Target intelligence / Profile preview

Solute carrier family 2, facilitated glucose transporter member 4 (GLUT4) (GLUT4)

Target
GLUT4
Molecular classification
Transporter, Solute carrier family, Facilitated glucose transporter
01

Overview

Solute carrier family 2, facilitated glucose transporter member 4 (GLUT4) is the primary insulin-regulated glucose transporter found in skeletal muscle, cardiac muscle, and adipose tissue. It plays a fundamental role in maintaining whole-body glucose homeostasis by facilitating the uptake of glucose from the bloodstream into these peripheral tissues. In the basal state, GLUT4 is predominantly sequestered within specialized intracellular vesicles known as GLUT4 storage vesicles (GSVs). Upon insulin stimulation or muscle contraction, these vesicles translocate to and fuse with the plasma membrane, thereby increasing the cell's capacity for glucose uptake. Dysregulation of GLUT4 expression or its trafficking mechanism is a hallmark of insulin resistance and is central to the pathophysiology of Type 2 Diabetes and metabolic syndrome. While many existing antidiabetic medications like metformin and thiazolidinediones indirectly enhance GLUT4 activity or expression, the transporter itself is a key focus for the development of novel insulin-sensitizing agents. Additionally, research into GLUT4 inhibitors has explored their potential in oncology, as some cancer cells upregulate glucose transporters to meet high metabolic demands.

Other names
SLC2A4Glucose transporter type 4Insulin-responsive glucose transporterGtr4Glut-4Solute carrier family 2 member 4
02

Mechanism of action

Facilitated diffusion of glucose across the plasma membrane; insulin-stimulated translocation from intracellular storage vesicles to the cell surface.

03

Biological functions

Glucose transportInsulin signalingGlucose homeostasisD-glucose transmembrane transportCellular response to insulin stimulus
04

Disease associations

Type 2 DiabetesInsulin resistanceObesityMetabolic syndromeCardiovascular disease
05

Safety considerations

HypoglycemiaTissue-specific delivery challengesPotential off-target inhibition of other GLUT isoforms (e.g., GLUT1, GLUT3)
06

Interacting drugs

Insulin

9 more in the full profile.

07

Biomarkers

HbA1cFasting plasma glucoseGLUT4 expression levels in muscle or adipose tissueHomeostatic Model Assessment for Insulin Resistance (HOMA-IR)

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