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Glycolysis inhibitors

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https://www.readbyqxmd.com/read/29151157/potent-apoptosis-inducing-activity-of-erypoegin-k-an-isoflavone-isolated-from-erythrina-poeppigiana-against-human-leukemia-hl-60-cells
#1
Kiyomi Hikita, Natsuki Hattori, Aya Takeda, Yuko Yamakage, Rina Shibata, Saori Yamada, Kuniki Kato, Tomiyasu Murata, Hitoshi Tanaka, Norio Kaneda
Erypoegin K is an isoflavone isolated from the stem bark of Erythrina poeppigiana. It contains a furan group at the A-ring of the core isoflavone structure and can inhibit the activity of glyoxalase I, an enzyme that catalyzes the detoxification of methylglyoxal (MG), a by-product of glycolysis. In the present study, we found that erypoegin K has a potent cytotoxic effect on human leukemia HL-60 cells. Its cytotoxic effect was much stronger than that of a known glyoxalase I inhibitor S-p-bromobenzylglutathione cyclopentyl diester...
November 18, 2017: Journal of Natural Medicines
https://www.readbyqxmd.com/read/29146491/respiratory-stress-in-mitochondrial-electron-transport-chain-complex-mutants-of-candida-albicans-activates-snf1-kinase-response
#2
Pengyi Zhang, Hongbin Li, Jie Cheng, April Y Sun, Liqing Wang, Gordana Mircevska, Richard Calderone, Dongmei Li
We have previously established that mitochondrial Complex I (CI) mutants of Candida albicans display reduced oxygen consumption, decreased ATP production, and increased reactive oxidant species (ROS) during cell growth. Using the Seahorse XF96 analyzer, the energetic phenotypes of Electron Transport Chain (ETC) complex mutants are further characterized in the current study. The underlying regulation of energetic changes in these mutants is determined in glucose and non-glucose conditions when compared to wild type (WT) cells...
November 13, 2017: Fungal Genetics and Biology: FG & B
https://www.readbyqxmd.com/read/29137417/inhibition-of-retinoic-acid-receptor-%C3%AE-signaling-confers-glycolytic-dependence-and-sensitization-to-dichloroacetate-in-melanoma-cells
#3
Cecilie Abildgaard, Christina Dahl, Ahmad Abdul-Al, Annette Christensen, Per Guldberg
Dysregulation of metabolism during melanoma progression is tightly associated with the acquisition of genetic and epigenetic alterations in regulators of metabolic pathways. Retinoic acid receptor beta (RARβ) is epigenetically silenced in a large proportion of melanomas, but a link between RARβ and metabolic rewiring of melanoma has not been established. Here, we show that in primary human melanocytes, all-trans retinoic acid (a RARβ agonist) induced growth inhibition accompanied by a decrease in both glycolytic and oxidative metabolism, whereas selective inhibition of RARβ led to an increase in the basal glycolytic rate and increased sensitivity to inhibition of glycolysis...
October 13, 2017: Oncotarget
https://www.readbyqxmd.com/read/29129024/metabolic-regulation-of-the-ccn-family-genes-by-glycolysis-in-chondrocytes
#4
Sho Akashi, Takashi Nishida, Abdellatif El-Seoudi, Masaharu Takigawa, Seiji Iida, Satoshi Kubota
The CCN family consists of 6 genes in the mammalian genome and produces multifunctional proteins involved in a variety of biological processes. Recent reports indicate the profound roles of CCN2 in energy metabolism in chondrocytes, and Ccn2 deficiency is known to alter the expression of 2 other family members including Ccn3. However, almost nothing is known concerning the regulation of the CCN family genes by energy metabolism. In order to gain insight into this critical issue, we initially and comprehensively evaluated the effect of inhibition of glycolysis on the expression of all of the CCN family genes in chondrocytic cells...
November 11, 2017: Journal of Cell Communication and Signaling
https://www.readbyqxmd.com/read/29121435/altered-intracellular-signaling-by-imatinib-increases-the-anti-cancer-effects-of-tyrosine-kinase-inhibitors-in-cml-cells
#5
Takuya Hirao, Masashi Yamaguchi, Megumi Kikuya, Hiroji Chibana, Kousei Ito, Shigeki Aoki
Tyrosine kinase inhibitors (TKIs), including imatinib (IM), improve the outcome of chronic myelogenous leukemia (CML) therapy. However, TKI treatment is long-term and can induce resistance to TKIs, which often leads to a poor clinical outcome in CML patients. Here, we examined the effect of continuous IM exposure on intracellular energy metabolism in K562 cells, a human Philadelphia chromosome-positive CML cell line, and its subsequent sensitivity to anti-cancer agents. Contrary to our expectations, we found that continuous IM exposure increased sensitivity to TKIs...
November 9, 2017: Cancer Science
https://www.readbyqxmd.com/read/29121144/positron-emission-tomography-computed-tomography-based-assessments-of-androgen-receptor-expression-and-glycolytic-activity-as-a-prognostic-biomarker-for-metastatic-castration-resistant-prostate-cancer
#6
Josef J Fox, Somali C Gavane, Estelle Blanc-Autran, Sadek Nehmeh, Mithat Gönen, Brad Beattie, Hebert A Vargas, Heiko Schöder, John L Humm, Samson W Fine, Jason S Lewis, Stephen B Solomon, Joseph R Osborne, Darren Veach, Charles L Sawyers, Wolfgang A Weber, Howard I Scher, Michael J Morris, Steven M Larson
Importance: Androgen receptor-signaling inhibitor (ARSi) drugs prolong life in metastatic castration-resistant prostate cancer (mCRPC), but such tumors eventually become resistant and progress. Comprehensive positron emission tomography/computed tomography (PET/CT) imaging using fluoro-2-D-deoxyglucose F 18 ([18F]-FDG) for glycolysis (Glyc) and fluorodihydrotestosterone F 18 ([18F]-FDHT) for androgen receptor (AR) expression determine heterogeneity of imaging phenotypes, which may be useful in distinguishing patients who will benefit from ARSi drugs from those who need alternative treatments...
November 9, 2017: JAMA Oncology
https://www.readbyqxmd.com/read/29120638/discovery-and-optimization-of-potent-cell-active-pyrazole-based-inhibitors-of-lactate-dehydrogenase-ldh
#7
Ganesha Rai, Kyle R Brimacombe, Bryan T Mott, Daniel J Urban, Xin Hu, Shyh-Ming Yang, Tobie D Lee, Dorian M Cheff, Jennifer Kouznetsova, Gloria A Benavides, Katie Pohida, Eric J Kuenstner, Diane K Luci, Christine M Lukacs, Douglas R Davies, David M Dranow, Hu Zhu, Gary Sulikowski, William J Moore, Gordon M Stott, Andrew J Flint, Matthew D Hall, Victor M Darley-Usmar, Leonard M Neckers, Chi V Dang, Alex G Waterson, Anton Simeonov, Ajit Jadhav, David J Maloney
We report the discovery and medicinal chemistry optimization of a novel series of pyrazole-based inhibitors of human lactate dehydrogenase (LDH). Utilization of a quantitative high-throughput screening paradigm facilitated hit identification, while structure-based design and multiparameter optimization enabled the development of compounds with potent enzymatic and cell-based inhibition of LDH enzymatic activity. Lead compounds such as 63 exhibit low nM inhibition of both LDHA and LDHB, submicromolar inhibition of lactate production, and inhibition of glycolysis in MiaPaCa2 pancreatic cancer and A673 sarcoma cells...
November 9, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29117556/cdk8-kinase-activity-promotes-glycolysis
#8
Matthew D Galbraith, Zdenek Andrysik, Ahwan Pandey, Maria Hoh, Elizabeth A Bonner, Amanda A Hill, Kelly D Sullivan, Joaquín M Espinosa
Aerobic glycolysis, also known as the Warburg effect, is a hallmark of cancerous tissues. Despite its importance in cancer development, our understanding of mechanisms driving this form of metabolic reprogramming is incomplete. We report here an analysis of colorectal cancer cells engineered to carry a single point mutation in the active site of the Mediator-associated kinase CDK8, creating hypomorphic alleles sensitive to bulky ATP analogs. Transcriptome analysis revealed that CDK8 kinase activity is required for the expression of many components of the glycolytic cascade...
November 7, 2017: Cell Reports
https://www.readbyqxmd.com/read/29113354/6-phosphofructo-2-kinase-fructose-2-6-bisphosphatase-isoform-3-spatially-mediates-autophagy-through-the-ampk-signaling-pathway
#9
Siyuan Yan, Xiaoli Wei, Shanshan Xu, Hui Sun, Weijun Wang, Ling Liu, Xuejun Jiang, Yongxiang Zhang, Yongsheng Che
6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase isoform 3 (PFKFB3), is a critical enzyme for glycolysis and highly expressed in cancer cells. It plays an essential role in regulating metabolism, angiogenesis, and inflammation. Although PFKFB3 is involved in modulating autophagy, its regulatory role appears to be either positive or negative, which remains to be clarified. Unlike other PFK-2/FBPase isoforms, PFKFB3 can localize in both nucleus and cytoplasm, leading to the speculation that subcellular localization of PFKFB3 may play a regulatory role in autophagy...
October 6, 2017: Oncotarget
https://www.readbyqxmd.com/read/29109024/ampk-regulates-immunometabolism-in-sepsis
#10
Jun Huang, Ke Liu, Shan Zhu, Min Xie, Rui Kang, Lizhi Cao, Daolin Tang
Sepsis and septic shock remain challenging for intensive care units worldwide and have limited treatment options; therefore, identification of targetable key players in systemic inflammation and multiple organ failure is urgently needed. Here, we show that AMP-activated protein kinase (AMPK) is a negative regulator of bioenergetic reprogramming in immune cells and suppresses sepsis development in vivo. Mechanistically, AMPK deficiency increases pyruvate kinase isozyme M2 (PKM2)-dependent aerobic glycolysis, which leads to the release of high mobility group box 1 (HMGB1, a late mediator of lethal systemic inflammation) in macrophages and monocytes...
November 3, 2017: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/29108965/interleukin-1-inhibitory-kappa-b-kinase-epsilon-induced-glycolysis-augment-epithelial-effector-function-and-promote-allergic-airways-disease
#11
Xi Qian, Reem Aboushousha, Cheryl van de Wetering, Shi B Chia, Eyal Amiel, Robert W Schneider, Jos Lj van der Velden, Karolyn G Lahue, Daisy A Hoagland, Dylan T Casey, Nirav Daphtary, Jennifer L Ather, Matthew J Randall, Minara Aliyeva, Kendall E Black, David G Chapman, Lennart K A Lundblad, David H McMillan, Anne E Dixon, Vikas Anathy, Charles G Irvin, Matthew E Poynter, Emiel F M Wouters, Pamela M Vacek, Monique Henket, Florence Schleich, Renaud Louis, Albert van der Vliet, Yvonne M W Janssen-Heininger
BACKGROUND: Emerging studies suggest that enhanced glycolysis accompanies inflammatory responses. Virtually nothing is known about the relevance of glycolysis in allergic asthma. OBJECTIVES: Here we sought to determine if glycolysis is altered in allergic asthma and to address its importance in the pathogenesis of allergic asthma. METHODS: We examined alterations in glycolysis in sputum samples from asthmatics and primary human nasal cells, and used murine models of allergic asthma as well as primary mouse tracheal epithelial cells to evaluate the relevance of glycolysis...
November 3, 2017: Journal of Allergy and Clinical Immunology
https://www.readbyqxmd.com/read/29107073/immunometabolic-determinants-of-chemoradiotherapy-response-and-survival-in-head-and-neck-squamous-cell-carcinoma
#12
Rosemarie Krupar, Matthias G Hautmann, Ravi R Pathak, Indu Varier, Cassandra McLaren, Doris Gaag, Claus Hellerbrand, Matthias Evert, Simon Laban, Christian Idel, Vlad Sandulache, Sven Perner, Anja K Bosserhoff, Andrew G Sikora
Tumor immune microenvironment and tumor metabolism are major determinants of chemoradiotherapy response. The interdependency and prognostic significance of specific immune and metabolic phenotypes in head and neck squamous cell carcinoma (HNSCC) were assessed and changes in reactive oxygen species were evaluated as a mechanism of treatment response in tumor spheroid/immunocyte co-cultures. Pretreatment tumor biopsies were immunohistochemically characterized in 73 HNSCC patients treated by definitive chemoradiotherapy and correlated with survival...
October 27, 2017: American Journal of Pathology
https://www.readbyqxmd.com/read/29106036/inhibition-of-mitochondrial-complex-i-improves-glucose-metabolism-independently-of-ampk-activation
#13
Wo-Lin Hou, Jun Yin, Miriayi Alimujiang, Xue-Ying Yu, Li-Gen Ai, Yu-Qian Bao, Fang Liu, Wei-Ping Jia
Accumulating evidences showed metformin and berberine, well-known glucose-lowering agents, were able to inhibit mitochondrial electron transport chain at complex I. In this study, we aimed to explore the antihyperglycaemic effect of complex I inhibition. Rotenone, amobarbital and gene silence of NDUFA13 were used to inhibit complex I. Intraperitoneal glucose tolerance test and insulin tolerance test were performed in db/db mice. Lactate release and glucose consumption were measured to investigate glucose metabolism in HepG2 hepatocytes and C2C12 myotubes...
November 6, 2017: Journal of Cellular and Molecular Medicine
https://www.readbyqxmd.com/read/29100699/glucose-starvation-impairs-dna-repair-in-tumour-cells-selectively-by-blocking-histone-acetylation
#14
Rena Ampferl, Hans Peter Rodemann, Claus Mayer, Tobias Tim Alexander Höfling, Klaus Dittmann
BACKGROUND AND PURPOSE: Tumour cells are characterized by aerobic glycolysis and thus have high glucose consumption. Because repairing radiation-induced DNA damage is an energy-demanding process, we hypothesized that glucose starvation combined with radiotherapy could be an effective strategy to selectively target tumour cells. MATERIAL AND METHODS: We glucose-starved tumour cells (A549, FaDu) in vitro and analysed their radiation-induced cell responses compared to normal fibroblasts (HSF7)...
October 31, 2017: Radiotherapy and Oncology: Journal of the European Society for Therapeutic Radiology and Oncology
https://www.readbyqxmd.com/read/29100387/metabolic-modulation-of-ewing-sarcoma-cells-inhibits-tumor-growth-and-stem-cell-properties
#15
Atreyi Dasgupta, Matteo Trucco, Nino Rainusso, Ronald J Bernardi, Ryan Shuck, Lyazat Kurenbekova, David M Loeb, Jason T Yustein
Ewing sarcoma (EWS) is a highly aggressive and metabolically active malignant tumor. Metabolic activity can broadly be characterized by features of glycolytic activity and oxidative phosphorylation. We have further characterized metabolic features of EWS cells to identify potential therapeutic targets. EWS cells had significantly more glycolytic activity compared to their non-malignant counterparts. Thus, metabolic inhibitors of glycolysis such as 2-deoxy-D-glucose (2DG) and of the mitochondrial respiratory pathway, such as metformin, were evaluated as potential therapeutic agents against a panel of EWS cell lines in vitro...
September 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/29095437/metformin-ameliorates-arsenic-trioxide-hepatotoxicity-via-inhibiting-mitochondrial-complex-i
#16
Sunbin Ling, Qiaonan Shan, Peng Liu, Tingting Feng, Xuanyu Zhang, Penghui Xiang, Kangchen Chen, Haiyang Xie, Penghong Song, Lin Zhou, Jimin Liu, Shusen Zheng, Xiao Xu
Arsenic trioxide (ATO) is a well-accepted chemotherapy agent in managing promyelocytic leukemia. ATO often causes severe health hazards such as hepatotoxicity, dermatosis, neurotoxicity, nephrotoxicity and cardiotoxicity. The production of reactive oxygen species, (ROS) play a significant role in ATO-induced hepatotoxicity. The oral hypoglycemic drug, metformin, is considered to be a potential novel agent for chemoprevention in the treatment of cancer. Moreover, metformin has also been shown to have hepatoprotective effects...
November 2, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/29093638/inhibition-of-hif1%C3%AE-and-pdk-induces-cell-death-of-glioblastoma-multiforme
#17
Jiwon Esther Han, Pyung Won Lim, Chul Min Na, You Sik Choi, Joo Young Lee, Yona Kim, Hyung Woo Park, Hyo Eun Moon, Man Seung Heo, Hye Ran Park, Dong Gyu Kim, Sun Ha Paek
Glioblastoma multiforme (GBM) is the most common and aggressive form of brain tumors. GBMs, like other tumors, rely relatively less on mitochondrial oxidative phosphorylation (OXPHOS) and utilize more aerobic glycolysis, and this metabolic shift becomes augmented under hypoxia. In the present study, we investigated the physiological significance of altered glucose metabolism and hypoxic adaptation in the GBM cell line U251 and two newly established primary GBMs (GBM28 and GBM37). We found that these three GBMs exhibited differential growth rates under hypoxia compared to those under normoxia...
October 2017: Experimental Neurobiology
https://www.readbyqxmd.com/read/29080556/a-new-mutation-independent-approach-to-cancer-therapy-inhibiting-oncogenic-ras-and-myc-by-targeting-mitochondrial-biogenesis
#18
Bela Ozsvari, Federica Sotgia, Michael P Lisanti
Here, we used MCF7 cells as a model system to interrogate how MYC/RAS co-operativity contributes to metabolic flux and stemness in breast cancer cells. We compared the behavior of isogenic MCF7 cell lines transduced with c-Myc or H-Ras (G12V), either individually or in combination. Cancer stem cell (CSC) activity was measured using the mammosphere assay. c-Myc augmented both mammosphere formation and mitochondrial respiration, without any effects on glycolytic flux. In contrast, H-Ras (G12V) synergistically augmented both mammosphere formation and glycolysis, but only in combination with c-Myc, directly demonstrating MYC/RAS co-operativity...
October 27, 2017: Aging
https://www.readbyqxmd.com/read/29078269/ko-of-5-insp7-kinase-activity-transforms-the-hct116-colon-cancer-cell-line-into-a-hypermetabolic-growth-inhibited-phenotype
#19
Chunfang Gu, Hoai-Nghia Nguyen, Douglas Ganini, Zhaowei Chen, Henning J Jessen, Zhen Gu, Huanchen Wang, Stephen B Shears
The inositol pyrophosphates 5-InsP7 (diphosphoinositol pentakisphosphate) and 1,5-InsP8 (bis-diphosphoinositol tetrakisphosphate) are highly energetic cellular signals interconverted by the diphosphoinositol pentakisphosphate kinases (PPIP5Ks). Here, we used CRISPR to KO PPIP5Ks in the HCT116 colon cancer cell line. This procedure eliminates 1,5-InsP8 and raises 5-InsP7 levels threefold. Expression of p53 and p21 was up-regulated; proliferation and G1/S cell-cycle transition slowed. Thus, PPIP5Ks are potential targets for tumor therapy...
October 25, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/29077242/contribution-of-the-%C3%AE-glucosidase-bglc-to-the-onset-of-the-pathogenic-lifestyle-of-streptomyces-scabies
#20
Samuel Jourdan, Isolde M Francis, Benoit Deflandre, Elodie Tenconi, Jennifer Riley, Sören Planckaert, Pierre Tocquin, Loïc Martinet, Bart Devreese, Rosemary Loria, Sébastien Rigali
Common scab disease on root and tuber plants is caused by Streptomyces scabies and related species which use the cellulose synthase inhibitor thaxtomin A as the main phytotoxin. Thaxtomin production is primarily triggered by the import of cello-oligosaccharides. Once inside the cell, the fate of the cello-oligosaccharides is dichotomized into i) fueling glycolysis with glucose for the saprophytic lifestyle through the action of β-glucosidase(s) (BG), and ii) eliciting the pathogenic lifestyle by inhibiting the CebR-mediated transcriptional repression of thaxtomin biosynthetic genes...
October 27, 2017: Molecular Plant Pathology
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