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Glycolysis inhibitors

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https://www.readbyqxmd.com/read/29784886/-legionella-pneumophila-is-directly-sensitive-to-2-deoxyglucose-phosphate-via-its-uhpc-transporter-but-is-indifferent-to-shifts-in-host-cell-glycolytic-metabolism
#1
Jordan V Price, Kallie Jiang, Abigail Galantowicz, Alana Freifeld, Russell E Vance
Toll-like receptor stimulation induces a pronounced shift to increased glycolytic metabolism in mammalian macrophages. We observed that bone marrow-derived macrophages (BMMs) increase glycolysis in response to infection with Legionella pneumophila ( L. pneumophila ), but the role of host macrophage glycolysis on intracellular L. pneumophila replication is not currently understood. Treatment with 2-deoxyglucose (2DG) blocks L. pneumophila replication in mammalian macrophages but has no effect on bacteria grown in broth...
May 21, 2018: Journal of Bacteriology
https://www.readbyqxmd.com/read/29784881/structural-basis-for-adp-dependent-glucokinase-inhibition-by-8-bromo-substituted-adenosine-nucleotide
#2
Przemyslaw Grudnik, Marcin M Kaminski, Krzysztof P Rembacz, Katarzyna Kuska, Mariusz Madej, Jan Potempa, Maciej Dawidowski, Grzegorz Dubin
In higher eukaryotes, several ATP-utilizing enzymes known as hexokinases activate glucose in the glycolysis pathway by phosphorylation to glucose-6-phosphate. In contrast to canonical hexokinases which use ATP, ADP-dependent glucokinase (ADPGK) catalyzes non-canonical phosphorylation of glucose to glucose-6-phosphate using ADP as a phosphate donor. Initially discovered in Archaea, the human homolog of ADPGK was described only recently. ADPGK's involvement in modified bioenergetics of activated T cells has been postulated and elevated ADPGK expression has been reported in various cancer tissues...
May 21, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29778974/metabolic-plasticity-during-transition-to-na%C3%A3-ve-like-pluripotency-in-canine-embryo-derived-stem-cells
#3
I C Tobias, R R Isaac, J G Dierolf, R Khazaee, R C Cumming, D H Betts
Pluripotent stem cells (PSCs) have been described in naïve or primed pluripotent states. Domestic dogs are useful translational models in regenerative medicine, but their embryonic stem cells (cESCs) remain narrowly investigated. Primed-like cESCs expanded in the presence of leukemia inhibitory factor and fibroblast growth factor 2 (LIF-FGF2) acquire features of naïve pluripotency when exposed to chemical inhibitors and LIF (2iL). However, proliferation of cESCs is influenced by the pluripotent state and is comparatively slower than human or mouse PSCs...
May 16, 2018: Stem Cell Research
https://www.readbyqxmd.com/read/29776912/targeting-glutaminase-may-overcome-resistance-to-mtor-inhibition
#4
(no author information available yet)
mTOR inhibitor-mediated suppression of glycolysis results in a compensatory increase in glutaminolysis.
May 18, 2018: Cancer Discovery
https://www.readbyqxmd.com/read/29764240/ferrous-glycinate-regulates-cell-energy-metabolism-by-restricting-hypoxia-induced-factor-1%C3%AE-expression-in-human-a549-cells
#5
Yung-Ting Kuo, Jhong-Huei Jheng, Mei-Chen Lo, Wei-Lu Chen, Shyang-Guang Wang, Horng-Mo Lee
Iron or oxygen regulates the stability of hypoxia inducible factor-1α (HIF-1α). We investigated whether ferrous glycinate would affect HIF-1α accumulation, aerobic glycolysis and mitochondrial energy metabolism in human A549 lung cancer cells. Incubation of A549 cells with ferrous glycinate decreased the protein levels of HIF-1α, which was abrogated by proteosome inhibitor, or prolyl hydroxylase inhibitor. Addition of ferrous glycinate decreased protein levels of glucose transporter-1, hexokinase-2, and lactate dehydrogenase A, and decreased pyruvate dehydrogenase kinase-1 (PDK-1) and pyruvate dehydrogenase (PDH) phosphorylation in A549 cells...
May 15, 2018: Free Radical Research
https://www.readbyqxmd.com/read/29763624/the-gsk3-signaling-axis-regulates-adaptive-glutamine-metabolism-in-lung-squamous-cell-carcinoma
#6
Milica Momcilovic, Sean T Bailey, Jason T Lee, Michael C Fishbein, Daniel Braas, James Go, Thomas G Graeber, Francesco Parlati, Susan Demo, Rui Li, Tonya C Walser, Michael Gricowski, Robert Shuman, Julio Ibarra, Deborah Fridman, Michael E Phelps, Karam Badran, Maie St John, Nicholas M Bernthal, Noah Federman, Jane Yanagawa, Steven M Dubinett, Saman Sadeghi, Heather R Christofk, David B Shackelford
Altered metabolism is a hallmark of cancer growth, forming the conceptual basis for development of metabolic therapies as cancer treatments. We performed in vivo metabolic profiling and molecular analysis of lung squamous cell carcinoma (SCC) to identify metabolic nodes for therapeutic targeting. Lung SCCs adapt to chronic mTOR inhibition and suppression of glycolysis through the GSK3α/β signaling pathway, which upregulates glutaminolysis. Phospho-GSK3α/β protein levels are predictive of response to single-therapy mTOR inhibition while combinatorial treatment with the glutaminase inhibitor CB-839 effectively overcomes therapy resistance...
May 14, 2018: Cancer Cell
https://www.readbyqxmd.com/read/29763606/mir-216a-5p-hexokinase-2-axis-regulates-uveal-melanoma-growth-through-modulation-of-warburg-effect
#7
Ying Liu, Yan Huo, Dajiang Wang, Yanhong Tai, Jie Li, Dongbo Pang, Yan Zhang, Wei Zhao, Nan Du, Yifei Huang
Hexokinase-2 (HK2), the initial as well as the rate-limiting step in glycolysis, is overexpressed in many human cancers, and correlates with poor clinical outcomes. Aerobic glycolysis is a hallmark of cancer, and drugs targeting its enzymes, including HK2, are being developed. However, the mechanisms of HK2 inhibition and the physiological significance of the HK2 inhibitors in cancer cells are rarely reported. Here, we show that microRNA-216a-5p (miR-216a-5p) inhibits HK2 expression by directly targeting its 3'-UTR in uveal melanoma cells...
May 12, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29760796/b-cell-lymphoma-with-different-metabolic-characteristics-show-distinct-sensitivities-to-metabolic-inhibitors
#8
Xiaoxia Liu, Li Wang, Weiye Jiang, Wenhua Lu, Jing Yang, Wenbiao Yang
Purpose: Cancer cells exhibit profound alterations in their metabolism (abnormal glucose and glutamine metabolism). Targeting cancer metabolism is a promising therapeutic strategy. Lymphoma can be classified into many different types and it is very complicated. Therefore, in this paper, we want to know whether the B cell lymphoma cells with different metabolic characteristics have distinct sensitivities to metabolic inhibitors. Methods: We classified 9 B cell lymphoma cell lines into different metabolic subtypes according to the dependency on glutamine and glucose...
2018: Journal of Cancer
https://www.readbyqxmd.com/read/29758295/systematic-bioinformatic-approaches-reveal-novel-gene-expression-signatures-associated-with-acquired-resistance-to-egfr-targeted-therapy-in-lung-cancer
#9
Marjan Mojtabavi Naeini, Manoochehr Tavassoli, Kamran Ghaedi
OBJECTIVES: Human non-small cell lung cancer (NSCLC) that harbors activating mutations in epidermal growth factor receptor (EGFR) initially responds to treatment with EGFR tyrosine kinase inhibitors (TKIs) such as gefitinib and erlotinib but eventually tumor cells acquire resistance. To date, several gene expression profiles have been reported in TKIs-resistant EGFR-mutant NSCLC. The objective of this study is to identify robust gene expression signatures, biological processes, and promising overcoming targets for TKIs-resistant EGFR-mutant NSCLC...
May 11, 2018: Gene
https://www.readbyqxmd.com/read/29754902/host-energy-source-is-important-for-disease-tolerance-to-malaria
#10
Katherine Cumnock, Avni S Gupta, Michelle Lissner, Victoria Chevee, Nicole M Davis, David S Schneider
Pathologic infections are accompanied by a collection of short-term behavioral perturbations collectively termed sickness behaviors [1, 2]. These include changes in body temperature, reduced eating and drinking, and lethargy and mimic behaviors of animals in torpor and hibernation [1, 3-6]. Sickness behaviors are important, pathogen-specific components of the host response to infection [1, 3, 7-9]. In particular, host anorexia has been shown to be beneficial or detrimental depending on the infection [7, 8]...
May 4, 2018: Current Biology: CB
https://www.readbyqxmd.com/read/29751418/in-vitro-ppar%C3%AE-agonistic-potential-of-chitin-synthesis-inhibitors-and-their-energy-metabolism-related-hepatotoxicity
#11
Xia Ning, Tingting Ku, Rui Gao, Xiaotong Ji, Guangke Li, Nan Sang
The extensive use of chitin synthesis inhibitors (CSIs) in integrated pest management programs has a detrimental effect on the surrounding environment. Recent studies reveal that CSIs may affect non-target organisms at sublethal concentrations, highlighting the need for further ecological and health risk investigations of these compounds. In this study, we characterized the peroxisome proliferator-activated receptor γ (PPARγ) agonistic activity of fourteen CSIs in HepG2 cells using an in vitro reporter gene assay...
February 15, 2018: Science of the Total Environment
https://www.readbyqxmd.com/read/29750903/targeting-cancer-metabolism-to-develop-human-lactate-dehydrogenase-hldh-5-inhibitors
#12
REVIEW
Shao-Lin Zhang, Yun He, Kin Yip Tam
Cancer cells feature a switch in glucose metabolism from oxidative phosphorylation to cytoplasm-based glycolysis. This altered cellular metabolic pathway meets the survival and proliferation needs for tumor progression. Targeting the metabolic remodeling could offer opportunities for developing effective anticancer therapeutics. Human lactate dehydrogenase (hLDH)5 plays a crucial part in the promotion of glycolysis and is overexpressed in various human tumors, and thus could be a potential anticancer drug target...
May 8, 2018: Drug Discovery Today
https://www.readbyqxmd.com/read/29749314/glycolysis-inhibition-as-a-strategy-for-hepatocellular-carcinoma-treatment
#13
Andreia Alves, Ana Catarina Mamede, Marco Alves, Pedro F Oliveira, Sandra Moreira Rocha, Filomena Botelho, Claudio Jorge Maia
Hepatocellular carcinoma (HCC) is the most frequently detected primary malignant liver tumor, representing a worldwide public health problem due to its high morbidity and mortality rates. The HCC is commonly detected in advanced stage, precluding the use of treatments with curative intent. For this reason, it is crucial to find effective therapies for HCC. Cancer cells have a high dependence of glycolysis for ATP production, especially under hypoxic environment. Such dependence provides a reliable possible strategy to specifically target cancer cells based on the inhibition of glycolysis...
April 30, 2018: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/29748183/aberrant-lck-signal-via-cd28-co-stimulation-augments-antigen-specific-functionality-and-tumor-control-by-redirected-t-cells-with-pd-1-blockade-in-humanized-mice
#14
Pratiksha Gulati, Julia Rühl, Abhilash Kannan, Magdalena Pircher, Petra Schuberth, Katarzyna Jozefa Nytko, Martin N Pruschy, Simon Sulser, Mark D Haefner, Shawn M Jensen, Alex Soltermann, Wolfgang Jungraithmayr, Maya Eisenring, Thomas Winder, Panagiotis Samaras, Annett Tabor, Rene Rs Stenger, Roger Stupp, Walter Weder, Christoph Renner, Christian Münz, Ulf Petrausch
PURPOSE: Combination therapy of adoptively transferred redirected T cells and checkpoint inhibitors aims for higher response rates in tumors poorly responsive to immunotherapy like malignant pleural mesothelioma (MPM). Only most recently the issue of an optimally active chimeric antigen receptor (CAR) and the combination with checkpoint inhibitors is starting to be addressed. EXPERIMENTAL DESIGN: Fibroblast Activation Protein (FAP)-specific CARs with different co-stimulatory domains including CD28, Δ-CD28 (lacking lck binding moiety) or 4-1BB were established...
May 10, 2018: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/29746779/energy-metabolism-drugs-block-triple-negative-breast-metastatic-cancer-cell-phenotype
#15
Silvia Cecilia Pacheco-Velazquez, Diana Xochiquetzal Robledo-Cadena, Ileana Hernández-Reséndiz, Juan Carlos Gallardo-Pérez, Rafael Moreno-Sánchez, Sara Rodríguez-Enríquez
To establish alternative targeted therapies against triple negative (TN) breast cancer, (1) the energy metabolism and (2) the sensitivity of cell growth, migration and invasiveness towards metabolic, canonical and NSAID inhibitors was analyzed in MDA-MB-231 and MDA-MB-468, two TN metastatic breast cancer cell lines, under both normoxia (21% O2) and hypoxia (0.1% O2). For comparative purposes, analysis was also carried out in the less-metastatic breast MCF-7 cancer cells. Under normoxia, oxidative phosphorylation (OxPhos) was significantly higher (2-times) in MDA-MB-468 than in MDA-MB-231 and MCF-7 whereas their glycolytic fluxes and OxPhos and glycolytic protein contents were all similar...
May 10, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29745454/effects-of-short-term-clomipramine-on-anxiety-like-behavior-cellular-metabolism-and-oxidative-stress-in-primary-fibroblast-cells-of-male-and-female-rats
#16
Ana G Jimenez, Joshua D Winward, Dana M Smith, Christina M Ragan
Anxiety is the most prevalent mental disorder among adults in the United States and females tend to have significantly higher rates of anxiety compared with men. Common treatments for anxiety include usage of selective serotonin reuptake inhibitors (SSRIs) and tricyclic antidepressants, however, sex differences in the efficacy of these drugs exist. In this study, we were interested in determining if acutely manipulating serotonin mechanisms at the whole-animal level affects cellular metabolism and oxidative stress in primary fibroblast cells from clomipramine-treated Sprague-Dawley rats...
May 2018: Physiological Reports
https://www.readbyqxmd.com/read/29741792/frontline-science-pathological-conditioning-of-human-neutrophils-recruited-to-the-airway-milieu-in-cystic-fibrosis
#17
Osric A Forrest, Sarah A Ingersoll, Marcela K Preininger, Julie Laval, Dominique H Limoli, Milton R Brown, Frances E Lee, Brahmchetna Bedi, Ruxana T Sadikot, Joanna B Goldberg, Vin Tangpricha, Amit Gaggar, Rabindra Tirouvanziam
RATIONALE: Recruitment of neutrophils to the airways, and their pathological conditioning therein, drive tissue damage and coincide with the loss of lung function in patients with cystic fibrosis (CF). So far, these key processes have not been adequately recapitulated in models, hampering drug development. Here, we hypothesized that the migration of naïve blood neutrophils into CF airway fluid in vitro would induce similar functional adaptation to that observed in vivo, and provide a model to identify new therapies...
May 9, 2018: Journal of Leukocyte Biology
https://www.readbyqxmd.com/read/29740154/additional-mitochondrial-dna-influences-the-interactions-between-the-nuclear-and-mitochondrial-genomes-in-a-bovine-embryo-model-of-nuclear-transfer
#18
Kanokwan Srirattana, Justin C St John
We generated cattle embryos using mitochondrial supplementation and somatic cell nuclear transfer (SCNT), named miNT, to determine how additional mitochondrial DNA (mtDNA) modulates the nuclear genome. To eliminate any confounding effects from somatic cell mtDNA in intraspecies SCNT, donor cell mtDNA was depleted prior to embryo production. Additional oocyte mtDNA did not affect embryo development rates but increased mtDNA copy number in blastocyst stage embryos. Moreover, miNT-derived blastocysts had different gene expression profiles when compared with SCNT-derived blastocysts...
May 8, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29735421/3-bromopyruvate-reverses-hypoxia-induced-pulmonary-arterial-hypertension-through-inhibiting-glycolysis-in-vitro-and-in-vivo-studies
#19
Fangzheng Chen, Heng Wang, Jiadan Lai, Shujing Cai, Linbo Yuan
BACKGROUND: Pulmonary arterial smooth muscle cell (PASMC) proliferation is vital to pulmonary vascular remodeling in pulmonary arterial hypertension (PAH) pathogenesis, and inhibiting PASMC metabolism could serve as a new possible therapy to reverse the process. 3-Bromopyruvate (3-BrPA) is an effective glycolysis inhibitor with its effect in PAH remains unclear. Our study aims to assess the therapeutic effect of 3-BrPA in PAH rats and investigate the possible mechanism of 3-BrPA in PASMC proliferation and apoptosis...
May 4, 2018: International Journal of Cardiology
https://www.readbyqxmd.com/read/29728578/propranolol-sensitizes-prostate-cancer-cells-to-glucose-metabolism-inhibition-and-prevents-cancer-progression
#20
Laura Brohée, Olivier Peulen, Betty Nusgens, Vincent Castronovo, Marc Thiry, Alain C Colige, Christophe F Deroanne
Propranolol, a widely used non-selective beta-adrenergic receptor blocker, was recently shown to display anticancer properties. Its potential to synergize with certain drugs has been also outlined. However, it is necessary to take into account all the properties of propranolol to select a drug that could be efficiently combined with. Propranolol was reported to block the late phase of autophagy. Hence, we hypothesized that in condition enhancing autophagy flux, cancer cells should be especially sensitive to propranolol...
May 4, 2018: Scientific Reports
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