ArticleAngewandte Chemie (International ed. in English)2019
Discovery of a Potent GLUT Inhibitor from a Library of Rapafucins by Using 3D Microarrays.
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Article in Angewandte Chemie (International ed. in English), 2019. 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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19citing papers in PubMed
1.9field-weighted citation impact, top 12% of its field
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Who cites it
19 citing papers in PubMed, 46 citations in OpenAlex.
- Solute Carrier transporters in tumor metabolism and immune modulation: implications for therapy.Journal of translational medicine · 2026Review
- Identification of Rapaglutin E as an Isoform-Specific Inhibitor of Glucose Transporter 1.ACS chemical biology · 2025Article
- Rapavir, a novel inhibitor of sodium taurocholate cotransporting polypeptide, potently blocks hepatitis B virus entry.Signal transduction and targeted therapy · 2025Article
- Progress of research on glucose transporter proteins in hepatocellular carcinoma.World journal of hepatology · 2025Review
- Development of an FKBP12-recruiting chemical-induced proximity DNA-encoded library and its application to discover an autophagy potentiator.Cell chemical biology · 2025Article
- Clinical application prospects of traditional Chinese medicine as adjuvant therapy for metabolic reprogramming in colorectal cancer.Frontiers in immunology · 2025Review
- The regulatory roles and clinical significance of glycolysis in tumor.Cancer communications (London, England) · 2024Review
- Enhanced Sampling Molecular Dynamics Simulations Reveal Transport Mechanism of Glycoconjugate Drugs through GLUT1.International journal of molecular sciences · 2024Article
- A rapid and simple non-radioactive assay for measuring uptake by solute carrier transporters.Frontiers in pharmacology · 2024Article
- Review
- Targeting Glucose Metabolism Enzymes in Cancer Treatment: Current and Emerging Strategies.Cancers · 2022Review
- TGF-β signaling in the tumor metabolic microenvironment and targeted therapies.Journal of hematology & oncology · 2022Review
- Article
- Picomolar FKBP inhibitors enabled by a single water-displacing methyl group in bicyclic [4.3.1] aza-amides.Chemical science · 2021Article
- Tyrosine Kinase Inhibitors Reduce Glucose Uptake by Binding to an Exofacial Site on hGLUT-1: Influence onClinical and translational science · 2021Article
- Metabolic Reprogramming and Renal Fibrosis.Frontiers in medicine · 2021Review
- Permuted 2,4-thiazolidinedione (TZD) analogs as GLUT inhibitors and their in-vitro evaluation in leukemic cells.European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences · 2020Article
- Glucometabolic Reprogramming in the Hepatocellular Carcinoma Microenvironment: Cause and Effect.Cancer management and research · 2020Review
- SilencingOncoTargets and therapy · 2020Article
Corrections and comments
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Authors and funding
20 authors at 6 institutions in 4 countries.
Zufeng GuoDepartment of Pharmacology and Molecular Sciences, The SJ Yan and HJ Mao Laboratory of Chemical Biology, Johns Hopkins University School of Medicine, Room 516, Hunterian Building, 725 N. Wolfe Street, Baltimore, MD, USA.
Zhiqiang ChengDepartment of Pharmacology and Molecular Sciences, The SJ Yan and HJ Mao Laboratory of Chemical Biology, Johns Hopkins University School of Medicine, Room 516, Hunterian Building, 725 N. Wolfe Street, Baltimore, MD, USA.
Jingxin WangDepartment of Pharmacology and Molecular Sciences, The SJ Yan and HJ Mao Laboratory of Chemical Biology, Johns Hopkins University School of Medicine, Room 516, Hunterian Building, 725 N. Wolfe Street, Baltimore, MD, USA.
Wukun LiuDepartment of Pharmacology and Molecular Sciences, The SJ Yan and HJ Mao Laboratory of Chemical Biology, Johns Hopkins University School of Medicine, Room 516, Hunterian Building, 725 N. Wolfe Street, Baltimore, MD, USA.
Hanjing PengDepartment of Pharmacology and Molecular Sciences, The SJ Yan and HJ Mao Laboratory of Chemical Biology, Johns Hopkins University School of Medicine, Room 516, Hunterian Building, 725 N. Wolfe Street, Baltimore, MD, USA.
Yuefan WangDepartment of Pharmacology and Molecular Sciences, The SJ Yan and HJ Mao Laboratory of Chemical Biology, Johns Hopkins University School of Medicine, Room 516, Hunterian Building, 725 N. Wolfe Street, Baltimore, MD, USA.
A V Subba RaoDepartment of Pharmacology and Molecular Sciences, The SJ Yan and HJ Mao Laboratory of Chemical Biology, Johns Hopkins University School of Medicine, Room 516, Hunterian Building, 725 N. Wolfe Street, Baltimore, MD, USA.
Ruo-Jing LiDepartment of Pharmacology and Molecular Sciences, The SJ Yan and HJ Mao Laboratory of Chemical Biology, Johns Hopkins University School of Medicine, Room 516, Hunterian Building, 725 N. Wolfe Street, Baltimore, MD, USA.
Xue YingDepartment of Pharmacology and Molecular Sciences, The SJ Yan and HJ Mao Laboratory of Chemical Biology, Johns Hopkins University School of Medicine, Room 516, Hunterian Building, 725 N. Wolfe Street, Baltimore, MD, USA.
Preethi KorangathDepartment of Oncology, Johns Hopkins University School of Medicine, USA.
Maria V LibertiDepartment of Pharmacology and Cancer Biology, Duke University School of Medicine, USA.
Yingjun LiDepartment of Pharmacology and Molecular Sciences, The SJ Yan and HJ Mao Laboratory of Chemical Biology, Johns Hopkins University School of Medicine, Room 516, Hunterian Building, 725 N. Wolfe Street, Baltimore, MD, USA.
Yongmei XieDepartment of Pharmacology and Molecular Sciences, The SJ Yan and HJ Mao Laboratory of Chemical Biology, Johns Hopkins University School of Medicine, Room 516, Hunterian Building, 725 N. Wolfe Street, Baltimore, MD, USA.
Sam Y HongDepartment of Pharmacology and Molecular Sciences, The SJ Yan and HJ Mao Laboratory of Chemical Biology, Johns Hopkins University School of Medicine, Room 516, Hunterian Building, 725 N. Wolfe Street, Baltimore, MD, USA.
Cordelia Schiene-FischerDepartment of Enzymology, Institute for Biochemistry and Biotechnology, Martin Luther University Halle-Wittenberg, Germany.
Gunter FischerDepartment of Enzymology, Institute for Biochemistry and Biotechnology, Martin Luther University Halle-Wittenberg, Germany.
Jason W LocasaleDepartment of Pharmacology and Cancer Biology, Duke University School of Medicine, USA.
Saraswati SukumarDepartment of Oncology, Johns Hopkins University School of Medicine, USA.
Heng ZhuDepartment of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine, USA.
Jun O LiuDepartment of Pharmacology and Molecular Sciences, The SJ Yan and HJ Mao Laboratory of Chemical Biology, Johns Hopkins University School of Medicine, Room 516, Hunterian Building, 725 N. Wolfe Street, Baltimore, MD, USA.ORCID 0000-0003-3842-9841
Johns Hopkins University · USDuke University · USLuther University · KRNanjing University of Chinese Medicine · CNShihezi University · CNUnited States Food and Drug Administration · US
Funding
Translational Research Central ServicesP30CA006973 · NCI · JOHNS HOPKINS UNIVERSITY · PI Rosalie Wollett · 1985 to 2026
$208.6MGeneration and Proteome-Wide Screening of Hybrid Combinatorial LibrariesDP1CA174428 · NCI · JOHNS HOPKINS UNIVERSITY · PI LIU, JUN O. · 2012 to 2014
$2.4MDamon Runyon Cancer Research FundFlight Attendant Medical Research InstituteNCI NIH HHS DP1 CA174428NCI NIH HHS P30 CA006973
Abstract
Glucose transporters play an essential role in cancer cell proliferation and survival and have been pursued as promising cancer drug targets. Using microarrays of a library of new macrocycles known as rapafucins, which were inspired by the natural product rapamycin, we screened for new inhibitors of GLUT1. We identified multiple hits from the rapafucin 3D microarray and confirmed one hit as a bona fide GLUT1 ligand, which we named rapaglutin A (RgA). We demonstrate that RgA is a potent inhibitor of GLUT1 as well as GLUT3 and GLUT4, with an IC
Indexed as
A549 CellsAntineoplastic AgentsApoptosisCell Cycle CheckpointsDrug Screening Assays, AntitumorGlucose Transport Proteins, FacilitativeHumansMacrolidesMCF-7 CellsMolecular StructurePhosphotransferases (Phosphate Group Acceptor)Protein Array AnalysisSignal TransductionSirolimusSmall Molecule LibrariesStructure-Activity RelationshipAMP-dependent kinase (ATP-forming)Antineoplastic AgentsGlucose Transport Proteins, FacilitativeMacrolidesPhosphotransferases (Phosphate Group Acceptor)SirolimusSmall Molecule LibrariesTacrolimusTacrolimus Binding ProteinsTOR Serine-Threonine Kinasesantitumor compoundsdrug discoveryGLUT1high-throughput screeninginhibitors
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