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https://www.readbyqxmd.com/read/28212490/vitamin-e-succinate-grafted-chitosan-oligosaccharide-rgd-conjugated-tpgs-mixed-micelles-loaded-with-paclitaxel-for-u87mg-tumor-therapy
#1
Yanzuo Chen, Shu Feng, Wenchao Liu, Zeting Yuan, Peihao Yin, Feng Gao
The poor therapeutic efficacy of hydrophobic chemotherapeutic drugs is an intrinsic limitation to successful chemotherapy. In the present study, a multi-task delivery system based on arginine-glycine-aspartic acid peptide (RGD) decorated vitamin E succinate (VES)-grafted-chitosan oligosaccharide (CSO)/RGD-conjugated D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS-RGD) mixed micelles (VeC/T-RGD MM) was first prepared for targeted delivery of paclitaxel (PTX), a hydrophobic anticancer drug, to improve the efficacy of U87MG tumor therapy...
February 17, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28211672/proteomic-analysis-of-post-synaptic-protein-complexes-underlying-neuronal-plasticity
#2
Anthony J Baucum
Normal neuronal communication and synaptic plasticity at glutamatergic synapses requires dynamic regulation of postsynaptic molecules. Protein expression and protein post-translational modifications regulate protein interactions that underlie this organization. In this review, we highlight data obtained over the last 20 years that have used qualitative and quantitative proteomics-based approaches to identify postsynaptic protein complexes. Herein, we describe how these proteomics studies have helped lay the foundation for understanding synaptic physiology and perturbations in synaptic signaling observed in different pathologies...
February 17, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28209776/distance-dependent-gradient-in-nmdar-driven-spine-calcium-signals-along-tapering-dendrites
#3
Alison S Walker, Guilherme Neves, Federico Grillo, Rachel E Jackson, Mark Rigby, Cian O'Donnell, Andrew S Lowe, Gema Vizcay-Barrena, Roland A Fleck, Juan Burrone
Neurons receive a multitude of synaptic inputs along their dendritic arbor, but how this highly heterogeneous population of synaptic compartments is spatially organized remains unclear. By measuring N-methyl-d-aspartic acid receptor (NMDAR)-driven calcium responses in single spines, we provide a spatial map of synaptic calcium signals along dendritic arbors of hippocampal neurons and relate this to measures of synapse structure. We find that quantal NMDAR calcium signals increase in amplitude as they approach a thinning dendritic tip end...
February 16, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28209540/in-vitro-characterization-of-ph-sensitive-azithromycin-loaded-methoxy-poly-ethylene-glycol-block-poly-aspartic-acid-graft-imidazole-micelles
#4
Fangfang Teng, Peizong Deng, Zhimei Song, Feilong Zhou, Runliang Feng, Na Liu
In order to improve azithromycin's antibacterial activity in acidic medium, monomethoxy poly (ethylene glycol)-block-poly (aspartic acid-graft-imidazole) copolymer was synthesized through allylation, free radical addition, ring-opening polymerization and amidation reactions with methoxy poly (ethylene glycol) as raw material. Drug loading capacity and encapsulation efficiency of azithromycin-loaded micelles prepared via thin film hydration method were 11.58±0.86% and 96.06±1.93%, respectively. The drug-loaded micelles showed pH-dependent property in the respects of particle size, zeta potential at the range of pH 5...
February 9, 2017: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/28207324/is-serum-angiotensin-converting-enzyme-level-useful-for-determining-necroinflammatory-activity-in-chronic-hepatitis-b-infection
#5
Ahmet Tay, Fatih Albayrak, Sevilay Ozmen, Ayse Albayrak, Kemalettin Ozden
AIM: The purpose of this study was to investigate the relationship between the findings from liver biopsy and the serum angiotensin-converting enzyme (ACE) level to determine whether ACE might serve as a potential noninvasive sign of necroinflammatory activity in patients with Chronic Hepatitis B (CHB) infection. METHODS: A total of 54 CHB patients referred for liver biopsy were enrolled in the study. Serum ACE levels were determined photometrically with a kinetic test...
February 2017: Genetic Testing and Molecular Biomarkers
https://www.readbyqxmd.com/read/28203242/sunlight-modulates-fruit-metabolic-profile-and-shapes-the-spatial-pattern-of-compound-accumulation-within-the-grape-cluster
#6
Noam Reshef, Natasha Walbaum, Nurit Agam, Aaron Fait
Vineyards are characterized by their large spatial variability of solar irradiance (SI) and temperature, known to effectively modulate grape metabolism. To explore the role of sunlight in shaping fruit composition and cluster uniformity, we studied the spatial pattern of incoming irradiance, fruit temperature and metabolic profile within individual grape clusters under three levels of sunlight exposure. The experiment was conducted in a vineyard of Cabernet Sauvignon cv. located in the Negev Highlands, Israel, where excess SI and midday temperatures are known to degrade grape quality...
2017: Frontiers in Plant Science
https://www.readbyqxmd.com/read/28202898/engineering-a-lys-asn-isopeptide-bond-into-an-immunoglobulin-like-protein-domain-enhances-its-stability
#7
Hanna Kwon, Paul G Young, Christopher J Squire, Edward N Baker
The overall stability of globular protein structures is marginal, a balance between large numbers of stabilizing non-covalent interactions and a destabilizing entropic term. Higher stability can be engineered by introduction of disulfide bonds, provided the redox environment is controlled. The discovery of stabilizing isopeptide bond crosslinks, formed spontaneously between lysine and asparagine (or aspartic acid) side chains in certain bacterial cell-surface proteins suggests that such bonds could be introduced by protein engineering as an alternative protein stabilization strategy...
February 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28202577/nimesulide-and-4-hydroxynimesulide-as-bile-acid-transporters-inhibitors-are-contributory-factors-for-drug-induced-cholestasis
#8
Lei Zhou, Xiaoyan Pang, Jingfang Jiang, Dafang Zhong, Xiaoyan Chen
Nimesulide (NIM) is a classic nonsteroidal anti-inflammatory drug. However, some patients treated with NIM suffered from cholestatic liver injury. For this reason, we investigated the potential mechanism underlying NIM-induced cholestasis by using in vivo and in vitro models. Oral administration of 100 mg/kg/day NIM to Wistar rats for 5 days increased the levels of plasma total bile acids, alkaline phosphatase, alanine aminotransferase, and aspartate aminotransferase by 1.49-, 1.31-, 1.60-, and 1.29-fold, respectively...
February 15, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28202572/differential-regulation-of-nmda-receptors-by-d-serine-and-glycine-in-mammalian-spinal-locomotor-networks
#9
David Acton, Gareth Brian Miles
Activation of N-methyl-D-aspartate receptors (NMDARs) requires the binding of a co-agonist, either D-serine or glycine, in addition to glutamate. Changes in occupancy of the co-agonist binding site are proposed to modulate neural networks including those controlling swimming in frog tadpoles. Here, we characterize regulation of the NMDAR co-agonist binding site in mammalian spinal locomotor networks. Blockade of NMDARs by D(-)-2-amino-5-phosphonopentanoic acid (D-APV) or 5,7-dichlorokynurenic acid reduced the frequency and amplitude of pharmacologically induced locomotor-related activity recorded from the ventral roots of spinal-cord preparations from neonatal mice...
February 15, 2017: Journal of Neurophysiology
https://www.readbyqxmd.com/read/28202112/-risk-factors-for-poor-prognosis-in-children-with-severe-adenovirus-pneumonia
#10
Miao Huang, Rong Luo, Zhou Fu
OBJECTIVE: To investigate the risk factors for poor prognosis of severe adenovirus pneumonia (SAP) in children. METHODS: The clinical data of 189 children with SAP were retrospectively analyzed. Univariate logistic regression analysis was performed to assess the risk factors for poor prognosis. RESULTS: The univariate logistic regression analysis showed that the patients with hemoglobin <90 g/L, plasma albumin <30 g/L, C-reactive protein >30 mg/L, procalcitonin >10 ng/mL, alanine aminotransferase >100 U/L, or aspartate aminotransferase >100 U/L had poor prognosis (P<0...
February 2017: Zhongguo Dang Dai Er Ke za Zhi, Chinese Journal of Contemporary Pediatrics
https://www.readbyqxmd.com/read/28198441/pdi-regulates-seizure-activity-via-nmda-receptor-redox-in-rats
#11
Ji Yang Kim, Ah-Rhem Ko, Hye-Won Hyun, Su-Ji Min, Ji-Eun Kim
Redox modulation of cysteine residues is one of the post-translational modifications of N-methyl-D-aspartate receptor (NMDAR). Protein disulfide isomerases (PDI), an endoplasmic reticulum (ER) chaperone, plays a crucial role in catalyzing disulfide bond formation, reduction, and isomerization. In the present study, we found that PDI bound to NMDAR in the normal hippocampus, and that this binding was increased in chronic epileptic rats. In vitro thiol reductase assay revealed that PDI increased the amount of thiols on full-length recombinant NR1 protein...
February 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28198207/neurophysiological-symptoms-and-aspartame-what-is-the-connection
#12
Arbind Kumar Choudhary, Yeong Yeh Lee
Aspartame (α-aspartyl-l-phenylalanine-o-methyl ester), an artificial sweetener, has been linked to behavioral and cognitive problems. Possible neurophysiological symptoms include learning problems, headache, seizure, migraines, irritable moods, anxiety, depression, and insomnia. The consumption of aspartame, unlike dietary protein, can elevate the levels of phenylalanine and aspartic acid in the brain. These compounds can inhibit the synthesis and release of neurotransmitters, dopamine, norepinephrine, and serotonin, which are known regulators of neurophysiological activity...
February 15, 2017: Nutritional Neuroscience
https://www.readbyqxmd.com/read/28197933/garlic-extract-attenuates-immobilization-stress-induced-alterations-in-plasma-antioxidant-oxidant-parameters-and-hepatic-function-in-rats
#13
Syed Kashif Zaidi, Shakeel Ahmed Ansari, Shams Tabrez, Md Nasrul Hoda, Ghulam Md Ashraf, Mohd Shahnawaz Khan, Sultan Alnohair, Naheed Banu, Mohammed Hussain Al-Qahtani
OBJECTIVE: To investigate the oxidative stress induced by 6 h of immobilization stress in Albino Wistar rats. Further, the pre- and post-treatment of aqueous garlic extract was studied to evaluate its preventive and curative efficacy on stress-induced altered oxidative parameters in rats. METHODS: Albino Wistar rats were exposed to 6 h of immobilization stress, and received garlic extract (100 mg/kg body weight) treatment pre- or post-stress exposure. The oxidative status of plasma after various treatments were evaluated by determining the levels of reduced glutathione, glucose, uric acid, thiobarbituric acid reactive substances, aspartate aminotransferase (AST), alanine transaminase (ALT), alkaline phosphatase (ALP) and the activities of superoxide dismutase, catalase and glutathione-S-transferase by standardized procedures...
February 15, 2017: Chinese Journal of Integrative Medicine
https://www.readbyqxmd.com/read/28195728/room-temperature-neutron-crystallography-of-drug-resistant-hiv-1-protease-uncovers-limitations-of-x-ray-structural-analysis-at-100k
#14
Oksana O Gerlits, David A Keen, Matthew P Blakeley, John M Louis, Irene T Weber, Andrey Y Kovalevsky
HIV-1 protease inhibitors are crucial for treatment of HIV-1/AIDS, but their effectiveness is thwarted by rapid emergence of drug resistance. To better understand binding of clinical inhibitors to resistant HIV-1 protease, we used room-temperature joint X-ray/Neutron (XN) crystallography to obtain an atomic-resolution structure of the protease triple mutant (V32I/I47V/V82I) in complex with amprenavir. The XN structure reveals a D+ ion located midway between the inner Oδ1 oxygen atoms of the catalytic aspartic acid residues...
February 14, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28194754/requirement-of-extracellular-ca-2-binding-to-specific-amino-acids-for-heat-evoked-activation-of-trpa1
#15
Erkin Kurganov, Shigeru Saito, Claire T Saito, Makoto Tominaga
Transient receptor potential ankyrin 1 (TRPA1) is a homotetrameric nonselective cation-permeable channel that has six transmembrane domains and cytoplasmic N- and C-termini. The N-terminus is characterized by an unusually large number of ankyrin repeats. Although the 3-dimensional structure of human TRPA1 has been determined, and TRPA1 channels from insects to birds are known to be activated by heat stimulus, the mechanism for temperature-dependent TRPA1 activation is unclear. We previously reported that extracellular Ca(2+) , but not intracellular Ca(2+) , plays an important role in heat-evoked TRPA1 activation in green anole lizards (gaTRPA1)...
February 14, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28194553/acidic-domains-differentially-read-histone-h3-lysine-4-methylation-status-and-are-widely-present-in-chromatin-associated-proteins
#16
Meng Wu, Wei Wei, Jiwei Chen, Rong Cong, Tieliu Shi, Jiwen Li, Jiemin Wong, James X Du
Histone methylation is believed to provide binding sites for specific reader proteins, which translate histone code into biological function. Here we show that a family of acidic domain-containing proteins including nucleophosmin (NPM1), pp32, SET/TAF1β, nucleolin (NCL) and upstream binding factor (UBF) are novel H3K4me2-binding proteins. These proteins exhibit a unique pattern of interaction with methylated H3K4, as their binding is stimulated by H3K4me2 and inhibited by H3K4me1 and H3K4me3. These proteins contain one or more acidic domains consisting mainly of aspartic and/or glutamic residues that are necessary for preferential binding of H3K4me2...
February 13, 2017: Science China. Life Sciences
https://www.readbyqxmd.com/read/28194143/novel-immunity-proteins-associated-with-colicin-m-like-bacteriocins-exhibit-promiscuous-protection-in-pseudomonas
#17
Maarten G K Ghequire, Lieselore Kemland, René De Mot
Bacteriocins related to colicin M, acting via cleavage of the cell wall precursor lipid II, have been characterized in γ- and β-proteobacteria. Depending on the species, immunity is provided by either an inner membrane-anchored periplasmic protein or by an integral membrane protein. In Pseudomonas however, the immunity partner of colicin M-like bacteriocins remains unknown. Based on an in silico analysis in pseudomonad genomes, we here identify a gene encoding a putative immunity partner that represents a novel type of integral membrane protein (PmiA, Pseudomonas colicin M-like immunity type A)...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28193602/preference-for-and-learning-of-amino-acids-in-larval-drosophila
#18
Nana Kudow, Daisuke Miura, Michael Schleyer, Naoko Toshima, Bertram Gerber, Teiichi Tanimura
Relative to other nutrients, less is known about how animals sense amino acids and how behaviour is organized accordingly. This is a significant gap in our knowledge, because amino acids are required for protein synthesis-and hence for life as we know it. Choosing larvae as a study case, we provide the first systematic analysis of both the preference behaviour for and the learning of all 20 canonical amino acids in Drosophila We report that preference for individual amino acids differs according to the kind of amino acid, both in first-instar and in third-instar larvae...
February 13, 2017: Biology Open
https://www.readbyqxmd.com/read/28193531/mutation-of-a-putative-map-kinase-consensus-site-regulates-ncam-endocytosis-and-ncam-dependent-neurite-outgrowth
#19
Tobias Goschzik, Harold Cremer, Vinayaga S Gnanapragassam, Rüdiger Horstkorte, Kaya Bork, Simone Diestel
The cytoplasmic domain of the neural cell adhesion molecule NCAM contains several putative serine/threonine phosphorylation sites whose functions are largely unknown. Human NCAM140 (NCAM140) possesses a potential MAP kinase phosphorylation site at threonine (T) 803. The aim of this study was to analyze a possible phosphorylation of NCAM140 by MAP kinases and to identify the functional role of T803. We found that NCAM140 is phosphorylated by the MAP kinase ERK2 in vitro. Exchange of T803 to aspartic acid (D) which mimics constitutive phosphorylation at the respective position resulted in increased endocytosis compared to NCAM140 in neuroblastoma cells and primary neurons...
February 10, 2017: Neuroscience Research
https://www.readbyqxmd.com/read/28193330/conversion-of-cysteine-to-3-mercaptopyruvic-acid-by-bacterial-aminotransferases
#20
Christina Andreeßen, Vanessa Gerlt, Alexander Steinbüchel
3-Mercaptopyruvate (3MPy), a structural analog of 3-mercaptopropionic acid, is a precursor compound for biosynthesis of polythioesters in bacteria. The cost-effectiveness and sustainability of the whole process could be greatly improved by using the cysteine degradation pathway for an intracellular supply of 3MPy. Transamination of cysteine to its corresponding α-keto acid 3MPy is catalyzed by cysteine aminotransferases (CAT). However, CAT activity has so far not been described for bacterial aminotransferases (AT), and it was unknown whether they can be applied for the conversion of cysteine to 3MPy...
April 2017: Enzyme and Microbial Technology
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