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Glycolysis inhibitors

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https://www.readbyqxmd.com/read/28107631/overcoming-the-heat-endurance-of-tumor-cells-by-interfering-the-anaerobic-glycolysis-metabolism-for-improved-photothermal-therapy
#1
Wei-Hai Chen, Guo-Feng Luo, Qi Lei, Sheng Hong, Wen-Xiu Qiu, Li-Han Liu, Si-Xue Cheng, Xian-Zheng Zhang
In this study, we developed a general method to decorate plasmonic gold nanorods (GNRs) with a CD44-targeting functional polymer, containing hyaluronic acid (HA) targeting moiety and a small molecule Glut1 inhibitor of diclofenac (DC), to obtain GNR/HA-DC. This nanosystem exhibited the superiority of selectively sensitizing tumor cells for photothermal therapy (PTT) by inhibiting the unique anaerobic glycolysis. Upon specifically targeting CD44, sequentially time-dependent DC release could be achieved by the trigger of hyaluronidase (HAase), which abundantly existed in tumor tissue...
January 20, 2017: ACS Nano
https://www.readbyqxmd.com/read/28104391/na-h-exchanger-mediated-hydrogen-ion-extrusion-as-a-carcinogenic-signal-in-triple-negative-breast-cancer-etiopathogenesis-and-prospects-for-its-inhibition-in-therapeutics
#2
REVIEW
Schammim Ray Amith, Larry Fliegel
Breast cancer is the leading cause of cancer-related death in women in Europe and North America, and metastasis is the primary cause of fatality in patients with breast cancer. While some breast cancers are quite treatable, the triple-negative breast cancers are more metastatic and resistant to chemotherapy. There is clearly an urgent need for better treatments for this form of the disease. Breast cancer is characterized by genetically complex intra-tumour heterogeneity, particularly within the triple-negative clinical subtype...
January 16, 2017: Seminars in Cancer Biology
https://www.readbyqxmd.com/read/28100784/mitochondrial-o-glcnac-transferase-mogt-regulates-mitochondrial-structure-function-and-survival-in-hela-cells
#3
Juliana L Sacoman, Raul Y Dagda, Amanda R Burnham-Marusich, Ruben K Dagda, Patricia M Berninsone
O-linked N-acetylglucosamine transferase (OGT) catalyzes O-GlcNAcylation of target proteins and regulates numerous biological processes. OGT is encoded by a single gene that yields nucleocytosolic and mitochondrial isoforms. To date, the role of the mitochondrial isoform of OGT (mOGT) remains largely unknown. Using high-throughput proteomics, we identified 84 candidate mitochondrial glycoproteins, of which 44 are novel. Notably, two of the candidate glycoproteins identified (cytochrome oxidase 2 (COX2) and NADH: ubiquinone oxidoreductase core subunit 4 (MT-ND4)) are encoded by mitochondrial DNA...
January 18, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28094552/glucose-metabolism-in-cancer-and-ischemia-possible-therapeutic-consequences-of-the-warburg-effect
#4
Spela Salamon, Eva Podbregar, Peter Kubatka, Dietrich Büsselberg, Martin Caprnda, Radka Opatrilova, Vanda Valentova, Mariusz Adamek, Peter Kruzliak, Matej Podbregar
The Warburg effect states that the main source of energy for cancer cells is not aerobic respiration, but glycolysis-even in normoxia. The shift from one to the other is governed by mutually counteracting enzymes: pyruvate dehydrogenase and pyruvate dehydrogenase kinase (PDK). Anaerobic metabolism of cancer cells promotes cell proliferation, local tissue immunosuppression, resistance to hypoxic conditions, and metastatic processes. By switching glucose back to oxidative metabolism, these effects might be reversed...
January 17, 2017: Nutrition and Cancer
https://www.readbyqxmd.com/read/28081256/inhibition-of-acetyl-coa-carboxylase-1-acc1-and-2-acc2-reduces-proliferation-and-de-novo-lipogenesis-of-egfrviii-human-glioblastoma-cells
#5
Jessica E C Jones, William P Esler, Rushi Patel, Adhiraj Lanba, Nicholas B Vera, Jeffrey A Pfefferkorn, Cecile Vernochet
Tumor cell proliferation and migration processes are regulated by multiple metabolic pathways including glycolysis and de novo lipogenesis. Since acetyl-CoA carboxylase (ACC) is at the junction of lipids synthesis and oxidative metabolic pathways, we investigated whether use of a dual ACC inhibitor would provide a potential therapy against certain lipogenic cancers. The impact of dual ACC1/ACC2 inhibition was investigated using a dual ACC1/ACC2 inhibitor as well as dual siRNA knock down on the cellular viability and metabolism of two glioblastoma multiform cancer cell lines, U87 and a more aggressive form, U87 EGFRvIII...
2017: PloS One
https://www.readbyqxmd.com/read/28077309/physical-and-biological-characteristics-of-multi-drug-resistance-mdr-an-integral-approach-considering-ph-and-drug-resistance-in-cancer
#6
REVIEW
Ziad Omran, Paula Scaife, Simon Stewart, Cyril Rauch
The role of the Warburg effect in cancer remains to be elucidated with a resurgence in research efforts over the past decade. Why a cancer cell would prefer to use energy inefficient glycolysis, leading to an alteration of pH both inside and outside of the cell, remains to be uncovered. The development of MDR represents a major challenge in the treatment of cancer and it is explained, so far, by the over expression of drug transporters such as the well-known and archetypal P-glycoprotein (Pgp). However, controversies exist regarding the function of Pgp in multi-drug resistance...
January 8, 2017: Seminars in Cancer Biology
https://www.readbyqxmd.com/read/28058736/effect-of-mitochondrial-uncoupling-and-glycolysis-inhibition-on-ram-sperm-functionality
#7
Jda Losano, Dsr Angrimani, A Dalmazzo, B R Rui, M M Brito, C M Mendes, Gkv Kawai, C I Vannucchi, Meoa Assumpção, V H Barnabe, M Nichi
Studies have demonstrated the importance of mitochondria to sperm functionality, as the main source of ATP for cellular homoeostasis and motility. However, the role of mitochondria on sperm metabolism is still controversial. Studies indicate that, for some species, glycolysis may be the main mechanism for sperm energy production. For ram sperm, such pathway is not clear. Thus, we evaluated ram sperm in response to mitochondrial uncoupling and glycolysis inhibition aiming to assess the importance of each pathway for sperm functionality...
January 6, 2017: Reproduction in Domestic Animals, Zuchthygiene
https://www.readbyqxmd.com/read/28047565/su-g-tep3-10-radiation-induces-prompt-live-cell-metabolic-fluxes
#8
D Campos, W Peeters, K Nickel, B Burkel, J Bussink, R Kimple, A van der Kogel, K Eliceiri, M Kissick
PURPOSE: To compare metabolic dynamics and HIF-1α expression following radiation between a cancerous cell line (UM-SCC-22B) and a normal, immortalized cell line, NOK (Normal Oral Keratinocyte). HIF-1 is a key factor in metabolism and radiosensitivity. A better understanding of how radiation affects the interplay of metabolism and HIF-1 might give a better understanding of the mechanisms responsible for radiosensitivity. METHODS: Changes in cellular metabolism in response to radiation are tracked by fluorescence lifetime of NADH...
June 2016: Medical Physics
https://www.readbyqxmd.com/read/28039467/targeting-cancer-stem-cell-propagation-with-palbociclib-a-cdk4-6-inhibitor-telomerase-drives-tumor-cell-heterogeneity
#9
Gloria Bonuccelli, Maria Peiris-Pages, Bela Ozsvari, Ubaldo E Martinez-Outschoorn, Federica Sotgia, Michael P Lisanti
In this report, we systematically examined the role of telomerase activity in lung and ovarian cancer stem cell (CSC) propagation. For this purpose, we indirectly gauged telomerase activity, by linking the hTERT-promoter to eGFP. Using lung (A549) and ovarian (SKOV3) cancer cells, transduced with the hTERT-GFP reporter, we then employed GFP-expression levels to fractionate these cell lines into GFP-high and GFP-low populations. We functionally compared the phenotype of these GFP-high and GFP-low populations...
December 25, 2016: Oncotarget
https://www.readbyqxmd.com/read/28030597/enoblock-does-not-inhibit-the-activity-of-the-glycolytic-enzyme-enolase
#10
Nikunj Satani, Yu-Hsi Lin, Naima Hammoudi, Sudhir Raghavan, Dimitra K Georgiou, Florian L Muller
Inhibition of glycolysis is of great potential for the treatment of cancer. However, inhibitors of glycolytic enzymes with favorable pharmacological profiles have not been forthcoming. Due to the nature of their active sites, most high-affinity transition-state analogue inhibitors of glycolysis enzymes are highly polar with poor cell permeability. A recent publication reported a novel, non-active site inhibitor of the glycolytic enzyme Enolase, termed ENOblock (N-[2-[2-2-aminoethoxy)ethoxy]ethyl]4-4-cyclohexylmethyl)amino]6-4-fluorophenyl)methyl]amino]1,3,5-triazin-2-yl]amino]benzeneacetamide)...
2016: PloS One
https://www.readbyqxmd.com/read/28025745/microrna-98-suppress-warburg-effect-by-targeting-hk2-in-colon-cancer-cells
#11
Weimin Zhu, Yijiao Huang, Qi Pan, Pei Xiang, Nanlan Xie, Hao Yu
BACKGROUND: Warburg effect is a hallmark of cancer cells. Accumulating evidence suggests that microRNAs (miRs) could regulate such metabolic reprograming. Aberrant expression of miR-98 has been observed in many types of cancers. However, its functions and significance in colon cancer remain largely elusive. AIMS: To investigate miR-98 expression and the biological functions in colon cancer progression. METHODS: miR-98 expression levels were determined by quantitative RT-PCR in 215 cases of colon cancer samples...
December 26, 2016: Digestive Diseases and Sciences
https://www.readbyqxmd.com/read/28017777/the-cardioprotective-effect-of-sildenafil-is-mediated-by-the-activation-of-malate-dehydrogenase-and-an-increase-in-the-malate-aspartate-shuttle-in-cardiomyocytes
#12
Gevi Federica, Campolo Federica, Naro Fabio, Zolla Lello
Recent evidence has shown showed the cardioprotective effect of PDE5 inhibition in myocardial ischemia/reperfusion injury, heart failure and cardiac hypertrophy. To investigate the biochemical changes that occur during PDE5 inhibition in cardiac cells, this study assessed the metabolic profile of the HL1 cell line, a murine atrial cell line with adult cardiomyocyte properties. After one hour of treatment with sildenafil, glycolysis was moderately but selectively stimulated, unlike the pentose phosphate pathway and the Krebs cycle...
December 22, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/27997810/glut-1-dependent-glycolysis-is-increased-during-aging-related-lung-fibrosis-and-phloretin-inhibits-lung-fibrosis
#13
Soo Jung Cho, Jong-Seok Moon, Chang-Min Lee, Augustine M K Choi, Heather W Stout-Delgado
RATIONAL: Aging is associated with metabolic diseases such as type 2 diabetes mellitus, cardiovascular disease, cancer and neurodegeneration. Aging contributes to common processes including metabolic dysfunction, DNA damage and reactive oxygen species generation. While glycolysis has been linked to cell growth and proliferation, the mechanisms by which the activation of glycolysis by aging regulates fibrogenesis in lung remain unclear. OBJECTIVES: To determine if glucose transport 1 (GLUT1)-induced glycolysis regulates age-dependent fibrogenesis of the lung...
December 20, 2016: American Journal of Respiratory Cell and Molecular Biology
https://www.readbyqxmd.com/read/27997591/the-role-of-glucose-metabolism-on-porcine-oocyte-cytoplasmic-maturation-and-its-possible-mechanisms
#14
Bao Yuan, Shuang Liang, Jeong-Woo Kwon, Yong-Xun Jin, Shun-Ha Park, Hai-Yang Wang, Tian-Yi Sun, Jia-Bao Zhang, Nam-Hyung Kim
In the present study, we investigated the potential role of glucose and pyruvate in the cytoplasmic maturation of porcine oocytes by investigating the effect of glucose and/or pyruvate supplementation, in the presence or absence of 10% porcine follicular fluid (PFF), on meiotic maturation and subsequent embryo development. In the absence of 10% PFF, without exogenous addition of glucose and pyruvate, the medium seemed unable to support maturation. In the presence of 10% PFF, the addition of 5.6 mM glucose and/or 2 mM pyruvate during in vitro maturation of cumulus enclosed oocytes increased MII oocyte and blastocyst rates...
2016: PloS One
https://www.readbyqxmd.com/read/27989750/the-antioxidant-uncoupling-protein-2-stimulates-hnrnpa2-b1-glut1-and-pkm2-expression-and-sensitizes-pancreas-cancer-cells-to-glycolysis-inhibition
#15
Jessica Brandi, Daniela Cecconi, Marco Cordani, Margalida Torrens-Mas, Raffaella Pacchiana, Elisa Dalla Pozza, Giovanna Butera, Marcello Manfredi, Emilio Marengo, Jordi Oliver, Pilar Roca, Ilaria Dando, Massimo Donadelli
Several evidence indicate that metabolic alterations play a pivotal role in cancer development. Here, we report that the mitochondrial uncoupling protein 2 (UCP2) sustains the metabolic shift from mitochondrial oxidative phosphorylation (mtOXPHOS) to glycolysis in pancreas cancer cells. Indeed, we show that UCP2 sensitizes pancreas cancer cells to the treatment with the glycolytic inhibitor 2-deoxy-D-glucose. Through a bidimensional electrophoresis analysis, we identify 19 protein species differentially expressed after treatment with the UCP2 inhibitor genipin and, by bioinformatic analyses, we show that these proteins are mainly involved in metabolic processes...
October 27, 2016: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/27989748/nox4-supports-glycolysis-and-promotes-glutamine-metabolism-in-non-small-cell-lung-cancer-cells
#16
Cheng Zeng, Qipeng Wu, Jing Wang, Bei Yao, Lei Ma, Zhicheng Yang, Juan Li, Bing Liu
Our previous studies have confirmed that NADPH oxidase 4 (NOX4) is abundantly expressed in non-small cell lung cancer (NSCLC) and contributes to cancer progression. Nevertheless, the comprehensive mechanisms for NOX4-mediated malignant progression and oxidative resistance of cancer cells remain largely unknown. This study found that NOX4 directed glucose metabolism not only to the glycolysis but also to pentose phosphate pathway (PPP) pathway for production of NADPH in non-small cell lung cancer (NSCLC) cell lines...
October 27, 2016: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/27978620/reprogramming-the-transcriptional-response-to-hypoxia-with-a-chromosomally-encoded-cyclic-peptide-hif-1-inhibitor
#17
Ishna N Mistry, Ali Tavassoli
The cellular response to hypoxia is orchestrated by HIF-1, a heterodimeric transcription factor composed of an α and a β subunit that enables cell survival under low oxygen conditions by altering the transcription of over 300 genes. There is significant evidence that inhibition of HIF-1 would be beneficial for cancer therapy. We recently reported a cyclic hexapeptide that inhibits the HIF-1α/HIF-1β protein-protein interaction in vitro and prevents HIF-1-mediated hypoxia-response signaling in cells. This cyclic peptide was identified from a library of 3...
November 23, 2016: ACS Synthetic Biology
https://www.readbyqxmd.com/read/27965531/fatty-acid-biosynthesis-inhibition-increases-reduction-potential-in-neuronal-cells-under-hypoxia
#18
Stephen A Brose, Svetlana A Golovko, Mikhail Y Golovko
Recently, we have reported a novel neuronal specific pathway for adaptation to hypoxia through increased fatty acid (FA) biosynthesis followed by esterification into lipids. However, the biological role of this pathway under hypoxia remains to be elucidated. In the presented study, we have tested our hypothesis that activation of FA synthesis maintains reduction potential and reduces lactoacidosis in neuronal cells under hypoxia. To address this hypothesis, we measured the effect of FA synthesis inhibition on [Formula: see text]/NAD(+) and [Formula: see text]/NADP(+) ratios, and lactic acid levels in neuronal SH-SY5Y cells exposed to normoxic and hypoxic conditions...
2016: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/27959421/advances-in-the-targeting-of-hif-1%C3%AE-and-future-therapeutic-strategies-for-glioblastoma-multiforme-review
#19
Gang Wang, Jun-Jie Wang, Xing-Li Fu, Rui Guang, Shing-Shun Tony To
Cell metabolism can be reprogrammed by tissue hypoxia leading to cell transformation and glioblastoma multiforme (GBM) progression. In response to hypoxia, GBM cells are able to express a transcription factor called hypoxia inducible factor-1 (HIF-1). HIF-1 belongs to a family of heterodimeric proteins that includes HIF-1α and HIF-1β subunits. HIF-1α has been reported to play a pivotal role in GBM development and progression. In the present review, we discuss the role of HIF-1α in glucose uptake, cancer proliferation, cell mobility and chemoresistance in GBM...
February 2017: Oncology Reports
https://www.readbyqxmd.com/read/27938509/sorafenib-and-2-deoxyglucose-synergistically-inhibit-proliferation-of-both-sorafenib-sensitive-and-resistant-hcc-cells-by-inhibiting-atp-production
#20
Ryan Reyes, Nissar Wani, Kalpana Ghoshal, Samson Jacob, Tasneem Motiwala
Hepatocellular carcinoma (HCC) is one of the leading causes of cancer-related deaths globally. Sorafenib is the only first-line systemic drug for advanced HCC, but it has very limited survival benefits because patients treated with sorafenib either suffer from side effects or show disease progression after initial response. Thus, there is an urgent need to develop novel strategies for first-line and second-line therapy. The association between sorafenib resistance and glycolysis prompted us to screen several drugs with known anti-glycolytic activity to identify those that will sensitize cells to sorafenib...
16, 2016: Gene Expression
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