Target intelligence / Profile preview

Cationic amino acid transporter 1 (CAT-1 (also SLC7A1))

Target
CAT-1 (also SLC7A1)
Molecular classification
Transporter, Solute carrier family 7 (SLC7), Amino acid transporter
01

Overview

Cationic amino acid transporter 1 (CAT-1, SLC7A1) is a high-affinity, low-capacity permease responsible for mediating the sodium-independent uptake and efflux of cationic amino acids—primarily arginine, but also lysine and ornithine—across the plasma membrane of non-hepatic mammalian cells. This transporter is essential for supplying cells with arginine, a vital substrate for nitric oxide (NO) synthesis and a regulator of key metabolic and signaling pathways, including the mTORC1 axis. CAT-1 belongs to the solute carrier family 7 (SLC7) and is widely expressed except in adult liver. It has become a focus of interest as a potential cancer therapeutic target based on findings that some tumor cells (such as chronic lymphocytic leukemia) exhibit a unique dependency on CAT-1-mediated arginine import to support their growth and survival. Inhibition of CAT-1 affects processes including cellular metabolism, immune responses (by modulating NO production), and cell proliferation. Pharmacological targeting remains a challenge due to its widespread physiological roles and the risk of on-target toxicity.

Other names
CAT-1SLC7A1High affinity cationic amino acid transporter 1hCAT-1Arginine transporter 1
02

Mechanism of action

Inhibition of CAT-1 reduces cellular uptake of arginine and related cationic amino acids, impairing NO synthesis and mTOR signaling, which can affect cell proliferation and survival—especially in tumor cells reliant on extracellular arginine

03

Biological functions

Amino acid transportRegulation of cellular arginine, lysine, and ornithine uptakeRegulation of nitric oxide (NO) synthesis (via substrate provision)Regulation of mTOR pathway signalingMaintenance of cationic amino acid homeostasis
04

Disease associations

Cancer (notably in chronic lymphocytic leukemia and arginine-auxotrophic tumors)Cardiovascular disease (altered NO metabolism/vasoregulation due to arginine transport impairment)Immune regulation and inflammation (via substrate supply for nitric oxide synthase)
05

Safety considerations

Broad tissue distribution, so systemic inhibition could disrupt arginine/NOS/NO pathways, leading to cardiovascular and metabolic side effectsPotential impact on immune function due to limits on macrophage or T cell NO productionGeneral disruption of amino acid homeostasis could have pleiotropic toxicities
06

Interacting drugs

Verapamil (weak inhibitor)

2 more in the full profile.

07

Biomarkers

Cellular expression levels of CAT-1 (SLC7A1) as a biomarker for arginine dependency in cancer cellsArginine uptake rates as functional biomarker of CAT-1 activity in cell assaysPlasma concentrations of arginine, asymmetric dimethylarginine (ADMA), and homoarginine may reflect alterations in CAT-1 activity

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