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9728530
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The human gene SLC5A2 encodes sodium/glucose cotransporter 2...
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[LiteratureReference:9728522] The effects of sodium-glucose cotransporter 2 inhibitors on left ventricular function: current evidence and future directions
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[LiteratureReference:9728525] Dapagliflozin treatment in patients with different stages of type 2 diabetes mellitus: effects on glycaemic control and body weight
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[LiteratureReference:9728169] Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models
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[LiteratureReference:9728167] Empagliflozin, a novel selective sodium glucose cotransporter-2 (SGLT-2) inhibitor: characterisation and comparison with other SGLT-2 inhibitors
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[LiteratureReference:9728233] LX4211, a dual SGLT1/SGLT2 inhibitor, improved glycemic control in patients with type 2 diabetes in a randomized, placebo-controlled trial
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[LiteratureReference:9728121] Discovery of tofogliflozin, a novel C-arylglucoside with an O-spiroketal ring system, as a highly selective sodium glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes
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[LiteratureReference:9728184] Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors
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[LiteratureReference:9728148] Pharmacological profile of ipragliflozin (ASP1941), a novel selective SGLT2 inhibitor, in vitro and in vivo
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[LiteratureReference:9728515] Sodium glucose cotransporter-2 inhibitor was associated with an improvement in left ventricular systolic function in patients with type 2 diabetes mellitus with impaired left ventricular systolic function
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[LiteratureReference:9728531] SGLT-2 Inhibitors: A New Mechanism for Glycemic Control
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The human gene SLC5A2 encodes sodium/glucose cotransporter 2 (SGLT2). At the plasma membrane, it co-transports extracellular sodium ions and glucose into the cytosol. SLC5A2 is located in the early proximal tubule, and absorbs 80-90% of the glucose filtered by the kidney glomerulus. The majority of the remaining glucose is absorbed by sodium/glucose cotransporter 1 (SLC5A1, SGLT1) in more distal sections of the proximal tubule.
SLC5A2 inhibitors, collectively called 'gliflozins', inhibit SLC5A2 in proximal tubules of renal glomeruli, causing inhibition of glucose reabsorption, resulting in glycosuria in diabetics which in turn lowers plasma glucose levels (Katsuno et al. 2007, Pajor et al. 2008, Hummel et al. 2012, review - Chao 2014). Therefore, gliflozins can be used in the treatment of type II diabetes mellitus (T2DM); dapagliflozin (Zhang et al. 2010), ertugliflozin (Mascitti et al. 2011), canagliflozin (Liang et al. 2012), sotagliflozin (Zambrowicz et al. 2012), tofogliflozin (Grempler et al. 2012), tofogliflozin (Ohtake et al. 2012), and ipragliflozin (Imamura et al. 2012). Dapagliflozin was the first gliflozin approved for the treatment of T2DM. They are most often used as second- or third-line treatment of T2DM because other anti-diabetics have better safety records and are less expensive than gliflozins. They are good options for diabetics who fail with metformin monotherapy or in combination therapy, for example metformin plus gliflozin. The most common adverse effect of gliflozin treatment is genital infections.
Gliflozins have shown protective effects in heart failure. This is primarily due to haemodynamic effects, where gliflozins potently reduce intravascular volume through osmotic diuresis and natriuresis. Consequently, this may lead to a reduction in cardiac workload and improving left ventricular function (Lan et al. 2019, Chan et al. 2020).