Sodium/glucose cotransporter
From Proteopedia
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- | <StructureSection load=' | + | <StructureSection load='8hez' size='340' side='right' caption='Human glycosylated SGLT2 (cyan) complex with PDZK1-interacting protein (green), drug dapagliflozin and Na+ ion (PDB code [[8hez]])' scene='10/1042600/Cv/1'> |
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== Function == | == 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<ref>PMID:26125647</ref>. | + | '''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<ref>PMID:26125647</ref>. |
== Disease == | == Disease == | ||
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== Relevance == | == Relevance == | ||
- | SGLT2 inhibitors aid in hypertension, acute cardiac failure, bradycardia, acute pulmonary oedema, asthma, bronchitis and COPD<ref>PMID:36819350</ref> | + | SGLT2 inhibitors aid in hypertension, acute cardiac failure, bradycardia, acute pulmonary oedema, asthma, bronchitis and COPD<ref>PMID:36819350</ref>. |
== Structural highlights == | == Structural highlights == | ||
- | + | The drug Dapagliflozin contains a <scene name='10/1042600/Cv/5'>glucose moiety which stacks against residue Y290</scene> of SGLT2. The <scene name='10/1042600/Cv/6'>glucose moiety forms multiple H-bonds</scene> to SGLT2<ref>PMID:38057552</ref>. Water molecule is shown as red sphere. | |
+ | See also: | ||
+ | *[[Canagliflozin]] | ||
+ | *[[Dapagliflozin]] | ||
+ | *[[Empagliflozin]] | ||
==3D structures of sodium/glucose cotransporter== | ==3D structures of sodium/glucose cotransporter== | ||
- | + | [[Sodium/glucose cotransporter 3D structures]] | |
</StructureSection> | </StructureSection> |
Current revision
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References
- ↑ 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