Target intelligence / Profile preview

Sodium-glucose cotransporter type 2 (SGLT2)

Target
SGLT2
Molecular classification
Transporter, Solute carrier family
01

Overview

Sodium-glucose cotransporter type 2 (SGLT2) is an integral membrane protein predominantly expressed in the early proximal tubule of the kidney, encoded by the SLC5A2 gene. It is responsible for reabsorbing approximately 90% of filtered glucose from the renal tubular lumen. SGLT2 is the molecular target for several FDA-approved antidiabetic drugs (SGLT2 inhibitors or gliflozins), which reduce blood glucose independently of insulin by blocking renal glucose reabsorption and promoting glycosuria. Beyond glycemic control in type 2 diabetes, SGLT2 inhibition provides cardio- and renoprotective effects, and is increasingly recognized for benefits in chronic kidney disease and heart failure. SGLT2 expression is also implicated as a diagnostic and therapeutic biomarker in certain cancers, notably early lung adenocarcinoma[1][2][3][4][5][7].

Other names
Sodium-glucose transport protein 2Solute carrier family 5 member 2SLC5A2SGLT-2
02

Mechanism of action

Inhibition of glucose reabsorption in the proximal renal tubule, Increased urinary glucose excretion, Lowering of blood glucose, Cardioprotective and renoprotective mechanisms (multifactorial)

03

Biological functions

Renal glucose reabsorptionGlucose homeostasisFluid and electrolyte balanceEnergy metabolism
04

Disease associations

Type 2 diabetes mellitusChronic kidney diseaseHeart failureCardiovascular diseaseCancer (lung adenocarcinoma, experimental/biomarker role)
05

Safety considerations

Genital mycotic infectionsUrinary tract infectionsEuglycemic diabetic ketoacidosisVolume depletion/hypotensionAcute kidney injuryIncreased risk of lower limb amputation (canagliflozin)Potential bone fracture risk
06

Interacting drugs

Canagliflozin

9 more in the full profile.

07

Biomarkers

Urinary glucose excretionHemoglobin A1cEstimated glomerular filtration rate (eGFR)Urinary albuminMe4FDG PET tracer uptake (experimental for some cancers)

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