptakeNeurotransmitter regulationImmune cell activation and differentiationProtein catabolismRegulation of cellular amino acid poolsProtein synthesis regulation
04

Disease associations

Cancer (metabolic reprogramming, glutamine addiction)Neurological disease (neurotransmitter imbalance)Immune and inflammatory disease (T-cell activation)Metabolic disorders (aminoacidurias)Infection
05

Safety considerations

Off-target effects on nutrient homeostasisRisk of neurotransmitter imbalance (e.g., seizures from altered GABA transport)Gastrointestinal side effects (diarrhea, malabsorption)Immunosuppression or immune dysregulation
06

Interacting drugs

Lisinopril and other peptide-based drugs (via PepT1/PepT2)

2 more in the full profile.

07

Biomarkers

SLC1A5/ASCT2 expression in cancer for glutamine dependenceLAT1 expression for tumor metabolismPepT1/PepT2 mRNA/protein for renal and intestinal functionGAT1/GAT2 protein in neurological disease

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