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TitleStructural basis of inhibition of the human SGLT2-MAP17 glucose transporter.
Journal, issue, pagesNature, Vol. 601, Issue 7892, Page 280-284, Year 2022
Publish dateDec 8, 2021
AuthorsYange Niu / Rui Liu / Chengcheng Guan / Yuan Zhang / Zhixing Chen / Stefan Hoerer / Herbert Nar / Lei Chen /
PubMed AbstractHuman sodium-glucose cotransporter 2 (hSGLT2) mediates the reabsorption of the majority of filtrated glucose in the kidney. Pharmacological inhibition of hSGLT2 by oral small-molecule inhibitors, ...Human sodium-glucose cotransporter 2 (hSGLT2) mediates the reabsorption of the majority of filtrated glucose in the kidney. Pharmacological inhibition of hSGLT2 by oral small-molecule inhibitors, such as empagliflozin, leads to enhanced excretion of glucose and is widely used in the clinic to manage blood glucose levels for the treatment of type 2 diabetes. Here we determined the cryogenic electron microscopy structure of the hSGLT2-MAP17 complex in the empagliflozin-bound state to an overall resolution of 2.95 Å. Our structure shows eukaryotic SGLT-specific structural features. MAP17 interacts with transmembrane helix 13 of hSGLT2. Empagliflozin occupies both the sugar-substrate-binding site and the external vestibule to lock hSGLT2 in an outward-open conformation, thus inhibiting the transport cycle. Our work provides a framework for understanding the mechanism of SLC5A family glucose transporters and also develops a foundation for the future rational design and optimization of new inhibitors targeting these transporters.
External linksNature / PubMed:34880493
MethodsEM (single particle)
Resolution2.95 Å
Structure data

31558

7vsi

EMDB-31558, PDB-7vsi:
Structure of human SGLT2-MAP17 complex bound with empagliflozin
Method: EM (single particle) / Resolution: 2.95 Å

Chemicals

ChemComp-PLM:
PALMITIC ACID

ChemComp-7R3:
(2S,3R,4R,5S,6R)-2-[4-chloranyl-3-[[4-[(3S)-oxolan-3-yl]oxyphenyl]methyl]phenyl]-6-(hydroxymethyl)oxane-3,4,5-triol / medication*YM

Source
  • homo sapiens (human)
KeywordsTRANSPORT PROTEIN / glucose transporter / SGLT2 / SGLT

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