Target intelligence / Profile preview

Solute carrier family 2 facilitated glucose transporter (GLUT) (GLUT)

Target
GLUT
Molecular classification
Transporter, Solute carrier family, Major Facilitator Superfamily (MFS)
01

Overview

The Solute carrier family 2 (SLC2A), commonly known as the GLUT family, consists of 14 facilitative membrane proteins that mediate the transport of glucose and other hexoses across cell membranes down their concentration gradients (PMID: 23506882). These transporters are essential for maintaining systemic glucose homeostasis and cellular energy production, with specific isoforms exhibiting distinct tissue distributions and substrate affinities; for example, GLUT1 is critical for glucose uptake across the blood-brain barrier, while GLUT4 is the primary insulin-responsive transporter in muscle and adipose tissue (PMID: 28123924). Dysregulation of GLUT expression is implicated in various diseases, most notably in cancer, where GLUT1 and GLUT3 are often overexpressed to support the high glycolytic demands of tumor cells, a phenomenon known as the Warburg effect (PMID: 23506882). Additionally, genetic mutations in SLC2A members lead to metabolic disorders such as GLUT1 deficiency syndrome and Fanconi-Bickel syndrome (PMID: 31513340). Pharmacological modulation of GLUTs is a significant area of drug development, with research focusing on GLUT1 inhibitors like Bay-876 to starve cancer cells, although achieving isoform selectivity is crucial to minimize off-target effects on healthy tissues like the brain and heart (PMID: 27171337).

Other names
SLC2A familyFacilitative glucose transporter familyGlucose transporter memberGLUT family
02

Mechanism of action

Facilitated diffusion of glucose, fructose, and other hexoses across the plasma membrane, moving substrates down their concentration gradient without the consumption of metabolic energy (ATP) (PMID: 23506882).

03

Biological functions

Glucose transportHexose transportMetabolic homeostasisFacilitated diffusionGlucose sensing
04

Disease associations

CancerType 2 diabetes mellitusGLUT1 deficiency syndromeFanconi-Bickel syndromeObesityAlzheimer's disease
05

Safety considerations

Neuroglycopenia (brain glucose deprivation) (PMID: 31513340)Systemic hypoglycemiaImpaired insulin sensitivity (PMID: 15159444)Potential cardiotoxicityDisruption of glucose sensing in the liver and pancreas (PMID: 28123924)
06

Interacting drugs

Ritonavir (PMID: 15159444)

5 more in the full profile.

07

Biomarkers

GLUT1 protein expression (IHC) (PMID: 23506882)18F-FDG uptake in PET imaging (PMID: 23506882)Cerebrospinal fluid (CSF) to blood glucose ratio (PMID: 31513340)Erythrocyte GLUT1 expression levels (PMID: 31513340)

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