ArticleNature communications2022
Structural mechanism of SGLT1 inhibitors.
Article in Nature communications, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 42 citations in OpenAlex.
- Article
- Structural basis for multivitamin recognition and transport by human SMVT.Nature communications · 2026Article
- Revisiting vSGLT: Non-Radioactive Characterization of the Vibrio NaInternational journal of molecular sciences · 2026Article
- Inhibitory Effect ofInternational journal of molecular sciences · 2025Article
- Mechanism of substrate recognition and release of human SGLT2.Nature communications · 2025Article
- SGLT2 Inhibitors: From Molecular Mechanisms to Clinical Outcomes in Cardiology and Diabetology.Molecules (Basel, Switzerland) · 2025Review
- Pathogenesis and Therapeutic Perspectives of Tubular Injury in Diabetic Kidney Disease: An Update.Biomedicines · 2025Review
- Molecular mechanisms and computational insights into human SGLTs: advancing toward selective SGLT1 inhibition.Frontiers in molecular biosciences · 2025Review
- ATP-Binding Cassette and Solute Carrier Transporters: Understanding Their Mechanisms and Drug Modulation Through Structural and Modeling Approaches.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Correction of preferred orientation-induced distortion in cryo-electron microscopy maps.Science advances · 2024Article
- Sodium-glucose cotransporter 1 promotes the biofunctions of perivascular preadipocytes mediated by Akt/mTOR/p70S6K signaling pathway.American journal of physiology. Cell physiology · 2024Article
- Membrane transporters in drug development and as determinants of precision medicine.Nature reviews. Drug discovery · 2024Review
- Transport mechanism of presynaptic high-affinity choline uptake by CHT1.Nature structural & molecular biology · 2024Article
- Transport and inhibition mechanism of the human SGLT2-MAP17 glucose transporter.Nature structural & molecular biology · 2024Article
- SGLT5 is the renal transporter for 1,5-anhydroglucitol, a major player in two rare forms of neutropenia.Cellular and molecular life sciences : CMLS · 2023Article
- Insights on the Hypoglycemic Potential ofInternational journal of molecular sciences · 2023Article
- Structures of human SGLT in the occluded state reveal conformational changes during sugar transport.Nature communications · 2023Article
- HA-tag CD63 is a novel conditional transgenic approach to track extracellular vesicle interactions with sperm and their transfer at conception.Scientific reports · 2023Article
- Substrate Recognition Properties from an Intermediate Structural State of the UreA Transporter.International journal of molecular sciences · 2022Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Sodium glucose co-transporters (SGLT) harness the electrochemical gradient of sodium to drive the uphill transport of glucose across the plasma membrane. Human SGLT1 (hSGLT1) plays a key role in sugar uptake from food and its inhibitors show promise in the treatment of several diseases. However, the inhibition mechanism for hSGLT1 remains elusive. Here, we present the cryo-EM structure of the hSGLT1-MAP17 hetero-dimeric complex in the presence of the high-affinity inhibitor LX2761. LX2761 locks the transporter in an outward-open conformation by wedging inside the substrate-binding site and the extracellular vestibule of hSGLT1. LX2761 blocks the putative water permeation pathway of hSGLT1. The structure also uncovers the conformational changes of hSGLT1 during transitions from outward-open to inward-open states.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.