- |||||||||| deoxyglucose / Generic mfg.
Journal, FDG PET: Incidentally Detected Gallbladder Carcinoma: Can F-18 FDG PET/CT Aid in Staging and Prognostication? (Pubmed Central) - Apr 18, 2024
Incidental gallbladder carcinoma (IGBC) is diagnosed in post-cholecystectomy specimens for benign indications, where the role of 2-fluro-2-deoxyglucose positron emission tomography/computed tomography(FDG-PET/CT) is not clearly defined...A higher stage of the disease on the FDG-PET/CT (loco-regional disease-HR 4.86, p?=?0.006; metastatic disease-HR 7.53, p?<?0.001) and the presence of liver infiltration (HR-1.92, p?=?0.003) were independent predictors of poor survival outcomes. FDG-PET/CT detects residual and metastatic disease in patients with IGBC, enabling the institution of appropriate management and acting as a tool for prognostication of survival.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Hypoglycemic effects of mountain caviar extract and inhibitory mechanism of saponins, including momordin Ic, on glucose absorption. (Pubmed Central) - Apr 8, 2024
Intestinal glucose absorption was evaluated by the incorporation of 2-deoxyglucose (2-DG) into Caco-2 cell layers and mouse duodenum wall vesicles...Collectively, these results suggest that MCE, particularly the principal saponin, momordin Ic, preferably suppressed glucose-induced blood glucose elevations and delayed carbohydrate-induced glucose elevations in mice. The underlying mechanism was found to involve the suppression of GE and intestinal glucose absorption.
- |||||||||| deoxyglucose / Generic mfg.
Review, Journal: The Impact of Glycolysis and Its Inhibitors on the Immune Response to Inflammation and Autoimmunity. (Pubmed Central) - Apr 1, 2024
Moreover, this knowledge is crucial for revealing new ways to target inflammatory pathologic states, such as autoimmunity and hyperinflammation. Here, we discuss the role of glycolysis in immune cell activity in physiological and pathological conditions, and the potential use of inhibitors of glycolysis for disease treatment.
- |||||||||| deoxyglucose / Generic mfg.
Glycolysis and HIF-1? signaling are important for granulocytic myeloid-derived suppressor cell activity during Staphylococcus aureus biofilm infection (Exhibit Hall F1; Poster Board Number: B617) - Mar 29, 2024 - Abstract #IMMUNOLOGY2024IMMUNOLOGY_1897;
Increased glycolytic activity in G-MDSCs was confirmed following S. aureus biofilm co-culture and attenuating glycolysis with either 2-deoxyglucose or granulocyte-specific HIF-1a deletion reduced bacterial growth during S. aureus PJI...scRNA-seq of samples from PJI patients revealed heightened glycolysis and hypoxia signatures, supporting findings with the mouse PJI model. Together, these results suggest that glycolysis and HIF-1a pathways are critical for the anti-inflammatory activity of G-MDSCs during S. aureus biofilm infection.
- |||||||||| deoxyglucose / Generic mfg.
2-Deoxy-D-glucose as a potential therapeutic agent for reducing neuroinflammation following spinal cord injury (Exhibit Hall F1; Poster Board Number: B660) - Mar 29, 2024 - Abstract #IMMUNOLOGY2024IMMUNOLOGY_1275;
Globally, our results seem to indicate that this 2-DG treatment paradigm could create a neuroinflammatory state in healthy animals, without altering or modulating the already installed spinal inflammation in injured rats. Given the established beneficial effects of 2-DG observed in other studies on neuronal activity and inflammation, adapted2-DG doses and/or longer treatment duration should be explored for reducing deleterious inflammatory processes occurring after SCI.
- |||||||||| deoxyglucose / Generic mfg.
Journal, FDG PET, Machine learning: Machine Learning and Texture Analysis of [18F]FDG PET/CT Images for the Prediction of Distant Metastases in Non-Small-Cell Lung Cancer Patients. (Pubmed Central) - Mar 28, 2024
The aim of our study was to predict the occurrence of distant metastases in non-small-cell lung cancer (NSCLC) patients using machine learning methods and texture analysis of 18F-labeled 2-deoxy-d-glucose Positron Emission Tomography/Computed Tomography {[18F]FDG PET/CT} images...The best combination of features included shape sphericity, gray level run length matrix_run length non-uniformity (GLRLM_RLNU), Total Lesion Glycolysis (TLG), Metabolic Tumor Volume (MTV), and shape compacity. The combination of these features with the decision tree method could predict the occurrence of distant metastases with an accuracy of 74.4% and an AUC of 0.63 in NSCLC patients.
- |||||||||| deoxyglucose / Generic mfg.
Glycolysis and HIF-1? signaling are important for granulocytic myeloid-derived suppressor cell activity during Staphylococcus aureus biofilm infection (Room W179) - Mar 22, 2024 - Abstract #IMMUNOLOGY2024IMMUNOLOGY_569;
Increased glycolytic activity in G-MDSCs was confirmed following S. aureus biofilm co-culture and attenuating glycolysis with either 2-deoxyglucose or granulocyte-specific HIF-1a deletion reduced bacterial growth during S. aureus PJI...scRNA-seq of samples from PJI patients revealed heightened glycolysis and hypoxia signatures, supporting findings with the mouse PJI model. Together, these results suggest that glycolysis and HIF-1a pathways are critical for the anti-inflammatory activity of G-MDSCs during S. aureus biofilm infection.
- |||||||||| deoxyglucose / Generic mfg.
PARKIN GENETIC DELETION AMPLIFIES PANCREATITIS RISKS FROM ALCOHOL AND SMOKING (Hall A, Poster Hall - Walter E. Washington Convention Center) - Mar 14, 2024 - Abstract #DDW2024DDW_7200;
The findings suggest that the pancreatitis-associated risk factors, EtOH and CS induce acinar cell injury and mitochondrial dysfunction, especially in the absence of parkin, effects likely linked to dysfunctional mitophagy. Future studies will explore the therapeutic efficacy of parkin activators in the setting of acute and chronic pancreatitis.
- |||||||||| pantoprazole / Generic mfg.
PANTOPRAZOLE ATTENUATES AND AMELIORATES LIVER FIBROSIS IN MICE (Hall A, Poster Hall - Walter E. Washington Convention Center) - Mar 14, 2024 - Abstract #DDW2024DDW_5944;
2deoxyDglucose (2DG), a glycolysis inhibitor, inhibited the mRNA expression levels of CXCL1, CCL2, CCL5, CCl20, IL1?, and TGF?, in hepatic macrophages and HSCs. PPZ attenuates and ameliorates the CCL4-, CDAHFD-, and BDL-induced liver fibrosis in mice through the inhibition of glycolysis and Na + /H + exchange, suggesting that PPZ is a potential preventive and therapeutic drugs against liver fibrosis.
- |||||||||| deoxyglucose / Generic mfg.
Preclinical, Journal: Transcriptome analysis reveals organ-specific effects of 2-deoxyglucose treatment in healthy mice. (Pubmed Central) - Mar 11, 2024
These findings suggest that 2DG has a systemic impact that varies across organs, potentially affecting multiple pathways and functions. The study provides insights into the potential therapeutic benefits of 2DG across different diseases and highlights the importance of understanding its systemic effects for future research and clinical applications.
- |||||||||| Zelboraf (vemurafenib) / Roche
Journal: Autophagy sustains mitochondrial respiration and determines resistance to BRAFV600E inhibition in thyroid carcinoma cells. (Pubmed Central) - Mar 4, 2024
In agreement, downregulation of the glycolytic pathway results in enhanced mitochondrial respiration and vemurafenib resistance. Our work provides new insights into the role of autophagy in thyroid cancer metabolism and supports mitochondrial targeting in combination with vemurafenib to eliminate BRAFV600E-positive thyroid carcinoma cells.Abbreviations: AMP: adenosine monophosphate; ATC: anaplastic thyroid carcinoma; ATG: autophagy related; ATP: adenosine triphosphate; BRAF: B-Raf proto-oncogene, serine/threonine kinase; Cas9: CRISPR-associated protein; CREB: cAMP responsive element binding protein; CRISPR: clustered regularly interspaced short palindromic repeats; 2DG: 2-deoxyglucose; FA: fatty acid; FAO: fatty acid oxidation; FASN: fatty acid synthase; FCCP: trifluoromethoxy carbonyl cyanide phenylhydrazone; LAMP1: lysosomal associated membrane protein 1; LIPE/HSL: lipase E, hormone sensitive type; MAP1LC3/LC3: microtubule associated protein 1 light chain 3; OCR: oxygen consumption rate; OXPHOS: oxidative phosphorylation; PRKA/PKA: protein kinase cAMP-activated; PTC: papillary thyroid carcinoma; SREBF1/SREBP1: sterol regulatory element binding transcription factor 1.
- |||||||||| deoxyglucose / Generic mfg.
Glycolytic Reprogramming of Alveolar Macrophages Contributes to Reduced Vesicular Socs3 Secretion in Tumor-bearing Lungs (San Diego Convention Center, Room 2 (Upper Level)) - Feb 20, 2024 - Abstract #ATS2024ATS_7541;
In our Kras model, this shift in glycolysis occurs in a time-dependent manner and correlates inversely with their capacity to secrete Socs3, suggesting that a reduction in Socs3 secretion is an acquired characteristic governed by the evolving tumor microenvironment. Finally, restoration of AM Socs3 secretion via inhibition of glycolysis reveals a potential therapeutic target that warrants further investigation in vivo.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Lesion of NPY Receptor-expressing Neurons in Perifornical Lateral Hypothalamus Attenuates Glucoprivic Feeding. (Pubmed Central) - Feb 18, 2024
We have previously shown that glucoprivation, induced by an anti-glycolygic agent 2-Deoxy-D-glucose (2DG), activates perifornical lateral hypothalamus (PeFLH) neurons and that expression of NPY in the VLM CA/NPY neurons is required for glucoprivic feeding...Interestingly, PeFLH NPY-SAP lesioned male rats had reduced body weights and decreased dark cycle feeding, but this effect was not seen in female rats. We conclude that a NPY projection to the PeFLH is necessary for glucoprivic feeding, but not locomotor activity, hyperglycemia, or corticosterone release, in both male and female rats.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Nano-energy interference: A novel strategy for blunting tumor adaptation and metastasis. (Pubmed Central) - Feb 15, 2024
Then, the glucose analog, 2-Deoxy-D-glucose (2-DG), linked to the LNP, efficiently targets tumors and competitively inhibits the tumor's normal glucose uptake...Ultimately, the disruption of both mitochondria and ribosomes depletes energy supply and new protein-generating capacity, weakening tumor's ability to adapt to environmental stress and thereby inhibiting growth and metastasis. Comprehensively, this nano-energy interference device, by controlling the tumor's stress-sensing ability, provides a novel therapeutic strategy for refractory tumors.
- |||||||||| deoxyglucose / Generic mfg.
Preclinical, Journal: Fish oil minimizes feed intake and improves insulin sensitivity in Zucker fa/fa rats. (Pubmed Central) - Feb 14, 2024
Liver insulin sensitivity (euglycaemic-hyperinsulinaemic clamp + 2 deoxyglucose) was improved in ZOFO rats, linked to changes in phosphoenolpyruvate carboxykinase expression, activity and glucose-6-phosphatase activity...Hypothalamic ceramides levels were lower in ZO than in ZO. Our study demonstrates that LC n-3 PUFA can minimize weight gain, possibly by alleviating hypothalamic lipotoxicity, and liver insulin-resistance in genetically obese Zucker rats.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Role of G protein-coupled receptor kinases (GRKs) in ?2 -adrenoceptor-mediated glucose uptake. (Pubmed Central) - Feb 13, 2024
Following receptor activation by ?2 -AR agonists, cAMP accumulation, GLUT4 translocation, [3 H]-2-deoxyglucose uptake, and ?2 -AR internalization were measured...Thus, GRK phosphorylation of the ?2 -AR is not associated with isoprenaline- or BRL37344-stimulated glucose uptake. However, GRKs acting as scaffold proteins are important for glucose uptake as GRK2 knock-down or GRK2 inhibition reduces isoprenaline-stimulated glucose uptake.
- |||||||||| salubrinal / Soochow University, Tudcabil (tauroursodeoxycholic acid) / Bruschettini
Journal: Novel insight on IRE1 in the regulation of chondrocyte dedifferentiation through ER stress independent pathway. (Pubmed Central) - Feb 10, 2024
Moreover, when IRE1 overexpression was correlated with the inflammation pathway, nuclear factor-kappa B (NF?B), IRE1 substantially increased the expression of p50 while decreasing the expression of nuclear factor kappa light polypeptide alpha (I?B?). These results suggest that IRE1 induces dedifferentiation in chondrocytes by modulating inflammatory pathways that cause dedifferentiation by disrupting type II collagen expression.
- |||||||||| deoxyglucose / Generic mfg.
Trial completion, Trial completion date, Trial primary completion date: Pharmacokinetics Study of Oral 2-Deoxy-D-Glucose (2DG) in Subjects With a Confirmed Diagnosis of Epilepsy (clinicaltrials.gov) - Feb 7, 2024
P2, N=9, Completed,
These results suggest that IRE1 induces dedifferentiation in chondrocytes by modulating inflammatory pathways that cause dedifferentiation by disrupting type II collagen expression. Recruiting --> Completed | Trial completion date: Oct 2023 --> Feb 2024 | Trial primary completion date: Oct 2023 --> Feb 2024
- |||||||||| deoxyglucose / Generic mfg.
Journal: Mitochondrial dynamics and metabolic regulation control T cell fate in the thymus. (Pubmed Central) - Feb 3, 2024
In addition, the glucose/IL-7R connection affects the TN3 to TN4 transition (also called ?-selection transition), by enhancing the percentage of TN3, leading to a decrease in the total number of thymocytes. Thus, we identified additional components, essential during ?-selection transition and playing a major role in thymic development.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Modulation of Cellular Levels of Adenosine Phosphates and Creatine Phosphate in Cultured Primary Astrocytes. (Pubmed Central) - Jan 15, 2024
This study revealed that the antitumor effects of ARHGAP10 in vivo and in vitro possibly suppress oncogenic glycolysis through the PI3K/AKT/HK2-regulated glycolysis metabolism pathway. In glucose-deprived astrocytes, the high cellular ATP and CrP contents were rapidly depleted within minutes after application of the glycolysis inhibitor 2-deoxyglucose and the respiratory chain inhibitor antimycin A. For those conditions, the decline in CrP levels always preceded that of ATP
- |||||||||| nibrozetone (RRx-001) / EpicentRx, RG7112 / Roche, Verzenio (abemaciclib) / Eli Lilly
Journal: Multi-omics joint analysis revealed the metabolic profile of retroperitoneal liposarcoma. (Pubmed Central) - Jan 2, 2024
Of particular importance, the glycolytic inhibitor 2-deoxy-D-glucose and pentose phosphate pathway (PPP) inhibitor RRX-001 significantly promoted the antitumor effects of the MDM2 inhibitor RG7112 and CDK4 inhibitor abemaciclib. Our study not only describes the metabolic profiles of RDDLPS and RWDLPS, but also offers potential therapeutic targets and strategies for RLPS.
- |||||||||| metformin / Generic mfg., deoxyglucose / Generic mfg.
Journal: Repurposing Metabolic Inhibitors in the Treatment of Colon Adenocarcinoma Patient-Derived Models. (Pubmed Central) - Dec 26, 2023
The effect of agonists on AMP-activated protein kinase (AMPK), mainly metformin and phenformin, has been appreciated in the treatment of multiple types of tumors...Phenformin with 2-deoxy-D-glucose (2DG) inhibited tumor cell growth in cancer cell lines, including HT29 cells harboring BRAF- and p53-mutations...Co-treatment of biguanides with chemotherapeutics efficiently reduced the growth of patient-derived colon models in comparison to treatment with a single agent. These results strongly suggest that significant therapeutic advantages would be achieved by combining AMPK activators such as phenformin and cancer metabolic inhibitors such as 2DG.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Molecular Cloning, Expression Analysis, and Functional Analysis of Nine IbSWEETs in Ipomoea batatas (L.) Lam. (Pubmed Central) - Dec 9, 2023
A yeast mutant complementation assay showed that IbSWEET7 had fructose, mannose, and glucose transport activity; IbSWEET15 had glucose transport activity and weaker sucrose transport activity; and all nine IbSWEETs could transport 2-deoxyglucose. These results provide a basis for further elucidating the functions of SWEET genes and promoting molecular breeding in sweet potato.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Carrier-free nanodrug targeting glucose metabolism for enhanced rheumatoid arthritis treatment. (Pubmed Central) - Dec 7, 2023
2-deoxy-D-glucose (2-DG) is a well-characterized glycolysis inhibitor...Our results indicated that 2-DCNP treatment could effectively inhibit glycolysis level to finally achieve desirable therapeutic efficacy in arthritic rats. This carrier-free nanodrug aiming at regulating glucose metabolism in inflamed joints might provide new insight for RA therapy.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Uncoupling protein 2 modulates polarization and metabolism of human primary macrophages via glycolysis and the NF??B pathway. (Pubmed Central) - Nov 30, 2023
UCP2 knockdown in M2 macrophages exacerbated inflammation and oxidative stress by promoting glycolysis, which was attenuated by the glycolysis inhibitor 2-deoxyglucose. These findings highlight the critical role of UCP2 in regulating macrophage polarization, metabolism, inflammation and oxidative stress through its effects on glycolysis, providing valuable insights into potential therapeutic strategies for macrophage-driven inflammatory and metabolic diseases.
- |||||||||| deoxyglucose / Generic mfg.
Journal: PKM2 Promotes Pro-Inflammatory Macrophage Activation in Ankylosing Spondylitis. (Pubmed Central) - Nov 27, 2023
Both inhibitors reduced pro-inflammatory function and reversed the overactive status of AS macrophages, suggesting their potential utility in treating the disease. These data place PKM2 at the cross-talk between glucose metabolic changes and the activation of inflammatory macrophages in AS patients.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Senescent Endothelial Cells Sustain Their Senescence-Associated Secretory Phenotype (SASP) through Enhanced Fatty Acid Oxidation. (Pubmed Central) - Nov 25, 2023
Interestingly, blockade of glycolysis with 2-deoxy-D-glucose in young cells resulted in enhanced production of proinflammatory cytokines, while the inhibition of carnitine palmitoyltransferase 1 (CPT1), a key rate-limiting enzyme of fatty acid oxidation, ameliorated the SASP in senescent ECs. In summary, metabolic changes in senescent ECs are complex, and this research seeks to uncover potential strategies for modulating these metabolic pathways to influence the SASP.
- |||||||||| ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Ubenimex suppresses glycolysis mediated by CD13/Hedgehog signaling to enhance the effect of cisplatin in liver cancer. (Pubmed Central) - Nov 16, 2023
The glycolysis inhibitor 2-deoxy-D-glucose enhanced the antiproliferative effect of ubenimex and CDDP...Moreover, ubenimex inhibited the production of lactic acid and adenosine triphosphate (ATP), as well as the expression of key proteins involved in glycolysis, which was similar to the effects caused by the Hh inhibitor cyclopamine...Ubenimex inhibits glycolysis by targeting the CD13/Hh pathway, thus playing an anti-tumor role together with CDDP. This study demonstrated the adjuvant effect of ubenimex from the perspective of Hh signal-dependent glycolysis regulation.
- |||||||||| deoxyglucose / Generic mfg.
Journal: Intermittent Hypoxia Promotes TAM-Induced Glycolysis in Laryngeal Cancer Cells via Regulation of HK1 Expression through Activation of ZBTB10. (Pubmed Central) - Nov 3, 2023
The hexokinase inhibitor 2-deoxy-D-glucose and HK1 shRNA were applied to verify this finding, confirming that M2-like TAMs enhanced glycolysis in laryngeal cancer cells through HK1 under intermittent hypoxic conditions...Finally, the CLEC3B level of the M2 supernatant is significantly higher in the IH group and showed a protumor effect on Hep2 cells. As ZBTB10-mediated regulation of HK1 affects glycolysis in laryngeal cancer, our findings may provide new potential therapeutic targets for laryngeal cancer.
- |||||||||| deoxyglucose / Generic mfg.
Estrogen replacement therapy restores cerebral glucose uptake and attenuates cognitive decline in ovariectomized Bri-A?42 mice (WCC Halls A-C) - Nov 3, 2023 - Abstract #Neuroscience2023NEUROSCIENCE_4654;
At 16 weeks of age, a subset of mice underwent glucose tolerance tests (GTT) and a 2-deoxyglucose (2DG) assay of CMRglc...Loss of estrogen production during menopause has been shown to precede cognitive decline in AD, while treatment with HRT may attenuate the onset of these symptoms. Here, we show that loss of estrogen in a model predisposed to amyloidosis may affect cognitive function via glucose metabolism.
- |||||||||| biomarker Driven Strategies for Targeted Elimination of Hypoxia Adapted Lymphoma Cells (SDCC - Halls G-H) - Nov 3, 2023 - Abstract #ASH2023ASH_5812;
Sensitivity of HA cells to 2-deoxyglucose, an inhibitor of glycolysis was markedly increased ( Figure 1 )...Sensitivity of HA cells to a panel of the tested cytotoxic drugs (cytarabin, cisplatin, bortezomib) and targeted agents (venetoclax, S63545, A1155463, TRAIL, polatuzumab vedotin, IM-156, copanlisib) was either unchanged or increased (compared to sensitivity of the original cell lines cultured under normoxia)...In translation, P4HA1, BCL-XL, and structural proteins of the glycolytic pathway may represent novel drugable targets for more effective elimination of hypoxia-adapted lymphoma cells. Financial Support: Ministry of Health of the Czech Republic AZV NU23-03-00172, Grant Agency of the Czech Republic GA23-05377S, and National Institute for Cancer Research (EXCELES) LX22NPO5102.
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