Target intelligence / Profile preview

Solute carrier family 2 members (Class I and III glucose transporters) (GLUTs (Class I/III))

Target
GLUTs (Class I/III)
Molecular classification
Transporter, Solute carrier family
01

Overview

The 'Other class I/III GLUTs' refers to a broad group of proteins within the Solute Carrier Family 2 (SLC2A), specifically encompassing the Class I (GLUT1-4) and Class III (GLUT6, 8, 10, 12, and 13) facilitated glucose transporters (Mueckler & Thorens, 2013). These transporters are essential for the movement of glucose, fructose, and other hexoses across cellular membranes, following a concentration gradient. Class I members like GLUT1 and GLUT3 are critical for basal glucose uptake in the brain and erythrocytes, while GLUT4 is the primary insulin-responsive transporter in muscle and adipose tissue (Thorens & Mueckler, 2010). Class III members are less characterized but are implicated in metabolic regulation and are often overexpressed in various malignancies to support the high glycolytic demands of cancer cells (Szablewski, 2013). Pharmacologically, these transporters are targeted by broad-spectrum inhibitors like Phloretin and Cytochalasin B, as well as certain HIV protease inhibitors like Ritonavir, which can cause off-target metabolic side effects (Hruz, 2011). Because of their diverse tissue distribution and vital roles in systemic glucose homeostasis, non-selective modulation of these transporters poses significant safety risks, including hypoglycemia and insulin resistance.

Other names
Other class I/III GLUTsSLC2 familyGlucose transportersFacilitated glucose transportersClass I GLUTsClass III GLUTs
02

Mechanism of action

Inhibition of facilitated glucose transport across the plasma membrane

03

Biological functions

Glucose transportHexose transportCarbohydrate metabolismHomeostasis
04

Disease associations

CancerDiabetes mellitusGLUT1 deficiency syndromeFanconi-Bickel syndromeArterial tortuosity syndromeObesity
05

Safety considerations

HypoglycemiaNeuroglycopeniaInsulin resistanceMalabsorptionBlood-brain barrier transport impairment
06

Interacting drugs

Phloretin

6 more in the full profile.

07

Biomarkers

18F-FDG uptake (PET imaging)Blood glucose levelsGLUT expression levels (IHC)Insulin sensitivity indices

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