deoxyglucose / Generic mfg. 
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  • ||||||||||  deoxyglucose / Generic mfg.
    Preclinical, Journal:  Development of a Rapid In Vitro Screening Assay Using Metabolic Inhibitors to Detect Highly Selective Anticancer Agents. (Pubmed Central) -  Jul 27, 2021   
    An evaluation of 11 mammalian cell lines against 30 novel compounds and two metabolic inhibitors is reported. The inclusion of metabolic inhibitors during an initial screening process, and not simply during mechanistic investigations of a previously identified hit compound, provides a rapid and sensitive tool for identifying drug candidates potentially overlooked by other methods.
  • ||||||||||  deoxyglucose / Generic mfg.
    Journal:  Novel Facet of an Old Dietary Molecule? Direct Influence of Caffeine on Glucose and Biogenic Amine Handling by Human Adipocytes. (Pubmed Central) -  Jul 23, 2021   
    Glucose transport into fat cells freshly isolated from mice, rats, or humans was monitored by determining [H]-2-deoxyglucose (2-DG) uptake, while the incorporation of radiolabeled glucose into cell lipids was used as an index of lipogenic activity...Insulin increased uptake by 3.86 ± 1.11 fold when tested alone at 100 nM, and by 3.21 ± 0.80 when combined with caffeine. Our results reinforce the recommendation of caffeine's potential in the treatment or prevention of obesity complications.
  • ||||||||||  deoxyglucose / Generic mfg.
    Preclinical, Journal:  Adherence Affects Monocyte Innate Immune Function and Metabolic Reprogramming after Lipopolysaccharide Stimulation In Vitro. (Pubmed Central) -  Jul 21, 2021   
    To determine the role of glycolysis in LPS-induced immune responses, this pathway was inhibited by glucose deprivation or the glucose analogue 2-deoxy-d-glucose (2DG)...Inhibition of oxidative phosphorylation affected TNF and IL-10 release in a similar way as 2DG. Collectively, these data suggest that adherence may modify the metabolic and immunological profile of monocytes and that inhibition of glycolysis and oxidative phosphorylation, but not inhibition of glycolysis alone, has a profound effect on immune functions of monocytes exposed to LPS.
  • ||||||||||  deoxyglucose / Generic mfg.
    Journal:  Preliminary screening and correlation analysis for lncRNAs related to radiosensitivity in melanoma cells by inhibiting glycolysis. (Pubmed Central) -  Jul 20, 2021   
    Collectively, these data suggest that adherence may modify the metabolic and immunological profile of monocytes and that inhibition of glycolysis and oxidative phosphorylation, but not inhibition of glycolysis alone, has a profound effect on immune functions of monocytes exposed to LPS. Microarray chip screens the expression profiles of differentially expressed lncRNA related to the radiosensitivity of melanoma cells via inhibiting glycolysis, and lncRNA RPL34-AS1 might be a potential biological target for melanoma radiotherapy.
  • ||||||||||  deoxyglucose / Generic mfg.
    Preclinical, Journal:  AMPK is indispensable for overload-induced muscle glucose uptake and glycogenesis but dispensable for inducing hypertrophy in mice. (Pubmed Central) -  Jul 17, 2021   
    After 14 days, parameters, including muscle fiber cross-sectional area (CSA), glycogen level, and in vivo [ H]-2-deoxy-D-glucose uptake, were assessed...This study demonstrated that AMPK activation is indispensable for overload-induced muscle glucose uptake and glycogenesis; however, it is dispensable for the induction of hypertrophy in AMPK-DN mice. Furthermore, the AMPK/GLUT4 and HKII axes may regulate overload-induced muscle glucose uptake and glycogenesis.
  • ||||||||||  Miostat (carbachol) / Novartis
    Journal:  Ghrelin acts in the brain to block colonic hyperpermeability in response to lipopolysaccharide through the vagus nerve. (Pubmed Central) -  Jul 9, 2021   
    Intracisternal (D-Lys3)-GHRP-6, a selective ghrelin receptor antagonist, significantly blocked improvement of intestinal barrier function by intravenously administered 2-deoxy-d-glucose, central vagal stimulant...These results suggest that exogenously administered or endogenously released ghrelin acts centrally to improve a disturbed intestinal barrier function through orexinergic signaling and the vagal cholinergic pathway. Central ghrelin may be involved in the pathophysiology and be a novel therapeutic option in not only gastrointestinal diseases such as irritable bowel syndrome but also non-gastrointestinal diseases associated with the altered intestinal permeability.
  • ||||||||||  deoxyglucose / Generic mfg.
    Journal:  Influence of the reporter vector backbone on 2-deoxyglucose dependent promoter activation. (Pubmed Central) -  Jul 9, 2021   
    We have found that depending on the backbone of the reporter vector, pGL3 or pGL2, different results are obtained for a eukaryotic promoter's activation by metabolic changes. These observations were done in the course of investigation of the MMP2 (matrix metalloproteinase-2) promoter regulation in response to inhibition of glycolysis.
  • ||||||||||  glibenclamide / Generic mfg.
    Journal:  Hypoxia induces the translocation of glucose transporter 1 to the plasma membrane in vascular endothelial cells. (Pubmed Central) -  Jul 9, 2021   
    Interestingly, the translocation of GLUT1 induced by hypoxia was inhibited by the ATP-sensitive potassium (KATP) channel inhibitor glibenclamide, while the mitochondrial KATP channel inhibitor 5-HD did not influence GLUT1 translocation during hypoxia. These observations indicate that a decrease of intracellular ATP triggers GLUT1 translocation to the plasma membrane and is mediated by KATP channels, which would contribute to glucose uptake in HUVECs during hypoxia.
  • ||||||||||  deoxyglucose / Generic mfg.
    Review, Journal:  'Sugarcoating' 2-deoxyglucose: mechanisms that suppress its toxic effects. (Pubmed Central) -  Jul 8, 2021   
    Here we review the cellular and metabolic pathways that play a role in 2-deoxyglucose sensitivity and discuss how the modifications to these pathways result in acquisition of 2-deoxyglucose resistance. Insights gained from genetic and proteomic studies in yeast provide new ideas for the design of combinatorial therapies for cancer treatment.
  • ||||||||||  deoxyglucose / Generic mfg.
    Journal:  LncRNA PVT1 links Myc to glycolytic metabolism upon CD4 T cell activation and Sjögren's syndrome-like autoimmune response. (Pubmed Central) -  Jul 7, 2021   
    Treatment with 2-deoxy-d-glucose (2-DG), an inhibitor of glycolysis, significantly decreased the extent of lymphocyte infiltration and CD4 T cell numbers and attenuated the defect of salivary flow in the lesioned submandibular glands of NOD/Ltj mice...Inhibition of glycolysis could attenuate the proliferation of CD4 T cells and the SS-like autoimmune response. Our study provides a novel mechanistic function of lncRNA PVT1 in the pathogenesis of SS.
  • ||||||||||  deoxyglucose / Generic mfg.
    Journal:  Patterns of MTT reduction in mammalian spermatozoa. (Pubmed Central) -  Jul 7, 2021   
    Subsequent studies indicated that this extra-mitochondrial activity was suppressed by the presence of diphenylene iodonium, zinc, 2-deoxyglucose, co-enzyme Q, an SOD mimetic and NADPH oxidase inhibitors. We conclude that the pattern of MTT reduction to formazan by spermatozoa is species specific and conveys significant information about the relative importance of mitochondrial versus extra-mitochondrial redox activity that, in turn, defines the functional qualities of these cells.
  • ||||||||||  deoxyglucose / Generic mfg.
    Biomarker, Review, Journal, Tumor microenvironment:  Tumor Microenvironment-Derived Metabolites: A Guide to Find New Metabolic Therapeutic Targets and Biomarkers. (Pubmed Central) -  Jul 4, 2021   
    An assessment of dysregulated intratumor metabolism has long since been exploited for cancer diagnosis, monitoring and therapy, as exemplified by 18F-2-deoxyglucose positron emission tomography imaging...Here, we review altered cancer metabolism and its crosstalk with the tumor microenvironment to focus on energy and biomass sources, oncometabolites and the production of immunosuppressive metabolites. We provide an overview of current pharmacological approaches targeting such dysregulated metabolic landscapes and noninvasive approaches to characterize cancer metabolism for diagnosis, therapy and efficacy assessment.
  • ||||||||||  Herceptin (trastuzumab) / Roche
    Review, Journal:  Targeting mTOR and Glycolysis in HER2-Positive Breast Cancer. (Pubmed Central) -  Jul 4, 2021   
    Combination therapies against HER2 with inhibition of mTOR improve clinical outcomes compared to HER2 inhibition alone. Here, we review the role of the HER2 receptor, mTOR pathway, and glycolysis in HER2-positive breast cancer, along with signaling mechanisms and the efficacy of treatment strategies of HER2-positive breast cancer.
  • ||||||||||  deoxyglucose / Generic mfg.
    Journal:  Glycolytic inhibition: an effective strategy for developing calorie restriction mimetics. (Pubmed Central) -  Jul 3, 2021   
    Although many dozens of candidates could be discussed, the compounds selected to be reviewed are the following: 2-deoxyglucose, 3-bromopyruvate, chrysin, genistein, astragalin, resveratrol, glucosamine, mannoheptulose, and D-allulose. Some candidates have been investigated extensively with both positive and negative results, while others are only beginning to be studied.
  • ||||||||||  deoxyglucose / Generic mfg.
    Preclinical, Journal:  Sirtuin 1 is not required for contraction-stimulated glucose uptake in mouse skeletal muscle. (Pubmed Central) -  Jul 2, 2021   
    Using a radioactive 2-deoxyglucose uptake (2DOGU) approach, we measured ex vivo glucose uptake in unstimulated (rested) and electrically stimulated (100 Hz contraction every 15 s for 10 min; contracted) extensor digitorum longus (EDL) and soleus from ∼15-wk-old male and female mice with muscle-specific knockout of SIRT1 deacetylase activity and their wild-type littermates...Taken together, our findings demonstrate that SIRT1 is not required for contraction-stimulated glucose uptake in mouse skeletal muscle. Moreover, to our knowledge, this is the first demonstration of sex-based differences in contraction-stimulated glucose uptake in mouse skeletal muscle.
  • ||||||||||  Myrbetriq (mirabegron) / Astellas
    Journal:  The metabolic effects of mirabegron are mediated primarily by β -adrenoceptors. (Pubmed Central) -  Jul 1, 2021   
    Furthermore, in UCP1 knockout mice, the effects of mirabegron on glucose tolerance were attenuated. Thus, mirabegron had effects on cellular metabolism in adipocytes that improved glucose handling in vivo, and were primarily due to actions at the β -adrenoceptor.
  • ||||||||||  deoxyglucose / Generic mfg.
    Journal:  The rate of aerobic glycolysis is a pivotal regulator of tumor progression. (Pubmed Central) -  Jun 29, 2021   
    MDA-MB-231 (Warburg phenomenon) and MCF-7 (oxidative) cell lines were cultured in DMEM and exposed to three different glucose accessibility medium for 48 h (5.5 mM as normal glucose (NG), 25 mM as high glucose (HG) and 2-Deoxyglucose (2-DG) as restricted glucose accessibility)...Expression of VEGF had similar pattern with HIF-1α in different conditions. Our findings revealed the rate of Warburg effect is an important indicator for tumor promotion and invasion due to its impacts on important transcription factors like HIF-1α.
  • ||||||||||  deoxyglucose / Generic mfg.
    Journal:  Acute myeloid leukemia sensitivity to metabolic inhibitors: glycolysis showed to be a better therapeutic target. (Pubmed Central) -  Jun 26, 2021   
    The sensitivity to 2-deoxy-D-glucose (2-DG; glycolysis inhibitor) and oligomycin (OXPHOS inhibitor) was tested in six AML cell lines (HEL, HL-60, K-562, KG-1, NB-4, THP-1)...In conclusion, HEL and KG-1 show to be more glycolytic, whereas HL-60 was more OXPHOS dependent. Results suggest that AML cells reprogram their metabolism to overcome OXPHOS inhibition suggesting that glycolysis may be a better therapeutic target.
  • ||||||||||  deoxyglucose / Generic mfg.
    Journal:  Mitigation of radiation-induced pulmonary fibrosis by small-molecule dye IR-780. (Pubmed Central) -  Jun 26, 2021   
    Finally, IR-780 induces tumour cell apoptosis and enhances radiosensitivity in representative H460 and A549 cell lines. These findings indicate that IR-780 is a potential therapeutic small-molecule dye during thoracic radiotherapy.
  • ||||||||||  deoxyglucose / Generic mfg.
    Journal:  Involvement of GLUT1 and GLUT3 in the growth of canine melanoma cells. (Pubmed Central) -  Jun 26, 2021   
    Cancer cells produce ATP by glycolysis rather than oxidative phosphorylation under aerobic conditions, a process termed as the "Warburg effect." In the present study, we treated canine melanoma cells with the glucose analog 2-deoxy-D-glucose (2-DG) and investigated its effect on cell growth...The growth, glucose consumption and lactate secretion of melanoma cells transfected with siRNAs of specific for GLUT1 and GLUT3 was suppressed. These findings suggest that glucose uptake via GLUT1 and GLUT3 plays a crucial role for the growth of canine melanoma cells.
  • ||||||||||  metformin / Generic mfg., deoxyglucose / Generic mfg.
    Journal:  Spinal AMP Kinase Activity Differentially Regulates Phrenic Motor Plasticity. (Pubmed Central) -  Jun 24, 2021   
    5-HT2A (DOI hydrochloride) or 5HT7 (AS-19) receptor agonists were administered intrathecally at C4 (3 injections, 5-min intervals) while recording integrated phrenic nerve activity in anesthetized, vagotomized, paralyzed and ventilated rats. Consistent with our hypothesis, spinal AMPK activation with 2-deoxyglucose (2-DG) or metformin blocked 5-HT7, but not 5-HT2A receptor-induced pMF; in both cases, pMF inhibition was reversed by spinal administration of the AMPK inhibitor compound C. Thus, AMPK differentially regulates cellular mechanisms of serotonin-induced phrenic motor plasticity.
  • ||||||||||  deoxyglucose / Generic mfg.
    Journal:  Cytosolic 5'-Nucleotidase II Is a Sensor of Energy Charge and Oxidative Stress: A Possible Function as Metabolic Regulator. (Pubmed Central) -  Jun 24, 2021   
    NT5C2, differently from other enzyme activities, was inactivated and not rescued by dithiothreitol in a astrocytoma cell line (ADF) incubated with hydrogen peroxide. The incubation of a human lung carcinoma cell line (A549) with 2-deoxyglucose lowered the cell energy charge and impaired the interaction of NT5C2 with the ice protease-activating factor (IPAF), a protein involved in innate immunity and inflammation.
  • ||||||||||  deoxyglucose / Generic mfg.
    Journal:  Insulin Resistance Is Not Sustained Following Denervation in Glycolytic Skeletal Muscle. (Pubmed Central) -  Jun 23, 2021   
    Strikingly, while denervation impaired submaximal insulin-stimulated [H]-2-deoxyglucose uptake ~30% in the soleus, it enhanced submaximal (~120%) and maximal (~160%) insulin-stimulated glucose uptake in the EDL...Loss of GLUT4 prevented the denervation-induced increase in insulin-stimulated glucose uptake. In conclusion, the denervation results sustained insulin resistance in the soleus but enhanced insulin sensitivity in the EDL due to increased GLUT4 protein levels.
  • ||||||||||  deoxyglucose / Generic mfg.
    Preclinical, Journal:  Activation of adipose tissue glycerokinase contributes to increased white adipose tissue mass in mice fed a high-fat diet. (Pubmed Central) -  Jun 22, 2021   
    In conclusion, the denervation results sustained insulin resistance in the soleus but enhanced insulin sensitivity in the EDL due to increased GLUT4 protein levels. The data suggest that direct phosphorylation of glycerol by glycerokinase may be responsible for maintaining the supply of G3P for the existing rates of FA esterification and TAG synthesis in RWAT and EWAT from HFD-fed mice, contributing, along with a lower lipolytic response to norepinephrine, to higher adiposity.
  • ||||||||||  deoxyglucose / Generic mfg.
    Journal:  Regulations of Glycolytic Activities on Macrophages Functions in Tumor and Infectious Inflammation. (Pubmed Central) -  Jun 22, 2021   
    2-Deoxy-D-glucose (2-DG) treatments, which blocks the key enzyme hexokinase of glycolysis, efficiently inhibits a specific switch to M1 lineage, decreasing the secretion of pro-inflammatory cytokines and expressions of co-stimulatory molecules associated with relieving infectious inflammation in vitro and in vivo...Glycolysis is also required for macrophage M2 differentiation. Thus, these data provide a basis for a comprehensively understanding the role of glycolysis and OXPHOS in macrophage differentiation during anti-infection and anti-tumor inflammation.
  • ||||||||||  deoxyglucose / Generic mfg., etoposide IV / Generic mfg.
    Journal:  NHS: a novel pharmacological inhibitor of the mitochondrial F F -ATPase which represses viability of cancerous cells. (Pubmed Central) -  Jun 22, 2021   
    Thus, our findings suggest that Tsc1-associated mTORC1 signaling mediates the progression of kidney interstitial fibrosis by regulating glycolysis in proximal tubular epithelial cells. This study describes a new pharmacological inhibitor of the mitochondrial F F -ATPase that is able, by selectively blocking ATP hydrolysis, to perturb the bioenergetic homeostasis of cancer cells leading to a non-apoptotic type of cell death.
  • ||||||||||  deoxyglucose / Generic mfg.
    Review, Journal:  Relevance of the Warburg Effect in Tuberculosis for Host-Directed Therapy. (Pubmed Central) -  Jun 22, 2021   
    In addition, the shortcomings of using 2-deoxyglucose as an inhibitor of glycolysis are discussed. We conclude by proposing experimental criteria that are essential for future studies on the Warburg effect in TB to assist with the research for HDTs to combat TB.
  • ||||||||||  sirolimus / Generic mfg.
    Journal:  Enhanced Fatty Acid Synthesis Leads to Subset Imbalance and IFN-γ Overproduction in T Helper 1 Cells. (Pubmed Central) -  Jun 22, 2021   
    In memory CD4 cells of SLE patients, inhibition of fatty acid synthesis, but not β-oxidation, suppressed IFN-γ production, and up-regulated of Foxp3 expression in T-betFoxp3 cells. Metabolic regulators such as fatty acid synthesis inhibitors may improve the pathological status by correcting Th1 subset imbalance and overproduction of IFN-γ in SLE.
  • ||||||||||  deoxyglucose / Generic mfg.
    Journal:  Melatonin Is a Promising Silage Additive: Evidence From Microbiota and Metabolites. (Pubmed Central) -  Jun 16, 2021   
    Melatonin addition also dramatically affected the metabolites of sylo silage, such as raised malonic acid and some amino acid metabolism(glycine, threonine, methionine and ornithine), while reduced nucleic acid metabolism(2-deoxyuridine and thymine) and carbon metabolism(allose and 2-deoxy-D-glucose). Collectively, our results confirmed that the lowest melatonin addition (5 mg/kg) could improve the fermentation quality, and the potential mechanisms might be associated with the microbiota and metabolites in stylo.
  • ||||||||||  deoxyglucose / Generic mfg.
    Journal:  CD28 costimulation drives tumor-infiltrating T cell glycolysis to promote inflammation. (Pubmed Central) -  Jun 12, 2021   
    These phenotypes were dependent on glucose metabolism, as the glycolytic inhibitor 2-deoxyglucose both prevented changes to mitochondria and suppressed RCC CD8+ TIL activation and function. These data show that CD28 costimulation can restore RCC CD8+ TIL metabolism and function through rescue of T cell glycolysis that supports mitochondrial mass and activity.
  • ||||||||||  deoxyglucose / Generic mfg.
    [VIRTUAL] Understanding the Role of Mitochondria in Platelet Function (Room 2) -  Jun 9, 2021 - Abstract #ISTH2021ISTH_2639;    
    Clot contraction was inhibited by using glycolysis inhibitor (2-Deoxyglucose, 2DG), which was rescued by adding the downstream metabolite pyruvate...Conclusions : Our data show that glycolysis, glycogen breakdown and OxPhos all contribute to the energy pool for clot contraction. The data confirm platelets’ metabolic flexibility and show that mitochondrial bioenergetics is important for function.
  • ||||||||||  deoxyglucose / Generic mfg.
    [VIRTUAL] Construction of the Advanced Producer of Riboflavin on Whey in the Flavinogenic Yeast Candida Famata () -  Jun 9, 2021 - Abstract #WMF2021WMF_5690;    
    The strains expressed central regulatory gene SEF1 under control of the LAC4 promoter and resistant to 2-deoxy-D-glucose were constructed...The strains able to production riboflavin on concentrated whey (12% of lactose) were selected. The developed scheme of cultivation and further improvement of riboflavin overproducers are prerequisites to their industrial application.
  • ||||||||||  deoxyglucose / Generic mfg.
    Journal:  NTS Catecholamine Neurons Mediate Hypoglycemic Hunger via Medial Hypothalamic Feeding Pathways. (Pubmed Central) -  Jun 2, 2021   
    Neuroanatomical tracing results suggested that ARC-projecting orexigenic NTS neurons are largely distinct from neighboring catecholamine neurons projecting to parabrachial nucleus (PBN) that promotes satiety. Collectively, we describe a circuit organization in which an ascending pathway from brainstem stimulates appetite through key hunger neurons in the hypothalamus in response to hypoglycemia.
  • ||||||||||  deoxyglucose / Generic mfg.
    Journal:  Breast Cancer Diagnosed by MRI Using Mesoporous TiO₂-Coated (Fe₃O₄) Nanoparticles. (Pubmed Central) -  Jun 1, 2021   
    Objective: This study aimed to determine the effects of dimer captosuccinic acid-coated Fe₃O₄ (super paramagnetic) nanoparticles (NP) on 2-deoxy-d-glucose in targeted cancer cells with high rates of glucose metabolism...Absorption was also not evident in HMEPiC incubated with Fe₃O₄@DMSA-DG NP and Fe₃O₄@DMSA NP. The tumor targeting efficacy of 2-DG coated Fe₃O₄@DMSA NP was improved over Fe₃O₄,@DMSA NP in cancer cells with high rates of glucose metabolism.