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dichloroacetate

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https://www.readbyqxmd.com/read/28516168/selective-surface-pegylation-of-uio-66-nanoparticles-for-enhanced-stability-cell-uptake-and-ph-responsive-drug-delivery
#1
Isabel Abánades Lázaro, Salame Haddad, Sabrina Sacca, Claudia Orellana-Tavra, David Fairen-Jimenez, Ross S Forgan
The high storage capacities and excellent biocompatibilities of metal-organic frameworks (MOFs) have made them emerging candidates as drug-delivery vectors. Incorporation of surface functionality is a route to enhanced properties, and here we report on a surface-modification procedure-click modulation-that controls their size and surface chemistry. The zirconium terephthalate MOF UiO-66 is (1) synthesized as ∼200 nm nanoparticles coated with functionalized modulators, (2) loaded with cargo, and (3) covalently surface modified with poly(ethylene glycol) (PEG) chains through mild bioconjugate reactions...
April 13, 2017: Chem
https://www.readbyqxmd.com/read/28505181/overexpression-of-pyruvate-dehydrogenase-kinase-1-in-retinoblastoma-a-potential-therapeutic-opportunity-for-targeting-vitreous-seeds-and-hypoxic-regions
#2
Swatishree Sradhanjali, Devjyoti Tripathy, Suryasnata Rath, Ruchi Mittal, Mamatha M Reddy
Pyruvate dehydrogenase kinase 1 (PDK1), a key enzyme implicated in metabolic reprogramming of tumors, is induced in several tumors including glioblastoma, breast cancer and melanoma. However, the role played by PDK1 is not studied in retinoblastoma (RB). In this study, we have evaluated the expression of PDK1 in RB clinical samples, and studied its inhibition as a strategy to decrease cell growth and migration. We show that PDK1 is specifically overexpressed in RB patient samples especially in vitreous seeds and hypoxic regions and cell lines compared to control retina using immunohistochemistry and real-time PCR...
2017: PloS One
https://www.readbyqxmd.com/read/28483502/oxidative-stress-a-key-regulator-of-leiomyoma-cell-survival
#3
Nicole M Fletcher, Mohammed S Abusamaan, Ira Memaj, Mohammed G Saed, Ayman Al-Hendy, Michael P Diamond, Ghassan M Saed
OBJECTIVE: To determine the effects of attenuating oxidative stress with the use of dichloroacetate (DCA) on the expression of key redox enzymes myeloperoxidase (MPO) and inducible nitric oxide synthase (iNOS) as well as on apoptosis. DESIGN: Prospective experimental study. SETTING: University medical center. PATIENT(S): Cells established from myometrium and uterine fibroid from the same patients. INTERVENTION(S): Cells were exposed to normal (20% O2) or hypoxic (2% O2) conditions for 24 hours with or without DCA (20 μg/mL), a metabolic modulator that shifts anaerobic to aerobic metabolism...
May 5, 2017: Fertility and Sterility
https://www.readbyqxmd.com/read/28445868/suppressionof-pyruvate-dehydrogenase-kinase-2-re-sensitizes-paclitaxel-resistant-human-lung-cancer-cells-to-paclitaxel
#4
Hong Sun, Anyou Zhu, Xiang Zhou, Fengchao Wang
Despite impressive initial clinical responses, the majority of lung cancer patients treated with paclitaxel eventually develop resistance to the drug. Pyruvate dehydrogenase kinase-2 (PDK2) is a key regulator of glycolysis and oxidative phosphorylation, and its expression is increased in a variety of tumors. In this study, the role of PDK2 in mediating paclitaxel resistance in lung cancer cells was investigated using biochemical and isotopic tracing methods. Increased expression of PDK2 was observed in paclitaxel-resistant cells ascompared totheir parental cells...
April 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/28445816/disinfection-byproduct-formation-in-drinking-water-sources-a-case-study-of-yuqiao-reservoir
#5
Hongyan Zhai, Xizhen He, Yan Zhang, Tingting Du, Adeyemi S Adeleye, Yao Li
This study investigated the potential formation of disinfection byproducts (DBPs) during chlorination and chloramination of 20 water samples collected from different points of Yuqiao reservoir in Tianjin, China. The concentrations of dissolved organic matter and ammonia decreased downstream the reservoir, while the specific UV absorbance (SUVA: the ratio of UV254 to dissolved organic carbon) increased [from 0.67 L/(mg*m) upstream to 3.58 L/(mg*m) downstream]. The raw water quality played an important role in the formation of DBPs...
April 15, 2017: Chemosphere
https://www.readbyqxmd.com/read/28431577/dichloroacetic-acid-induced-testicular-toxicity-in-male-rats-and-the-protective-effect-of-date-fruit-extract
#6
Amira El Arem, Lamia Lahouar, Emna Behija Saafi, Amira Thouri, Fatma Ghrairi, Zohra Houas, Fadoua Neffati, Lotfi Achour
BACKGROUND: The present study was designed to investigate the protective effect of aqueous date extract (ADE) against the dichloroacetic acid (DCA)-induced testicular injury in rats. METHODS: Forty-eight male Wistar rats were randomly divided into six groups of eight: group I served as the control; group II was given ADE (4 ml/kg) by gavage; groups III and IV received DCA at 0.5 and 2 g/L drinking water, respectively; and groups V and VI received DCA at 0.5 and 2 g/L drinking water, respectively, before ADE administration...
April 22, 2017: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28426747/metabolic-analysis-of-radioresistant-medulloblastoma-stem-like-clones-and-potential-therapeutic-targets
#7
Lue Sun, Takashi Moritake, Kazuya Ito, Yoshitaka Matsumoto, Hironobu Yasui, Hidehiko Nakagawa, Aki Hirayama, Osamu Inanami, Koji Tsuboi
Medulloblastoma is a fatal brain tumor in children, primarily due to the presence of treatment-resistant medulloblastoma stem cells. The energy metabolic pathway is a potential target of cancer therapy because it is often different between cancer cells and normal cells. However, the metabolic properties of medulloblastoma stem cells, and whether specific metabolic pathways are essential for sustaining their stem cell-like phenotype and radioresistance, remain unclear. We have established radioresistant medulloblastoma stem-like clones (rMSLCs) by irradiation of the human medulloblastoma cell line ONS-76...
2017: PloS One
https://www.readbyqxmd.com/read/28410193/metabolic-targeting-of-egfrviii-pdk1-axis-in-temozolomide-resistant-glioblastoma
#8
Kiran K Velpula, Maheedhara R Guda, Kamlesh Sahu, Jack Tuszynski, Swapna Asuthkar, Sarah E Bach, Justin D Lathia, Andrew J Tsung
Glioblastomas are characterized by amplification of EGFR. Approximately half of tumors with EGFR over-expression also express a constitutively active ligand independent EGFR variant III (EGFRvIII). While current treatments emphasize surgery followed by radiation and chemotherapy with Temozolomide (TMZ), acquired chemoresistance is a universal feature of recurrent GBMs. To mimic the GBM resistant state, we generated an in vitro TMZ resistant model and demonstrated that dichloroacetate (DCA), a metabolic inhibitor of pyruvate dehydrogenase kinase 1 (PDK1), reverses the Warburg effect...
March 31, 2017: Oncotarget
https://www.readbyqxmd.com/read/28362300/evaluation-of-dbps-formation-from-smps-exposed-to-chlorine-chloramine-and-ozone
#9
Beibei Zhang, Qiming Xian, Jian Lu, Tingting Gong, Aimin Li, Jianfang Feng
Soluble microbial products (SMPs) are an important group of components in wastewater effluents. In this study, the formation of disinfection by-products (DBPs), including trihalomethanes (THMs), haloacetic acids (HAAs), chlorinated solvents (CSs), haloketones (HKs), haloacetonitriles (HANs) and trichloronitromethane (TCNM) (chloropicrin), from SMPs during chlorination, chloramination and ozonation was investigated. More carbonaceous DBPs (C-DBPs: THMs, HAAs, CSs and HKs) and nitrogenous DBPs (N-DBPs: HANs and TCNM) were formed in chlorination than chloramination...
April 2017: Journal of Water and Health
https://www.readbyqxmd.com/read/28339028/2-methoxyestradiol-enhances-radiosensitivity-in-radioresistant-melanoma-mda-mb-435r-cells-by-regulating-glycolysis-via-hif-1%C3%AE-pdk1-axis
#10
Hong Zhao, Huangang Jiang, Zheng Li, Yafei Zhuang, Yinyin Liu, Shuliang Zhou, Youde Xiao, Conghua Xie, Fuxiang Zhou, Yunfeng Zhou
HIF-1α overexpression is associated with radio-resistance of various cancers. A radioresistant human melanoma cell model MDA-MB-435R (435R) was established by us previously. Compared with the parental cells MDA-MB‑435 (435S), an elevated level of HIF-1α expression in 435R cells was demonstrated in our recent experiments. Therefore, in the current study, we sought to determine whether selective HIF-1α inhibitors could radiosensitize the 435R cells to X-ray, and to identify the potential mechanisms. Our data demonstrated that inhibition of HIF-1α with 2-methoxyestradiol (2-MeOE2) significantly enhanced radiosensitivity of 435R cells...
May 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28163135/a-mechanism-based-pharmacokinetic-enzyme-turnover-model-for-dichloroacetic-acid-autoinhibition-in-rats
#11
Yu Jiang, Gary Milavetz, Margaret O James, Guohua An
Dichloroacetic acid (DCA), a halogenated organic acid, is a pyruvate dehydrogenase kinase inhibitor that has been used to treat congenital or acquired lactic acidosis and is currently in early-phase clinical trials for cancer treatment. DCA was found to inhibit its own metabolism by irreversibly inactivating glutathione transferase zeta 1 (GSTZ1-1), resulting in nonlinear kinetics and abnormally high accumulation ratio after repeated dosing. In this analysis, a semi-mechanistic pharmacokinetic enzyme turnover model was developed for the first time to capture DCA autoinhibition, gastrointestinal region-dependent absorption, and time-dependent change in bioavailability in rats...
February 3, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28161516/identification-and-determination-of-disinfection-byproducts-in-chlorine-containing-household-cleansing-products
#12
Ho-Sang Shin, Hyun-Hee Lim
Seven halogenated volatile organic compounds (HVOCs) and two haloacetic acids were detected and quantified in 15 household products, including sodium hypochlorite, by gas chromatography-mass spectrometry (GC-MS). Chloroform was detected in a range of 0.2-30.2 mg kg(-1) in all products, and carbon tetrachloride was observed in 13 samples in a range of 0.05-352 mg kg(-1). Dichloroacetic acid and trichloroacetic acid were also detected up to 94 and 146 mg kg(-1) in household products. The estimated human exposures of chloroform, carbon tetrachloride, dichloroacetic acid and trichloroacetic acid were calculated to 0...
May 2017: Chemosphere
https://www.readbyqxmd.com/read/28123081/histone-deacetylase-inhibitors-protect-against-pyruvate-dehydrogenase-dysfunction-in-huntington-s-disease
#13
Luana Naia, Teresa Cunha-Oliveira, Joana Rodrigues, Tatiana R Rosenstock, Ana Oliveira, Márcio Ribeiro, Catarina Carmo, Sofia I Oliveira-Sousa, Ana I Duarte, Michael R Hayden, A Cristina Rego
Transcriptional deregulation and changes in mitochondrial bioenergetics, including pyruvate dehydrogenase (PDH) dysfunction, have been described in Huntington's disease (HD). We previously showed that histone deacetylase inhibitors (HDACi), trichostatin A and sodium butyrate (SB), ameliorate mitochondrial function in cells expressing mutant huntingtin. In this work we investigated the effect of HDACi on regulation of PDH activity in striatal cells derived from HD knock-in mice and YAC128 mice. Mutant cells exhibited decreased PDH activity and increased PDH E1alpha phosphorylation/inactivation, accompanied by enhanced protein levels of PDH kinases (PDK)1/3...
January 25, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28094765/selective-antagonism-of-muscarinic-receptors-is-neuroprotective-in-peripheral-neuropathy
#14
Nigel A Calcutt, Darrell R Smith, Katie Frizzi, Mohammad Golam Sabbir, Subir K Roy Chowdhury, Teresa Mixcoatl-Zecuatl, Ali Saleh, Nabeel Muttalib, Randy Van der Ploeg, Joseline Ochoa, Allison Gopaul, Lori Tessler, Jürgen Wess, Corinne G Jolivalt, Paul Fernyhough
Sensory neurons have the capacity to produce, release, and respond to acetylcholine (ACh), but the functional role of cholinergic systems in adult mammalian peripheral sensory nerves has not been established. Here, we have reported that neurite outgrowth from adult sensory neurons that were maintained under subsaturating neurotrophic factor conditions operates under cholinergic constraint that is mediated by muscarinic receptor-dependent regulation of mitochondrial function via AMPK. Sensory neurons from mice lacking the muscarinic ACh type 1 receptor (M1R) exhibited enhanced neurite outgrowth, confirming the role of M1R in tonic suppression of axonal plasticity...
February 1, 2017: Journal of Clinical Investigation
https://www.readbyqxmd.com/read/28094552/glucose-metabolism-in-cancer-and-ischemia-possible-therapeutic-consequences-of-the-warburg-effect
#15
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...
February 2017: Nutrition and Cancer
https://www.readbyqxmd.com/read/28074362/the-determination-and-fate-of-disinfection-by-products-from-ozonation-chlorination-of-fulvic-acid
#16
Xin Zhong, Chongwei Cui, Shuili Yu
Ozonation of fulvic acid (FA) can result in diverse intermediate oxidation by-products, significantly affecting disinfection by-product (DBP) formation following chlorination. The objective of this study was to provide insight into ozone reaction intermediates and reveal the possible formation pathway of DBPs from ozonation of FA due to the formation of intermediate oxidation by-products. Aldehydes, aromatic acids, short-chain acids, chloroform, and dichloroacetic acid were detected at various ozone dosage additions...
January 10, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28040265/pyruvate-dehydrogenase-kinase-4-deficiency-attenuates-cisplatin-induced-acute-kidney-injury
#17
Chang Joo Oh, Chae-Myeong Ha, Young-Keun Choi, Sungmi Park, Mi Sun Choe, Nam Ho Jeoung, Yang Hoon Huh, Hyo-Jeong Kim, Hee-Seok Kweon, Ji-Min Lee, Sun Joo Lee, Jae-Han Jeon, Robert A Harris, Keun-Gyu Park, In-Kyu Lee
Clinical prescription of cisplatin, one of the most widely used chemotherapeutic agents, is limited by its side effects, particularly tubular injury-associated nephrotoxicity. Since details of the underlying mechanisms are not fully understood, we investigated the role of pyruvate dehydrogenase kinase (PDK) in cisplatin-induced acute kidney injury. Among the PDK isoforms, PDK4 mRNA and protein levels were markedly increased in the kidneys of mice treated with cisplatin, and c-Jun N-terminal kinase activation was involved in cisplatin-induced renal PDK4 expression...
December 28, 2016: Kidney International
https://www.readbyqxmd.com/read/27996252/formation-and-occurrence-of-n-chloro-2-2-dichloroacetamide-a-previously-overlooked-nitrogenous-disinfection-byproduct-in-chlorinated-drinking-waters
#18
Yun Yu, David A Reckhow
Haloacetamides (HAMs) are a class of newly identified nitrogenous disinfection byproducts (N-DBPs) whose occurrence in drinking waters has recently been reported in several DBP surveys. As the most prominent HAM species, it is commonly acknowledged that 2,2-dichloroacetamide (DCAM) is mainly generated from dichloroacetonitrile (DCAN) hydrolysis because the concentrations of these two compounds are often well correlated. Instead of DCAM, a previously unreported N-DBP, N-chloro-2,2-dichloroacetamide (N-Cl-DCAM), was confirmed in this study as the actual DCAN degradation product in chlorinated drinking waters...
January 13, 2017: Environmental Science & Technology
https://www.readbyqxmd.com/read/27939695/ag311-a-small-molecule-inhibitor-of-complex-i-and-hypoxia-induced-hif-1%C3%AE-stabilization
#19
Anja Bastian, Satoshi Matsuzaki, Kenneth M Humphries, Gavin A Pharaoh, Arpit Doshi, Nilesh Zaware, Aleem Gangjee, Michael A Ihnat
Cancer cells have a unique metabolic profile and mitochondria have been shown to play an important role in chemoresistance, tumor progression and metastases. This unique profile can be exploited by mitochondrial-targeted anticancer therapies. A small anticancer molecule, AG311, was previously shown to possess anticancer and antimetastatic activity in two cancer mouse models and to induce mitochondrial depolarization. This study defines the molecular effects of AG311 on the mitochondria to elucidate its observed efficacy...
March 1, 2017: Cancer Letters
https://www.readbyqxmd.com/read/27913098/succinyl-coa-synthetase-sucla2-deficiency-in-two-siblings-with-impaired-activity-of-other-mitochondrial-oxidative-enzymes-in-skeletal-muscle-without-mitochondrial-dna-depletion
#20
Xiaoping Huang, Jirair K Bedoyan, Didem Demirbas, David J Harris, Alexander Miron, Simone Edelheit, George Grahame, Suzanne D DeBrosse, Lee-Jun Wong, Charles L Hoppel, Douglas S Kerr, Irina Anselm, Gerard T Berry
Mutations in SUCLA2 result in succinyl-CoA ligase (ATP-forming) or succinyl-CoA synthetase (ADP-forming) (A-SCS) deficiency, a mitochondrial tricarboxylic acid cycle disorder. The phenotype associated with this gene defect is largely encephalomyopathy. We describe two siblings compound heterozygous for SUCLA2 mutations, c.985A>G (p.M329V) and c.920C>T (p.A307V), with parents confirmed as carriers of each mutation. We developed a new LC-MS/MS based enzyme assay to demonstrate the decreased SCS activity in the siblings with this unique genotype...
March 2017: Molecular Genetics and Metabolism
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