Drug intelligence / Profile preview

G3iA

Development stage
Preclinical
Modality
Small Molecules
01

Overview

G3iA is a selective small molecule inhibitor of glucose transporter 3 (GLUT3), a protein frequently upregulated in aggressive cancers such as triple-negative breast cancer (TNBC). By selectively blocking GLUT3, G3iA reduces glucose uptake, glycolysis, and ATP production in cancer cells. This metabolic stress triggers the activation of the energy-sensing AMP-activated protein kinase (AMPK) and the cAMP-Protein Kinase A (PKA) signaling pathways. These pathways collectively suppress myosin activity and impair actin polymerization—the latter through the regulation of vasodilator-stimulated phosphoprotein (VASP) via the YAP-TEAD axis. Preclinical studies indicate that G3iA treatment reduces cancer cell stiffness, contractility, and motility, ultimately diminishing the metastatic potential of TNBC cells in vivo.

02

Targets

G3BP1 (Ras GTPase-activating protein-binding protein 1)SLC2A3 (Glucose transporter type 3)G3BP2 (G3BP stress granule assembly factor 2)

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