ArticleCancer & metabolism2021
A small-molecule pan-class I glucose transporter inhibitor reduces cancer cell proliferation in vitro and tumor growth in vivo by targeting glucose-based metabolism.
Article in Cancer & metabolism, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers.
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Who cites it
33 citing papers in PubMed, 56 citations in OpenAlex.
- Targeting GLUTs in Cancer: Mechanisms, Combination Strategies, and Translational Challenges.Current medical science · 2026Review
- Two-Step Loss of GLUTs in the High-Metabolism Passerines.Integrative zoology · 2026Article
- Carbohydrates metabolic reprogramming and tumor microenvironment in pancreatic cancer: targeting pathways.Molecular biology reports · 2026Review
- Learning Shapes the Energy Cost of Neural Tasks.bioRxiv : the preprint server for biology · 2026Article
- Development of Type II Glucose Transporter Inhibitors: Phloretin as a GLUT-2 Screening Template fromBiomedicines · 2026Article
- Review
- Targeting Metabolic Vulnerabilities in Glioblastoma: a Framework for Multi-node Combination Therapy.Current oncology reports · 2026Review
- The regulatory roles and therapeutic strategies of the solute carrier transporters in cancer metabolism.NPJ precision oncology · 2026Review
- A novel pan class-I glucose transporter inhibitor DRB18 exhibits synergistic effects with paclitaxelbioRxiv : the preprint server for biology · 2025Article
- Profiling the effect of low frequency mechanical vibration on the metabolic and oxidative stress responses of A431 carcinoma.FEBS open bio · 2025Article
- Combination treatment with Phloretin enhances the anti-tumor efficacy of radiotherapy in lung cancer models.Discover oncology · 2025Article
- GLUT1 inhibition by BAY-876 induces metabolic changes and cell death in human colorectal cancer cells.BMC cancer · 2025Article
- Role of disulfide death in cancer (Review).Oncology letters · 2025Review
- Iron Regulates Cellular Proliferation by Enhancing the Expression of Glucose Transporter GLUT3 in the Liver.Cells · 2024Article
- GLUT1 promotes cell proliferation via binds and stabilizes phosphorylated EGFR in lung adenocarcinoma.Cell communication and signaling : CCS · 2024Article
- Unravelling the Triad of Lung Cancer, Drug Resistance, and Metabolic Pathways.Diseases (Basel, Switzerland) · 2024Review
- Disulfidptosis, A Novel Cell Death Pathway: Molecular Landscape and Therapeutic Implications.Aging and disease · 2024Review
- Article
- Connection between nutrition and oncology in dogs and cats: perspectives, evidence, and implications-a comprehensive review.Frontiers in veterinary science · 2024Review
- Diverse temporal and spatial mechanisms work, partially through Stanniocalcin-1, V-ATPase and senescence, to activate the extracellular ATP-mediated drug resistance in human cancer cells.Frontiers in oncology · 2024Article
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
Abstract
backgroundCancer cells drastically increase the uptake of glucose and glucose metabolism by overexpressing class I glucose transporters (GLUT1-4) to meet their energy and biomass synthesis needs and are very sensitive and vulnerable to glucose deprivation. Although targeting glucose uptake via GLUTs has been an attractive anticancer strategy, the relative anticancer efficacy of multi-GLUT targeting or single GLUT targeting is unclear. Here, we report DRB18, a synthetic small molecule, is a potent anticancer compound whose pan-class I GLUT inhibition is superior to single GLUT targeting.
methodsGlucose uptake and MTT/resazurin assays were used to measure DRB18's inhibitory activities of glucose transport and cell viability/proliferation in human lung cancer and other cancer cell lines. Four HEK293 cell lines expressing GLUT1-4 individually were used to determine the IC
resultsDRB18 reduced glucose uptake mediated via each of GLUT1-4 with different IC
conclusionsDRB18 is a potent pan-class I GLUT inhibitor in vitro and in vivo in cancer cells. Mechanistically, it is likely to bind the outward open conformation of GLUT1-4, reducing tumor growth through inhibiting GLUT1-4-mediated glucose transport and metabolisms. Pan-class I GLUT inhibition is a better strategy than single GLUT targeting for inhibiting tumor growth.
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Registered trials
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.