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https://www.readbyqxmd.com/read/27898047/inhibition-of-urease-by-disulfiram-an-fda-approved-thiol-reagent-used-in-humans
#1
Ángel Gabriel Díaz-Sánchez, Emilio Alvarez-Parrilla, Alejandro Martínez-Martínez, Luis Aguirre-Reyes, Jesica Aline Orozpe-Olvera, Miguel Armando Ramos-Soto, José Alberto Núñez-Gastélum, Bonifacio Alvarado-Tenorio, Laura Alejandra de la Rosa
Urease is a nickel-dependent amidohydrolase that catalyses the decomposition of urea into carbamate and ammonia, a reaction that constitutes an important source of nitrogen for bacteria, fungi and plants. It is recognized as a potential antimicrobial target with an impact on medicine, agriculture, and the environment. The list of possible urease inhibitors is continuously increasing, with a special interest in those that interact with and block the flexible active site flap. We show that disulfiram inhibits urease in Citrullus vulgaris (CVU), following a non-competitive mechanism, and may be one of this kind of inhibitors...
November 26, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27895076/mesothelial-cells-create-a-novel-tissue-niche-that-facilitates-gastric-cancer-invasion
#2
Masamitsu Tanaka, Sei Kuriyama, Go Itoh, Daichi Maeda, Akiteru Goto, Yutaro Tamiya, Kazuyoshi Yanagihara, Masakazu Yashiro, Namiko Aiba
Peritoneal mesothelial cells (PMC) cover organ surfaces in the abdominal cavity. In this study, lineage tracing revealed that PMC guide cancer cell invasion in the gastric wall and in peritoneal metastatic lesions. Serosal PMC covering the stomach surface entered the gastric wall to create a novel niche that favored gastric cancer cell invasion. PMC infiltration was induced by incorporation of cancer cell-derived, Wnt3a-containing extracellular vesicles (EV). Infiltrated PMC in turn promoted subserosal invasion of cancer cells...
November 28, 2016: Cancer Research
https://www.readbyqxmd.com/read/27894956/disulfiram-induces-anoikis-and-suppresses-lung-colonization-in-triple-negative-breast-cancer-via-calpain-activation
#3
Ji Young Kim, Nahyun Lee, Yoon-Jae Kim, Youngkwan Cho, Hyunsook An, Eunhye Oh, Tae-Min Cho, Daeil Sung, Jae Hong Seo
Triple-negative breast cancers (TNBC) often exhibit an aggressive phenotype. Disulfiram (DSF) is an approved drug for the treatment of alcohol dependence, but has also been shown to kill TNBC cells in a copper (Cu)-dependent manner. Exactly how this occurs has not been clearly elucidated. We sought to investigate the mechanisms responsible for DSF/Cu-dependent induction of apoptosis and suppression of lung colonization by TNBC cells. DSF/Cu induced anoikis and significantly suppressed cell migration and invasion with negative effects on focal adhesions, coinciding with vimentin breakdown and calpain activation in TNBC cells...
November 25, 2016: Cancer Letters
https://www.readbyqxmd.com/read/27882330/aldh2-inhibition-potentiates-high-glucose-stress-induced-injury-in-cultured-cardiomyocytes
#4
Guodong Pan, Mandar Deshpande, Rajarajan A Thandavarayan, Suresh Selvaraj Palaniyandi
Aldehyde dehydrogenase (ALDH) gene superfamily consists of 19 isozymes. They are present in various organs and involved in metabolizing aldehydes that are biologically generated. For instance, ALDH2, a cardiac mitochondrial ALDH isozyme, is known to detoxify 4-hydroxy-2-nonenal, a reactive aldehyde produced upon lipid peroxidation in diabetic conditions. We hypothesized that inhibition of ALDH leads to the accumulation of unmetabolized 4HNE and consequently exacerbates injury in cells subjected to high glucose stress...
2016: Journal of Diabetes Research
https://www.readbyqxmd.com/read/27846399/sensory-motor-axonal-polyneuropathy-involving-cranial-nerves-an-uncommon-manifestation-of-disulfiram-toxicity
#5
Telma Santos, António Martins Campos, Hugo Morais
Disulfiram (tetraethylthiuram disulfide) has been used for the treatment of alcohol dependence. An axonal sensory-motor polyneuropathy with involvement of cranial pairs due to disulfiram is exceedingly rare. The authors report a unique case of an extremely severe axonal polyneuropathy involving cranial nerves that developed within weeks after a regular dosage of 500mg/day disulfiram. To the authors best knowledge, such a severe and rapidly-progressive course has never been described with disulfiram dosages of only 500mg/day...
November 10, 2016: Clinical Neurology and Neurosurgery
https://www.readbyqxmd.com/read/27831632/disulfiram-as-a-candidate-nf-%C3%AE%C2%BAb-and-proteasome-inhibitor-prevents-endometriotic-implant-growing-in-a-rat-model-of-endometriosis
#6
O Celik, A Ersahin, M Acet, N Celik, Y Baykus, R Deniz, E Ozerol, I Ozerol
OBJECTIVE: Disulfiram (DSF) exerts its therapeutic effects through oxidative, proteasome, and nuclear factor kappa beta (NF-κB) pathways. The study was planned to test the impact of DSF on growing of endometriotic implants in rats with experimentally induced endometriosis. PATIENTS AND METHODS: Thirty rats were labeled as the control (n = 8), sham (n = 6), GnRH-agonist (n = 8) and the DSF (n = 8) groups. The rats in the group 3 exposed to single dose leuprolide acetate...
October 2016: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/27803460/an-ophthalmic-formulation-of-disulfiram-nanoparticles-prolongs-drug-residence-time-in-lens
#7
Noriaki Nagai, Yu Mano, Yoshimasa Ito
Disulfiram (DSF) is a dimer of diethyldithiocarbamate (DDC) that we previously added to a solution of 2-hydroxypropyl-β-cyclodextrin (DSF solution). We found that the instillation of this DSF solution delayed lens opacification in a hereditary cataractous ICR/f rat. In this study, we attempted to design an ophthalmic formulation containing DSF nanoparticles for use as a lens targeted drug delivery system (nano-DSF suspension), and investigated the changes in drug content in the lens after the instillation of DSF solution or nano-DSF suspension...
2016: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27793743/dopamine-beta-hydroxylase-participate-in-the-immunoendocrine-responses-of-hypothermal-stressed-white-shrimp-litopenaeus-vannamei
#8
Winton Cheng, Ya-Wen Ka, Chin-Chyuan Chang
Dopamine beta-hydroxylase (DBH) plays a critical role in catecholamine (CA) synthesis of neuroendocrine regulatory network, and is suggested to be involved in the immunoendocrine responses of invertebrate against bacterial challenge. DBH has been identified in white shrimp, Litopenaeus vannamei, and further investigation on its potential function was conducted after hypothermal stress, pharmaceutical inhibition and gene silencing in the present study. Cloned DBH L. vannamei (LvDBH), belonging to the Copper type II, ascorbate-dependent monooxygenases, was characterized by a DOMON domain, a Cu2_monooxygen domain and three glycosylation sites, and its expression was abundant in thoracic ganglia and haemocytes determined by quantitative real-time PCR...
December 2016: Fish & Shellfish Immunology
https://www.readbyqxmd.com/read/27754304/lbos-02-05-inhibitors-of-dopamine-%C3%AE-hydroxylase-obtained-by-structure-based-methods-exhibited-anti-hypertensive-effect-in-l-name-induced-hypertensive-rats
#9
Sanjay Kumar Dey, Pankaj Prabhakar, Manisha Saini, Toyanji Joseph, B K Thelma, Subir K Maulik, Suman Kundu
OBJECTIVE: To identify novel inhibitors of dopamine beta hydroxylase (DBH) and evaluate their antihypertensive properties in L-NAME induced hypertensive rat model. DESIGN AND METHOD: An experimentally validated computational model for hDBH, built in our lab, was used for structure-based, rational drug-design. The three-dimensional model was used for virtual-screening against small molecule databases from NCI, USA and elsewhere. Identified top hits were then tested in vitro against DBH with known inhibitors nepicastat and disulfiram as controls...
September 2016: Journal of Hypertension
https://www.readbyqxmd.com/read/27725388/design-of-novel-ophthalmic-formulation-containing-drug-nanoparticles-and-its-usefulness-as-anti-glaucoma-drugs
#10
Noriaki Nagai
 The ophthalmic application of drugs is the primary route of administration for the therapy of glaucoma; however, in traditional formulations, only small amounts of the administered drug penetrate the cornea to reach the desired intraocular tissue due to corneal barriers. Recently, nanoparticulate drug delivery is expected as a technology to overcome the difficulties in delivering drugs across biological barriers (improvement of bioavailability). In this study, we attempted to establish a new method for preparing solid drug nanoparticles by using a bead mill and various additives, and succeeded in preparing a high quality dispersion containing drug nanoparticles...
2016: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
https://www.readbyqxmd.com/read/27708770/the-cytotoxic-mechanisms-of-disulfiram-and-copper-ii-in-cancer-cells
#11
Patricia Erebi Tawari, Zhipeng Wang, Mohammad Najlah, Chi Wai Tsang, Vinodh Kannappan, Peng Liu, Christopher McConville, Bin He, Angel L Armesilla, Weiguang Wang
The anticancer activity of disulfiram (DS) is copper(ii) (Cu)-dependent. This study investigated the anticancer mechanisms of DS/Cu using in vitro cytotoxicity and metabolic kinetic analysis. Our study indicates that DS/Cu targets cancer cells by the combination of two types of actions: (1) instant killing executed by DS/Cu reaction generated reactive oxygen species; (2) delayed cytotoxicity introduced by the end product, DDC-Cu. Nanoencapsulation of DS might shed light on repositioning of DS into cancer treatment...
November 19, 2015: Toxicology Research
https://www.readbyqxmd.com/read/27699226/aldehyde-dehydrogenase-inhibition-blocks-mucosal-fibrosis-in-human-and-mouse-ocular-scarring
#12
Sarah D Ahadome, David J Abraham, Suryanarayana Rayapureddi, Valerie P Saw, Daniel R Saban, Virginia L Calder, Jill T Norman, Markella Ponticos, Julie T Daniels, John K Dart
Mucous membrane pemphigoid (MMP) is a systemic mucosal scarring disease, commonly causing blindness, for which there is no antifibrotic therapy. Aldehyde dehydrogenase family 1 (ALDH1) is upregulated in both ocular MMP (OMMP) conjunctiva and cultured fibroblasts. Application of the ALDH metabolite, retinoic acid (RA), to normal human conjunctival fibroblasts in vitro induced a diseased phenotype. Conversely, application of ALDH inhibitors, including disulfiram, to OMMP fibroblasts in vitro restored their functionality to that of normal controls...
August 4, 2016: JCI Insight
https://www.readbyqxmd.com/read/27651711/cisplatin-resistance-reversal-by-disulfiram-and-caffeine
#13
Ashish R Kadia, Gaurang B Shah
No abstract text is available yet for this article.
July 2016: Journal of Pharmacology & Pharmacotherapeutics
https://www.readbyqxmd.com/read/27650066/aldehyde-dehydrogenase-2-in-aplastic-anemia-fanconi-anemia-and-hematopoietic-stem-cells
#14
REVIEW
Lauren D Van Wassenhove, Daria Mochly-Rosen, Kenneth I Weinberg
Maintenance of the hematopoietic stem cell (HSC) compartment depends on the ability to metabolize exogenously and endogenously generated toxins, and to repair cellular damage caused by such toxins. Reactive aldehydes have been demonstrated to cause specific genotoxic injury, namely DNA interstrand cross-links. Aldehyde dehydrogenase 2 (ALDH2) is a member of a 19 isoenzyme ALDH family with different substrate specificities, subcellular localization, and patterns of expression. ALDH2 is localized in mitochondria and is essential for the metabolism of acetaldehyde, thereby placing it directly downstream of ethanol metabolism...
September 2016: Molecular Genetics and Metabolism
https://www.readbyqxmd.com/read/27643306/lbos-02-05-inhibitors-of-dopamine-%C3%AE-hydroxylase-obtained-by-structure-based-methods-exhibited-anti-hypertensive-effect-in-l-name-induced-hypertensive-rats
#15
Sanjay Kumar Dey, Pankaj Prabhakar, Manisha Saini, Toyanji Joseph, B K Thelma, Subir K Maulik, Suman Kundu
OBJECTIVE: To identify novel inhibitors of dopamine beta hydroxylase (DBH) and evaluate their antihypertensive properties in L-NAME induced hypertensive rat model. DESIGN AND METHOD: An experimentally validated computational model for hDBH, built in our lab, was used for structure-based, rational drug-design. The three-dimensional model was used for virtual-screening against small molecule databases from NCI, USA and elsewhere. Identified top hits were then tested in vitro against DBH with known inhibitors nepicastat and disulfiram as controls...
September 2016: Journal of Hypertension
https://www.readbyqxmd.com/read/27642863/compounds-that-select-against-the-tetracycline-resistance-efflux-pump
#16
Laura K Stone, Michael Baym, Tami D Lieberman, Remy Chait, Jon Clardy, Roy Kishony
We developed a competition-based screening strategy to identify compounds that invert the selective advantage of antibiotic resistance. Using our assay, we screened over 19,000 compounds for the ability to select against the TetA tetracycline-resistance efflux pump in Escherichia coli and identified two hits, β-thujaplicin and disulfiram. Treating a tetracycline-resistant population with β-thujaplicin selects for loss of the resistance gene, enabling an effective second-phase treatment with doxycycline.
November 2016: Nature Chemical Biology
https://www.readbyqxmd.com/read/27634040/activity-dependent-regulation-of-histone-lysine-demethylase-kdm1a-by-a-putative-thiol-disulfide-switch
#17
Emily L Ricq, Jacob M Hooker, Stephen J Haggarty
Lysine demethylation of proteins such as histones is catalyzed by several classes of enzymes, including the FAD-dependent amine oxidases KDM1A/B. The KDM1 family is homologous to the mitochondrial monoamine oxidases MAO-A/B and produces hydrogen peroxide in the nucleus as a byproduct of demethylation. Here, we show KDM1A is highly thiol-reactive in vitro and in cellular models. Enzyme activity is potently and reversibly inhibited by the drug disulfiram and by hydrogen peroxide. Hydrogen peroxide produced by KDM1A catalysis reduces thiol labeling and inactivates demethylase activity over time...
November 18, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27633982/multifaceted-academic-detailing-program-to-increase-pharmacotherapy-for-alcohol-use-disorder-interrupted-time-series-evaluation-of-effectiveness
#18
Alex H S Harris, Thomas Bowe, Hildi Hagedorn, Andrea Nevedal, Andrea K Finlay, Risha Gidwani, Craig Rosen, Chad Kay, Melissa Christopher
BACKGROUND: Active consideration of effective medications to treat alcohol use disorder (AUD) is a consensus standard of care, yet knowledge and use of these medications are very low across diverse settings. This study evaluated the overall effectiveness a multifaceted academic detailing program to address this persistent quality problem in the US Veterans Health Administration (VHA), as well as the context and process factors that explained variation in effectiveness across sites. METHODS: An interrupted time series design, analyzed with mixed-effects segmented logistic regression, was used to evaluate changes in level and rate of change in the monthly percent of patients with a clinically documented AUD who received naltrexone, acamprosate, disulfiram, or topiramate...
September 15, 2016: Addiction Science & Clinical Practice
https://www.readbyqxmd.com/read/27611191/exogenous-modulation-of-retinoic-acid-signaling-affects-adult-rgc-survival-in-the-frog-visual-system-after-optic-nerve-injury
#19
Mildred V Duprey-Díaz, Jonathan M Blagburn, Rosa E Blanco
After lesions to the mammalian optic nerve, the great majority of retinal ganglion cells (RGCs) die before their axons have even had a chance to regenerate. Frog RGCs, on the other hand, suffer only an approximately 50% cell loss, and we have previously investigated the mechanisms by which the application of growth factors can increase their survival rate. Retinoic acid (RA) is a vitamin A-derived lipophilic molecule that plays major roles during development of the nervous system. The RA signaling pathway is also present in parts of the adult nervous system, and components of it are upregulated after injury in peripheral nerves but not in the CNS...
2016: PloS One
https://www.readbyqxmd.com/read/27602492/anti-hepatocellular-carcinoma-properties-of-the-anti-alcoholism-drug-disulfiram-discovered-to-enzymatically-inhibit-the-ampk-related-kinase-snark-in-vitro
#20
Kaku Goto, Naoya Kato, Raymond T Chung
We recently described that the anti-apoptotic AMPK-related kinase, SNARK, promotes transforming growth factor (TGF)-β signaling in hepatocellular carcinoma (HCC) cells, as a potentially new therapeutic target. Here we explored FDA-approved drugs inhibiting the enzymatic activity of SNARK, using an in vitro luminescence kinase assay system. Interestingly, the long-used anti-alcoholism drug disulfiram (DSF), also known as Antabuse, emerged as the top hit. Enzymatic kinetics analyses revealed that DSF inhibited SNARK kinase activity in a noncompetitive manner to ATP or phosphosubstrates...
September 2, 2016: Oncotarget
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