Target intelligence / Profile preview

Cationic amino acid transporter (CAT) (CAT)

Target
CAT
Molecular classification
Transporter, Solute carrier family
01

Overview

Arginine transport systems, primarily the Cationic Amino Acid Transporters (CATs) belonging to the SLC7 family, mediate the uptake of L-arginine into cells [UniProt P30825]. L-arginine is a versatile amino acid essential for protein synthesis and serves as a precursor for nitric oxide, polyamines, and creatine [PubMed 30154018]. In the context of oncology, many tumors exhibit arginine auxotrophy due to the loss of argininosuccinate synthetase 1 (ASS1), making them dependent on these transport systems for survival [PubMed 27103444]. This dependency creates a therapeutic vulnerability that can be exploited by depleting extracellular arginine or potentially inhibiting the transporters directly [ClinicalTrials.gov NCT02709512]. Beyond cancer, these systems are involved in regulating vascular tone and immune cell activation by controlling the availability of arginine for nitric oxide synthase [PubMed 21169519]. Current clinical approaches primarily utilize arginine-depleting enzymes like pegargiminase to starve tumor cells, while research into direct inhibitors of CAT-1 and related transporters continues as a means to treat both metabolic and inflammatory disorders [PubMed 31431546].

Other names
Arginine transport systemsSystem y+SLC7 familyArginine transporterCationic amino acid transport systemHigh affinity cationic amino acid transporter
02

Mechanism of action

Inhibition of cellular arginine uptake or depletion of extracellular arginine to induce metabolic starvation in arginine-auxotrophic cells.

03

Biological functions

Amino acid transportNitric oxide biosynthetic processProtein synthesisCell proliferationImmune response modulation
04

Disease associations

CancerInflammationCardiovascular diseaseInfection
05

Safety considerations

ImmunosuppressionImpaired wound healingGastrointestinal toxicityHyperammonemiaVascular tone dysregulation
06

Interacting drugs

Pegargiminase (ADI-PEG 20)

4 more in the full profile.

07

Biomarkers

Argininosuccinate synthetase 1 (ASS1) deficiencySLC7A1 expression levelsPlasma arginine concentrationArgininosuccinate lyase (ASL) expression

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