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3 bromopyruvate

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https://www.readbyqxmd.com/read/28816773/synergistic-antitumor-effect-of-3-bromopyruvate-and-5-fluorouracil-against-human-colorectal-cancer-through-cell-cycle-arrest-and-induction-of-apoptosis
#1
Dianlong Chong, Linyan Ma, Fang Liu, Zhirui Zhang, Surong Zhao, Qiang Huo, Pei Zhang, Hailun Zheng, Hao Liu
3-Bromopyruvic acid (3-BP) is a well-known inhibitor of energy metabolism. It has been proposed as an anticancer agent as well as a chemosensitizer for use in combination with anticancer drugs. 5-Fluorouracil (5-FU) is the first-line chemotherapeutic agent for colorectal cancer; however, most patients develop resistance to 5-FU through various mechanisms. The aim of this study was to investigate whether 3-BP has a synergistic antitumor effect with 5-FU on human colorectal cancer cells. In our study, combined 3-BP and 5-FU treatment upregulated p53 and p21, whereas cyclin-dependent kinase CDK4 and CDK2 were downregulated, which led to G0/G1 phase arrest...
September 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28733531/dual-inhibition-of-glycolysis-and-glutaminolysis-as-a-therapeutic-strategy-in-the-treatment-of-ovarian-cancer
#2
Li Sun, Yajie Yin, Leslie H Clark, Wenchuan Sun, Stephanie A Sullivan, Arthur-Quan Tran, Jianjun Han, Lu Zhang, Hui Guo, Esther Madugu, Tommy Pan, Amanda L Jackson, Joshua Kilgore, Hannah M Jones, Timothy P Gilliam, Chunxiao Zhou, Victoria L Bae-Jump
Cancer cell metabolism is required to support the biosynthetic demands of cell growth and cell division, and to maintain reduction oxidaton (redox) homeostasis. This study was designed to test the effects of glucose and glutamine on ovarian cancer cell growth and explore the inter-relationship between glycolysis and glutaminolysis. The SKOV3, IGROV-1 and Hey ovarian cancer cell lines were assayed for glucose, pyruvate and glutamine dependence by analyzing cytotoxicity, cell cycle progression, apoptosis and ATP production...
June 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/28720669/muc1-mediated-metabolic-alterations-regulate-response-to-radiotherapy-in-pancreatic-cancer
#3
Venugopal Gunda, Joshua J Souchek, Jaime Abrego, Surendra K Shukla, Gennifer D Goode, Enza Vernucci, Aneesha Dasgupta, Nina CHaika, Ryan J King, Sicong Li, Shuo Wang, Fang Yu, Tadayoshi Bessho, Chi Lin, Pankaj K Singh
Purpose: MUC1, an oncogene overexpressed in multiple solid tumors including pancreatic cancer, reduces overall survival and imparts resistance to radiation and chemotherapies. We previously identified that MUC1 facilitates growth promoting metabolic alterations in pancreatic cancer cells. The present study investigates the role of MUC1-mediated metabolism in radiation resistance of pancreatic cancer by utilizing cell lines and in vivo models. <p>Experimental design: We used MUC1 knockdown and overexpressed cell line models for evaluating the role of MUC1-mediated metabolism in radiation resistance through in vitro cytotoxicity, clonogenicity, DNA damage response and metabolomic evaluations...
July 18, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28539279/-monocarboxylate-transporter-1-enhances-the-sensitivity-of-breast-cancer-cells-to-3-bromopyruvate-in-vitro
#4
Qi-Xiang Li, Pei Zhang, Fang Liu, Xian-Zhi Wang, Lu Li, Zhong-Kun Wang, Chen-Chen Jiang, Hai-Lun Zheng, Hao Liu
OBJECTIVE: To investigate the role of monocarboxylate transporter 1 (MCT1) in enhancing the sensitivity of breast cancer cells to 3-bromopyruvate (3-BrPA). METHODS: The inhibitory effect of 3-BrPA on the proliferation of breast cancer cells was assessed with MTT assay, and brominated propidium bromide single staining flow cytometry was used for detecting the cell apoptosis. An ELISA kit was used to detect the intracellular levels of hexokinase II, lactate dehydrogenase, lactate, and adenosine triphosphate, and Western blotting was performed to detect the expression of MCT1...
May 20, 2017: Nan Fang Yi Ke da Xue Xue Bao, Journal of Southern Medical University
https://www.readbyqxmd.com/read/28507026/lineage-specific-metabolic-properties-and-vulnerabilities-of-t-cells-in-the-demyelinating-central-nervous-system
#5
Scott M Seki, Max Stevenson, Abagail M Rosen, Sanja Arandjelovic, Lelisa Gemta, Timothy N J Bullock, Alban Gaultier
Multiple sclerosis (MS) is a disease that is characterized by immune-mediated destruction of CNS myelin. Current MS therapies aim to block peripheral immune cells from entering the CNS. Although these treatments limit new inflammatory activity in the CNS, no treatment effectively prevents long-term disease progression and disability accumulation in MS patients. One explanation for this paradox is that current therapies are ineffective at targeting immune responses already present in the CNS. To this end, we sought to understand the metabolic properties of T cells that mediate ongoing inflammation in the demyelinating CNS...
June 15, 2017: Journal of Immunology: Official Journal of the American Association of Immunologists
https://www.readbyqxmd.com/read/28471808/3-bromopyruvate-enhances-trail-induced-apoptosis-in-human-nasopharyngeal-carcinoma-cells-through-chop-dependent-upregulation-of-trail-r2
#6
Zhou Can, Song Lele, Zhang Zhirui, Pan Qiong, Chen Yuzhong, Liu Lingling, Zhao Surong, Sun Yiming, Zhang Pei, Jiang Chenchen, Hao Liu
Past reports have shown that the sensitivity of cancer cells to TRAIL-induced apoptosis is related to their expression of TRAIL-death receptors on the cell surface. However, the level of TRAIL-death receptors expression on cancer cells is always low. Our previous research showed that nasopharyngeal carcinoma (NPC) cells have a poor sensitivity to low doses of TRAIL. Here, we evaluated combined treatment with the energy inhibitor 3-bromopyruvate (3BP) and TRAIL as a method to produce an increased apoptotic response in NPC cells...
August 2017: Anti-cancer Drugs
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
#7
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/28450161/a-perillyl-alcohol-conjugated-analog-of-3-bromopyruvate-without-cellular-uptake-dependency-on-monocarboxylate-transporter-1-and-with-activity-in-3-bp-resistant-tumor-cells
#8
Thomas C Chen, Jiali Yu, Eslam Nouri Nigjeh, Weijun Wang, Phyo Thazin Myint, Ebrahim Zandi, Florence M Hofman, Axel H Schönthal
The anticancer agent 3-bromopyruvate (3-BP) is viewed as a glycolytic inhibitor that preferentially kills glycolytic cancer cells through energy depletion. However, its cytotoxic activity is dependent on cellular drug import through transmembrane monocarboxylate transporter 1 (MCT-1), which restricts its anticancer potential to MCT-1-positive tumor cells. We created and characterized an MCT-1-independent analog of 3-BP, called NEO218. NEO218 was synthesized by covalently conjugating 3-BP to perillyl alcohol (POH), a natural monoterpene...
April 24, 2017: Cancer Letters
https://www.readbyqxmd.com/read/28440498/differentiation-of-human-induced-pluripotent-stem-cells-in-william-s-e-initiation-medium-supplemented-with-3%C3%A2-bromopyruvate-and-2%C3%A2-deoxy%C3%A2-d%C3%A2-glucose
#9
Minoru Tomizawa, Fuminobu Shinozaki, Yasufumi Motoyoshi, Takao Sugiyama, Shigenori Yamamoto, Naoki Ishige
Hepatocyte selection medium (HSM) is deprived of glucose and supplemented with galactose, and is based on Leibovitz's‑15 (L15) medium. HSM may promote the differentiation of human induced pluripotent stem (iPS) cells towards hepatocyte lineage. These culture conditions result in increased expression of galactokinase (GALK)‑1 and GALK2. However, iPS cells do not survive in HSM. Two potential alternatives to glucose deprivation are treatment with 3‑bromopyruvate (3BP), an analogue of pyruvate, and 2‑deoxy‑d‑glucose (2DG), an analogue of glucose...
June 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28433571/antitumor-and-chemosensitizing-action-of-3-bromopyruvate-implication-of-deregulated-metabolism
#10
Saveg Yadav, Shrish Kumar Pandey, Ajay Kumar, Praveen Kumar Kujur, Rana Pratap Singh, Sukh Mahendra Singh
3-Bromopyruvate (3-BP), brominated derivative of pyruvate, possesses strong antitumor potential, owing to its ability to inhibit multiple target molecules crucial for survival of neoplastic cells. Although, 3-BP displays cytotoxicity against a wide variety of tumors, there is no report with respect to malignancies of thymic origin. Therefore, we investigated its antineoplastic action in vitro against tumor cells of a murine transplantable lymphoma of thymoma origin, designated as Dalton's lymphoma (DL). 3-BP treatment of tumor cells inhibited metabolism and survival with augmented induction of apoptosis and necrosis...
May 25, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28387379/relationship-between-porcine-sperm-motility-and-sperm-enzymatic-activity-using-paper-based-devices
#11
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/28362858/3-bromopyruvate-and-buthionine-sulfoximine-effectively-kill-anoikis-resistant-hepatocellular-carcinoma-cells
#12
Minjong Lee, Ara Jo, Seulki Lee, Jong Bin Kim, Young Chang, Joon Yeul Nam, Hyeki Cho, Young Youn Cho, Eun Ju Cho, Jeong-Hoon Lee, Su Jong Yu, Jung-Hwan Yoon, Yoon Jun Kim
BACKGROUND & AIMS: Acquisition of anoikis resistance is a prerequisite for metastasis in hepatocellular carcinoma (HCC). However, little is known about how energy metabolism and antioxidant systems are altered in anoikis-resistant (AR) HCC cells. We evaluated anti-tumor effects of a combination treatment of 3-bromopyruvate (3-BP) and buthionine sulfoximine (BSO) in AR HCC cells. METHODS: We compared glycolysis, reactive oxygen species (ROS) production, and chemoresistance among Huh-BAT, HepG2 HCC cells, and the corresponding AR cells...
2017: PloS One
https://www.readbyqxmd.com/read/28236852/the-promising-anticancer-drug-3-bromopyruvate-is-metabolized-through-glutathione-conjugation-which-affects-chemoresistance-and-clinical-practice-an-evidence-based-view
#13
Salah Mohamed El Sayed, Hussam Baghdadi, Mohammed Zolaly, Hamdi H Almaramhy, Mongi Ayat, Jagadish G Donki
3-Bromopyruvate (3BP) is a promising effective anticancer drug against many different tumors in children and adults. 3BP exhibited strong anticancer effects in both preclinical and human studies e.g. energy depletion, oxidative stress, anti-angiogenesis, anti-metastatic effects, targeting cancer stem cells and antagonizing the Warburg effect. There is no report about 3BP metabolism to guide researchers and oncologists to improve clinical practice and prevent drug resistance. In this article, we provide evidences that 3BP is metabolized through glutathione (GSH) conjugation as a novel report where 3BP was confirmed to be attached to GSH followed by permanent loss of pharmacological effects in a picture similar to cisplatin...
March 2017: Medical Hypotheses
https://www.readbyqxmd.com/read/28186160/3-bromopyruvate-ameliorate-autoimmune-arthritis-by-modulating-th17-treg-cell-differentiation-and-suppressing-dendritic-cell-activation
#14
Takaichi Okano, Jun Saegusa, Keisuke Nishimura, Soshi Takahashi, Sho Sendo, Yo Ueda, Akio Morinobu
Recent studies have shown that cellular metabolism plays an important role in regulating immune cell functions. In immune cell differentiation, both interleukin-17-producing T (Th17) cells and dendritic cells (DCs) exhibit increased glycolysis through the upregulation of glycolytic enzymes, such as hexokinase-2 (HK2). Blocking glycolysis with 2-deoxyglucose was recently shown to inhibit Th17 cell differentiation while promoting regulatory T (Treg) cell generation. However, 2-DG inhibits all isoforms of HK. Thus, it is unclear which isoform has a critical role in Th17 cell differentiation and in rheumatoid arthritis (RA) pathogenesis...
February 10, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28164760/the-typical-metabolic-modifiers-conferring-improvement-in-cancer-resistance
#15
Wen Tan, Zhangfeng Zhong, Shengpeng Wang, Hui Liu, Hua Yu, Rui Tan, Xiaodong Hu, Tingrui Pan, Yitao Wang
BACKGROUND: Cancer metabolic reprogramming rekindles enthusiasm for the research of metabolic regulation in cancer drug resistance. A growing number of metabolic modifiers combined with cancer drugs obtain the expected efficacy in in vitro or in vivo studies, also in clinical trial studies, indicating a good potential of enhancing efficacy and reducing resistance. Hence, a comprehensive review on the attenuations of metabolic modifiers in cancer drug resistance is necessary for rational drug design and clinical cancer drug research...
February 3, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28101249/3-bromopyruvate-inhibits-human-gastric-cancer-tumor-growth-in-nude-mice-via-the-inhibition-of-glycolysis
#16
Shu-Lin Xian, Wei Cao, Xiao-Dong Zhang, Yun-Fei Lu
[This retracts the article DOI: 10.3892/ol.2014.2779.].
December 2016: Oncology Letters
https://www.readbyqxmd.com/read/28010062/covalent-modulators-of-the-vacuolar-atpase
#17
Ying-Chu Chen, Keriann M Backus, Maria Merkulova, Christina Yang, Dennis Brown, Benjamin F Cravatt, Chao Zhang
The vacuolar H(+) ATPase (V-ATPase) is a complex multisubunit machine that regulates important cellular processes through controlling acidity of intracellular compartments in eukaryotes. Existing small-molecule modulators of V-ATPase either are restricted to targeting one membranous subunit of V-ATPase or have poorly understood mechanisms of action. Small molecules with novel and defined mechanisms of inhibition are thus needed to functionally characterize V-ATPase and to fully evaluate the therapeutic relevance of V-ATPase in human diseases...
January 18, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/27983708/the-hk2-dependent-warburg-effect-and-mitochondrial-oxidative-phosphorylation-in-cancer-targets-for-effective-therapy-with-3-bromopyruvate
#18
REVIEW
Paweł Lis, Mariusz Dyląg, Katarzyna Niedźwiecka, Young H Ko, Peter L Pedersen, Andre Goffeau, Stanisław Ułaszewski
This review summarizes the current state of knowledge about the metabolism of cancer cells, especially with respect to the "Warburg" and "Crabtree" effects. This work also summarizes two key discoveries, one of which relates to hexokinase-2 (HK2), a major player in both the "Warburg effect" and cancer cell immortalization. The second discovery relates to the finding that cancer cells, unlike normal cells, derive as much as 60% of their ATP from glycolysis via the "Warburg effect", and the remaining 40% is derived from mitochondrial oxidative phosphorylation...
December 15, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27982259/hepatotoxicity-and-nephrotoxicity-of-3-bromopyruvate-in-mice
#19
Qiong Pan, Yiming Sun, Qili Jin, Qixiang Li, Qing Wang, Hao Liu, Surong Zhao
PURPOSE: To investigate the hepatotoxicity and nephrotoxicity of 3-Bromopyruvate (3BP) in mice. METHODS: Fifteen nude mice were grafted subcutaneously in the left flank with MDA-MB-231 cells, then all mice were divided into control group (PBS), 3BP group (8 mg/kg), positive group (DNR: 0.8 mg/kg) when tumor volume reached approximately 100 mm3. 28 days later, tumors, livers and kidneys were stored in 4 % formalin solution and stained with hematoxylin and eosin staining...
November 2016: Acta Cirúrgica Brasileira
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 A Wani, Kalpana Ghoshal, Samson T 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 therapies. The association between sorafenib resistance and glycolysis prompted us to screen several drugs with known antiglycolytic activity to identify those that will sensitize cells to sorafenib...
February 10, 2017: Gene Expression
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