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

The Solute carrier family 2 (SLC2A), or glucose transporter (GLUT) family, comprises 14 protein members that facilitate the passive transport of glucose and other hexoses across plasma membranes [1, 2]. Glucose transporter 3 (GLUT3) is notable for its high affinity and high turnover rate, primarily serving as the main glucose transporter in neurons to meet the brain's high metabolic demands [1, 5]. Other isoforms, such as GLUT1, provide basal glucose uptake in most tissues, while GLUT4 is uniquely regulated by insulin in muscle and adipose tissues [2]. In many cancers, GLUT1 and GLUT3 are significantly upregulated to facilitate the increased glucose consumption required for rapid tumor growth, making them attractive targets for anti-cancer therapies [3, 6]. Pharmacological inhibition of these transporters, using small molecules like WZB117 or natural products like phloretin, aims to starve cancer cells of their primary energy source [4, 6]. However, the high sequence homology between isoforms and their critical roles in the brain and red blood cells pose significant challenges for achieving therapeutic selectivity and safety [2, 5]. Citations: [1] UniProt P11169; [2] PMID: 23506862; [3] PMID: 27107434; [4] PMID: 22306015; [5] PMID: 18383304; [6] PMID: 26778147.

Other names

SLC2A familyGlucose transporter familyFacilitative glucose transporterGlucose transporter 3 (GLUT3)Solute carrier family 2 member 3 (SLC2A3)

Inhibition of facilitated diffusion by binding to the endofacial or exofacial sites of the transporter, thereby preventing the conformational change required for glucose translocation across the plasma membrane [2, 4].