- |||||||||| deoxyglucose / Generic mfg.
Overexpression Of AMPD3 Does Not Alter Glucose Uptake In Cultured Muscle (Exhibit Hall F) - Jun 2, 2022 - Abstract #ACSM2022ACSM_2575;
These data suggest that AMPD3 overexpression in cultured muscle cells does not influence GU during uncoupled respiration. Additional research into other isoforms of AMPD as well as loss of function is warranted.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Interferon Signaling-Dependent Contribution of Glycolysis to Rubella Virus Infection. (Pubmed Central) - May 30, 2022
In conclusion, we identified a positive signaling circuit of type III IFN signaling on the generation of IFN β during RuV infection and an IFN signaling-dependent contribution of glycolysis to RuV infection. This study on epithelial A549 cells emphasizes the interaction between glycolysis and antiviral IFN signaling and notably, the antiviral activity of type III IFNs against RuV infection, especially in the absence of both type I and III IFN signaling, the RuV replication cycle was enhanced.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Discrimination of Receptor-Mediated Endocytosis by Surface-Enhanced Raman Scattering. (Pubmed Central) - May 27, 2022
In this study, receptor-mediated endocytosis was investigated with SERS by inhibiting endocytosis with ATP depletion agents: sodium azide (NaN) and 2-deoxy-d-glucose (dG)...An attempt to relate the spectral changes in the cellular spectra to the studied cellular events, receptor-mediated endocytosis inhibition, was made. It was found that the effect of two different ATP depletion agents can be discriminated by SERS, and hence receptor-mediated endocytosis can be tracked from single living cells with the technique without using a label and with limited sample preparation.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Ga-labeled dendrimer-entrapped gold nanoparticles for PET/CT dual-modality imaging and immunotherapy of tumors. (Pubmed Central) - May 22, 2022
In this study, generation 5 poly(amidoamine) (PAMAM) dendrimers were first modified to have 8.2 DOTA and 7.3 polyethylene glycol with the other end functionalized with 2-amino-2-deoxy-D-glucose (DG) for each dendrimer, entrapped with Au NPs, and then radiolabeled with Ga through the DOTA chelation...Compared with the DG-free polyplexes, the developed DG-Au DENPs/CpG polyplexes show a much more sensitive imaging effect and better inhibition effect of tumors. These findings demonstrate a unique design of Ga-labeled DG-Au DENPs, a promising theranostic nanoplatform that may be extended to tackle different tumor types.
- |||||||||| deoxyglucose / Generic mfg.
Preclinical, Journal: Inhibition of Glucose Use Improves Structural Recovery of Injured Achilles Tendon in Mice. (Pubmed Central) - May 19, 2022
After the surgery, mice were treated with the 2-deoxy-d-glucose (2DG) that inhibits conversion of glucose to glucose-6-phosphate, an initial step of glucose metabolism as an energy source and precursors of monosaccharides of GAGs...The modulus of the 2DG-treated groups were higher than that in the vehicle group, but not of statistical significance. Our findings suggest that mucoid degeneration in injured tendons may result from upregulated expression of genes involved synthesis of sulfate proteoglycans and can be inhibited by reduction of glucose utilization.
- |||||||||| metformin / Generic mfg., deoxyglucose / Generic mfg.
Journal: The function of glucose metabolism in embryonic diapause of annual killifish. (Pubmed Central) - May 19, 2022
In contrast, 2-deoxy-d-glucose, metformin, and insulin could prolong the hatching time and reduce the hatching rate. The results further confirmed that glucose metabolism played an important role in the diapause and hatching of annual killifish.
- |||||||||| deoxyglucose / Generic mfg.
Metabolic reprogramming is essential for myeloid cell-dependent haemostatic activity (ExCel Center, ICC Capital Suite Room 17) - May 13, 2022 - Abstract #ISTH2022ISTH_586;
Treatment of macrophages or monocytes with 2-Deoxy-D-glucose (2-DG; hexokinase inhibitor) reduced F3 gene expression and significantly extended TF-dependent lag-time in a novel assay of myeloid cell-dependent thrombin generation. We next assessed how inhibition of glycolysis restricts TF-dependent procoagulant activity by measuring the impact of 2-DG on cellular determinants of cell surface TF decryption.
- |||||||||| Crixivan (indinavir sulfate) / Merck (MSD)
Journal: A novel phenolic formulation for treating hepatic and peripheral insulin resistance by regulating GLUT4-mediated glucose uptake. (Pubmed Central) - May 10, 2022
We report here that a formula consisting of resveratrol, ferulic acid and epigallocatechin-3-O-gallate is more effective in ameliorating muscle and hepatic insulin resistance than the anti-diabetic drugs, metformin and AICAR...On the other hand, this formula also showed anti-diabetic potential by the reduction of lipid content in the myotubes, hepatocytes, and adipocytes. This study demonstrated that the three phenolic compounds in the formula could work in distinct mechanisms and enhance both insulin-dependent and independent vesicles trafficking and glucose transport mechanisms to improve carbohydrate and lipid metabolism.
- |||||||||| deoxyglucose / Generic mfg.
Journal: 2 deoxy-D-glucose augments the mitochondrial respiratory chain in heart. (Pubmed Central) - May 5, 2022
The increase in the heart respiratory chain proteome suggests an increase in mitochondrial oxidative capacity, which could compensate for the energy deficit caused by the inhibition of glycolysis. Thus, 2DG in the murine heart appears to induce a metabolic configuration that is the opposite of SARS-CoV-2 infected cells, which could explain the compound's ability to restrict the propagation of the virus to the benefit of patients with COVID-19 disease.
- |||||||||| deoxyglucose / Generic mfg.
Review, Journal: 2-Deoxy-D-Glucose and its Derivatives for the COVID-19 Treatment: An Update. (Pubmed Central) - May 3, 2022
Clinical studies of 2-DG corroborate that it aids in faster recovery of hospitalized patients and decreases supplemental oxygen. Herein, we describe the development process, synthesis, mechanism of viral eradication, and preclinical and clinical development of 2-DG and its derivatives as molecularly targeted therapeutics for COVID-19 treatment.
- |||||||||| deoxyglucose / Generic mfg.
Preclinical, Journal: Pharmacologically Inferred Glycolysis and Glutaminolysis Requirement of B Cells in Lupus-Prone Mice. (Pubmed Central) - Apr 28, 2022
Starting before the onset of autoimmunity, B cells from triple-congenic mice showed an elevated glycolysis and mitochondrial respiration, which were normalized in vivo by inhibiting glycolysis with a 2-deoxy-d-glucose (2DG) treatment...B cells from lupus-prone and control mice have different intrinsic metabolic requirements or different responses toward 2DG and 6-diazo-5-oxo-l-norleucine, which mirrors our previous results obtained with follicular Th cells. Overall, these results predict that targeting glucose metabolism may provide an effective therapeutic approach for systemic autoimmunity by eliminating both autoreactive follicular Th and B cells, although it may also impair TI responses.
- |||||||||| SB202190 / Amgen
HEXOKINASE 2, A GLYCOLYTIC ENZYME, REGULATES INTESTINAL STEM CELL FATE (Poster Hall - San Diego Convention Center) - Apr 25, 2022 - Abstract #DDW2022DDW_4434;
Mechanistically, HK2 KO increased the level of p-p38 MAPK, which promotes secretory cell differentiation; inhibition of p38 MAPK signaling using p38 inhibitors SB202190 or SB203580 attenuated the phenotypes induced by HK2 KO in intestinal organoids...Conclusion S. Our Results show that HK2 regulates ISC proliferation and differentiation through the activation of p38 MAPK signaling pathway. Moreover, our findings demonstrate an essential role for glycolysis in the maintenance of intestinal homeostasis.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Attenuation of the Counter-Regulatory Glucose Response in CVLM C1 Neurons: A Possible Explanation for Anorexia of Aging. (Pubmed Central) - Apr 23, 2022
Male Sprague Dawley rats aged 3 months and 24 months old were divided into two subgroups: the treatment group with 2-deoxy-d-glucose (2DG) and the control group...These findings suggest the participation of CVLM C1 neurons in counter-regulatory responses among young and old rats. Altering protein changes in aged CVLM C1 neurons may attenuate responses to glucoprivation, thus explaining the decline in food intake among the elderly.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Effects of Growth Hormone Receptor Ablation in Corticotropin-Releasing Hormone Cells. (Pubmed Central) - Apr 19, 2022
GHR ablation in CRH cells did not cause significant changes in body weight, body composition, food intake, substrate oxidation, locomotor activity, glucose tolerance, insulin sensitivity, counterregulatory response to 2-deoxy-D-glucose and ghrelin-induced food intake...In summary, GHR ablation, specifically in CRH-expressing neurons, does not lead to major alterations in metabolism, hypothalamic-pituitary-adrenal axis, acute stress response or anxiety in mice. Considering the previous studies showing that central GHR signaling regulates homeostasis in situations of metabolic stress, future studies are still necessary to identify the potential physiological importance of GH action on CRH neurons.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Oxidative phosphorylation promotes vascular calcification in chronic kidney disease. (Pubmed Central) - Apr 19, 2022
Besides, 2-deoxy-d-glucose (2-DG) exacerbated vascular calcification by upregulating OXPHOS...Suppressing COX sufficiently attenuated vascular calcification. Our findings verify the relationship between OXPHOS and calcification, and may provide potential therapeutic approaches for vascular calcification in CKD.
- |||||||||| deoxyglucose / Generic mfg., cyclosporin A microemulsion / Generic mfg.
Journal: Natterin-Induced Neutrophilia Is Dependent on cGAS/STING Activation via Type I IFN Signaling Pathway. (Pubmed Central) - Apr 19, 2022
In addition, we observed that, compared with the WT Natterin-injected mice, DPI and cyclosporin A treated mice had a lower number of neutrophils in the peritoneal exudate...Finally, using cgas KO, sting KO, or irf3 KO mice we found that recruitment of neutrophils to peritoneal cavities was virtually abolished in response to Natterin. These findings reveal cytosolic DNA sensors as critical regulators for Natterin-induced neutrophilia.
- |||||||||| deoxyglucose / Generic mfg.
Journal, IO biomarker: Metabolic Reconfiguration Activates Stemness and Immunomodulation of PDLSCs. (Pubmed Central) - Apr 19, 2022
Interestingly, PDLSCs immunomodulation is significantly increased after curcumin treatment through activation of prostaglandin E2-Indoleamine 2,3 dioxygenase (PGE2-IDO) signaling, whereas inhibition of glycolysis activity by 2-deoxyglucose (2-DG) largely blocked immunomodulatory capacity of PDLSCs. Taken together, this study provides a novel pharmacological approach to activate endogenous stem cells through metabolic reprogramming for immunomodulation and tissue regeneration.
- |||||||||| deoxyglucose / Generic mfg.
Review, Journal: Technological Advancements in External Beam Radiation Therapy (EBRT): An Indispensable Tool for Cancer Treatment. (Pubmed Central) - Apr 19, 2022
In this review, we present the technological advancements in various types of EBRT methods and discuss their clinical utility and associated limitations. We also reveal novel approaches of using biocompatible yttrium oxide scintillator-photosensitizer complex (YSM) that can generate X-ray induced cytotoxic reactive oxygen species, facilitating X-ray activated photodynamic therapy (XPDT (external beam) and/or iXPDT (internal X-ray source)) and azido-derivatives of 2-deoxy-D-glucose (2-DG) as agents for site-specific radiation-induced DNA damage.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Novel mutation in hexokinase 2 confers resistance to 2-deoxyglucose by altering protein dynamics. (Pubmed Central) - Apr 13, 2022
These findings shed new light on Hxk2 dynamics and highlight how allosteric changes can influence catalysis, providing new structural insights into this critical regulator of carbohydrate metabolism. Given that hexokinases are upregulated in some cancers and that 2DG and its derivatives have been studied in anti-cancer trials, the present work also provides insights that may apply to cancer biology and drug resistance.
- |||||||||| deoxyglucose / Generic mfg.
Journal: NEDD9 sustains hexokinase expression to promote glycolysis. (Pubmed Central) - Apr 13, 2022
Reciprocally, depletion of HK1 or HK2 elevated NEDD9 expression, as did the treatment of cells with 2-deoxyglucose (2DG), an inhibitor of glycolysis; whereas overexpression of hexokinases promoted NEDD9 dephosphorylation, associated with reduced NEDD9 activity. Together, these data for the first time suggest a negative feedback circuit involving NEDD9 and glycolytic enzymes that may contribute to NEDD9 action in promoting the aggressive growth of advanced tumors.
- |||||||||| arsenic trioxide / Generic mfg.
Journal: Metabolic adaptation drives arsenic trioxide resistance in acute promyelocytic leukemia. (Pubmed Central) - Apr 12, 2022
We have generated stable ATO-resistant promyelocytic cell lines that are less sensitive to all-trans retinoic acid (ATRA) and the combination of ATO and ATRA compared with the sensitive cell line...Glycolytic inhibition by 2-deoxyglucose (2-DG) was sufficient and comparable to the standard of care (ATO) in targeting the sensitive APL cell line...We further show that this combination has the potential in the treatment of non-M3 AML and relapsed APL. The translation of this approach in the clinic needs to be explored further.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Enhanced glycolysis in granulosa cells promotes the activation of primordial follicles through mTOR signaling. (Pubmed Central) - Apr 9, 2022
The blockade of glycolysis by 2-deoxyglucose (2-DG), but not the blockade of the communication network between pre-granulosa cells and oocyte by KIT inhibitor ISCK03, decreased short-term pyruvate deprivation-promoted mTOR activity...Taken together, the enhanced glycolysis in granulosa cells promotes the activation of primordial follicles through mTOR signaling. These findings provide new insight into the relationship between glycolytic disorders and POI/PCOS.
- |||||||||| deoxyglucose / Generic mfg.
The gut microbiota transfers the therapeutic effect of inhibiting glucose metabolism in lupus-prone mice (Exhibit Hall; P612) - Apr 8, 2022 - Abstract #IMMUNOLOGY2022IMMUNOLOGY_2450;
We have shown that treatment with 2-deoxy-D-glucose (2DG), a glycolysis inhibitor, reduced the expansion of germinal centers and eliminated the production of autoantibodies, ameliorating disease in lupus-prone mice, including (NZB × NZW)F1 and (NZW x BXSB)F1...Overall, our results demonstrated for the first time that the therapeutic effect of glucose inhibition in lupus is transferable through the gut microbiota. This implicates either a direct effect of glucose on pathogenic gut bacteria, or an indirect effect through the immune system normalized by glucose inhibition.
- |||||||||| deoxyglucose / Generic mfg.
Clinical, Journal, CAR T-Cell Therapy, PD(L)-1 Biomarker, IO biomarker: Disrupting N-glycan expression on tumor cells boosts chimeric antigen receptor T cell efficacy against solid malignancies. (Pubmed Central) - Apr 7, 2022
To overcome this barrier, we exploited the high metabolic demand of tumors to safely inhibit N-glycans synthesis with the glucose/mannose analog 2-deoxy-d-glucose (2DG)...The combined 2DG and CAR T cell therapy was successful against multiple carcinomas besides PAC, including those arising from the lung, ovary, and bladder, and with different clinically relevant CAR specificities, such as CD44v6 and CEA. Overall, our results indicate that tumor N-glycosylation regulates the quality and magnitude of CAR T cell responses, paving the way for the rational design of improved therapies against solid malignancies.
- |||||||||| deoxyglucose / Generic mfg.
Journal: The Interferon Response Dampens the Usutu Virus Infection-Associated Increase in Glycolysis. (Pubmed Central) - Apr 7, 2022
Moreover, glycolysis contributed to production of virus progeny, as inhibition of glycolysis with 2-deoxy-D-glucose reduced virus yield on Vero by one log step...This study provides evidence for glycolysis as a possible target for therapeutic intervention of USUV replication. Moreover, presented data highlight type I and type III IFN system as a determinant for human host cell permissiveness and for the infection-associated impact on glycolysis.
- |||||||||| deoxyglucose / Generic mfg.
Preclinical, Journal: Endogenous Androgens Diminish Food Intake and Activation of Orexin A Neurons in Response to Reduced Glucose Availability in Male Rats. (Pubmed Central) - Apr 2, 2022
To elucidate the role of endogenous androgens in the feeding regulation induced by reduced glucose availability, we examined the effect of gonadectomy (orchiectomy) on food intake and orexin A neuron's activity in the lateral hypothalamic/perifornical area (LH/PFA) in response to reduced glucose availability (glucoprivation) induced by 2-deoxy-d-glucose (2DG) administration in male rats...The number and percentage of c-Fos-expressing orexin A neurons in the LH/PFA and c-Fos expression in the dorsomedial Arc were significantly higher in the ORX group than the Sham group. This indicates that endogenous androgen, possibly testosterone, diminishes the food intake induced by reduced glucose availability, possibly via the attenuated activity of orexin A neuron in the LH/PFA and neurons in the dorsomedial Arc.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Inverse regulation of GSDMD and GSDME gene expression during LPS-induced pyroptosis in RAW264.7 macrophage cells. (Pubmed Central) - Mar 24, 2022
The effect of LPS on GSDMD expression is abolished by 2-deoxyglucose (2DG), confirming that glycolysis plays crucial roles in the increasing effect of LPS...Taken together, LPS regulates GSDMD and GSDME expression in opposite directions through, at least in part, its effect on glycolysis. This transcriptional regulation may contribute to the execution of pyroptosis in a GSDMD-dependent manner.
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