Sodium/glucose cotransporter

Function

Sodium/glucose cotransporter (SGLT) is responsible for glucose absorption across membranes. SGLT1 and SGLT2 which are expressed in different tissues, have similar active sites but differ in their non-active site structures. SGLT1 is responsible of glucose absorption in the small intestine and SGLT2 in kidney^[1].

Disease

Mutations in SGLT1 cause malabsorption of glucose and galactose^[2].

Relevance

SGLT2 inhibitors aid in hypertension, acute cardiac failure, bradycardia, acute pulmonary oedema, asthma, bronchitis and COPD^[3].

Structural highlights

The drug Dapagliflozin contains a of SGLT2. The to SGLT2^[4]. Water molecule is shown as red sphere.

3D structures of sodium/glucose cotransporter

Sodium/glucose cotransporter 3D structures

Human glycosylated SGLT2 (cyan) complex with PDZK1-interacting protein (green), drug dapagliflozin and Na+ ion (PDB code 8hez)

Drag the structure with the mouse to rotate

ReferencesReferences

↑ Poulsen SB, Fenton RA, Rieg T. Sodium-glucose cotransport. Curr Opin Nephrol Hypertens. 2015 Sep;24(5):463-9. PMID:26125647 doi:10.1097/MNH.0000000000000152
↑ Dominguez Rieg JA, Rieg T. What does sodium-glucose co-transporter 1 inhibition add: Prospects for dual inhibition. Diabetes Obes Metab. 2019 Apr;21 Suppl 2(Suppl 2):43-52. PMID:31081587 doi:10.1111/dom.13630
↑ Jasleen B, Vishal GK, Sameera M, Fahad M, Brendan O, Deion S, Pemminati S. Sodium-Glucose Cotransporter 2 (SGLT2) Inhibitors: Benefits Versus Risk. Cureus. 2023 Jan 18;15(1):e33939. PMID:36819350 doi:10.7759/cureus.33939
↑ Hiraizumi M, Akashi T, Murasaki K, Kishida H, Kumanomidou T, Torimoto N, Nureki O, Miyaguchi I. Transport and inhibition mechanism of the human SGLT2-MAP17 glucose transporter. Nat Struct Mol Biol. 2024 Jan;31(1):159-169. PMID:38057552 doi:10.1038/s41594-023-01134-0

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Michal Harel, Jaime Prilusky, Alexander Berchansky

[1] Poulsen SB, Fenton RA, Rieg T. Sodium-glucose cotransport. Curr Opin Nephrol Hypertens. 2015 Sep;24(5):463-9. PMID:26125647 doi:10.1097/MNH.0000000000000152

[2] Dominguez Rieg JA, Rieg T. What does sodium-glucose co-transporter 1 inhibition add: Prospects for dual inhibition. Diabetes Obes Metab. 2019 Apr;21 Suppl 2(Suppl 2):43-52. PMID:31081587 doi:10.1111/dom.13630

[3] Jasleen B, Vishal GK, Sameera M, Fahad M, Brendan O, Deion S, Pemminati S. Sodium-Glucose Cotransporter 2 (SGLT2) Inhibitors: Benefits Versus Risk. Cureus. 2023 Jan 18;15(1):e33939. PMID:36819350 doi:10.7759/cureus.33939

[4] Hiraizumi M, Akashi T, Murasaki K, Kishida H, Kumanomidou T, Torimoto N, Nureki O, Miyaguchi I. Transport and inhibition mechanism of the human SGLT2-MAP17 glucose transporter. Nat Struct Mol Biol. 2024 Jan;31(1):159-169. PMID:38057552 doi:10.1038/s41594-023-01134-0

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