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3 bromopyruvate

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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
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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
#8
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
https://www.readbyqxmd.com/read/27890797/3-bromopyruvate-treatment-induces-alterations-of-metabolic-and-stress-related-pathways-in-glioblastoma-cells
#9
Davide Chiasserini, Magdalena Davidescu, Pier Luigi Orvietani, Federica Susta, Lara Macchioni, Maya Petricciuolo, Emilia Castigli, Rita Roberti, Luciano Binaglia, Lanfranco Corazzi
Glioblastoma (GBM) is the most common and aggressive brain tumour of adults. The metabolic phenotype of GBM cells is highly dependent on glycolysis; therefore, therapeutic strategies aimed at interfering with glycolytic pathways are under consideration. 3-Bromopyruvate (3BP) is a potent antiglycolytic agent, with a variety of targets and possible effects on global cell metabolism. Here we analyzed the changes in protein expression on a GBM cell line (GL15 cells) caused by 3BP treatment using a global proteomic approach...
January 30, 2017: Journal of Proteomics
https://www.readbyqxmd.com/read/27863474/hypoxic-resistance-of-kras-mutant-tumor-cells-to-3-bromopyruvate-is-counteracted-by-prima-1-and-reversed-by-n-acetylcysteine
#10
Andrea Orue, Valery Chavez, Mary Strasberg-Rieber, Manuel Rieber
BACKGROUND: The metabolic inhibitor 3-bromopyruvate (3-BrPA) is a promising anti-cancer alkylating agent, shown to inhibit growth of some colorectal carcinoma with KRAS mutation. Recently, we demonstrated increased resistance to 3-BrPA in wt p53 tumor cells compared to those with p53 silencing or mutation. Since hypoxic microenvironments select for tumor cells with diminished therapeutic response, we investigated whether hypoxia unequally increases resistance to 3-BrPA in wt p53 MelJuso melanoma harbouring (Q61L)-mutant NRAS and wt BRAF, C8161 melanoma with (G12D)-mutant KRAS (G464E)-mutant BRAF, and A549 lung carcinoma with a KRAS (G12S)-mutation...
November 18, 2016: BMC Cancer
https://www.readbyqxmd.com/read/27729975/lactate-pyruvate-transporter-mct-1-is-a-direct-wnt-target-that-confers-sensitivity-to-3-bromopyruvate-in-colon-cancer
#11
Stephanie Sprowl-Tanio, Amber N Habowski, Kira T Pate, Miriam M McQuade, Kehui Wang, Robert A Edwards, Felix Grun, Yung Lyou, Marian L Waterman
BACKGROUND: There is increasing evidence that oncogenic Wnt signaling directs metabolic reprogramming of cancer cells to favor aerobic glycolysis or Warburg metabolism. In colon cancer, this reprogramming is due to direct regulation of pyruvate dehydrogenase kinase 1 (PDK1) gene transcription. Additional metabolism genes are sensitive to Wnt signaling and exhibit correlative expression with PDK1. Whether these genes are also regulated at the transcriptional level, and therefore a part of a core metabolic gene program targeted by oncogenic WNT signaling, is not known...
2016: Cancer & Metabolism
https://www.readbyqxmd.com/read/27668346/transport-of-haloacids-across-biological-membranes
#12
REVIEW
Xianbin Su, Ruihong Li, Ka-Fai Kong, Jimmy S H Tsang
Haloacids are considered to be environmental pollutants, but some of them have also been tested in clinical research. The way that haloacids are transported across biological membranes is important for both biodegradation and drug delivery purposes. In this review, we will first summarize putative haloacids transporters and the information about haloacids transport when studying carboxylates transporters. We will then introduce MCT1 and SLC5A8, which are respective transporter for antitumor agent 3-bromopyruvic acid and dichloroacetic acid, and monochloroacetic acid transporters Deh4p and Dehp2 from a haloacids-degrading bacterium...
December 2016: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/27661124/characterization-of-acetate-transport-in-colorectal-cancer-cells-and-potential-therapeutic-implications
#13
Suellen Ferro, João Azevedo-Silva, Margarida Casal, Manuela Côrte-Real, Fatima Baltazar, Ana Preto
Acetate, together with other short chain fatty acids has been implicated in colorectal cancer (CRC) prevention/therapy. Acetate was shown to induce apoptosis in CRC cells. The precise mechanism underlying acetate transport across CRC cells membrane, that may be implicated in its selectivity towards CRC cells, is not fully understood and was addressed here. We also assessed the effect of acetate in CRC glycolytic metabolism and explored its use in combination with the glycolytic inhibitor 3-bromopyruvate (3BP)...
September 21, 2016: Oncotarget
https://www.readbyqxmd.com/read/27582536/glutathione-may-have-implications-in-the-design-of-3-bromopyruvate-treatment-protocols-for-both-fungal-and-algal-infections-as-well-as-multiple-myeloma
#14
Katarzyna Niedźwiecka, Mariusz Dyląg, Daria Augustyniak, Grażyna Majkowska-Skrobek, Magdalena Cal-Bąkowska, Young H Ko, Peter L Pedersen, Andre Goffeau, Stanisław Ułaszewski
In different fungal and algal species, the intracellular concentration of reduced glutathione (GSH) correlates closely with their susceptibility to killing by the small molecule alkylating agent 3-bromopyruvate (3BP). Additionally, in the case of Cryptococcus neoformans cells 3BP exhibits a synergistic effect with buthionine sulfoximine (BSO), a known GSH depletion agent. This effect was observed when 3BP and BSO were used together at concentrations respectively of 4-5 and almost 8 times lower than their Minimal Inhibitory Concentration (MIC)...
October 4, 2016: Oncotarget
https://www.readbyqxmd.com/read/27534909/abcb1-overexpressing-mdck-ii-cells-are-hypersensitive-to-3-bromopyruvic-acid
#15
Izabela Sadowska-Bartosz, Jacek Grębowski, Ewa Kępka, Maciej Studzian, Grzegorz Bartosz, Łukasz Pułaski
AIMS: Cancer cells, due to the Warburg effect, are more dependent on glycolysis than normal cells, so glycolytic inhibitor 3-bromopyruvic acid (3-BP) was proposed as a promising candidate for anticancer therapy. Overexpression of multidrug transporters is the main reason of resistance of cancer cells to chemotherapy. As the activity of multidrug transporters imposes an energetic burden on the cells, it can be expected that inhibition of ATP generation may exert a selective cytotoxicity to cells overexpressing multidrug transporters...
October 1, 2016: Life Sciences
https://www.readbyqxmd.com/read/27530389/impaired-mitochondrial-functions-contribute-to-3-bromopyruvate-toxicity-in-primary-rat-and-mouse-hepatocytes
#16
Ondřej Sobotka, René Endlicher, Zdeněk Drahota, Otto Kučera, David Rychtrmoc, Marjan Raad, Khurum Hakeem, Zuzana Červinková
A compound with promising anticancer properties, 3-bromopyruvate (3-BP) is a synthetic derivative of a pyruvate molecule; however, its toxicity in non-malignant cells has not yet been fully elucidated. Therefore, we elected to study the effects of 3-BP on primary hepatocytes in monolayer cultures, permeabilized hepatocytes and isolated mitochondria. After a 1-h treatment with 100 μM 3-BP cell viability of rat hepatocytes was decreased by 30 % as measured by the WST-1 test (p < 0.001); after 3-h exposure to ≥200 μM 3-BP lactate dehydrogenase leakage was increased (p < 0...
August 2016: Journal of Bioenergetics and Biomembranes
https://www.readbyqxmd.com/read/27530298/differential-3-bromopyruvate-inhibition-of-cytosolic-and-mitochondrial-human-serine-hydroxymethyltransferase-isoforms-key-enzymes-in-cancer-metabolic-reprogramming
#17
Alessandro Paiardini, Angela Tramonti, Doug Schirch, Giulia Guiducci, Martino Luigi di Salvo, Alessio Fiascarelli, Alessandra Giorgi, Bruno Maras, Francesca Cutruzzolà, Roberto Contestabile
The cytosolic and mitochondrial isoforms of serine hydroxymethyltransferase (SHMT1 and SHMT2, respectively) are well-recognized targets of cancer research, since their activity is critical for purine and pyrimidine biosynthesis and because of their prominent role in the metabolic reprogramming of cancer cells. Here we show that 3-bromopyruvate (3BP), a potent novel anti-tumour agent believed to function primarily by blocking energy metabolism, differentially inactivates human SHMT1 and SHMT2. SHMT1 is completely inhibited by 3BP, whereas SHMT2 retains a significant fraction of activity...
November 2016: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/27471592/1-25-dihydroxyvitamin-d3-modulates-calcium-transport-in-goat-mammary-epithelial-cells-in-a-dose-and-energy-dependent-manner
#18
Feifei Sun, Yangchun Cao, Chao Yu, Xiaoshi Wei, Junhu Yao
BACKGROUND: Calcium is a vital mineral and an indispensable component of milk for ruminants. The regulation of transcellular calcium transport by 1,25-dihydroxyvitamin D3 (1,25-(OH)2D3, the active form of vitamin D) has been confirmed in humans and rodents, and regulators, including vitamin D receptor (VDR), calcium binding protein D9k (calbindin-D9k), plasma membrane Ca(2+)-ATPase 1b (PMCA1b), PMAC2b and Orai1, are involved in this process. However, it is still unclear whether 1,25-(OH)2D3 could stimulate calcium transport in the ruminant mammary gland...
2016: Journal of Animal Science and Biotechnology
https://www.readbyqxmd.com/read/27457582/the-anticancer-agent-3-bromopyruvate-a-simple-but-powerful-molecule-taken-from-the-lab-to-the-bedside
#19
REVIEW
J Azevedo-Silva, O Queirós, F Baltazar, S Ułaszewski, A Goffeau, Y H Ko, P L Pedersen, A Preto, M Casal
At the beginning of the twenty-first century, 3-bromopyruvate (3BP), a simple alkylating chemical compound was presented to the scientific community as a potent anticancer agent, able to cause rapid toxicity to cancer cells without bystander effects on normal tissues. The altered metabolism of cancers, an essential hallmark for their progression, also became their Achilles heel by facilitating 3BP's selective entry and specific targeting. Treatment with 3BP has been administered in several cancer type models both in vitro and in vivo, either alone or in combination with other anticancer therapeutic approaches...
August 2016: Journal of Bioenergetics and Biomembranes
https://www.readbyqxmd.com/read/27437085/targeting-cancer-metabolism-revisiting-the-warburg-effects
#20
REVIEW
Quangdon Tran, Hyunji Lee, Jisoo Park, Seon-Hwan Kim, Jongsun Park
After more than half of century since the Warburg effect was described, this atypical metabolism has been standing true for almost every type of cancer, exhibiting higher glycolysis and lactate metabolism and defective mitochondrial ATP production. This phenomenon had attracted many scientists to the problem of elucidating the mechanism of, and reason for, this effect. Several models based on oncogenic studies have been proposed, such as the accumulation of mitochondrial gene mutations, the switch from oxidative phosphorylation respiration to glycolysis, the enhancement of lactate metabolism, and the alteration of glycolytic genes...
July 2016: Toxicological Research
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