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Glycolysis inhibitors

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https://www.readbyqxmd.com/read/28433696/foxc2-positively-regulates-yap-signaling-and-promotes-the-glycolysis-of-nasopharyngeal-carcinoma
#1
Lijuan Song, Hongbo Tang, Wenjing Liao, Xinggu Luo, Yanmei Li, Tao Chen, Xiaowen Zhang
YAP signaling has been reported to be dysregulated in numerous cancer types. However, its roles in nasopharyngeal carcinoma (NPC) are poorly understood. Although several studies have shown that FOXC2 promotes the progression of NPC, the underlying molecular mechanism remains largely unknown. Here, we have shown that FOXC2 interacted with YAP and TEAD, and activated YAP signaling. Furthermore, FOXC2-YAP signaling positively regulated the expression of Hexokinase 2 (HK2) and promoted the glycolysis. Moreover, the inhibitor of HK2, 3-BrPA effectively inhibited the tumorigenesis of NPC cells in vitro and in vivo...
April 19, 2017: Experimental Cell Research
https://www.readbyqxmd.com/read/28427443/benserazide-a-dopadecarboxylase-inhibitor-suppresses-tumor-growth-by-targeting-hexokinase-2
#2
Wei Li, Mengzhu Zheng, Shuangping Wu, Suyu Gao, Mei Yang, Zhimei Li, Qiuxia Min, Weiguang Sun, Lixia Chen, Guangya Xiang, Hua Li
BACKGROUND: Hexokinase (HK) is the rate-limiting enzyme in the first reaction of glycolysis. And Hexokinase 2 (HK2) is most closely related to malignant tumor which expresses at higher level compared with normal cells. HK2 plays a pivotal role in tumor initiation and maintenance, which provides a new target for cancer therapy. METHODS: Structure-based virtual ligand screening was used in hit identification from ZINC Drug Database. Microscale thermophoresis assay was performed to evaluate the binding affinity...
April 20, 2017: Journal of Experimental & Clinical Cancer Research: CR
https://www.readbyqxmd.com/read/28423651/succinate-dehydrogenase-b-deficient-cancer-cells-are-highly-sensitive-to-bromodomain-and-extra-terminal-inhibitors
#3
Satoshi Kitazawa, Shunsuke Ebara, Ayumi Ando, Yuji Baba, Yoshinori Satomi, Tomoyoshi Soga, Takahito Hara
Mutations in succinate dehydrogenase B (SDHB) gene are frequently observed in several tumors and associated with poor prognosis in these tumors. Therefore, drugs effective for SDHB-deficient tumors could fulfill an unmet medical need. In addition, such drugs would have an advantage in that selection of patients with SDHB-mutant cancer could increase the probability of success in clinical trials. Currently, however, the characteristics of SDHB-deficient cancers are not completely understood. Here, we established SDHB knockout cancer cell lines from human colon cancer HCT116 cells using the clustered regularly interspaced short palindromic repeat (CRISPR)/Cas9 knockout system, and clarified its metabolic characteristics...
March 7, 2017: Oncotarget
https://www.readbyqxmd.com/read/28413646/role-of-malate-dehydrogenase-in-facilitating-lactate-dehydrogenase-to-support-the-glycolysis-pathway-in-tumors
#4
Siavash Mansouri, Ali Shahriari, Hadi Kalantar, Taraneh Moini Zanjani, Mojtaba Haghi Karamallah
High aerobic glycolysis, as one of the hallmarks of cancer cells, requires nicotinamide adenine dinucleotide (NAD(+)) as a vital co-factor, to guarantee the flow of glycolysis. Malate dehydrogenase (MDH), as an important enzyme in cancer metabolism, is a source of NAD(+) additional to lactate dehydrogenase (LDH). The current study aimed to elucidate the kinetic parameters of MDH in human breast cancer and evaluate its supportive role in the glycolysis pathway. The Michaelis-Menten constant (Km) and maximum velocity (Vmax) of MDH were determined in the crude extracts of human breast tumors and healthy tissue samples, which were obtained directly from the operating theatre...
April 2017: Biomedical Reports
https://www.readbyqxmd.com/read/28409826/glycogen-phosphorylase-inhibition-improves-%C3%AE-cell-function
#5
Lilla Nagy, Judit Márton, András Vida, Gréta Kis, Éva Bokor, Sándor Kun, Mónika Gönczi, Tibor Docsa, Attila Tóth, Miklós Antal, Pál Gergely, Balázs Csóka, Pal Pacher, László Somsák, Péter Bai
BACKGROUND AND PURPOSE: Glycogen phosphorylase (GP) is the key enzyme for glycogen degradation. GP inhibitors (GPi-s) are glucose lowering agents trapping glucose in the liver as glycogen. Glycogen metabolism has implications in β-cell function; glycogen degradation can maintain cellular glucose levels, which feeds into catabolism to maintain insulin secretion, and elevated glycogen degradation levels contribute to glucotoxicity. The purpose of this study was to assess whether influencing glycogen metabolism in β-cells by GPi-s impacts β-cell function...
April 13, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28399896/glutaminase-1-plays-a-key-role-in-the-cell-growth-of-fibroblast-like-synoviocytes-in-rheumatoid-arthritis
#6
Soshi Takahashi, Jun Saegusa, Sho Sendo, Takaichi Okano, Kengo Akashi, Yasuhiro Irino, Akio Morinobu
BACKGROUND: The recent findings of cancer-specific metabolic changes, including increased glucose and glutamine consumption, have provided new therapeutic targets for consideration. Fibroblast-like synoviocytes (FLS) from rheumatoid arthritis (RA) patients exhibit several tumor cell-like characteristics; however, the role of glucose and glutamine metabolism in the aberrant proliferation of these cells is unclear. Here, we evaluated the role of these metabolic pathways in RA-FLS proliferation and in autoimmune arthritis in SKG mice...
April 11, 2017: Arthritis Research & Therapy
https://www.readbyqxmd.com/read/28392736/preanalytical-external-quality-assessment-of-the-croatian-society-of-medical-biochemistry-and-laboratory-medicine-and-croqalm-finding-undetected-weak-spots
#7
Nora Nikolac, Jasna Lenicek Krleza, Ana-Maria Simundic
INTRODUCTION: The aim of this paper is to present results of first two years of preanalytical external quality assessment (EQA) in Croatia. MATERIALS AND METHODS: This paper summarizes results from 6 rounds of preanalytical EQA during 2014-2016 in 161-175 Croatian laboratories (number ranged between cycles). EQA was designed as an online survey of the compliance with National recommendations for phlebotomy (NRP). Forty-seven questions in 5 categories are analyzed (materials and equipment, patient identification, patient preparation, sampling and storage)...
February 15, 2017: Biochemia Medica: časopis Hrvatskoga Društva Medicinskih Biokemičara
https://www.readbyqxmd.com/read/28388555/targeting-mantle-cell-lymphoma-metabolism-and-survival-through-simultaneous-blockade-of-mtor-and-nuclear-transporter-exportin-1
#8
Kazumasa Sekihara, Kaori Saitoh, Lina Han, Stefan Ciurea, Shinichi Yamamoto, Mika Kikkawa, Saiko Kazuno, Hikari Taka, Naoko Kaga, Hajime Arai, Takashi Miida, Michael Andreeff, Marina Konopleva, Yoko Tabe
Mantle cell lymphoma (MCL) is an aggressive B-cell lymphoma with poor prognosis, characterized by aberrant expression of growth-regulating and oncogenic effectors and requiring novel anticancer strategies. The nuclear transporter exportin-1 (XPO1) is highly expressed in MCL and is associated with its pathogenesis. mTOR signaling, a central regulator of cell metabolism, is frequently activated in MCL and is also an important therapeutic target in this cancer. This study investigated the antitumor effects and molecular/metabolic changes induced by the combination of the small-molecule selective inhibitor XPO1 inhibitor KPT-185 and the dual mTORC1/2 kinase inhibitor AZD-2014 on MCL cells...
March 27, 2017: Oncotarget
https://www.readbyqxmd.com/read/28387379/relationship-between-porcine-sperm-motility-and-sperm-enzymatic-activity-using-paper-based-devices
#9
Koji Matsuura, Han-Wei Huang, Ming-Cheng Chen, Yu Chen, Chao-Min Cheng
Mammalian sperm motility has traditionally been analyzed to determine fertility using computer-assisted semen analysis (CASA) systems. To develop low-cost and robust male fertility diagnostics, we created a paper-based MTT assay and used it to estimate motile sperm concentration. When porcine sperm motility was inhibited using sperm enzyme inhibitors for sperm enzymes related to mitochondrial activity and glycolysis, we simultaneously recorded sperm motility and enzymatic reactivity using a portable motility analysis system (iSperm) and a paper-based MTT assay, respectively...
April 7, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28385782/inhibition-of-monocarboxylate-transporter-1-by-azd3965-as-a-novel-therapeutic-approach-for-the-treatment-of-diffuse-large-b-cell-lymphoma-and-burkitt-lymphoma
#10
Richard A Noble, Natalie Bell, Helen Blair, Arti Sikka, Huw Thomas, Nicole Phillips, Sirintra Nakjang, Satomi Miwa, Rachel Crossland, Vikki Rand, Despina Televantou, Anna Long, Hector C Keun, Chris M Bacon, Simon Bomken, Susan E Critchlow, Stephen R Wedge
Inhibition of monocarboxylate transporter 1 has been proposed as a therapeutic approach to perturb lactate shuttling in tumor cells that lack monocarboxylate transporter 4. We examined the monocarboxylate transporter 1 inhibitor AZD3965, currently in phase I clinical studies, as a potential therapy for diffuse large B-cell lymphoma and Burkitt lymphoma. Whilst extensive monocarboxylate transporter 1 protein was found in 120 diffuse large B-cell lymphoma and 10 Burkitt lymphoma patient tumors, monocarboxylate transporter 4 protein expression was undetectable in 73% of the diffuse large B-cell lymphoma samples and undetectable or negligible in each Burkitt lymphoma sample...
April 6, 2017: Haematologica
https://www.readbyqxmd.com/read/28382170/obatoclax-and-ly3009120-efficiently-overcome-vemurafenib-resistance-in-differentiated-thyroid-cancer
#11
Wei-Jun Wei, Zhen-Kui Sun, Chen-Tian Shen, Hong-Jun Song, Xin-Yun Zhang, Zhong-Ling Qiu, Quan-Yong Luo
Although the prognosis of differentiated thyroid cancer (DTC) is relatively good, 30-40% of patients with distant metastases develop resistance to radioactive iodine therapy due to tumor dedifferentiation. For DTC patients harboring BRAF(V600E) mutation, Vemurafenib, a BRAF kinase inhibitor, has dramatically changed the therapeutic landscape, but side effects and drug resistance often lead to termination of the single agent treatment. In the present study, we showed that either LY3009120 or Obatoclax (GX15-070) efficiently inhibited cell cycle progression and induced massive death of DTC cells...
2017: Theranostics
https://www.readbyqxmd.com/read/28376210/estrogen-receptor-%C3%AE-as-a-therapeutic-target-in-breast-cancer-stem-cells
#12
Ran Ma, Govindasamy-Muralidharan Karthik, John Lövrot, Felix Haglund, Gustaf Rosin, Anne Katchy, Xiaonan Zhang, Lisa Viberg, Jan Frisell, Cecilia Williams, Stig Linder, Irma Fredriksson, Johan Hartman
Background: Breast cancer cells with tumor-initiating capabilities (BSCs) are considered to maintain tumor growth and govern metastasis. Hence, targeting BSCs will be crucial to achieve successful treatment of breast cancer. Methods: We characterized mammospheres derived from more than 40 cancer patients and two breast cancer cell lines for the expression of estrogen receptors (ERs) and stem cell markers. Mammosphere formation and proliferation assays were performed on cells from 19 cancer patients and five healthy individuals after incubation with ER-subtype selective ligands...
March 1, 2017: Journal of the National Cancer Institute
https://www.readbyqxmd.com/read/28373542/biosynthesis-of-the-pyrrolidine-protein-synthesis-inhibitor-anisomycin-involves-novel-gene-ensemble-and-cryptic-biosynthetic-steps
#13
Xiaoqing Zheng, Qiuxiang Cheng, Fen Yao, Xiaozheng Wang, Lingxin Kong, Bo Cao, Min Xu, Shuangjun Lin, Zixin Deng, Yit-Heng Chooi, Delin You
The protein synthesis inhibitor anisomycin features a unique benzylpyrrolidine system and exhibits diverse biological and pharmacologic activities. Its biosynthetic origin has remained obscure for more than 60 y, however. Here we report the identification of the biosynthetic gene cluster (BGC) of anisomycin in Streptomyces hygrospinosus var. beijingensis by a bioactivity-guided high-throughput screening method. Using a combination of bioinformatic analysis, reverse genetics, chemical analysis, and in vitro biochemical assays, we have identified a core four-gene ensemble responsible for the synthesis of the pyrrolidine system in anisomycin: aniQ, encoding a aminotransferase that catalyzes an initial deamination and a later reamination steps; aniP, encoding a transketolase implicated to bring together an glycolysis intermediate with 4-hydroxyphenylpyruvic acid to form the anisomycin molecular backbone; aniO, encoding a glycosyltransferase that catalyzes a cryptic glycosylation crucial for downstream enzyme processing; and aniN, encoding a bifunctional dehydrogenase that mediates multistep pyrrolidine formation...
April 3, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28371597/role-of-proton-pumps-in-tumorigenesis
#14
REVIEW
V A Kobliakov
One of the differences between normal and cancer cells is lower pH of the extracellular space in tumors. Low pH in the extracellular space activates proteases and stimulates tumor invasion and metastasis. Tumor cells display higher level of the HIF1α transcription factor that promotes cell switch from mitochondrial respiration to glycolysis. The terminal product of glycolysis is lactate. Lactate formation from pyruvate is catalyzed by the specific HIF1α-dependent isoform of lactate dehydrogenase A. Because lactate accumulation is deleterious for the cell, it is actively exported by monocarboxylate transporters...
April 2017: Biochemistry. Biokhimii︠a︡
https://www.readbyqxmd.com/read/28368517/enhanced-glycolytic-metabolism-contributes-to-cardiac-dysfunction-in-polymicrobial-sepsis
#15
Zhibo Zheng, He Ma, Xia Zhang, Fei Tu, Xiaohui Wang, Tuanzhu Ha, Min Fan, Li Liu, Jingjing Xu, Kaiking Yu, Ruitao Wang, John Kalbfleisch, Race Kao, David Williams, Chuanfu Li
Background: Cardiac dysfunction is present in >40% of sepsis patients and is associated with mortality rates of up to 70%. Recent evidence suggests that glycolytic metabolism plays a critical role in host defense and inflammation. Activation of Toll-like receptors on immune cells can enhance glycolytic metabolism. This study investigated whether modulation of glycolysis by inhibition of hexokinase will be beneficial to septic cardiomyopathy. Methods: Male C57B6/J mice were treated with a hexokinase inhibitor (2-deoxy-D-glucose, 2-DG, 0...
March 22, 2017: Journal of Infectious Diseases
https://www.readbyqxmd.com/read/28356961/2-deoxyglucose-and-sorafenib-synergistically-suppress-the-proliferation-and-motility-of-hepatocellular-carcinoma-cells
#16
Minoru Tomizawa, Fuminobu Shinozaki, Yasufumi Motoyoshi, Takao Sugiyama, Shigenori Yamamoto, Naoki Ishige
Cancer cells consume more glucose than normal cells, mainly due to their increased rate of glycolysis. 2-Deoxy-d-glucose (2DG) is an analogue of glucose, and sorafenib is a kinase inhibitor and molecular agent used to treat hepatocellular carcinoma (HCC). The present study aimed to demonstrate whether combining 2DG and sorafenib suppresses tumor cell proliferation and motility more effectively than either drug alone. HLF and PLC/PRF/5 HCC cells were incubated with sorafenib with or without 1 µM 2DG, and subjected to a proliferation assay...
February 2017: Oncology Letters
https://www.readbyqxmd.com/read/28350075/co-treatment-of-breast-cancer-cells-with-pharmacologic-doses-of-2-deoxy-d-glucose-and-metformin-starving-tumors
#17
Ulrike Wokoun, Martin Hellriegel, Günter Emons, Carsten Gründker
A characteristic of tumor cells is the increased aerobic glycolysis for energy production. Thus, inhibition of glycolysis represents a selective therapeutic option. It has been shown that glycolysis inhibitor 2-deoxy-D-glucose (2DG) induces apoptotic cell death in different tumor entities. In addition, the antitumor activity of the anti-diabetic drug metformin has been demonstrated. In the present study, we aimed to ascertain whether the combination of pharmacologic doses of 2DG with metformin increases the antitumor efficacy...
April 2017: Oncology Reports
https://www.readbyqxmd.com/read/28348059/the-glycolytic-enzyme-pfkfb3-is-involved-in-estrogen-mediated-angiogenesis-via-gper1
#18
Annalisa Trenti, Serena Tedesco, Carlotta Boscaro, Nicola Ferri, Andrea Cignarella, Lucia Trevisi, Chiara Bolego
The endogenous estrogen 17β-estradiol (E2) is a key factor in promoting endothelial healing and angiogenesis. Recently, proangiogenic signals including vascular endothelial growth factor and others have been shown to converge onto endothelial cell metabolism. Because inhibition of the glycolytic enzyme activator phosphofructokinase-2/fructose-2,6-bisphosphatase 3 (PFKFB3) reduces pathological angiogenesis and estrogen receptor (ER) signaling stimulates glucose uptake and glycolysis by inducing PFKFB3 in breast cancer, we hypothesized that E2 triggers angiogenesis in endothelial cells via rapid ER signaling that requires PFKFB3 as a downstream effector...
March 27, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28347773/synthesis-and-biological-evaluation-of-r-3-3-3-trifluoro-2-hydroxy-2-methylpropionamides-as-pyruvate-dehydrogenase-kinase-1-pdk1-inhibitors-to-reduce-the-growth-of-cancer-cells
#19
Shao-Lin Zhang, Wen Zhang, Zheng Yang, Xiaohui Hu, Kin Yip Tam
Most cancer cells exhibit a high rate of glycolysis and reduced capacity in mitochondrial oxidative phosphorylation. The expression of pyruvate dehydrogenase kinases (PDKs) was found to be increased in many cancer cells. Inhibition of PDKs increases the oxidative phosphorylation of glucose, which may disrupt the balance between the demand and supply of oxygen in cancer cell, thus leading to cell death. Several reports suggested that compounds containing (R)-3,3,3-trifluoro-2-hydroxy-2-methylpropionamide group could inhibit PDKs in pyruvate dehydrogenase primary enzymatic assay...
March 24, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28343085/guava-fruit-extract-and-its-triterpene-constituents-have-osteoanabolic-effect-stimulation-of-osteoblast-differentiation-by-activation-of-mitochondrial-respiration-via-the-wnt-%C3%AE-catenin-signaling
#20
Konica Porwal, Subhashis Pal, Kapil Dev, Shyamsundar Pal China, Yogesh Kumar, Chandan Singh, Tarun Barbhuyan, Neeraj Sinha, Sabyasachi Sanyal, Arun Kumar Trivedi, Rakesh Maurya, Naibedya Chattopadhyay
The aim of this study was to evaluate the skeletal effect of guava triterpene-enriched extract (GE) in rats and identify osteogenic compounds thereof, and determine their modes of action. In growing female rats, GE at 250 mg/kg dose increased parameters of peak bone mass including femur length, bone mineral density (BMD) and biomechanical strength, suggesting that GE promoted modeling-directed bone growth. GE also stimulated bone regeneration at the site of bone injury. In adult osteopenic rats (osteopenia induced by ovariectomy, OVX) GE completely restored the lost bones at both axial and appendicular sites, suggesting a strong osteoanabolic effect...
March 8, 2017: Journal of Nutritional Biochemistry
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