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https://www.readbyqxmd.com/read/28350440/identification-of-trypanosoma-brucei-adometdc-inhibitors-using-a-high-throughput-mass-spectrometry-based-assay
#1
Oleg A Volkov, Casey C Cosner, Anthony J Brockway, Martin Kramer, Michael Booker, Shihua Zhong, Ariel Ketcherside, Shuguang Wei, Jamie Longgood, Melissa K McCoy, Thomas E Richardson, Stephen A Wring, Michael Peel, Jeffrey D Klinger, Bruce A Posner, Jef K De Brabander, Margaret A Phillips
Human African trypanosomiasis (HAT) is a fatal infectious disease caused by the eukaryotic pathogen Trypanosoma brucei. Available treatments are difficult to administer and have significant safety issues. S-Adenosylmethionine decarboxylase (AdoMetDC) is an essential enzyme in the parasite polyamine biosynthetic pathway. Previous attempts to develop TbAdoMetDC inhibitors into anti-HAT therapies failed due to poor brain exposure. Here, we describe a large screening campaign of two small-molecule libraries (~400,000 compounds) employing a new high-throughput (~7 s per sample) mass spectrometry-based assay for AdoMetDC activity...
March 28, 2017: ACS Infectious Diseases
https://www.readbyqxmd.com/read/28346093/a-label-free-continuous-fluorescence-based-assay-for-monitoring-ornithine-decarboxylase-activity-with-a-synthetic-putrescine-receptor
#2
Mohamed Nilam, Philip Gribbon, Jeanette Reinshagen, Kathrin Cordts, Edzard Schwedhelm, Werner M Nau, Andreas Hennig
Polyamines play an important role in cell growth, differentiation, and cancer development, and the biosynthetic pathway of polyamines is established as a drug target for the treatment of parasitic diseases, neoplasia, and cancer chemoprevention. The key enzyme in polyamine biosynthesis is ornithine decarboxylase (ODC). We report herein an analytical method for the continuous fluorescence monitoring of ODC activity based on the supramolecular receptor cucurbit[6]uril (CB6) and the fluorescent dye trans-4-[4-(dimethylamino)styryl]-1-methylpyridinium iodide (DSMI)...
January 1, 2017: SLAS Discov
https://www.readbyqxmd.com/read/28345120/fission-yeast-srm1-is-involved-in-stress-response-and-cell-cycle
#3
Aslıhan Örs Gevrekci
Polyamines are well-conserved, multifunctional polycations that contribute to a number of processes in the cells such as cell cycle, apoptosis, stress response, and gene expression. Therefore, polyamine levels should be kept under strict regulation by specific polyamine transporters and polyamine synthases. In this study, the aim is to experimentally characterize a predicted spermidine synthase gene srm1, which was identified upon sequence similarity, in fission yeast Schizosaccharomyces pombe. In an attempt to understand the role of this gene in cell cycle and stress response, deletion mutant of srm1 was generated and analyzed in terms of cell cycle regulation and environmental stress response...
March 27, 2017: Current Microbiology
https://www.readbyqxmd.com/read/28341457/thyroid-hormone-transport-across-l-type-amino-acid-transporters-what-can-molecular-modelling-tell-us
#4
Gerd Krause, Katrin Manuela Hinz
Thyroid hormones (THs) and their derivatives require transmembrane transporters (TTs) to mediate their translocation across the cell membrane. Among these TTs, the L-type amino acid transporters (LAT) not only transport amino acids (AAs) but also certain THs and their derivatives. This review summarizes available knowledge concerning structure function patterns of the TH transport by LAT1 and LAT2. For example, LAT2 imports 3,3'-T2 and T3, but not rT3 and T4. In contrast to amino acids, THs are not at all exported by LAT2...
March 21, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28338318/iron-ii-complexes-with-scorpiand-like-macrocyclic-polyamines-kinetico-mechanistic-aspects-of-complex-formation-and-oxidative-dehydrogenation-of-coordinated-amines
#5
M Paz Clares, Laura Acosta-Rueda, Carmen E Castillo, Salvador Blasco, Hermas R Jiménez, Enrique García-España, Manuel G Basallote
The Fe(II) coordination chemistry of a pyridinophane tren-derived scorpiand type ligand containing a pyridine ring in the pendant arm is explored by potentiometry, X-ray, NMR, and kinetics methods. Equilibrium studies in water show the formation of a stable [FeL](2+) complex that converts to monoprotonated and monohydroxylated species when the pH is changed. A [Fe(H-2L)](2+) complex containing an hexacoordinated dehydrogenated ligand has been isolated, and its crystal structure shows the formation of an imine bond involving the aliphatic nitrogen of the pendant arm...
March 24, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28336105/tolerance-and-efficacy-of-a-polyamine-deficient-diet-for-the-treatment-of-perioperative-pain
#6
Jean-Pierre Estebe, Cécile Degryse, Gilles Rezzadori, Florin Dimache, Georges Daccache, Alain Le Naoures, Anissa Belbachir, Pierre Schoeffler, Anne-Laure Sérandour
BACKGROUND: Polyamines have been identified as pain agonists and interact with N-methyl-D-aspartate receptors. A prospective, randomized, multicenter, and blinded phase II clinical trial was conducted to evaluate a polyamine-deficient diet for the treatment of perioperative pain in patients during spinal surgery. METHODS: All analyses followed the intention-to-treat principle. The trial was designed to evaluate the dose-ranging effect of a low polyamine diet with respect to a total (group 1) or partial (group 2) polyamine diet on perioperative pain (7 d before and 5 d after surgery)...
April 2017: Nutrition
https://www.readbyqxmd.com/read/28332831/layer-by-layer-assembly-of-amine-reactive-multilayers-using-an-azlactone-functionalized-polymer-and-small-molecule-diamine-linkers
#7
Yashira M Zayas-Gonzalez, Benjamin J Ortiz, David M Lynn
We report the reactive layer-by-layer assembly of amine-reactive polymer multilayers using an azlactone-functionalized polymer and small-molecule diamine linkers. This approach yields crosslinked polymer/linker-type films that can be further functionalized, after fabrication, by treatment with functional primary amines, and provides opportunities to incorporate other useful functionality that can be difficult to introduce using other polyamine building blocks. Films fabricated using poly(2-vinyl-4,4-dimethylazlactone) (PVDMA) and three model non-degradable aliphatic diamine linkers yielded reactive thin films that were stable upon incubation in physiologically relevant media...
March 23, 2017: Biomacromolecules
https://www.readbyqxmd.com/read/28330789/schiff-bases-of-putrescine-with-methylglyoxal-protect-from-cellular-damage-caused-by-accumulation-of-methylglyoxal-and-reactive-oxygen-species-in-dictyostelium-discoideum
#8
Seong-Jun Park, Min-Kyu Kwak, Sa-Ouk Kang
Polyamines protect protein glycation in cells against the advanced glycation end product precursor methylglyoxal, which is inevitably produced during glycolysis, and the enzymes that detoxify this α-ketoaldehyde have been widely studied. Nonetheless, nonenzymatic methylglyoxal-scavenging molecules have not been sufficiently studied either in vitro or in vivo. Here, we hypothesized reciprocal regulation between polyamines and methylglyoxal modeled in Dictyostelium grown in a high-glucose medium. We based our hypothesis on the reaction between putrescine and methylglyoxal in putrescine-deficient (odc(-)) or putrescine-overexpressing (odc(oe)) cells...
March 18, 2017: International Journal of Biochemistry & Cell Biology
https://www.readbyqxmd.com/read/28330558/altered-expression-of-polyamine-transporters-reveals-a-role-for-spermidine-in-the-timing-of-flowering-and-other-developmental-response-pathways
#9
Sheaza Ahmed, Menaka Ariyaratne, Jigar Patel, Alexander E Howard, Andrea Kalinoski, Vipaporn Phuntumart, Paul F Morris
Changes in the levels of polyamines are correlated with the activation or repression of developmental response pathways, but the role of polyamine transporters in the regulation of polyamine homeostasis and thus indirectly gene expression, has not been previously addressed. Here we show that the A. thaliana and rice transporters AtPUT5 and OsPUT1 were localized to the ER, while the AtPUT2, AtPUT3, and OsPUT3 were localized to the chloroplast by transient expression in N. benthamiana. A. thaliana plants that were transformed with OsPUT1 under the control the PUT5 promoter were delayed in flowering by 16days...
May 2017: Plant Science: An International Journal of Experimental Plant Biology
https://www.readbyqxmd.com/read/28330220/involvement-of-exogenous-polyamines-enhances-regeneration-and-agrobacterium-mediated-genetic-transformation-in-half-seeds-of-soybean
#10
Muthukrishnan Arun, Arunachalam Chinnathambi, Kondeti Subramanyam, Sivabalan Karthik, Ganeshan Sivanandhan, Jeevaraj Theboral, Sulaiman Ali Alharbi, Chang Kil Kim, Andy Ganapathi
The present work demonstrates the participation of polyamines (PAs) to improve direct regeneration and Agrobacterium-mediated transformation in soybean half-seeds. The inclusion of PAs to culture medium along with optimal plant growth regulators (PGRs) enhanced shoot induction [98.3 %; 4.44 µM N(6)-benzyladenine (BA) and 103.27 µM spermidine] and elongation [90.0 %; 1.45 µM gibberellic acid (GA3) and 49.42 µM spermine]. The polyamine putrescine (62.08 µM) alone greatly enriched root induction (96...
December 2016: 3 Biotech
https://www.readbyqxmd.com/read/28328973/differing-metabolic-responses-to-salt-stress-in-wheat-barley-addition-lines-containing-different-7h-chromosomal-fragments
#11
Eva Darko, Krisztián Gierczik, Orsolya Hudák, Péter Forgó, Magda Pál, Edina Türkösi, Viktória Kovács, Sándor Dulai, Imre Majláth, István Molnár, Tibor Janda, Márta Molnár-Láng
Salinity-induced osmotic, ionic and oxidative stress responses were investigated on Asakaze/Manas wheat/barley addition lines 7H, 7HL and 7HS, together with their barley (salt-tolerant) and wheat (relatively salt-sensitive) parents. Growth, photosynthetic activity, chlorophyll degradation, proline, glycine betaine accumulation, sugar metabolism, Na+ and K+ uptake and transport processes and the role of polyamines and antioxidants were studied in young plants grown in hydroponic culture with or without salt treatment...
2017: PloS One
https://www.readbyqxmd.com/read/28328538/hyperbranched-polyamine-assisted-synthesis-of-dual-luminescent-gold-composite-with-ph-responsive-character
#12
Zhiqin Yuan, Yi Du, Yan He
We present a facile one-pot, two-step strategy to prepare water-soluble dual-luminescent gold nanodots (AuNDs) and few-atom gold nanocluster composites simultaneously by using high molecular weight and hyperbranched polyethyleneimine (hPEI) as the protection ligand and stabilization agent. It was found that in the presence of hPEI, Au(III) ion can be reduced to a metastable Au(I) charge state in aqueous solution. Subsequently, adding 11-mercaptoundonioic acid induces parallel pathways of restricted Au(I) assembly, leading to the formation of both red-emitting hPEI stabilized AuNDs and blue-emitting hPEI-protected Au8 nanoclusters...
March 22, 2017: Methods and Applications in Fluorescence
https://www.readbyqxmd.com/read/28324173/effect-of-oaz1-overexpression-on-goose-ovarian-granulosa-cells
#13
Bo Kang, Dongmei Jiang, Hui He, Rong Ma, Ziyu Chen, Zhixin Yi
Ornithine decarboxylase antizyme 1 (OAZ1) regulates both polyamine biosynthesis and transport and acts as a tumor suppressor because of its functions in the regulation of cell proliferation, apoptosis and growth. However, the roles of OAZ1 in the regulation of polyamine metabolism, cell proliferation, apoptosis and hormone receptor expression in granulosa cells (GCs) from geese have not been determined. To define the roles of OAZ1 in primary GCs, we constructed and transfected an Oaz1 overexpression vector with a thymidine deletion into primary GCs...
March 21, 2017: Amino Acids
https://www.readbyqxmd.com/read/28323015/simultaneously-achieve-soluble-expression-and-biomimetic-immobilization-of-candida-antarctica-lipase-b-by-introducing-polyamine-tags
#14
Xiaoxue Zhou, Yu Han, Zheng Lv, Xuemei Tian, Han Li, Panpan Xie, Liangyu Zheng
Polyamine tags fused in Candida antarctica lipase B (CalB) can help achieve high soluble expression of CalB in E. coli and can directly mediate silicification, which leads to rapid formation of a CalB-silica particle complex through a one-step approach. After optimization experiments, the fused lipase CalB tagged with 6-histidine at the N terminal and 10-lysine at the C terminal (6His-CalB-10Lys) is effectively expressed with high solubility (0.1mg/mL) and specific activity (10.1U/mg), and easily cross-linked in silica particles with a high immobilization efficiency of 96...
March 16, 2017: Journal of Biotechnology
https://www.readbyqxmd.com/read/28322056/preparation-of-ultrathin-robust-nanohybrid-capsules-through-a-beyond-biomineralization-method
#15
Shaohua Zhang, Zhongyi Jiang, Weilun Qian, Jiafu Shi, Xiaoli Wang, Lei Tang, Hongjian Zou, Hua Liu
Herein, a facile and generic method is developed to prepare ultrathin, robust nanohybrid capsules by manipulating the dynamic structure of supramolecular nanocoatings on CaCO3 sacrificial templates through incorporating multivalent-anion substitution process into biomineralization. Above biomineralization level, multivalent anions, e.g., phosphate, sulfate or citrate, are employed to initiate the assembly of polyamine into continuous (non-segregated) polyamine-anion supramolecular nanocoatings on CaCO3 sacrificial templates...
March 21, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28321369/developmental-and-loco-like-effects-of-a-swainsonine-induced-inhibition-of-%C3%AE-mannosidase-in-the-honey-bee-apis-mellifera
#16
Laura Wedd, Regan Ashby, Sylvain Foret, Ryszard Maleszka
BACKGROUND: Deficiencies in lysosomal a-mannosidase (LAM) activity in animals, caused either by mutations or by consuming toxic alkaloids, lead to severe phenotypic and behavioural consequences. Yet, epialleles adversely affecting LAM expression exist in the honey bee population suggesting that they might be beneficial in certain contexts and cannot be eliminated by natural selection. METHODS: We have used a combination of enzymology, molecular biology and metabolomics to characterise the catalytic properties of honey bee LAM (AmLAM) and then used an indolizidine alkaloid swainsonine to inhibit its activity in vitro and in vivo...
2017: PeerJ
https://www.readbyqxmd.com/read/28318590/supplementation-with-rumen-protected-methionine-or-choline-during-the-transition-period-influences-whole-blood-immune-response-in-periparturient-dairy-cows
#17
M Vailati-Riboni, Z Zhou, C B Jacometo, A Minuti, E Trevisi, D N Luchini, J J Loor
Methionine, together with Lys, is the most limiting AA for milk production in dairy cows. Besides its crucial role in milk production, Met and its derivate metabolites (e.g., glutathione, taurine, polyamines) are well-known immunonutrients in nonruminants, helping support and boost immune function and activity. In the present study, the effects of Met or choline, as its precursor, were investigated using an ex vivo whole blood challenge. The study involved 33 multiparous Holstein cows (from a larger cohort with a factorial arrangement of treatments) assigned from d -21 to +30 relative to parturition to a basal control (CON) diet, CON plus rumen-protected Met (MET, Smartamine M, Adisseo NA, Alpharetta, GA) at a rate of 0...
March 16, 2017: Journal of Dairy Science
https://www.readbyqxmd.com/read/28317753/bioactive-amines-and-phenolic-compounds-in-cocoa-beans-are-affected-by-fermentation
#18
Brenda de Nazaré do Carmo Brito, Renan Campos Chisté, Rosinelson da Silva Pena, Maria Beatriz Abreu Gloria, Alessandra Santos Lopes
Cocoa is the target of increased scientific research as it is one of the richest source of bioactive compounds. The formation of bioactive amines and their changes in cocoa beans during seven days of traditional fermentation was investigated for the first time. In addition, total phenolic compounds, anthocyanins contents and the scavenging capacity against ABTS radical were determined to monitor the fermentation process. Only two biogenic amines (tryptamine and tyramine) and two polyamines (spermidine and spermine) were detected in cocoa beans during fermentation...
August 1, 2017: Food Chemistry
https://www.readbyqxmd.com/read/28316010/protective-effect-of-lactobacillus-casei-on-dmh-induced-colon-carcinogenesis-in-mice
#19
Cesar Antonio Irecta-Nájera, María Del Rosario Huizar-López, Josefina Casas-Solís, Patricia Castro-Félix, Anne Santerre
The administration of probiotics is a promising approach to reduce the prevalence of colon cancer, a multifactorial disease, with hereditary factors, as well as environmental lifestyle-related risk factors. Biogenic polyamines, putrescine, spermidine, and spermine are small cationic molecules with great roles in cell proliferation and differentiation as well as regulation of gene expression. Ornithine decarboxylase is the first rate-limiting enzyme for polyamine synthesis, and upregulation of ornithine decarboxylase activity and polyamine metabolism has been associated with abnormal cell proliferation...
March 18, 2017: Probiotics and Antimicrobial Proteins
https://www.readbyqxmd.com/read/28315656/expression-of-odc1-spd-spm-and-azin1-in-the-hypothalamus-ovary-and-uterus-during-rat-estrous-cycle
#20
Joseph R D Fernandes, Sammit Jain, Arnab Banerjee
The aim of the present study was to investigate variation in the expression pattern of ornithine decarboxylase (ODC1), spermine (SPM), spermidine (SPD) and antizyme inhibitor (AZIN1) in hypothalamus, ovary and uterus during the estrous cycle of rats. Further, to understand any correlation between polyamines and GnRH I expression in hypothalamus; effect of putrescine treatment on GnRH I expression in hypothalamus and progesterone and estradiol levels in serum were investigated. The study also aims in quantifying all the immunohistochemistry images obtained based on pixel counting algorithm to yield the relative pixel count...
March 16, 2017: General and Comparative Endocrinology
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