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https://www.readbyqxmd.com/read/29151270/asct2-defined-by-enzyme-mediated-activation-of-radical-sources-enhances-malignancy-of-gd2-plus-small-cell-lung-cancer
#1
Nobutoshi Esaki, Yuki Ohkawa, Noboru Hashimoto, Yuhsuke Tsuda, Yuhsuke Ohmi, Robiul H Bhuiyan, Norihiro Kotani, Koichi Honke, Atsushi Enomoto, Masahide Takahashi, Keiko Furukawa, Koichi Furukawa
Ganglioside GD2 is specifically expressed in small cell lung cancer (SCLC) cells, leading to enhancement of malignant phenotypes, such as cell proliferation and migration. However, how GD2 promotes malignant phenotypes in SCLC cells is not well known. In this study, to reveal mechanisms by which GD2 increases malignant phenotypes in SCLC cells, we performed enzyme-mediated activation of radical sources combined with mass spectrometry in GD2 positive (+) SCLC cells. Consequently, we identified ASC amino-acid transporter 2 (ASCT2), a major glutamine transporter, which coordinately works with GD2...
November 19, 2017: Cancer Science
https://www.readbyqxmd.com/read/29151157/potent-apoptosis-inducing-activity-of-erypoegin-k-an-isoflavone-isolated-from-erythrina-poeppigiana-against-human-leukemia-hl-60-cells
#2
Kiyomi Hikita, Natsuki Hattori, Aya Takeda, Yuko Yamakage, Rina Shibata, Saori Yamada, Kuniki Kato, Tomiyasu Murata, Hitoshi Tanaka, Norio Kaneda
Erypoegin K is an isoflavone isolated from the stem bark of Erythrina poeppigiana. It contains a furan group at the A-ring of the core isoflavone structure and can inhibit the activity of glyoxalase I, an enzyme that catalyzes the detoxification of methylglyoxal (MG), a by-product of glycolysis. In the present study, we found that erypoegin K has a potent cytotoxic effect on human leukemia HL-60 cells. Its cytotoxic effect was much stronger than that of a known glyoxalase I inhibitor S-p-bromobenzylglutathione cyclopentyl diester...
November 18, 2017: Journal of Natural Medicines
https://www.readbyqxmd.com/read/29151076/modulation-of-the-endocannabinoid-system-by-the-fatty-acid-amide-hydrolase-monoacylglycerol-and-diacylglycerol-lipase-inhibitors-as-an-attractive-target-for-secretory-diarrhoea-therapy
#3
A Wasilewski, A Misicka, M Sacharczuk, J Fichna
Secretory diarrhoea is a leading cause of mortality and morbidity worldwide. Our aim was to characterize the effect of inhibition of selected enzymes involved in the synthesis or degradation of endocannabinoids on electrolyte equilibrium in the mouse colonic tissue. The aim of this study was to evaluate the effects of PF-3845, JZL-184 and RHC-80267, as inhibitors of fatty acid amide hydrolase (FAAH), monoacylglycerol (MAGL) and diacylglycerol lipase (DAGL), respectively on epithelial ion transport in isolated mouse colon stimulated by forskolin (FSK), veratridine (VER) and bethanechol (BET)...
August 2017: Journal of Physiology and Pharmacology: An Official Journal of the Polish Physiological Society
https://www.readbyqxmd.com/read/29150960/epithelial-cell-adhesion-molecule-fragments-and-signaling-in-primary-human-liver-cells
#4
Jörg C Gerlach, Hubert G Foka, Robert L Thompson, Bruno Gridelli, Eva Schmelzer
Epithelial Cell Adhesion Molecule (EpCAM), or CD326, is a trans-membrane glycoprotein expressed by multiple normal epithelia as well as carcinoma. Human hepatic stem cells and bile duct epithelium of the liver are EpCAM positive. In tumor cell lines, its intracellular domain can be released after cleavage of the extracellular domain. Within the cell nucleus it induces cell proliferation, but cleavage depends on cell contact. Fragments of various lengths have been described in tumor cells. Despite of its described important role in proliferation in tumor cells, there is not much known about the expression and role of EpCAM fragments in primary human liver cells...
November 18, 2017: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/29150677/phosphatidylserine-decarboxylase-ct699-lysophospholipid-acyltransferase-ct775-and-acyl-acp-synthase-ct776-provide-membrane-lipid-diversity-to-chlamydia-trachomatis
#5
Eric Soupene, Frans A Kuypers
De novo lipid synthesis and scavenging of fatty acids (FA) are processes essential for the formation of the membrane of the human pathogen Chlamydia trachomatis (C.t.). Host FA are assimilated via esterification by the bacterial acyl-acyl carrier protein (ACP) synthase AasC but inhibitors of the host acyl-CoA synthetase enymes ACSL also impaired growth of C.t. in human cells. In E. coli, activity of AasC was sensitive to triacsin C and rosiglitazone G. The absence of a triacsin C-insensitive pathway and the increased inhibition by rosiglitazone G confirmed the sensitivity of the bacterial acyl-ACP synthase to these drugs in infected human cells...
November 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29150471/biochemical-monitoring-after-initiation-of-aldosterone-antagonist-therapy-in-users-of-renin-angiotensin-system-blockers-a-uk-primary-care-cohort-study
#6
Sarah-Jo Sinnott, Kathryn E Mansfield, Morten Schmidt, Krishnan Bhaskaran, Liam Smeeth, Dorothea Nitsch, Laurie A Tomlinson
OBJECTIVE: To determine the frequency of biochemical monitoring after initiation of aldosterone antagonists(AA) in patients also using angiotensin-converting enzyme inhibitors/angiotensin receptor blockers (ACEI/ARB). SETTING: UK primary care. PARTICIPANTS: ACEI/ARB users who initiated AA between 2004 and 2014. OUTCOMES: We calculated the proportions with: (1) biochemical monitoring ≤2 weeks post initiation of AA, (2) adverse biochemical values ≤2 months (potassium ≥6 mmol/L, creatinine ≥220 µmol/L and ≥30% increase in creatinine from baseline) and (3) discontinuers of AA in those with an adverse biochemical value...
November 16, 2017: BMJ Open
https://www.readbyqxmd.com/read/29150398/glycyrrhiza-glabra-extract-and-quercetin-reverses-cisplatin-resistance-in-triple-negative-mda-mb-468-breast-cancer-cells-via-inhibition-of-cytochrome-p450-1b1-enzyme
#7
Rajni Sharma, Linda Gatchie, Ibidapo S Williams, Shreyans K Jain, Ram A Vishwakarma, Bhabatosh Chaudhuri, Sandip B Bharate
The development of multi-drug resistance to existing anticancer drugs is one of the major challenges in cancer treatment. The over-expression of cytochrome P450 1B1 enzyme has been reported to cause resistance to cisplatin. With an objective to discover cisplatin-resistance reversal agents, herein, we report the evaluation of Glycyrrhiza glabra (licorice) extracts and its twelve chemical constituents for inhibition of CYP1B1 (and CYP1A1) enzyme in Sacchrosomes and live human cells. The hydroalcoholic extract showed potent inhibition of CYP1B1 in both Sacchrosomes as well as in live cells with IC50 values of 21 and 16 µg/mL, respectively...
November 7, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29150361/post-translational-mechanisms-of-host-subversion-by-bacterial-effectors
#8
REVIEW
Nichollas E Scott, Elizabeth L Hartland
Bacterial effector proteins are a specialized class of secreted proteins that are translocated directly into the host cytoplasm by bacterial pathogens. Effector proteins have diverse activities and targets, and many mediate post-translational modifications of host proteins. Effector proteins offer potential in novel biotechnological and medical applications as enzymes that may modify human proteins. Here, we discuss the mechanisms used by effectors to subvert the human host through blocking, blunting, or subverting immune mechanisms...
November 14, 2017: Trends in Molecular Medicine
https://www.readbyqxmd.com/read/29150330/the-structural-requirements-of-histone-deacetylase-inhibitors-c4-modified-saha-analogs-display-dual-hdac6-hdac8-selectivity
#9
Ahmed T Negmeldin, Joseph R Knoff, Mary Kay H Pflum
Histone deacetylase (HDAC) enzymes govern the post-translational acetylation state of lysine residues on protein substrates, leading to regulatory changes in cell function. Due to their role in cancers, HDAC proteins have emerged as promising targets for cancer treatment. Four HDAC inhibitors have been approved as anti-cancer therapeutics, including SAHA (Suberoylanilide hydroxamic acid, Vorinostat, Zolinza). SAHA is a nonselective HDAC inhibitor that targets most of the eleven HDAC isoforms. The nonselectivity of SAHA might account for its clinical side effects, but certainly limits its use as a chemical tool to study cancer-related HDAC cell biology...
October 31, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29149534/novel-n-propylphthalimide-and-4-vinylbenzyl-substituted-benzimidazole-salts-synthesis-characterization-and-determination-of-their-metal-chelating-effects-and-inhibition-profiles-against-acetylcholinesterase-and-carbonic-anhydrase-enzymes
#10
Yakup Sarı, Aydın Aktaş, Parham Taslimi, Yetkin Gök, İlhami Gulçin
The novel N-propylphthalimide-substituted and 4-vinylbenzyl-substituted N-heterocyclic carbene (NHC) precursors were synthesized by N-substituted benzimidazolium with aryl halides. The novel N-propylphthalimide-substituted and 4-vinylbenzyl-substituted NHC precursors have been characterized by using (1) H NMR, (13) C NMR, FTIR spectroscopy, and elemental analysis techniques. They were tested for the inhibition of AChE and hCA enzymes and demonstrated efficient inhibition profiles with Ki values in the range of 351...
November 17, 2017: Journal of Biochemical and Molecular Toxicology
https://www.readbyqxmd.com/read/29149530/proteases-and-protease-inhibitors-in-infectious-diseases
#11
REVIEW
Ayodeji A Agbowuro, Wilhelmina M Huston, Allan B Gamble, Joel D A Tyndall
There are numerous proteases of pathogenic organisms that are currently targeted for therapeutic intervention along with many that are seen as potential drug targets. This review discusses the chemical and biological makeup of some key druggable proteases expressed by the five major classes of disease causing agents, namely bacteria, viruses, fungi, eukaryotes, and prions. While a few of these enzymes including HIV protease and HCV NS3-4A protease have been targeted to a clinically useful level, a number are yet to yield any clinical outcomes in terms of antimicrobial therapy...
November 17, 2017: Medicinal Research Reviews
https://www.readbyqxmd.com/read/29149072/different-inhibitory-potencies-of-oseltamivir-carboxylate-zanamivir-and-several-tannins-on-bacterial-and-viral-neuraminidases-as-assessed-in-a-cell-free-fluorescence-based-enzyme-inhibition-assay
#12
Stefanie Quosdorf, Anja Schuetz, Herbert Kolodziej
Neuraminidaseis a key enzyme in the life cycle of influenza viruses and is present in some bacterial pathogens. We here assess the inhibitory potency of plant tannins versus clinically used inhibitors on both a viral and a bacterial model neuraminidase by applying the 2'-(4-methylumbelliferyl)-α-d-N-acetylneuraminic acid (MUNANA)-based activity assay. A range of flavan-3-ols, ellagitannins and chemically defined proanthocyanidin fractions was evaluated in comparison to oseltamivir carboxylate and zanamivir for their inhibitory activities against viral influenza A (H1N1) and bacterial Vibrio cholerae neuraminidase (VCNA)...
November 17, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29148818/dissociation-constants-of-cytochrome-p450-2c9-cytochrome-p450-reductase-complexes-in-a-lipid-bilayer-membrane-depend-on-nadph-a-single-protein-tracking-study
#13
Carlo Barnaba, Evan Taylor, James A Brozik
Cytochrome P450-Reductase (CPR) is a versatile NADPH-dependent electron donor located in the cytoplasmic side of the endoplasmic reticulum. It is an electron transferase that is able to deliver electrons to a variety of membrane-bound oxidative partners, including the drug-metabolizing enzymes of the cytochrome P450s (P450). CPR is also stoichiometrically limited compared to its oxidative counterparts and hypotheses have arisen about possible models that can overcome the stochiometric imbalance, including quaternary organization of P450 and diffusion-limited models...
November 17, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29148803/hsdhodh-microdomain-membrane-interactions-are-influenced-by-the-lipid-composition
#14
Eduardo Festozo Vicente, Indra Dev Sahu, Edson Crusca, Luis Guilherme Mansor Basso, Claudia Elisabeth Munte, Antonio Jose Costa-Filho, Gary A Lorigan, Eduardo Maffud Maffud Cilli
Human dihydroorotate dehydrogenase (HsDHODH) enzyme has been studied as selective target for inhibitors to block the enzyme activity, intending to prevent proliferative diseases. The N-terminal microdomain seems to play an important role in the enzyme function. However, the molecular mechanism of action and dynamics of this region are not totally understood yet. This study analyzes the interaction and conformation in model membranes of HsDHODH microdomain using peptide analogues containing the paramagnetic amino acid TOAC at strategic positions...
November 17, 2017: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/29148769/azetidine-and-piperidine-carbamates-as-efficient-covalent-inhibitors-of-monoacylglycerol-lipase
#15
Christopher R Butler, Elizabeth M Beck, Anthony R Harris, Zhen Huang, Laura A McAllister, Christopher W Am Ende, Kimberly F Fennell, Timothy L Foley, Kari R Fonseca, Steven J Hawrylik, Douglas S Johnson, John D Knafels, Scot Mente, Stephen Noell, Jayvardhan Pandit, Tracy B Phillips, Justin R Piro, Bruce N Rogers, Tarek A Samad, Jane Wang, Shuangyi Wan, Michael A Brodney
Monoacylglycerol lipase (MAGL) is the main enzyme responsible for degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG) in the CNS. MAGL catalyzes the conversion of 2-AG to arachidonic acid (AA), a precursor to the pro-inflammatory eicosannoids such as prostaglandins. Herein we describe highly efficient MAGL inhibitors, identified through a parallel medicinal chemistry approach that highlighted the improved efficiency of azetidine and piperidine-derived carbamates. The discovery and optimization of 3-substituted azetidine carbamate irreversible inhibitors of MAGL was aided by the generation of inhibitor-bound MAGL crystal structures...
November 17, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29148180/dna-methylation-in-the-central-and-efferent-limbs-of-the-chemo-reflex-requires-carotid-body-neural-activity
#16
Jayasri Nanduri, Ying-Jie Peng, Ning Wang, Shakil A Khan, Gregg L Semenza, Nanduri R Prabhakar
Long-term exposure to intermittent hypoxia (LT-IH; 30 days), simulating blood O2 profiles during sleep apnea, has been shown to repress anti-oxidant enzyme (AOE) gene expression by DNA methylation in the carotid body (CB) reflex pathway, resulting in persistent elevation of plasma catecholamine levels and blood pressure. The present study examined the mechanisms by which LT-IH induces DNA methylation. Adult rats exposed to LT-IH showed elevated reactive oxygen species (ROS) in the CB, nucleus tractus solitarius (nTS) and rostroventrolateral medulla (RVLM) and adrenal medulla (AM), which represent the central and efferent limbs of the CB reflex, respectively...
November 17, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/29148053/effective-inactivation-of-a-wide-range-of-viruses-by-pasteurization
#17
Albrecht Gröner, Connie Broumis, Randel Fang, Thomas Nowak, Birgit Popp, Wolfram Schäfer, Nathan J Roth
BACKGROUND: Careful selection and testing of plasma reduces the risk of blood-borne viruses in the starting material for plasma-derived products. Furthermore, effective measures such as pasteurization at 60°C for 10 hours have been implemented in the manufacturing process of therapeutic plasma proteins such as human albumin, coagulation factors, immunoglobulins, and enzyme inhibitors to inactivate blood-borne viruses of concern. A comprehensive compilation of the virus reduction capacity of pasteurization is presented including the effect of stabilizers used to protect the therapeutic protein from modifications during heat treatment...
November 16, 2017: Transfusion
https://www.readbyqxmd.com/read/29147551/development-of-proteolytically-stable-n-methylated-peptide-inhibitors-of-aggregation-of-the-amylin-peptide-implicated-in-type-2-diabetes
#18
Idira Obasse, Mark Taylor, Nigel J Fullwood, David Allsop
Islet amyloid polypeptide, also known as amylin, is the main component of the amyloid deposits present in approximately 90% of people with type 2 diabetes mellitus (T2DM). In this disease, amylin aggregates into multimeric β-pleated sheet structures which cause damage to pancreatic islet β-cells. Inhibitors of early-stage amylin aggregation could therefore provide a disease-modifying treatment for T2DM. In this study, overlapping peptides were designed to target the 'binding' region (RLANFLVHSS, residues 11-20) of human amylin, and their effects on amyloid fibril formation were determined by thioflavin-T assay...
December 6, 2017: Interface Focus
https://www.readbyqxmd.com/read/29147019/identification-and-characterization-of-serine-protease-inhibitors-in-a-parasitic-wasp-pteromalus-puparum
#19
Lei Yang, Yaotian Mei, Qi Fang, Jiale Wang, Zhichao Yan, Qisheng Song, Zhe Lin, Gongyin Ye
Serine protease inhibitors (SPIs) regulate protease-mediated activities by inactivating their cognate proteinases, and are involved in multiple physiological processes. SPIs have been extensively studied in vertebrates and invertebrates; however, little SPI information is available in parasitoids. Herein, we identified 57 SPI genes in total through the genome of a parasitoid wasp, Pteromalus puparum. Gene structure analyses revealed that these SPIs contain 7 SPI domains. Depending on their mode of action, these SPIs can be categorized into serpins, canonical inhibitors and alpha-2-macroglobulins (A2Ms)...
November 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29146868/vasohibins-svbp-are-tubulin-carboxypeptidases-tcp-that-regulate-neuron-differentiation
#20
Chrystelle Aillaud, Christophe Bosc, Leticia Peris, Anouk Bosson, Pierre Heemeryck, Juliette Van Dijk, Julien Le Friec, Benoit Boulan, Frédérique Vossier, Laura E Sanman, Salahuddin Syed, Neri Amara, Yohann Couté, Laurence Lafanechère, Eric Denarier, Christian Delphin, Laurent Pelletier, Sandrine Humbert, Matthew Bogyo, Annie Andrieux, Krzysztof Rogowski, Marie-Jo Moutin
Reversible detyrosination of α-tubulin is crucial to microtubule dynamics and functions and defects have been implicated in cancer, brain disorganization, and cardiomyopathies. The identity of the tubulin tyrosine carboxypeptidase (TCP) responsible for detyrosination has remained unclear. We used chemical proteomics with a potent unique irreversible inhibitor to show that the major brain TCP is a complex of vasohibin-1 (VASH1) with the Small Vasohibin Binding Protein (SVBP). VASH1 and its homolog VASH2, when complexed with SVBP, exhibited robust and specific Tyr/Phe carboxypeptidase activity on microtubules...
November 16, 2017: Science
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