Target intelligence / Profile preview

Solute carrier family 2 (GLUT family) (GLUT)

Target
GLUT
Molecular classification
Transporter, Solute carrier family
01

Overview

The Solute carrier family 2 (GLUT family) consists of 14 transmembrane proteins that facilitate the bidirectional transport of glucose and other hexoses across cell membranes (UniProt, 2024). These transporters are essential for cellular metabolism, operating via facilitated diffusion to move glucose down its concentration gradient (StatPearls, 2023). The family is divided into three classes based on sequence homology: Class I (GLUT1-4), Class II (GLUT5, 7, 9, 11), and Class III (GLUT6, 8, 10, 12, 13/HMIT) (PubMed, 2016). GLUT1 is critical for glucose transport across the blood-brain barrier, while GLUT4 is the primary insulin-responsive transporter in muscle and adipose tissue (NIH, 2023). In oncology, many tumors overexpress GLUT1 and GLUT3 to sustain high glycolytic rates, a phenomenon known as the Warburg effect, making these transporters viable targets for anticancer therapy (PubMed, 2020). Conversely, loss-of-function mutations in GLUT1 lead to GLUT1 deficiency syndrome, characterized by seizures and developmental delays due to impaired brain energy supply (GARD, 2024). Pharmacological inhibitors like BAY-876 and WZB117 are currently being researched for their potential to selectively starve cancer cells of glucose (PubMed, 2016).

Other names
SLC2 familyFacilitated glucose transportersGlucose transporter familyHexose transporters
02

Mechanism of action

Inhibition of facilitated glucose transport across the plasma membrane by binding to the transporter's substrate-binding site or inducing a conformational change that prevents hexose translocation.

03

Biological functions

Glucose transportHexose transportFacilitated diffusionMetabolic regulationEnergy homeostasis
04

Disease associations

CancerDiabetes mellitusGLUT1 deficiency syndromeFanconi-Bickel syndromeObesityAlzheimer's disease
05

Safety considerations

Systemic hypoglycemiaNeuroglycopeniaOff-target inhibition of essential glucose uptake in the brain and erythrocytesMetabolic acidosisPotential for insulin resistance
06

Interacting drugs

BAY-876

7 more in the full profile.

07

Biomarkers

GLUT1 expression (IHC)18F-FDG uptake (PET imaging)Cerebrospinal fluid glucose levelsBlood glucose levelsCSF/Serum glucose ratio

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