ArticleThe Journal of biological chemistry2015
In Silico Modeling-based Identification of Glucose Transporter 4 (GLUT4)-selective Inhibitors for Cancer Therapy.
Article in The Journal of biological chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers.
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Who cites it
35 citing papers in PubMed, 69 citations in OpenAlex.
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- Envisioning Glucose Transporters (GLUTs and SGLTs) as Novel Intervention against Cancer: Drug Discovery Perspective and Targeting Approach.Current drug targets · 2025Review
- Discovering Potential in Non-Cancer Medications: A Promising Breakthrough for Multiple Myeloma Patients.Cancers · 2024Review
- Targeting the Warburg effect: A revisited perspective from molecular mechanisms to traditional and innovative therapeutic strategies in cancer.Acta pharmaceutica Sinica. B · 2024Review
- Harnessing glucose metabolism with nanomedicine for cancer treatment.Theranostics · 2024Review
- Interactions between HIV protease inhibitor ritonavir and human DNA repair enzyme ALKBH2: a molecular dynamics simulation study.Molecular diversity · 2023Article
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- ID-Checker Technology for the Highly Selective Macroscale Delivery of Anticancer Agents to the Cancer Cells.Journal of medicinal chemistry · 2022Article
- The Route of the Malignant Plasma Cell in Its Survival Niche: Exploring "Multiple Myelomas".Cancers · 2022Review
- GLUT4 gene rs5418 polymorphism is associated with increased coronary heart disease risk in a Uygur Chinese population.BMC cardiovascular disorders · 2022Article
- GLUT3 inhibitor discovery through in silico ligand screening and in vivo validation in eukaryotic expression systems.Scientific reports · 2022Article
- Drug Discovery of Plausible Lead Natural Compounds That Target the Insulin Signaling Pathway: Bioinformatics Approaches.Evidence-based complementary and alternative medicine : eCAM · 2022Review
- Glucose Transporters as a Target for Anticancer Therapy.Cancers · 2021Review
- Insulin gene enhancer protein 1 mediates glycolysis and tumorigenesis of gastric cancer through regulating glucose transporter 4.Cancer communications (London, England) · 2021Article
- Subpopulation targeting of pyruvate dehydrogenase and GLUT1 decouples metabolic heterogeneity during collective cancer cell invasion.Nature communications · 2020Article
- Electron transport chain activity is a predictor and target for venetoclax sensitivity in multiple myeloma.Nature communications · 2020Article
- MARCKSL1 promotes the proliferation, migration and invasion of lung adenocarcinoma cells.Oncology letters · 2020Article
- A high-throughput screen identifies that CDK7 activates glucose consumption in lung cancer cells.Nature communications · 2019Article
- Discovery of novel Mnk inhibitors using mutation-based induced-fit virtual high-throughput screening.Chemical biology & drug design · 2019Article
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Authors and funding
11 authors at 4 institutions in 1 country.
Funding
Abstract
Tumor cells rely on elevated glucose consumption and metabolism for survival and proliferation. Glucose transporters mediating glucose entry are key proximal rate-limiting checkpoints. Unlike GLUT1 that is highly expressed in cancer and more ubiquitously expressed in normal tissues, GLUT4 exhibits more limited normal expression profiles. We have previously determined that insulin-responsive GLUT4 is constitutively localized on the plasma membrane of myeloma cells. Consequently, suppression of GLUT4 or inhibition of glucose transport with the HIV protease inhibitor ritonavir elicited growth arrest and/or apoptosis in multiple myeloma. GLUT4 inhibition also caused sensitization to metformin in multiple myeloma and chronic lymphocytic leukemia and a number of solid tumors suggesting the broader therapeutic utility of targeting GLUT4. This study sought to identify selective inhibitors of GLUT4 to develop a more potent cancer chemotherapeutic with fewer potential off-target effects. Recently, the crystal structure of GLUT1 in an inward open conformation was reported. Although this is an important achievement, a full understanding of the structural biology of facilitative glucose transport remains elusive. To date, there is no three-dimensional structure for GLUT4. We have generated a homology model for GLUT4 that we utilized to screen for drug-like compounds from a library of 18 million compounds. Despite 68% homology between GLUT1 and GLUT4, our virtual screen identified two potent compounds that were shown to target GLUT4 preferentially over GLUT1 and block glucose transport. Our results strongly bolster the utility of developing GLUT4-selective inhibitors as anti-cancer therapeutics.
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