Target intelligence / Profile preview

Sodium-dependent glucose co-transporter 2 (SGLT2)

Target
SGLT2
Molecular classification
Transporter, Sodium–solute symporter family, Membrane protein
01

Overview

Sodium-dependent glucose co-transporter 2 (SGLT2), also known as SLC5A2, is a membrane protein highly expressed in the renal proximal convoluted tubules, where it mediates active reabsorption of filtered glucose from the glomerular filtrate back into the bloodstream using the sodium electrochemical gradient[2][4][5]. SGLT2 has a single sodium:glucose stoichiometry and is the primary renal transporter responsible for the majority of glucose reuptake in humans. Pharmacological inhibition of SGLT2, by drugs termed "gliflozins," lowers blood glucose by increasing its urinary excretion and is used therapeutically in the treatment of type 2 diabetes, with additional cardiovascular and renal protective effects[2][5]. SGLT2 inhibition is associated with side effects related to increased urinary glucose, such as infections and rare metabolic complications[4].

Other names
Sodium–glucose cotransporter 2Sodium-glucose transport protein 2SGLT2SLC5A2 (solute carrier family 5 member 2)
02

Mechanism of action

SGLT2 inhibitors block glucose reabsorption in the renal proximal tubule, increasing urinary glucose excretion and lowering blood glucose[2][4][5]. - Some inhibitors also inhibit SGLT1 (dual SGLT1/2 inhibitors like sotagliflozin)[5].

03

Biological functions

Glucose reabsorption in the kidneyRegulation of systemic glucose homeostasisActive glucose transport (coupled to sodium gradient)
04

Disease associations

Diabetes mellitusCardiovascular diseaseKidney diseaseObesityAtherosclerosisNeurodegenerative disease (Alzheimer's disease)
05

Safety considerations

Urinary tract infectionsGenital mycotic infectionsEuglycemic diabetic ketoacidosisVolume depletion/hypotensionRenal function impairmentRisk of lower limb amputation (noted primarily with canagliflozin)
06

Interacting drugs

Canagliflozin

8 more in the full profile.

07

Biomarkers

Urinary glucose (for efficacy monitoring)Blood glucose (for efficacy monitoring)Estimated glomerular filtration rate (safety)Body weight (for some metabolic benefits)

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