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https://www.readbyqxmd.com/read/28544602/drug-residues-in-syringes-and-other-injecting-paraphernalia-in-hungary
#1
Anna Péterfi, József Csorba, Tamás Figeczki, József Kiss, Katalin Medgyesi-Frank, János Posta, V Anna Gyarmathy
The appearance and spread of new psychoactive substances (NPS) is a phenomenon detected throughout Europe since 2008. Synthetic cathinones, a group of NPS, have been self-reported as the drug injected by the vast majority of people who inject drugs (PWID) in Hungary. This study aims at updating our knowledge on what exactly the compounds injected by PWID. This multi-site study analysed residues from used injecting drug paraphernalia collected from PWID via low threshold services and from public places in Budapest, Debrecen, Miskolc, Szeged, Békéscsaba and Pécs between March 2015 and February 2016...
May 23, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28542923/the-polysialic-acid-mimetics-idarubicin-and-irinotecan-stimulate-neuronal-survival-and-neurite-outgrowth-and-signal-via-protein-kinase-c
#2
Gabriele Loers, Steven Astafiev, Yuliya Hapiak, Vedangana Saini, Bibhudatta Mishra, Sheraz Gul, Gurcharan Kaur, Melitta Schachner, Thomas Theis
Polysialic acid (PSA) is a large, negatively charged, linear homopolymer of alpha2-8-linked sialic acid residues. It is generated by two polysialyltransferases and attached to N- and/or O-linked glycans, and its main carrier is the neural cell adhesion molecule NCAM. PSA controls the development and regeneration of the nervous system by enhancing cell migration, axon pathfinding, synaptic targeting, synaptic plasticity, by regulating the differentiation of progenitor cells and by modulating cell-cell and cell-matrix adhesions...
May 24, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28542711/preventing-relapse-after-haematopoietic-stem-cell-transplantation-for-acute-leukaemia-the-role-of-post-transplantation-minimal-residual-disease-mrd-monitoring-and-mrd-directed-intervention
#3
REVIEW
Xiao-Dong Mo, Meng Lv, Xiao-Jun Huang
Relapse is the main cause of treatment failure after allogeneic haematopoietic stem cell transplantation (allo-HSCT) for acute leukaemia (AL). Post-transplantation minimal residual disease (MRD) monitoring enables risk stratification and identifies AL patients at higher risk of relapse. MRD assessment primarily involves the determination of leukaemia-associated immunophenotypic patterns using multiparameter flow cytometry, and the polymerase chain reaction (PCR)-based evaluation of expression levels of leukaemia-related genes (specific reciprocal gene rearrangements and other mutation types)...
May 23, 2017: British Journal of Haematology
https://www.readbyqxmd.com/read/28541812/engineering-humanized-antibody-framework-sequences-for-optimal-site-specific-conjugation-of-cytotoxins
#4
Jared L Spidel, Earl F Albone, Xin Cheng, Benjamin Vaessen, Sara Jacob, Andrew Z Milinichik, Arielle Verdi, J Bradford Kline, Luigi Grasso
The prevailing techniques used to generate antibody-drug conjugates (ADCs) involve random conjugation of the linker-drug to multiple lysines or cysteines in the antibody. Engineering natural and non-natural amino acids into an antibody has been demonstrated to be an effective strategy to produce homogeneous ADC products with defined drug-to-antibody ratios. We recently reported an efficient residue-specific conjugation technology (RESPECT) where thiol-reactive payloads can be efficiently conjugated to a native unpaired cysteine in position 80 (C80) of rabbit light chains...
May 25, 2017: MAbs
https://www.readbyqxmd.com/read/28541760/inhibition-of-proteases-activity-in-intestine-needs-a-sustainable-acidic-environment-rather-than-a-transient
#5
Chang Xing, Jin-Feng Xing, Zhi-Qiang Ge
α-Chymotrypsin (α-CT) and trypsin are important components of the enzymatic barrier. They could degrade the therapeutic proteins and peptides, inhibit their activity consequently, and thereby reduce their oral bioavailability. Acidic agents, as one type of indirect protease inhibitors, have shown proof of concept in clinical trials. We report here the inactivated proteases due to acid influence can be reactivated immediately by environmental pH recovery regardless of how long the inactivation last. To keep the inactivation time of proteases for 4 to 5 h, we designed and prepared a sustained-release tablet containing citric acid (CA) which can effectively reduce the pH below 5...
May 25, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28541476/7-8-dihydroxyflavone-ameliorates-cognitive-and-motor-deficits-in-a-huntington-s-disease-mouse-model-through-specific-activation-of-the-plc%C3%AE-1-pathway
#6
Gerardo García-Díaz Barriga, Albert Giralt, Marta Anglada-Huguet, Nuria Gaja-Capdevila, Javier G Orlandi, Jordi Soriano, Josep-Maria Canals, Jordi Alberch
Huntington's disease (HD) is a fatal neurodegenerative disease with motor, cognitive and psychiatric impairment. Dysfunctions in HD models have been related to reduced levels of striatal brain-derived neurotrophic factor (BDNF) and imbalance between its receptors TrkB and p75(NTR). Thus, molecules with activity on the BDNF/TrkB/p75 system can have therapeutic potential. 7,8-Dihydroxyflavone (7,8-DHF) was described as a TrkB agonist in several models of neuro-degenerative diseases, however, its TrkB activation profile needs further investigation due to its pleiotropic properties and divergence from BDNF effect...
May 24, 2017: Human Molecular Genetics
https://www.readbyqxmd.com/read/28539730/near-infrared-spectroscopy-as-a-process-analytical-technology-tool-for-monitoring-the-parching-process-of-traditional-chinese-medicine-based-on-two-kinds-of-chemical-indicators
#7
Kaiyue Li, Weiying Wang, Yanping Liu, Su Jiang, Guo Huang, Liming Ye
BACKGROUND: The active ingredients and thus pharmacological efficacy of traditional Chinese medicine (TCM) at different degrees of parching process vary greatly. OBJECTIVE: Near-infrared spectroscopy (NIR) was used to develop a new method for rapid online analysis of TCM parching process, using two kinds of chemical indicators (5-(hydroxymethyl) furfural [5-HMF] content and 420 nm absorbance) as reference values which were obviously observed and changed in most TCM parching process...
April 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28538757/brazilian-cross-cultural-adaptation-and-validation-of-the-list-of-threatening-events-questionnaire-lte-q
#8
Patrícia B de Abreu, Hugo Cogo-Moreira, Regina A Pose, Ronaldo Laranjeira, Raul Caetano, Carolina M Gaya, Clarice S Madruga
Objective: To perform a construct validation of the List of Threatening Events Questionnaire (LTE-Q), as well as convergence validation by identifying its association with drug use in a sample of the Brazilian population. Methods: This is a secondary analysis of the Second Brazilian National Alcohol and Drugs Survey (II BNADS), which used a cross-cultural adaptation of the LTE-Q in a probabilistic sample of 4,607 participants aged 14 years and older. Latent class analysis was used to validate the latent trait adversity (which considered the number of events from the list of 12 item in the LTE experienced by the respondent in the previous year) and logistic regression was performed to find its association with binge drinking and cocaine use...
May 22, 2017: Revista Brasileira de Psiquiatria
https://www.readbyqxmd.com/read/28535462/pharmaceutical-substances-in-ambient-particulates-a-preliminary-assessment
#9
Angelo Cecinato, Paola Romagnoli, Mattia Perilli, Catia Balducci
Till now, no attention has been paid to pharmaceuticals (PCs) in the air, though they are known to affect waters, soils, foods and biota. This paper describes the first attempt to characterize the PC occurrence in the air. Airborne particulates (PM10 or PM2.5 fractions, from Amsterdam, Netherland, Rome and Rende, Italy) were sampled on quartz fiber filter by means of pumping systems operating at medium-volume conditions (16 or 38.5 L min(-1)). The samples were solvent extracted through sonication with a dichloromethane:acetone:methanol mixture and reduced close to dryness; three fractions of the residue were separated through column chromatography; they comprised non polar, low polar and very polar organic compounds, respectively, and PCs were in the third one...
May 18, 2017: Chemosphere
https://www.readbyqxmd.com/read/28533430/heme-thiolate-sulfenylation-of-human-cytochrome-p450-4a11-functions-as-a-redox-switch-for-catalytic-inhibition
#10
Matthew E Albertolle, Donghak Kim, Leslie D Nagy, Chul-Ho Yun, Ambra Pozzi, Uzen Savas, Eric F Johnson, F Peter Guengerich
Cytochrome P450 (P450, CYP) 4A11 is a human fatty acid ω-hydroxylase that catalyzes the oxidation of arachidonic acid to the eicosanoid 20- hydroxyeicosatetraenoic acid (20-HETE), which plays important roles in regulating blood pressure regulation. Variants of P450 4A11 have been associated with high blood pressure and resistance to anti-hypertensive drugs, and 20-HETE has both pro- and antihypertensive properties relating to increased vasoconstriction and natriuresis, respectively. These physiological activities are likely influenced by the redox environment, but the mechanisms are unclear...
May 22, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28531794/binding-of-the-anticancer-drug-bi-2536-to-human-serum-albumin-a-spectroscopic-and-theoretical-study
#11
Jesús Fernández-Sainz, Pedro J Pacheco-Liñán, José M Granadino-Roldán, Iván Bravo, Andrés Garzón, Jaime Rubio-Martínez, José Albaladejo
BI-2536 is a potent Polo-like kinase inhibitor which induces apoptosis in diverse human cancer cell lines. The binding affinity of BI-2536 for human serum albumin (HSA) protein may define its pharmacokinetic and pharmacodynamic profile. We have studied the binding of BI-2536 to HSA by means of different spectroscopic techniques and docking calculations. We have experimentally observed that the affinity of BI-2536 for HSA is higher than that of other common HSA binding drugs. Therefore, it can be postulated that the drug dose should be increased to achieve a certain concentration of free drug in plasma, although BI-2536 could also reach tumour tissues by uptaking HSA/BI-2536 complex...
May 12, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28531373/identification-of-potential-inhibitors-for-hcv-ns3-genotype-4a-by-combining-protein-ligand-interaction-fingerprint-3d-pharmacophore-docking-and-dynamic-simulation
#12
Mahmoud Abd El-Monem El-Hasab, Eman Esmat El-Bastawissy, Tarek Faathy El-Moselhy
HCV NS3 protease domain has been one of the most attractive targets for developing new drugs for HCV infection and many drugs were successfully developed, but all of them were designed for targeting HCV genotype 1 infection. HCV genotype 4a dominant in Egypt has paid less attention. Here we describe our protocol of virtual screening in identification of novel potential potent inhibitors for HCV NS3 of genotype 4a using homology modelling, PLIF (protein ligand interaction fingerprint), docking, pharmacophore and dynamic simulation...
May 20, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28531330/structural-basis-for-substrate-binding-and-catalytic-mechanism-of-a-human-rna-m5c-methyltransferase-nsun6
#13
Ru-Juan Liu, Tao Long, Jing Li, Hao Li, En-Duo Wang
5-methylcytosine (m5C) modifications of RNA are ubiquitous in nature and play important roles in many biological processes such as protein translational regulation, RNA processing and stress response. Aberrant expressions of RNA:m5C methyltransferases are closely associated with various human diseases including cancers. However, no structural information for RNA-bound RNA:m5C methyltransferase was available until now, hindering elucidation of the catalytic mechanism behind RNA:m5C methylation. Here, we have solved the structures of NSun6, a human tRNA:m5C methyltransferase, in the apo form and in complex with a full-length tRNA substrate...
May 22, 2017: Nucleic Acids Research
https://www.readbyqxmd.com/read/28531225/protein-charge-distribution-in-proteomes-and-its-impact-on-translation
#14
Rodrigo D Requião, Luiza Fernandes, Henrique José Araujo de Souza, Silvana Rossetto, Tatiana Domitrovic, Fernando L Palhano
As proteins are synthesized, the nascent polypeptide must pass through a negatively charged exit tunnel. During this stage, positively charged stretches can interact with the ribosome walls and slow the translation. Therefore, charged polypeptides may be important factors that affect protein expression. To determine the frequency and distribution of positively and negatively charged stretches in different proteomes, the net charge was calculated for every 30 consecutive amino acid residues, which corresponds to the length of the ribosome exit tunnel...
May 22, 2017: PLoS Computational Biology
https://www.readbyqxmd.com/read/28530593/dummy-template-molecularly-imprinted-polymer-for-solid-phase-extraction-of-phenothiazines-in-meat-based-on-computational-simulation
#15
Yi Ping Song, Nan Li, Hui Cai Zhang, Geng Nan Wang, Ju Xiang Liu, Jing Liu, Jian Ping Wang
The 3D structures of two dummy templates and four phenothiazine drugs were studied by using computational simulation method. Then the two dummy templates were used to synthesize two molecularly imprinted polymers respectively. Results showed that the recognition abilities of the two polymers were consistent with the theoretical calculation. Then a solid phase extraction column was developed for extraction of the four phenothiazines in meat (pork, chicken) followed by determination with high performance liquid chromatography...
October 15, 2017: Food Chemistry
https://www.readbyqxmd.com/read/28529645/tumor-penetrating-theranostic-nanoparticles-for-enhancement-of-targeted-and-image-guided-drug-delivery-into-peritoneal-tumors-following-intraperitoneal-delivery
#16
Ning Gao, Erica N Bozeman, Weiping Qian, Liya Wang, Hongyu Chen, Malgorzata Lipowska, Charles A Staley, Y Andrew Wang, Hui Mao, Lily Yang
The major obstacles in intraperitoneal (i.p.) chemotherapy of peritoneal tumors are fast absorption of drugs into the blood circulation, local and systemic toxicities, inadequate drug penetration into large tumors, and drug resistance. Targeted theranostic nanoparticles offer an opportunity to enhance the efficacy of i.p. therapy by increasing intratumoral drug delivery to overcome resistance, mediating image-guided drug delivery, and reducing systemic toxicity. Herein we report that i.p. delivery of urokinase plasminogen activator receptor (uPAR) targeted magnetic iron oxide nanoparticles (IONPs) led to intratumoral accumulation of 17% of total injected nanoparticles in an orthotopic mouse pancreatic cancer model, which was three-fold higher compared with intravenous delivery...
2017: Theranostics
https://www.readbyqxmd.com/read/28528286/assessing-the-stable-conformations-of-ibuprofen-in-solution-by-means-of-residual-dipolar-couplings
#17
Maria Enrica Di Pietro, Giorgio Celebre, Christie Aroulanda, Denis Merlet, Giuseppina De Luca
Detailing the conformational equilibria between global and local minimum energy structures of anti-inflammatory α-arylpropionic acids directly in solution is of the utmost importance for a better understanding of the structure-activity relationships, hence providing valuable clues for rational structure-based drug design studies. Here the conformational preferences of the widely used pharmaceutical ibuprofen were investigated in solution by NMR spectroscopy in weakly ordering phases. A thorough theoretical treatment of the anisotropic interactions that are relevant for NMR spectra led to a conformational model characterized by six pairs of symmetry-related conformers, in particular four couples of gauche structures, with a total probability of 93%, and 2 couples of trans structures, counting for the remaining 7%...
May 17, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28527154/structure-based-classification-for-bile-salt-export-pump-bsep-inhibitors-using-comparative-structural-modeling-of-human-bsep
#18
Sankalp Jain, Melanie Grandits, Lars Richter, Gerhard F Ecker
The bile salt export pump (BSEP) actively transports conjugated monovalent bile acids from the hepatocytes into the bile. This facilitates the formation of micelles and promotes digestion and absorption of dietary fat. Inhibition of BSEP leads to decreased bile flow and accumulation of cytotoxic bile salts in the liver. A number of compounds have been identified to interact with BSEP, which results in drug-induced cholestasis or liver injury. Therefore, in silico approaches for flagging compounds as potential BSEP inhibitors would be of high value in the early stage of the drug discovery pipeline...
May 19, 2017: Journal of Computer-aided Molecular Design
https://www.readbyqxmd.com/read/28526827/activated-hepatic-stellate-cells-secrete-periostin-to-induce-stem-cell-like-phenotype-of-residual-hepatocellular-carcinoma-cells-after-heat-treatment
#19
Rui Zhang, Rong-Rong Yao, Jing-Huan Li, Gang Dong, Min Ma, Qiong-Dan Zheng, Dong-Mei Gao, Jie-Feng Cui, Zheng-Gang Ren, Rong-Xin Chen
Some evidences show that residual tumor after thermal ablation will progress rapidly. However, its mechanisms remain unclear. Here, we assessed whether activated HSCs could regulate stem cell-like property of residual tumor after incomplete thermal ablation to promote tumor progression. Human HCC cell lines were exposed to sublethal heat treatment to simulate the peripheral zone of thermal ablation. After residual HCC cells were cultured with conditional medium (CM) from activated HSCs, parameters of the stem cell-like phenotypes were analyzed...
May 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28526743/systematic-identification-of-functional-residues-of-artemisia-annua-amorpha-4-11-diene-synthase
#20
Xin Fang, Jian-Xu Li, Jin-Quan Huang, You-Li Xiao, Peng Zhang, Xiao-Ya Chen
Terpene synthases (TPSs) are responsible for the extremely diversified and complex structure of terpenoids. Amorpha-4,11-diene synthase (ADS) has a high (90%) fidelity in generating the sesquiterpene precursor for biosynthesis of artemisinin, an antimalarial drug, however, little is known about how active site residues of ADS involved in the carbocation rearrangement and cyclization reactions. Here, we identify seven residues that are key to most of the catalytic steps in ADS. By structural modeling and amino acid sequence alignments of ADS with two functionally relevant sesquiterpene synthases from Artemisia annua, we performed site-directed mutagenesis and found that a single substitution, T296V, impaired the ring closure activity almost completely, and tetra-substitutions (L374Y/L404V/L405I/G439S) led to an enzyme generating 80% monocyclic bisabolyl-type sesquiterpenes, whereas a double mutant (T399L/T447G) showed compromised activity in regioselective deprotonation to yield 34...
May 19, 2017: Biochemical Journal
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