- |||||||||| deoxyglucose / Generic mfg.
Circadian Rhythms Metabolically Regulate Bone Marrow Retained Primitive Hematopoietic Stem Cell Size and Function (SDCC - Halls G-H) - Nov 3, 2023 - Abstract #ASH2023ASH_3612;
Repeated administration of the glucose analog, 2-deoxyglucose (2-DG), during daylight mimicked the night phenotype and enhanced HSC engraftment potential...Our study reveals daily circadian cues dynamically determine Wnt-mediated FOXM1 bidirectional shuttling between the nucleus and the mitochondria, leading to metabolic switching of pHSCs to maintain their cellular fitness. Our data define key signaling pathways controlling pHSC quiescence and diverse circadian metabolic activities for accumulated ROS and old mitochondria clearance and turnover, keeping them ready for rapid activation in alarm situations.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Oxidative phosphorylation rather than glycolysis is the primary energy source for sperm motility in the mussels Mytilus edulis. (Pubmed Central) - Oct 29, 2023
Our results indicate that oligomycin, an inhibitor of the mitochondrial ATP synthase, immediately decreased sperm motility rate, velocity, and ATP content, while 2-deoxy-d-glucose, a glycolysis inhibitor, had no effect...Based on these findings, we conclude that OXPHOS is the primary energy source for sperm motility in marine mussels. Our study sheds light on the intricacies of mussel sperm physiology and highlights the importance of understanding the energy requirements for successful fertilization in broadcast-spawning marine invertebrates.
- |||||||||| deoxyglucose / Generic mfg.
Preclinical, Journal: Near-Infrared Fluorescence Imaging in Preclinical Models of Glioblastoma. (Pubmed Central) - Oct 27, 2023
In this work, we evaluate the tumor activity in two preclinical glioblastoma models by using fluorochrome (IRDye 800CW) coupled to different molecules: tripeptide Arg-Gly-Asp (RGD), 2-amino-2-deoxy-D-glucose (2-DG), and polyethylene glycol (PEG)...Glioblastoma tumors were presently detected with specificity and sensitivity by utilizing IRDye 800CW RGD, a near-infrared fluorophore combined with a marker of ?v?3 integrin expression. Further research is needed on its capacity to monitor tumor growth in glioblastoma after chemotherapy.
- |||||||||| BMS309403 / BMS
Journal, IO biomarker: Fatty (Pubmed Central) - Oct 22, 2023
The oxidation rate of H-oleic acid and microglial uptake of H-2-deoxy-D-glucose were modulated with LPS activation, processes which were restored with genetic and chemical inhibition of FABP4. This is the first study to report on the critical role of FABP4 in mediating the deleterious effects of LPS on microglial immunometabolism, suggesting that FABP4 may present as a novel therapeutic target to alleviate microglia-mediated neuroinflammation, a commonly reported factor in multiple neurodegenerative diseases.
- |||||||||| deoxyglucose / Generic mfg.
Trial completion: Safety and Pharmacokinetic Study of Intranasal 2-DG in Healthy Volunteers (clinicaltrials.gov) - Oct 12, 2023
P1, N=45, Completed,
In summary, the antitumor activity of CAPE in vitro was mainly via the modulation of the inflammatory mediators and the inhibition of key proteins and enzymes in glucose and lipid metabolism. Recruiting --> Completed
- |||||||||| deoxyglucose / Generic mfg.
Preclinical, Journal: 2-NBDG Uptake in Gossypium hirsutum in vitro ovules: exploring tissue-specific accumulation and its impact on hexokinase-mediated glycolysis regulation. (Pubmed Central) - Oct 11, 2023
This study investigates the phenotypic and metabolic impact of the exogenously fed glucose derivative, 2-(N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino)-2-deoxyglucose) (2-NBDG) on the fibers of Gossypium hirsutum (Upland cotton) ovule in vitro cultures...These results highlight the importance of considering fluorescent glucose derivatives as ready-to-use analogs for tracking glucose-related biological processes. However, a direct comparison between their mode of action and its extrapolation into biochemical considerations should go beyond microscopic inspection and include complementary analytical techniques.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Structure and Metabolically Oriented Efficacy of Fucoidan from Brown Alga Sargassum muticum in the Model of Colony Formation of Melanoma and Breast Cancer Cells. (Pubmed Central) - Oct 1, 2023
However, a direct comparison between their mode of action and its extrapolation into biochemical considerations should go beyond microscopic inspection and include complementary analytical techniques. This work reports the detailed structure of fucoidan from Sargassum miticum (2SmF2) and its ability to potentiate the inhibitory effect of glycolysis inhibitor 2-deoxy-d-glucose (2-DG)...However, in combination with low non-cytotoxic concentrations of 2-DG (0.5 or 2 mM), 2SmF2 could effectively inhibit the colony formation of SK-MEL-28 and MDA-MB-231 cells and decreased the number of colonies by more than 50% compared to control at the concentration of 200
- |||||||||| deoxyglucose / Generic mfg.
Journal: MAGED2 Depletion Promotes Stress-Induced Autophagy by Impairing the cAMP/PKA Pathway. (Pubmed Central) - Sep 13, 2023
Various other cellular stressors (brefeldin A, tunicamycin, 2-deoxy-D-glucose, and camptothecin) were analyzed, which all induced autophagy in the absence of MAGED2...In contrast to other MAGE proteins, MAGED2 has an inhibitory role on autophagy only under stress conditions. Hence, a prominent role of MAGED2 in the regulation of autophagy under stress conditions is evident, which may also contribute to impaired fetal renal salt reabsorption by promoting autophagy of salt-transporters in patients with MAGED2 mutation.
- |||||||||| deoxyglucose / Generic mfg.
Preclinical, Journal: Dual Tracer Test to measure tissue-specific insulin action in individual mice identifies in vivo insulin resistance without fasting hyperinsulinemia. (Pubmed Central) - Sep 12, 2023
This report describes the Dual Tracer Test, a robust method involving sequential retro-orbital injection of 14C-2-deoxyglucose (14C-2DG) alone, followed 40 min later by injection of 3H-2DG with a maximal dose of insulin to quantify both basal and insulin-stimulated 2DG uptake in the same mouse...By administering two tracers and accounting for both basal and insulin-stimulated glucose transport, this assay halves the required sample size for studies in inbred mice and demonstrates increased statistical power to detect insulin resistance, relative to other established approaches using a single tracer. The Dual Tracer Test is a valuable addition to the metabolic phenotyping toolbox.
- |||||||||| deoxyglucose / Generic mfg., doxorubicin hydrochloride / Generic mfg.
Preclinical, Journal: Advances in the Properties of Incomptine A: Cytotoxic Activity and Downregulation of Hexokinase II in Breast Cancer Cell Lines. (Pubmed Central) - Aug 12, 2023
Molecular docking and its in silico comparison with the 2-Deoxyglucose inhibitor suggest that IA could bind to Hexokinase II (HKII), decreasing its expression...The IA-HKII union would activate the voltage-gated anion channel 1 (VDAC1), resuming apoptosis. Therefore, we suggest that IA could be used against almost any subtype and that its cytotoxic effect could be due to the reactivation of apoptosis in breast cancer cells.
- |||||||||| thapsigargin / University of Nottingham, Pirbright Institute
Journal: Exploration of potential molecular mechanisms and genotoxicity of anti-cancer drugs using next generation knowledge discovery methods. (Pubmed Central) - Jul 26, 2023
Our mechanism based "NGKD" tools have more relevance for the identification of safer therapies and has the potential to lead to the rational screening of drug candidates targeting specific molecular networks and canonical pathways implicated in cancer and genotoxicity. In addition, the combination of protein, microRNA and metabolome profiles may be essential for the development of translatable biomarkers for the safety and efficacy of pharmacotherapeutic agents.Our research has laid the groundwork for the discovery of additional biomarkers that assess both the safety and the effectiveness of a treatment.
- |||||||||| deoxyglucose / Generic mfg.
Journal, IO biomarker: Glucose metabolism and its role in the maturation and migration of human CD1c dendritic cells following exposure to BCG. (Pubmed Central) - Jul 25, 2023
Pharmacological inhibition of glycolysis with 2-deoxy-D-glucose (2-DG) decreased cytokine secretion and altered cell surface expression of both CD40 and CCR7 on BCG-challenged, compared to untreated, mDCs...Our results provide the first evidence that glycolysis plays divergent roles in the maturation and migration of human CD1c mDC exposed to BCG, segregating with infection status. Further investigation of cellular metabolism in DC subsets will be required to determine whether glycolysis can be targeted to elicit better protective immunity against Mtb.
- |||||||||| deoxyglucose / Generic mfg.
The Relationship of FDG PET-SUVm and Glucose Metabolism and Contribution to Early-Stage Non-Small Cell Lung Cancer Survival (Exhibit Hall) - Jul 25, 2023 - Abstract #IASLCWCLC2023IASLC_WCLC_1420;
In early-stage NSCLC, SUVm does not correlate with 13C glycolytic intermediate enrichment indicating that SUVm does not provide sufficient tumor glycolysis information. Lactate/3PG enrichment ratios portend a poorer outcome.Table 1 Cohort CharacteristicsCharacteristicPatients (n=66)Age at the time of operation, median (range), y67 (43-87)SexMale25Female41Smoking HistoryNever18Pack-years, median (range)32 (0.25-150)Stage130225311Grade1132413743Size, median (range), cm2.6 (1-13)SubtypeAdenocarcinoma46Squamous cell carcinoma10Other10ProcedureWedge10Segmentectomy8Lobectomy36Bilobectomy2Pneumonectomy1Biopsy1SUVm mean (range)6.9 (1-29)
- |||||||||| deoxyglucose / Generic mfg.
Journal: Effect of 2-deoxyglucose-mediated inhibition of glycolysis on migration and invasion of HTR-8/SVneo trophoblast cells. (Pubmed Central) - Jul 24, 2023
Moreover, 2-DG inhibited the EMT of HTR-8/SVneo cells, down-regulated the expression of invasion-related factors matrix metalloproteinase 2/9 (MMP2/9) and up-regulated the expression of tissue inhibitor of matrix metalloproteinases 1/2 (TIMP1/2), thus inhibiting cell migration and invasion. This paper provides a foundation in the significance of aerobic glycolysis of trophoblasts in the process of invasion, and also provides ideas and insights for the promotion of embryo implantation.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Glycolytic interference blocks influenza A virus propagation by impairing viral polymerase-driven synthesis of genomic vRNA. (Pubmed Central) - Jul 17, 2023
Using 2-deoxy-d-glucose (2-DG) we examined how well inhibition of glycolysis is tolerated by host cells and which step of the IAV life cycle is affected...At the same time, minigenome assays showed no signs of a general reduction of replicative capacity of the viral polymerase. Therefore, our data suggest that the significant reduction in IAV replication by glycolytic interference occurs mainly due to an impairment of the dynamic regulation of the viral polymerase which conveys the transition of the enzyme's function from transcription to replication.
- |||||||||| deoxyglucose / Generic mfg.
Journal, Machine learning: Comparison of phasor analysis and biexponential decay curve fitting of autofluorescence lifetime imaging data for machine learning prediction of cellular phenotypes. (Pubmed Central) - Jul 17, 2023
Glycolysis and oxidative phosphorylation of MCF7 breast cancer cells were chemically inhibited with 2-deoxy-d-glucose and sodium cyanide, respectively; and fluorescence lifetime images of NAD(P)H and FAD were obtained using a multiphoton microscope...Machine learning models trained with features from curve fitting discriminate different macrophage phenotypes with improved performance over models trained using only phasor coordinates. Altogether, the results demonstrate that both curve fitting and phasor analysis of autofluorescence lifetime images can be used in machine learning models for classification of cell phenotype from the lifetime data.
- |||||||||| deoxyglucose / Generic mfg., colchicine / Generic mfg.
Preclinical, Journal: Ghrelin prevents lethality in a rat endotoxemic model through central effects on the vagal pathway and adenosine A2B signaling : Brain ghrelin and anti-septic action. (Pubmed Central) - Jul 14, 2023
We examined the effect of brain ghrelin on survival in a novel endotoxemic model achieved by treating rats with lipopolysaccharide (LPS) and colchicine...Moreover, intracisternal injection of a ghrelin receptor antagonist blocked the improved survival achieved by intracisternal ghrelin injection or intravenous 2-deoxy-d-glucose administration...Accordingly, activation of the vagal pathway and adenosine A2B receptors in the brain may be implicated in the ghrelin-induced increased survival. Since the efferent vagus nerve mediates anti-inflammatory mechanisms, we speculate that the vagal cholinergic anti-inflammatory pathway is implicated in the decreased septic lethality caused by brain ghrelin.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Directly Bound Deuterons Increase X-Nuclei Hyperpolarization using Dynamic Nuclear Polarization. (Pubmed Central) - Jul 11, 2023
Deuterated 13C sites in sugars (D-glucose and 2-deoxy-D-glucose) showed 6.3-to-17.5-fold higher solid-state dynamic nuclear polarization (DNP) levels than their respective protonated sites at 3.35T...These findings suggest a phenomenon related to DNP of X-nuclei directly bound to deuteron(s) as opposed to proton(s). It appears that direct binding to deuterons increases the solid-state DNP polarization level of X-nuclei which are otherwise bound to protons.
- |||||||||| deoxyglucose / Generic mfg.
Preclinical, Journal: Pharmacologic inhibition of glycolysis prevents the development of lupus by altering the gut microbiome in mice. (Pubmed Central) - Jul 7, 2023
The investigation has provided several compounds that display selective in vitro activity toward pancreatic cancer that warrant further development. The immune cells of lupus patients exhibit an increased glucose metabolism and treatments with 2-deoxy-D-glucose (2DG), a glycolysis inhibitor, are therapeutic in lupus-prone mice...In both models, FMT from 2DG-treated mice protected lupus-prone mice of the same strain from the development of glomerulonephritis, reduced autoantibody production as well as the activation of CD4 T
- |||||||||| deoxyglucose / Generic mfg.
Journal: Second-Generation Total Synthesis of Prorocentin. (Pubmed Central) - Jun 26, 2023
After a recent total synthesis had resolved all issues surrounding the constitution and stereostructure of prorocentin, it was possible to devise a new approach aiming at an improved supply of this scarce marine natural product; this compound is a cometabolite of the prototypical phosphatase inhibitor okadaic acid but still awaits detailed biological profiling. The revised entry starts from 2-deoxy-d-glucose; keys to success were a telescoped hemiacetal reduction/acetal cleavage and an exquisitely selective gold/Br
- |||||||||| deoxyglucose / Generic mfg.
Journal: Directed evolution of Saccharomyces cerevisiae for low volatile acidity during winemaking under aerobic conditions. (Pubmed Central) - Jun 12, 2023
However, even the most promising clones failed to reduce acetic acid production under aerobic conditions in bioreactors. Therefore, despite the concept of selecting low acetic acid producers by using 2-deoxyglucose as selective agent was found to be correct, especially at the population level, the recovery of strains with potential industrial utility by this experimental approach remains a challenge.
- |||||||||| deoxyglucose / Generic mfg.
Preclinical, Journal: Exercise alters cortico-basal ganglia network metabolic connectivity: a mesoscopic level analysis informed by anatomic parcellation defined in the mouse brain connectome. (Pubmed Central) - Jun 12, 2023
Mice were trained on a motorized treadmill for six weeks or remained sedentary (control), thereafter undergoing [C]-2-deoxyglucose metabolic brain mapping during wheel walking...Increased metabolic connectivity in the motor circuit in the absence of increases in rCGU strongly suggests greater network efficiency, which is also supported by the reduced involvement of PFC-mediated cognitive control during the performance of a new motor task. Our study delineates exercise-associated changes in functional circuitry at the subregional level and provides a framework for understanding the effects of exercise on functions of the cortico-basal ganglia-thalamic network.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Illuminating and Radiosensitizing Tumors with 2DG-Bound Gold-Based Nanomedicine for Targeted CT Imaging and Therapy. (Pubmed Central) - Jun 10, 2023
Herein, we developed 2-deoxy-d-glucose (2DG)-labeled poly(ethylene glycol) (PEG) gold nanodots (2DG-PEG-AuD) as a tumor-targeted computed tomography (CT) contrast agent and radiosensitizer...In tumor-bearing mice, 2DG-PEG-AuD showed excellent radiosensitizing functions after intravenous injection. Results from this work indicate that 2DG-PEG-AuD could greatly potentiate theranostic capabilities by providing high-resolution anatomical and functional images in a single CT scan and therapeutic capability.
- |||||||||| deoxyglucose / Generic mfg.
Journal: ERK/PKM2 Is Mediated in the Warburg Effect and Cell Proliferation in Arsenic-Induced Human L-02 Hepatocytes. (Pubmed Central) - May 27, 2023
L-02 cells were treated with 0.2 and 0.4 ?mol/L As, glycolysis inhibitor (2-deoxy-D-glucose,2-DG), ERK inhibitor [1,4-diamino-2,3-dicyano-1,4-bis(2-aminophenylthio)-butadiene, U0126] or transfected with PKM2 plasmid...Therefore, ERK/PKM2 plays a key role in the Warburg effect and proliferation of L-02 cells induced by arsenic, and also might be involved in arsenic-induced upregulation of GLUT1 and LDHA. This study provides a theoretical basis for further elucidating the carcinogenic mechanism of arsenic.
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