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Glucose transporter 4 (GLUT4) and Glucose transporter 2 (GLUT2) (GLUT4 (for skeletal muscle, adipose tissue) GLUT2 (for liver, pancreatic beta cells))

Target
GLUT4 (for skeletal muscle, adipose tissue) GLUT2 (for liver, pancreatic beta cells)
Molecular classification
Transporter, Facilitative glucose transporter, Membrane protein, SLC2A family
01

Overview

Glucose uptake in metabolically active tissues is regulated mainly by facilitative glucose transporters, particularly GLUT4 and GLUT2. GLUT4 is the major insulin-responsive transporter in skeletal muscle and adipose tissue, undergoing translocation to the plasma membrane in response to insulin or contraction, facilitating glucose entry for metabolism[1][3]. GLUT2, a low-affinity, high-capacity transporter, is expressed in hepatocytes, pancreatic beta cells, and the intestines, where it senses glucose levels and regulates insulin secretion and gene expression[2][3]. Increased uptake of glucose analogues (such as ^18F-FDG used in PET scans) reflects heightened metabolic activity, especially in tumors or during disease states like diabetes, where transporter function is often dysregulated[1][4]. The process is a critical determinant of energy metabolism, cell growth, and proliferation, making GLUTs both therapeutic and diagnostic targets.

Other names
Glucose transporter 4GLUT4Glucose transporter 2GLUT2facilitative glucose transporterSLC2A4SLC2A2
02

Mechanism of action

Facilitation of glucose entry into cells via translocation to plasma membrane (GLUT4, insulin-dependent) High-capacity glucose uptake (GLUT2, concentration-dependent, in liver, pancreas)

03

Biological functions

Glucose uptakeEnergy metabolismSignal transduction (via glucose sensing)Regulation of insulin secretionCell proliferation (especially in cancer)
04

Disease associations

Diabetes mellitus (type 2 diabetes)Insulin resistanceNon-alcoholic fatty liver diseaseCancer (increased uptake in metabolically active cancers)Cardiovascular disease
05

Safety considerations

Risk for hypoglycemia (with insulin or agents increasing glucose uptake)Off-target uptake in tumors (FDG PET imaging)Progression of insulin resistance if GLUT4 function impaired
06

Interacting drugs

Insulin (stimulates GLUT4 translocation)

4 more in the full profile.

07

Biomarkers

^18F-FDG uptake (PET imaging for cancer/metabolic activity)GLUT4/GLUT2 expression levels (as disease biomarkers in diabetes, cancer)

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