ArticleJournal of medicinal chemistry2012
Development of a novel class of glucose transporter inhibitors.
Article in Journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It has been retracted, and should not be counted. Cited by 16 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
16 citing papers in PubMed, 40 citations in OpenAlex.
- Cytometric proteome profiling of GFP-tagged yeast for characterizing novel antifungals.Communications biology · 2026Article
- GLUT1 production in cancer cells: a tragedy of the commons.NPJ systems biology and applications · 2022Article
- Facts and Perspectives: Implications of tumor glycolysis on immunotherapy response in triple negative breast cancer.Frontiers in oncology · 2022Review
- Chromopynones are pseudo natural product glucose uptake inhibitors targeting glucose transporters GLUT-1 and -3.Nature chemistry · 2018Article
- Upregulation of Glucose Uptake and Hexokinase Activity of Primary Human CD4+ T Cells in Response to Infection with HIV-1.Viruses · 2018Article
- Development of GLUT4-selective antagonists for multiple myeloma therapy.European journal of medicinal chemistry · 2017Article
- Identification and Optimization of the First Highly Selective GLUT1 Inhibitor BAY-876.ChemMedChem · 2016Article
- Anticancer agents interacting with membrane glucose transporters.MedChemComm · 2016Article
- Trienamine catalyzed asymmetric synthesis and biological investigation of a cytochalasin B-inspired compound collection.Organic & biomolecular chemistry · 2016Article
- Targeting the Warburg effect with a novel glucose transporter inhibitor to overcome gemcitabine resistance in pancreatic cancer cells.Carcinogenesis · 2014Article
- Prospects on strategies for therapeutically targeting oncogenic regulatory factors by small-molecule agents.Journal of cellular biochemistry · 2014Review
- Identifying novel targets in renal cell carcinoma: design and synthesis of affinity chromatography reagents.Bioorganic & medicinal chemistry · 2014Article
- Insulin-like growth factor-I receptor is suppressed through transcriptional repression and mRNA destabilization by a novel energy restriction-mimetic agent.Carcinogenesis · 2013Article
- Suppression of prostate epithelial proliferation and intraprostatic progrowth signaling in transgenic mice by a new energy restriction-mimetic agent.Cancer prevention research (Philadelphia, Pa.) · 2013Article
- The mRNA-stabilizing factor HuR protein is targeted by β-TrCP protein for degradation in response to glycolysis inhibition.The Journal of biological chemistry · 2012Article
- Glucose transporters in cancer metabolism.Current opinion in oncology · 2012Review
Corrections and comments
- Retraction · 2018-05-18Falsification/Fabrication of Image · Investigation by Company/Institution · Misconduct - Official Investigation(s) and/or Finding(s) · Misconduct by Author · · Ching-Shih Chen has institutional finding of misconduct;
- Retracted
Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
Abstract
On the basis of our finding that the antitumor effect of 5-{4-[(1-methylcyclohexyl)methoxy]benzyl}thiazolidine-2,4-dione, a thiazolidinedione peroxisome proliferator-activated receptor (PPAR)γ agonist, was, in part, attributable to its ability to block glucose uptake independently of PPARγ, we used its PPARγ-inactive analogue to develop a novel class of glucose transporter (GLUT) inhibitors. This lead optimization led to compound 30 {5-(4-hydroxy-3-trifluoromethylbenzylidene)-3-[4,4,4-trifluoro-2-methyl-2-(2,2,2-trifluoroethyl)butyl]thiazolidine-2,4-dione} as the optimal agent, which exhibited high antitumor potency through the suppression of glucose uptake (IC(50), 2.5 μM), while not cytotoxic to prostate and mammary epithelial cells. This glucose uptake inhibition was associated with the inhibition of GLUT1 (IC(50), 2 μM). Moreover, the mechanism of antitumor action of compound 30 was validated by its effect on a series of energy restriction-associated cellular responses. Homology modeling analysis suggests that the inhibitory effect of compound 30 on glucose entry was attributable to its ability to bind to the GLUT1 channel at a site distinct from that of glucose.
Indexed as
Identifiers
What OpenQuestion holds
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.