ArticleMolecules (Basel, Switzerland)2019
Conformational Studies of Glucose Transporter 1 (GLUT1) as an Anticancer Drug Target.
Article in Molecules (Basel, Switzerland), 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed.
- A Brønsted-based deep eutectic solvent as a green catalyst for the sustainable one-pot synthesis of 1,2,4,5-tetrasubstituted imidazole derivatives:RSC advances · 2026Article
- Direct targeting of GLUT1 in cancer: A decade of inhibitor discovery and medicinal chemistry insights.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026Review
- Glyco Ionic Liquids as Novel Nanoparticle Coatings to Enhance Triple-Negative Breast Cancer Drug Delivery.Advanced healthcare materials · 2025Article
- Metabolism, a Blossoming Target for Small-Molecule Anticancer Drugs.Molecules (Basel, Switzerland) · 2025Review
- The Impact of Metabolic Rewiring in Glioblastoma: The Immune Landscape and Therapeutic Strategies.International journal of molecular sciences · 2025Review
- Overcoming Challenges in Small-Molecule Drug Bioavailability: A Review of Key Factors and Approaches.International journal of molecular sciences · 2024Review
- Advances in active targeting of ligand-directed polymeric nanomicellesRSC advances · 2024Review
- Interaction of amisulpride with GLUT1 at the blood-brain barrier. Relevance to Alzheimer's disease.PloS one · 2023Article
- Discovery of New Glucose Uptake Inhibitors as Potential Anticancer Agents by Non-Radioactive Cell-Based Assays.Molecules (Basel, Switzerland) · 2022Article
- Advances in Fungal Phenaloenones-Natural Metabolites with Great Promise: Biosynthesis, Bioactivities, and an In Silico Evaluation of Their Potential as Human Glucose Transporter 1 Inhibitors.Molecules (Basel, Switzerland) · 2022Review
- A Mini-Review of Flavone Isomers Apigenin and Genistein in Prostate Cancer Treatment.Frontiers in pharmacology · 2022Review
- An appraisal of the current status of inhibition of glucose transporters as an emerging antineoplastic approach: Promising potential of new pan-GLUT inhibitors.Frontiers in pharmacology · 2022Review
- β-Boswellic Acid Suppresses Breast Precancerous LesionsFrontiers in oncology · 2022Article
- Ligand-based design of GLUT inhibitors as potential antitumor agents.Bioorganic & medicinal chemistry · 2020Article
- Targeted Prodrug-Based Self-Assembled Nanoparticles for Cancer Therapy.International journal of nanomedicine · 2020Article
- Molecular Modeling Studies on the Binding Mode of the PD-1/PD-L1 Complex Inhibitors.International journal of molecular sciences · 2019Article
Corrections and comments
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Authors and funding
4 authors.
Funding
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Abstract
Glucose transporter 1 (GLUT1) is a facilitative glucose transporter overexpressed in various types of tumors; thus, it has been considered as an important target for cancer therapy. GLUT1 works through conformational switching from an outward-open (OOP) to an inward-open (IOP) conformation passing through an occluded conformation. It is critical to determine which conformation is preferred by bound ligands because the success of structure-based drug design depends on the appropriate starting conformation of the target protein. To find out the most favorable GLUT 1 conformation for ligand binding, we ran systemic molecular docking studies for different conformations of GLUT1 using known GLUT1 inhibitors. Our data revealed that the IOP is the preferred conformation and that residues Phe291, Phe379, Glu380, Trp388, and Trp412 may play critical roles in ligand binding to GLUT1. Our data suggests that conformational differences in these five amino acids in the different conformers of GLUT1 may be used to design ligands that inhibit GLUT1.
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