Structural basis of inhibition of the human SGLT2–MAP17
WEBDec 8, 2021 · Using cryogenic electron microscopy, the structure of the human SGLT2–MAP17 complex captured in the empagliflozin-bound state reveals the inhibitory mechanism of these anti-diabetic drugs.
Structures of human SGLT in the occluded state reveal …
WEBMay 22, 2023 · Here the authors provided the cryo-EM structures of human SGLT1 and SGLT2 in the substrate-bound occluded state, uncovering the conformational changes of SGLT during sugar transport.
Structure and mechanism of the SGLT family of glucose …
WEBDec 8, 2021 · Human SGLT family transporters can be phylogenetically grouped into two main branches: one that transports sugars and myo-inositol (for example, SGLT1) and one that translocates key metabolites ...
Structures reveal how SGLT inhibitors work - Cell Press
WEBJun 18, 2024 · SGLT1 and SGLT2 are the most extensively studied transporters of the SGLTs. SGLT1 is primarily located in the small intestine, where it absorbs dietary glucose and galactose, and in the S3 segment of the renal proximal tubule, where it mediates glucose reabsorption [1].
Structure and mechanism of the SGLT family of glucose transporters
WEBHuman SGLT family transporters can be phylogenetically grouped into two main branches: one that transports sugars and myo-inositol (e.g., SGLT1) and one that translocates key metabolites such as monocarboxylates, iodide, and biotin (e.g., SMCT1).
SGLT2 Inhibitors: Physiology and Pharmacology - PMC
WEBDec 12, 2021 · The SGLT2 inhibitors bind to SGLT2 in the luminal membrane of the early (S1 and S2) segments of the nephron, where they may block up to 60% of glucose reabsorption. Glucose that escapes reabsorption in S1 and S2 segments is normally salvaged by SGLT1 in the late proximal tubule (S3).
Structural basis of inhibition of the human SGLT2-MAP17 glucose ...
WEBOur 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.
RCSB PDB - 7VSI: Structure of human SGLT2-MAP17 complex …
WEBDec 15, 2021 · 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.
An exhaustive perspective on structural insights of SGLT2
WEBOct 15, 2020 · Most of the inhibitors that target SGLT2 contain three basic moieties: glucose, two benzene rings (one is connected with glucose and the other with methylene), and the methylene bridge which are similar to dapagliflozin.
Transport and inhibition mechanism of the human SGLT2–MAP17 …
WEBDec 6, 2023 · SGLT2 is located in the S1 and S2 segments of the proximal tubule and absorbs 90% of the filtered glucose; SGLT1, which has higher glucose affinity, is located in the S3 segment of the...
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