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Glycolysis inhibitors

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https://www.readbyqxmd.com/read/28548950/enolase-1-stimulates-glycolysis-to-promote-chemoresistance-in-gastric-cancer
#1
Xiaoling Qian, Wenxia Xu, Jinye Xu, Qiqi Shi, Jiaqiu Li, Yu Weng, Zhinong Jiang, Lifeng Feng, Xian Wang, Jianwei Zhou, Hongchuan Jin
Chemotherapy is the major choice for the cancer treatment of early and advanced stages. However, intrinsic or acquired drug resistance significantly restricts the clinical efficacy of chemotherapy. It is critical to develop novel approaches to detect and overcome drug resistance. In this study, we demonstrated that accelerated glycolysis played a pivotal role in both intrinsic and acquired cisplatin-resistance of gastric cancer cells. The metabolic reprogramming of cisplatin-resistant cells was characterized by increased glycolysis dependence...
May 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28547952/mir-150-up-regulates-glut1-and-increases-glycolysis-in-osteosarcoma-cells
#2
Guangke Yuan, Yanqing Zhao, Dongjin Wu, Chunzheng Gao
Objective: Osteosarcoma (OS) is the most common malignant bone tumor in children and young adults. Many studies have shown that microRNAs play a critical role in proliferation and metastasis with this tumour type. However, whether aberrant expression might contribute to a metabolism switch in osteosarcoma cases is not clearly understood. In this study, we explored expression and function of miR-150 in osteosarcoma cells. Materials and methods: Expression of miR-150 was assessed by real-time PCR in cell lines and human patient tissues...
April 1, 2017: Asian Pacific Journal of Cancer Prevention: APJCP
https://www.readbyqxmd.com/read/28545687/synergistic-effect-of-mek-inhibitor-and-metformin-combination-in-low-grade-serous-ovarian-cancer
#3
Ismail Mert, Jasdeep Chhina, Ghassan Allo, Jing Dai, Shelly Seward, Mark S Carey, Marta Llaurado, Shailendra Giri, Ramandeep Rattan, Adnan R Munkarah
OBJECTIVE: Low-grade serous ovarian cancer (LGSOC) constitutes 5-8% of epithelial ovarian cancers and is refractory to chemotherapy. We and others have shown metformin to cause significant growth inhibition in high-grade ovarian cancer both in vitro and in vivo. Here, we aimed to analyze if metformin was effective in inhibiting proliferation of LGSOC alone and in combination with MEK inhibitor. METHODS: Three LGSOC lines (VOA1056, VOA1312 and VOA5646) were treated with metformin, trametinib or 2-deoxyglucose (2DG) alone or in combination with metformin...
May 22, 2017: Gynecologic Oncology
https://www.readbyqxmd.com/read/28539682/the-human-body-as-an-energetic-hybrid-new-perspectives-for-chronic-disease-treatment
#4
REVIEW
Michał Gajewski, Przemysław Rzodkiewicz, Sławomir Maśliński
Inflammatory response is accompanied by changes in cellular energy metabolism. Proinflammatory mediators like plasma C-reactive protein, IL-6, plasminogen activator inhibitor-1, TNF-α or monocyte chemoattractant protein-1 released in the site of inflammation activates immune cells and increase energy consumption. Increased demand for energy creates local hypoxia and lead in consequence to mitochondrial dysfunction. Metabolism of cells is switched to anaerobic glycolysis. Mitochondria continuously generate free radicals that what result in imbalance that causes oxidative stress, which results in oxidative damage...
2017: Reumatologia
https://www.readbyqxmd.com/read/28538182/targeting-metabolic-reprogramming-by-influenza-infection-for-therapeutic-intervention
#5
Heather S Smallwood, Susu Duan, Marie Morfouace, Svetlana Rezinciuc, Barry L Shulkin, Anang Shelat, Erika E Zink, Sandra Milasta, Resha Bajracharya, Ajayi J Oluwaseum, Martine F Roussel, Douglas R Green, Ljiljana Pasa-Tolic, Paul G Thomas
Influenza is a worldwide health and financial burden posing a significant risk to the immune-compromised, obese, diabetic, elderly, and pediatric populations. We identified increases in glucose metabolism in the lungs of pediatric patients infected with respiratory pathogens. Using quantitative mass spectrometry, we found metabolic changes occurring after influenza infection in primary human respiratory cells and validated infection-associated increases in c-Myc, glycolysis, and glutaminolysis. We confirmed these findings with a metabolic drug screen that identified the PI3K/mTOR inhibitor BEZ235 as a regulator of infectious virus production...
May 23, 2017: Cell Reports
https://www.readbyqxmd.com/read/28536031/lactate-induces-osteoblast-differentiation-by-stabilization-of-hif1%C3%AE
#6
Yu Wu, Miaomiao Wang, Haihua Feng, Ying Peng, Jieyun Sun, Xiuxia Qu, Chunping Li
Aerobic glycolysis is involved in osteoblast differentiation induced by Wnt signaling or PTH treatment. However, it is still unclear whether lactate, the end product of aerobic glycolysis, plays any role in osteoblast differentiation. Herein we report that in cultures of osteoblast-lineage cells, lactate promoted alkaline phosphatase-positive cell formation, increased the activity of alkaline phosphatase, and induced the expression of osteocalcin. This osteoblast differentiation-inducing effect of lactate can be inhibited by blocking its entry into cells with MCT1 siRNA or inhibitors, and by interfering with its metabolism by using specific siRNAs for LDHB and PDH...
May 20, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28532652/inhibition-of-glycolysis-by-a-novel-egfr-her2-inhibitor-ku004-suppresses-the-growth-of-her2-cancer
#7
Chongchong Tian, Ziqiao Yuan, Dengqiu Xu, Pingping Ding, Tao Wang, Luyong Zhang, Zhenzhou Jiang
Upregulation of glycolysis was often observed in human HER2-overexpressing cancers. In this study, we demonstrated that KU004, a dual novel EGFR/HER2 inhibitor, disrupted cancer cell proliferation via modulation of glycolysis. KU004, inhibited the Warburg effect by suppressing hexokinase II (HK2) expression at the transcptional and post-translational levels. Further study demonstrated that the downregulation of HKII by KU004 was mainly mediated by the PI3K/Akt signaling pathway. Furthermore, the role of HKII downregulation in KU004-mediated antitumor effect was also confirmed in our in vivo xenograft model...
May 19, 2017: Experimental Cell Research
https://www.readbyqxmd.com/read/28513986/pleiotropic-effects-of-chronic-phorbol-ester-treatment-to-improve-glucose-transport-in-insulin-resistant-cardiomyocytes
#8
Christelle Viglino, Bahareh Khoramdin, Guillaume Praplan, Christophe Montessuit
Stimulation of glucose transport is an important determinant of myocardial susceptibility to ischemia and reperfusion. Stimulation of glucose transport is markedly impaired in cardiomyocytes exposed to free fatty acids (FFA). Deactivation of the Focal Adhesion Kinase (FAK) by FFA contributes to glucose transport impairment, and could be corrected by chronic treatment with the phorbol ester TPA. However, TPA must have effects in addition to FAK reactivation to restore stimulated glucose transport. Chronic treatment with TPA improved basal and stimulated glucose transport in FFA-exposed, but not in control cardiomyocytes...
May 17, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28506645/multiple-roles-of-glyoxalase-1-mediated-suppression-of-methylglyoxal-glycation-in-cancer-biology-involvement-in-tumour-suppression-tumour-growth-multidrug-resistance-and-target-for-chemotherapy
#9
REVIEW
Naila Rabbani, Mingzhan Xue, Martin O Weickert, Paul J Thornalley
Glyoxalase 1 (Glo1) is part of the glyoxalase system in the cytoplasm of all human cells. It catalyses the glutathione-dependent removal of the endogenous reactive dicarbonyl metabolite, methylglyoxal (MG). MG is formed mainly as a side product of anaerobic glycolysis. It modifies protein and DNA to form mainly hydroimidazolone MG-H1 and imidazopurinone MGdG adducts, respectively. Abnormal accumulation of MG, dicarbonyl stress, increases adduct levels which may induce apoptosis and replication catastrophe. In the non-malignant state, Glo1 is a tumour suppressor protein and small molecule inducers of Glo1 expression may find use in cancer prevention...
May 12, 2017: Seminars in Cancer Biology
https://www.readbyqxmd.com/read/28493326/hyperglycaemia-and-aberrated-insulin-signalling-stimulate-tumour-progression-via-induction-of-the-extracellular-matrix-component-hyaluronan
#10
Sören Twarock, Christina Reichert, Ulrike Peters, Daniel J Gorski, Katharina Röck, Jens W Fischer
Epidemiological studies have detected a higher incidence of various tumour entities in diabetic patients. However, the underlying mechanisms remain insufficiently understood. Glucose-derived pericellular and extracellular hyaluronan (HA) promotes tumour progression and development. In this study, we tested the hypothesis that a diabetic metabolic state, characterised by hyperglycaemia and concomitant aberrant insulin signalling, stimulates tumour progression via the induction of HA synthesis. In a streptozotocin-induced diabetic nude mouse tumour xenograft model, hyperglycaemia and lack of insulin caused an increased formation of tumour-associated HA-matrix, which in turn accelerated tumour progression and neoangiogenesis...
May 10, 2017: International Journal of Cancer. Journal International du Cancer
https://www.readbyqxmd.com/read/28488541/microrna-124-suppresses-proliferation-and-glycolysis-in-non-small-cell-lung-cancer-cells-by-targeting-akt-glut1-hkii
#11
Xiaojian Zhao, Caiping Lu, Weiwei Chu, Bing Zhang, Qiang Zhen, Renfeng Wang, Yaxiao Zhang, Zhe Li, Baolei Lv, Huixian Li, Jiabao Liu
Non-small cell lung cancer accounts for 85% of all types of lung cancer and is the leading cause of worldwide cancer-associated mortalities. MiR-124 is epigenetically silenced in various types of cancer and plays important roles in tumor development and progression. MiR-124 was also significantly downregulated in non-small cell lung cancer patients. Glycolysis has been considered as a feature of cancer cells; hypoxia-inducible factor 1-alpha/beta and Akt are key enzymes in the regulation of glycolysis and energy metabolism in cancer cells...
May 2017: Tumour Biology: the Journal of the International Society for Oncodevelopmental Biology and Medicine
https://www.readbyqxmd.com/read/28487977/annexin-a2-functions-downstream-of-c%C3%A2-jun-n%C3%A2-terminal-kinase-to-promote-skin-fibroblast-cell-migration
#12
Youpei Wang, Xinmei Wu, Qing Wang, Meiqin Zheng, Lingxia Pang
Delayed healing of skin wounds is one of the outcomes of diabetes mellitus (DM), a condition that affects a significant number of patients worldwide. However, the underlying mechanisms remain unknown. In order to examine proteome alterations in DM, a rat model of type 1 diabetes was developed using streptozotocin injections. The proteomic responses of normal and DM rat skin were analyzed by two‑dimensional electrophoresis, and differentially expressed proteins were identified using a liquid chromatography/mass spectrometry system...
June 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28483672/acetoacetate-is-a-more-efficient-energy-yielding-substrate-for-human-mesenchymal-stem-cells-than-glucose-and-generates-fewer-reactive-oxygen-species
#13
Mary Board, Colleen Lopez, Christian van den Bos, Richard Callaghan, Kieran Clarke, Carolyn Carr
Stem cells have been assumed to demonstrate a reliance on anaerobic energy generation, suited to their hypoxic in vivo environment. However, we found that human mesenchymal stem cells (hMSCs) have an active oxidative metabolism with a range of substrates. More ATP was consistently produced from substrate oxidation than glycolysis by cultured hMSCs. Strong substrate preferences were shown with the ketone body, acetoacetate, being oxidised at up to 35 times the rate of glucose. ROS-generation was 45-fold lower during acetoacetate oxidation compared with glucose and substrate preference may be an adaptation to reduce oxidative stress...
May 5, 2017: International Journal of Biochemistry & Cell Biology
https://www.readbyqxmd.com/read/28481368/regulation-of-mir-483-3p-by-the-o-linked-n-acetylglucosamine-transferase-links-chemosensitivity-to-glucose-metabolism-in-liver-cancer-cells
#14
F Pepe, S Pagotto, S Soliman, C Rossi, P Lanuti, C Braconi, R Mariani-Costantini, R Visone, A Veronese
The miR-483-3p is upregulated in several tumors, including liver tumors, where it inhibits TP53-dependent apoptosis by targeting the pro-apoptotic gene BBC3/PUMA. The transcriptional regulation of the miR-483-3p could be driven by the β-catenin/USF1 complex, independently from its host gene IGF2, and we previously demonstrated that in HepG2 hepatoblastoma cells carrying wild-type TP53 the upregulation of the miR-483-3p overcomes the antitumoral effects of the tumor-suppressor miR-145-5p by a mechanism involving cellular glucose availability...
May 8, 2017: Oncogenesis
https://www.readbyqxmd.com/read/28481367/inhibition-of-malic-enzyme-1-disrupts-cellular-metabolism-and-leads-to-vulnerability-in-cancer-cells-in-glucose-restricted-conditions
#15
S Murai, A Ando, S Ebara, M Hirayama, Y Satomi, T Hara
Malic enzyme 1 (ME1) regulates one of the main pathways that provide nicotinamide adenine dinucleotide phosphate (NADPH), which is essential for cancer cell growth through maintenance of redox balance and biosynthesis processes in the cytoplasm. In this study, we found that ME1 inhibition disrupted metabolism in cancer cells and inhibited cancer cell growth by inducing senescence or apoptosis. In glucose-restricted culture conditions, cancer cells increased ME1 expression, and tracer experiments with labelled glutamine revealed that the flux of ME1-derived pyruvate to citrate was enhanced...
May 8, 2017: Oncogenesis
https://www.readbyqxmd.com/read/28473819/metabolic-profiles-in-cell-lines-infected-with-classical-swine-fever-virus
#16
Hongchao Gou, Mingqiu Zhao, Jin Yuan, Hailuan Xu, Hongxing Ding, Jinding Chen
Viruses require energy and biosynthetic precursors from host cells for replication. An understanding of the metabolic interplay between classical swine fever virus (CSFV) and host cells is important for exploring the complex pathological mechanisms of classical swine fever (CSF). In the current study, and for the first time, we utilized an approach involving gas chromatography coupled with mass spectrometry (GC-MS) to examine the metabolic profiles within PK-15 and 3D4/2 cells infected with CSFV. The differential metabolites of PK-15 cells caused by CSFV infection mainly included the decreased levels of glucose 6-phosphate [fold change (FC) = -1...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28473584/anti-inflammatory-effect-of-il-10-mediated-by-metabolic-reprogramming-of-macrophages
#17
W K Eddie Ip, Namiko Hoshi, Dror S Shouval, Scott Snapper, Ruslan Medzhitov
Interleukin 10 (IL-10) is an anti-inflammatory cytokine that plays a critical role in the control of immune responses. However, its mechanisms of action remain poorly understood. Here, we show that IL-10 opposes the switch to the metabolic program induced by inflammatory stimuli in macrophages. Specifically, we show that IL-10 inhibits lipopolysaccharide-induced glucose uptake and glycolysis and promotes oxidative phosphorylation. Furthermore, IL-10 suppresses mammalian target of rapamycin (mTOR) activity through the induction of an mTOR inhibitor, DDIT4...
May 5, 2017: Science
https://www.readbyqxmd.com/read/28467806/glut1-mediated-selective-tumor-targeting-with-fluorine-containing-platinum-ii-glycoconjugates
#18
Ran Liu, Zheng Fu, Meng Zhao, Xiangqian Gao, Hong Li, Qian Mi, Pengxing Liu, Jinna Yang, Zhi Yao, Qingzhi Gao
Increased glycolysis and overexpression of glucose transporters (GLUTs) are physiological characteristics of human malignancies. Based on the so-called Warburg effect, 18flurodeoxyglucose-positron emission tomography (FDG-PET) has successfully developed as clinical modality for the diagnosis and staging of many cancers. To leverage this glucose transporter mediated metabolic disparity between normal and malignant cells, in the current report, we focus on the fluorine substituted series of glucose, mannose and galactose-conjugated (trans-R,R-cyclohexane-1,2-diamine)-2-flouromalonato-platinum(II) complexes for a comprehensive evaluation on their selective tumor targeting...
April 13, 2017: Oncotarget
https://www.readbyqxmd.com/read/28463978/molecular-docking-studies-of-3-bromopyruvate-and-its-derivatives-to-metabolic-regulatory-enzymes-implication-in-designing-of-novel-anticancer-therapeutic-strategies
#19
Saveg Yadav, Shrish Kumar Pandey, Vinay Kumar Singh, Yugal Goel, Ajay Kumar, Sukh Mahendra Singh
Altered metabolism is an emerging hallmark of cancer, as malignant cells display a mammoth up-regulation of enzymes responsible for steering their bioenergetic and biosynthetic machinery. Thus, the recent anticancer therapeutic strategies focus on the targeting of metabolic enzymes, which has led to the identification of specific metabolic inhibitors. One of such inhibitors is 3-bromopyruvate (3-BP), with broad spectrum of anticancer activity due to its ability to inhibit multiple metabolic enzymes. However, the molecular characterization of its binding to the wide spectrum of target enzymes remains largely elusive...
2017: PloS One
https://www.readbyqxmd.com/read/28461244/mir-30a-5p-suppresses-breast-tumor-growth-and-metastasis-through-inhibition-of-ldha-mediated-warburg-effect
#20
Ling Li, Lei Kang, Wei Zhao, Yingying Feng, Wenpeng Liu, Tao Wang, Haixing Mai, Jun Huang, Siyu Chen, Yingchun Liang, Juqiang Han, Xiaojie Xu, Qinong Ye
Lactate dehydrogenase A (LDHA), a key enzyme regulating aerobic glycolysis, is overexpressed in many human cancers, and correlates with poor clinical outcomes. Aerobic glycolysis is a hallmark of cancer, and drugs targeting its regulators, including LDHA, are being developed. However, the mechanisms of LDHA inhibition and the physiological significance of the LDHA inhibitors in cancer cells are unclear. Here, we show that microRNA-30a-5p (miR-30a-5p) suppresses LDHA expression by directly targeting its 3'-UTR...
April 29, 2017: Cancer Letters
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