- |||||||||| metformin / Generic mfg., deoxyglucose / Generic mfg.
Preclinical, Journal: Alterations of the gut microbiota and metabolites by ShenZhu TiaoPi granule alleviates hyperglycemia in GK rats. (Pubmed Central) - Oct 7, 2024
The metformin (Met) and STG treatment time was 12 weeks...Moreover, STG also altered 2-deoxyglucose, beta-muricholic acid and dioxolithocholic acid production...Intestinimonas, D-maltose_and_alpha-lactose may be potential biomarkers for the effects of STG. STG alleviates hyperglycaemia via the gut microbiota and metabolites in GK rats.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Differentiating leukemia subtypes based on metabolic signatures using hyperpolarized 13C NMR. (Pubmed Central) - Sep 25, 2024
This was done using [1-13C]pyruvate and [1-13C]alanine as bioprobes for downstream metabolite quantification and kinetic analysis on cultured cells with and without 2-deoxy-D-glucose treatment...The data presented here demonstrate the potential of hyperpolarized 13C NMR spectroscopy as a method to differentiate between leukemia subtypes of similar origin. Combining this method with bioreactor setups could potentially allow for better leukemia disease management as metabolic signatures could be acquired from a single biopsy through repeated experimentation and intervention.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Molecular Mechanisms of Anticarcinogenic Potential of Hydrocotyle umbellata and Its Major Components. (Pubmed Central) - Sep 23, 2024
Analysis of the ethyl acetate and n-butanol fractions of HUE identified 1,3,4-trihydroxy-2-butanyl-?-d-glucopyranoside and caffeoylquinic acid derivatives as the major components responsible for the observed anticancer effects. In conclusion, our findings suggest that HUE and its two major components have the potential to be developed as effective therapeutic agents for a wide range of tumors by targeting cancer cell metabolism.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Role of AMPK in Atrial Metabolic Homeostasis and Substrate Preference. (Pubmed Central) - Sep 11, 2024
Thus, these results highlight the crucial homeostatic role of AMPK in the atrium, with loss of atrial AMPK leading to downregulation of the PGC1-?/PPAR? pathway and broad metabolic reprogramming with a loss of fatty acid oxidation, which may contribute to atrial remodeling and arrhythmia.
- |||||||||| dexamethasone / Generic mfg., deoxyglucose / Generic mfg.
Journal: Inflammatory stimulus-responsive polymersomes reprogramming glucose metabolism mitigates rheumatoid arthritis. (Pubmed Central) - Sep 2, 2024
Single 2-deoxy-d-glucose (2-DG, glycolysis inhibitor) treatment often cause elevated ROS, which is detrimental to RA remission...Herein, we designed a stimulus-responsive hyaluronic acid-triglycerol monostearate polymersomes (HTDD) co-delivering 2-DG and dexamethasone (Dex) to arthritic sites...Thus, the combinational strategy ultimately mitigated RA by inhibiting glycolysis and hindering inflammatory signaling. Our study demonstrated the great potential in RA therapy by reprogramming glucose metabolism in arthritic sites.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Reprogramming hematopoietic stem cell metabolism in lung cancer: glycolysis, oxidative phosphorylation, and the role of 2-DG. (Pubmed Central) - Aug 26, 2024
We measured glucose uptake using 2-[N-(7-Nitrobenz-2-oxa-1,3-diazol-4-yl)Amino]-2-Deoxyglucose (2-NBDG) and assessed levels of lactate, acetyl-coenzyme A, and ATP...Treatment with 2-DG led to decreased T-HSCs and MDSCs and an increased red blood cell count, highlighting its potential to influence metabolic and differentiation pathways in HSCs. This study provides novel insights into the metabolic reprogramming of HSCs in lung cancer, emphasizing the critical shift from glycolysis to OXPHOS and its implications for the therapeutic targeting of cancer-related metabolic pathways.
- |||||||||| deoxyglucose / Generic mfg., idebenone / Generic mfg.
Journal: SLC25A19 is required for NADH homeostasis and mitochondrial respiration. (Pubmed Central) - Aug 24, 2024
Consistently, addition of idebenone, an analog of coenzyme Q10, restores mitochondrial respiration and cell viability in SLC25A19 deficient cells. Together, our findings provide new insight into the functions of SLC25A19 in mitochondrial and cellular physiology, and suggest that restoring mitochondrial respiration could be a novel strategy for treating SLC25A19-associated disorders.
- |||||||||| deoxyglucose / Generic mfg.
Preclinical, Journal: Protective effect of PDE4B subtype-specific inhibition in an App knock-in mouse model for Alzheimer's disease. (Pubmed Central) - Aug 12, 2024
To interrogate the involvement of PDE4B in the manifestation of AD-related phenotypes, the effects of a hypomorphic mutation (Pde4bY358C) that decreases PDE4B's cAMP hydrolytic activity were evaluated in the AppNL-G-F knock-in mouse model of AD using the Barnes maze test of spatial memory, 14C-2-deoxyglucose autoradiography, thioflavin-S staining of ?-amyloid (A?) plaques, and inflammatory marker assay and transcriptomic analysis (RNA sequencing) of cerebral cortical tissue...To our knowledge, this is the first demonstration of a protective effect of PDE4B subtype-specific inhibition in a preclinical model of AD. It thus identifies PDE4B as a key regulator of disease manifestation in the AppNL-G-F model and a promising therapeutic target for AD.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Nanoparticle Targeting of Neutrophil Glycolysis Prevents Lung Ischemia-Reperfusion Injury. (Pubmed Central) - Aug 7, 2024
Lipid nanoparticles containing the glycolysis flux inhibitor 2-deoxyglucose (2-DG) were conjugated to neutrophil-specific Ly6G antibodies (NP-Ly6G[2-DG])...IRI protection was associated with less airspace neutrophil extracellular trap generation, reduced intragraft neutrophilia and enhanced alveolar macrophage efferocytotic clearance of neutrophils. Collectively, our data show that pharmacologically targeting glycolysis in neutrophils inhibits their activation and survival leading to reduced pulmonary IRI.
- |||||||||| metformin / Generic mfg., deoxyglucose / Generic mfg.
Journal: Tumor-targeted nano-assemblies for energy-blocking cocktail therapy in cancer. (Pubmed Central) - Jul 31, 2024
In our study, we developed a drug delivery strategy using metformin-derived nanomedicine (MA-dots) to load 2-DG. This approach enables the co-delivery of both drugs and their synergistic effect at the tumor site, disrupting both energy pathways and introducing an innovative "energy cocktail therapy."
- |||||||||| deoxyglucose / Generic mfg.
Journal: Multi-modal Ca2+ nanogenerator via reversing T cell exhaustion for enhanced chemo-immunotherapy. (Pubmed Central) - Jul 28, 2024
Here, we rationally designed a simple-yet-versatile Ca2+ nanogenerator to modulate iTME for enhancing 2-deoxyglucose (2-DG) mediated chemo-immunotherapy...We demonstrate that the multi-modal Ca2+ nanogenerator rescues T cells from exhaustion and inhibits tumor growth both in vitro and in vivo. More importantly, the study also facilitate the development of glucose metabolism inhibition-based tumor immunotherapy via Ca2+ overloading.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Comparison of [18F]FDG and [68 (Pubmed Central) - Jul 28, 2024
More importantly, the study also facilitate the development of glucose metabolism inhibition-based tumor immunotherapy via Ca2+ overloading. [68
- |||||||||| deoxyglucose / Generic mfg.
Individual and Combined Effects of Annonacin and 2-Deoxy-D-Glucose on Non-Small Cell Lung Cancer Cells (Exhibit Hall) - Jul 24, 2024 - Abstract #IASLCWCLC2024IASLC_WCLC_1705;
The observed increase in DNA damage and alterations in the oxidative stress response further support the potential of this combined treatment as an effective therapeutic strategy for NSCLC. These findings need further investigation to elucidate the detailed underlying mechanisms and explore the in vivo and clinical applicability details for the combined administration of Annonacin and 2DG
- |||||||||| deoxyglucose / Generic mfg.
Journal: Highly expressed lncRNA H19 in endometriosis promotes aerobic glycolysis and Histone lactylation. (Pubmed Central) - Jul 2, 2024
Altering aerobic glycolysis and histone lactylation levels through the addition of sodium lactate and 2-deoxy-d-glucose demonstrated that increased aerobic glycolysis and histone lactylation levels resulted in enhanced cell proliferation and cell migration, contributing to endometriosis...Taken together, these data demonstrate elevated expression levels of H19 in endometriosis patients promote abnormal glucose metabolism and elevated histone lactylation levels in vivo, enhancing cell proliferation and migration and promoting the progression of endometriosis. Our study provides a functional link between H19 expression and histone lactylation and glucose metabolism in endometriosis, providing new insights into disease mechanisms that could result in novel therapeutic approaches.
- |||||||||| deoxyglucose / Generic mfg.
Journal: FOXK2 facilitates the airway remodeling during chronic asthma by promoting glycolysis in a SIRT2-dependent manner. (Pubmed Central) - Jul 1, 2024
The binding of FOXK2 to SIRT2 was validated, and SIRT2 overexpression blocked the FOXK2 knockdown-mediated inhibition of EMT and glycolysis in TGF-?1-treated cells, which suggests that FOXK2 regulates EMT and glycolysis in TGF-?1-treated cells in a SIRT2-dependnet manner. Collectively, this study highlights the protective effect of FOXK2 knockdown on airway remodeling during chronic asthma.
- |||||||||| deoxyglucose / Generic mfg.
Journal: A Versatile Nanozyme-Based NADH Circulating Oxidation Reactor for Tumor Therapy through Triple Cellular Metabolism Disruption. (Pubmed Central) - Jun 26, 2024
In vitro and in vivo results demonstrate that the designed nanoreactor not only enhances the catalytic efficiency but also disrupts the tumor metabolic homeostasis, leading to efficient therapy outcome. This study develops a novel NADH circulating oxidation nanoreactor for tumor therapy through triple cellular metabolism disruption, which addresses the limitations of current nanozyme-based metabolism regulation for tumor therapy.
- |||||||||| deoxyglucose / Generic mfg., sirolimus / Generic mfg.
Journal, IO biomarker: Loss of ?2-integrin function results in metabolic reprogramming of dendritic cells, leading to increased dendritic cell functionality and anti-tumor responses. (Pubmed Central) - Jun 25, 2024
Surprisingly, although signaling through a central regulator of immune cell metabolisms, the mechanistic target of rapamycin (mTOR), was increased in BM-DCs with dysfunctional integrins, rapamycin treatment revealed that mTOR signaling was not involved in suppressing DC metabolism...Inversely, we found that induction of metabolic stress through treatment of cells with low levels of an inhibitor of glycolysis, 2-deoxyglucose (2DG), led to increased BM-DC activation...Finally, metabolic stress induced by 2DG treatment led to improved BM-DC-mediated anti-tumor responses in vivo in a melanoma cancer model, B16-OVA. In conclusion, our results indicate a role for ?2-integrin-mediated adhesion in regulating a novel type of metabolic reprogramming of DCs and DC-mediated anti-tumor responses, which may be targeted to enhance DC-mediated anti-tumor responses in cancer immunotherapy.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Loss of mitochondrial pyruvate transport initiates cardiac glycogen accumulation and heart failure. (Pubmed Central) - Jun 19, 2024
Cardiac uptake of 2-deoxyglucose was measured and western blotting performed to analyze insulin signaling and enzymatic regulators of glycogen synthesis and degradation...Our results indicate that loss of MPC in the heart causes glycogen accumulation and heart failure, while a ketogenic diet can reverse both the glycogen accumulation and heart failure. We conclude that maintaining mitochondrial pyruvate import and metabolism is critical for the heart, unless cardiac pyruvate metabolism is reduced by consumption of a ketogenic diet.
- |||||||||| deoxyglucose / Generic mfg., sirolimus / Generic mfg.
Journal: Ovarian Cancer Cell-Conditioning Medium Induces Cancer-Associated Fibroblast Phenoconversion through Glucose-Dependent Inhibition of Autophagy. (Pubmed Central) - Jun 19, 2024
Notably, the nutraceutical resveratrol (RV), known to inhibit glucose metabolism and to induce autophagy, promotes the phenoreversion of CAFs into normal fibroblasts even in the presence of ovarian cancer cell-conditioning medium. Overall, our data support the view of testing autophagy inducers for targeting the tumor-promoting stroma as an adjuvant strategy to improve therapy success rates, especially for tumors with a highly desmoplastic stroma, like ovarian cancer.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Inhibition of glycolysis and Src/Akt signaling reduces Caveolin-1-enhanced metastasis. (Pubmed Central) - Jun 19, 2024
We evaluated the effects of the glycolysis inhibitor 2-deoxy-D-glucose (2-DG) in metastatic melanoma and breast cancer cell lines expressing or not CAV1...Moreover, inhibition of Akt reduced CAV1-enhanced lung metastasis of B16-F10 cells. Collectively, these findings highlight the importance of CAV1-induced metabolic reprogramming for metastasis and point towards possible therapeutic approaches to prevent metastatic disease by inhibiting glycolysis and Src/Akt signaling.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Multiple metabolic signals in the CeA regulate feeding: The role of AMPK. (Pubmed Central) - Jun 1, 2024
Our findings identified that AMPK might be part of the signaling machinery in the CeA, which responds to nutrients and hormones contributing to feeding control. The results can contribute to understanding the pathophysiological mechanisms of altered feeding behavior/consumption, such as binge eating of caloric-dense, palatable food.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Glycolysis inhibition induces anti-tumor central memory CD8+T cell differentiation upon combination with microwave ablation therapy. (Pubmed Central) - Jun 1, 2024
In mouse models, glycolysis inhibition by 2-deoxy-D-glucose (2DG) in combination with MWA results in long-term anti-tumor effect via enhancing differentiation of tumor-specific CD44hiCD62L+CD8+ TCM cells...Importantly, in-vitro glycolysis inhibition in peripheral CD8+ T cells of patients with breast or liver tumors having been treated with MWA thrice leads to their differentiation into CD8+ TCM cells. Our work thus offers a potential strategy to avoid tumor recurrence following MWA therapy and lays down the proof-of-principle for future clinical trials.
- |||||||||| deoxyglucose / Generic mfg.
Effect of cellular stress and growth factors on COPD airway smooth muscle redox balance and glucose metabolism (PS-6; Poster board no. 3) - May 31, 2024 - Abstract #ERS2024ERS_2911;
TGF-?/FBS-stimulated COPD ASMCs showed greater proliferation (54%; p<0.05), which was more sensitive to inhibition by the glycolysis inhibitor 2-deoxy-D-glucose. COPD ASMCs show altered redox and metabolic balance in response to stress and growth factor stimulation, which may lead to aberrant survival and proliferation, and consequently to remodelling.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Salvia miltiorrhiza inhibited lung cancer through aerobic glycolysis suppression. (Pubmed Central) - May 26, 2024
The administration of DSS and DHI further reduced the level of HKII in lung cancer cell lines that had been inhibited with HK-II antagonists (2-deoxyglucose, 2-DG; 3-bromo-pyruvate, 3-BP) or knocked down with siRNA, thereby exerting an anti-lung cancer effect...Reiterating the main points, we have discovered that the anti-lung cancer effects of Salvia miltiorrhiza may be attributed to its ability to regulate HKII expression levels, thereby inhibiting aerobic glycolysis. This study not only provides a new research paradigm for the treatment of cancer by Salvia miltiorrhiza, but also highlights the important link between glucose metabolism and the effect of Salvia Miltiorrhiza.
- |||||||||| deoxyglucose / Generic mfg.
Hexokinase2 regulates glycoprotein VI mediated glycolysis and platelet activation (Exhibition Hall) - May 17, 2024 - Abstract #ISTH2024ISTH_1353;
While HK1 was widely expressed, HK2 was found exclusively in the membrane fraction. Stimulation of platelets with thrombin, convulxin or U46619 resulted in increased glucose uptake, glycolysis, glycolytic capacity and used glycoATP as the primary energy source.
- |||||||||| deoxyglucose / Generic mfg.
CD36-dependent metabolic rewiring and mitochondrial dysfunction in platelets in response to hyperlipidaemia (208 A-D) - May 17, 2024 - Abstract #ISTH2024ISTH_636;
In vitro oxLDL, but not nLDL, induced similar effects on glucose metabolism and was associated with elevated mitochondrial superoxide generation upstream of mitochondrial hyperpolarisation. In contrast to thrombin which cause a rapid and reversible activation of glycolysis, oxLDL caused a sustained and irreversible increase in glucose catabolism.
- |||||||||| deoxyglucose / Generic mfg.
Journal, IO biomarker: SPINK4 modulates inhibition of glycolysis against colorectal cancer progression. (Pubmed Central) - May 15, 2024
Besides, SPINK4 overexpression altered glycolytic activity, reduced 2-Deoxy-D-glucose (2-DG) absorption, and controlled critical glycolytic enzymes, resulting in alterations in metabolic pathways, whereas SPINK4 knockdown reversed this effect...Moreover, high expression of SPINK4, hexokinase 2 (HK2), glucose transporter 1 (GLUT1), lactate dehydrogenase A (LDHA), and pyruvate kinase M2 (PKM2) was observed in CRC tissues. As a key inhibitor of glycolytic metabolism in CRC, SPINK4 promises metabolic intervention in CRC therapy due to its impact on tumor growth and cell proliferation.
- |||||||||| deoxyglucose / Generic mfg.
Preclinical, Journal: Raphe glucose-sensing serotonergic neurons stimulate KNDy neurons to enhance LH pulses via 5HT2CR: rat and goat studies. (Pubmed Central) - May 4, 2024
The serotonergic reuptake inhibitor administration into the mediobasal hypothalamus (MBH), including the ARC, significantly blocked glucoprivic suppression of luteinizing hormone (LH) pulses and hyperglycemia induced by intravenous 2-deoxy-D-glucose (2DG) administration in female rats...Furthermore, central administration of serotonin or a 5HT2CR agonist immediately evoked GnRH pulse generator activity, and central 5HT2CR antagonism blocked the serotonin-induced facilitation of GnRH pulse generator activity in ovariectomized goats. These results suggest that DR serotonergic neurons sense high glucose availability to reduce gluconeogenesis and upregulate reproductive function by activating GnRH/LH pulse generator activity in mammals.
- |||||||||| deoxyglucose / Generic mfg.
Journal, PD(L)-1 Biomarker, IO biomarker: FOXA1/UBE2T Inhibits CD8+T Cell Activity by Inducing Mediates Glycolysis in Lung Adenocarcinoma. (Pubmed Central) - Apr 29, 2024
These results suggest that DR serotonergic neurons sense high glucose availability to reduce gluconeogenesis and upregulate reproductive function by activating GnRH/LH pulse generator activity in mammals. FOXA1 up-regulated the expression of UBE2T, which activated glycolysis, and thus inhibited activity of CD8+T cells, causing immune escape of LUAD.
- |||||||||| deoxyglucose / Generic mfg.
Preclinical, Journal: Mannose controls mesoderm specification and symmetry breaking in mouse gastruloids. (Pubmed Central) - Apr 18, 2024
We found that the glucose mimic, 2-deoxy-D-glucose (2-DG), blocked T/Bra expression and abolished axial elongation in gastruloids...Proteomics analysis demonstrated that mannose reversed glycosylation of the Wnt pathway regulator, secreted frizzled receptor Frzb. Our study showed how mannose controls mesoderm specification in mouse gastruloids.
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