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https://www.readbyqxmd.com/read/28330072/molecular-dynamic-simulations-of-escherichia-coli-l-asparaginase-to-illuminate-its-role-in-deamination-of-asparagine-and-glutamine-residues
#1
Rajeswara Reddy Erva, Satish Babu Rajulapati, Chandrasai Potla Durthi, Mayuri Bhatia, Madhuri Pola
Acute lymphocytic leukemia (ALL) is an outrageous disease worldwide. L-Asparagine (L-Asn) and L-Glutamine (L-Gln) deamination play a crucial role in ALL treatment. Role of Elspar(®) (L-asparaginase from Escherichia coli) in regulation of L-Asn and L-Gln has been confirmed by the other researchers through experimental studies. Therapeutic research against ALL remained elusive with the lack of information on molecular interactions of Elspar(®) with amino acid substrates. In the present study, using different docking tools binding cavities, key residues in binding and ligand binding mechanisms were identified...
June 2016: 3 Biotech
https://www.readbyqxmd.com/read/28329446/in-vitro-intrinsic-permeability-a-transporter-independent-measure-of-caco-2-cell-permeability-in-drug-design-and-development
#2
Linda Fredlund, Susanne Winiwarter, Constanze Hilgendorf
In-vitro permeability data have a central place in absorption risk assessments in drug discovery and development. For compounds where active efflux impacts permeability in vitro, the inherent passive membrane permeability ("intrinsic permeability"), gives a concentration-independent measure of the compound's permeability. This work describes the validation of an in-vitro intrinsic permeability assay and application of the data in a predictive in-silico model. Apparent intrinsic permeability (Papp) across Caco-2 cell monolayers is determined in presence of an optimized cocktail of chemical inhibitors towards the three major efflux transporters ABCB1, ABCC2, and ABCG2...
March 22, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28329081/a-new-preclinical-paradigm-for-testing-anti-aging-therapeutics
#3
Warren Ladiges, Jessica M Snyder, Erby Wilkinson, Denise M Imai, Tim Snider, Xuan Ge, Marcia Ciol, Christina Pettan-Brewer, Smitha P S Pillai, John Morton, Ellen Quarles, Peter Rabinovitch, Laura Niedernhofer, Denny Liggitt
Testing drugs for anti-aging effects has historically been conducted in mouse life-span studies, but are costly and time consuming, and more importantly, difficult to recapitulate in humans. In addition, life-span studies in mice are not well suited to testing drug combinations that target multiple factors involved in aging. Additional paradigms for testing therapeutics aimed at slowing aging are needed. A new paradigm, designated as the Geropathology Grading Platform (GGP), is based on a standardized set of guidelines developed to detect the presence or absence of low-impact histopathological lesions and to determine the level of severity of high-impact lesions in organs from aged mice...
February 22, 2017: Journals of Gerontology. Series A, Biological Sciences and Medical Sciences
https://www.readbyqxmd.com/read/28328833/drug-coated-balloon-in-combination-with-bare-metal-stent-strategy-for-de-novo-coronary-artery-disease-a-prisma-compliant-meta-analysis-of-randomized-clinical-trials
#4
Wenjie Lu, Yongjian Zhu, Zhanying Han, Xi Wang, Xule Wang, Chunguang Qiu
BACKGROUND: Studies examining the efficiency of drug-coated balloon (DCB) + bare metal stent (BMS) compared with stents alone for de novo lesions have reported inconsistent results. The present comprehensive meta-analysis of randomized controlled trials (RCTs) assessed and compared the clinical efficacy and safety of DCB + BMS with those of stents alone for de novo coronary artery disease. METHODS: We formally searched electronic databases before September 2016 to identify potential studies...
March 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28328306/integration-and-evaluation-of-substance-abuse-research-education-training-saret-into-a-master-of-social-work-program
#5
Ellen Tuchman, Kathleen Hanley, Madeline Naegle, Frederick More, Sewit Bereket, Marc N Gourevitch
BACKGROUND: The Substance Abuse Research and Education Training (SARET) program is funded by the National Institutes of Drug Abuse in 2006 as a novel approach to spark interest in substance abuse research among medical, dental, nursing, and social work graduate students through a Web-based curriculum and research mentorships. This report presents the initial integration of the intervention in a Master of Social Work (MSW) program, the components of the program, and the mixed-methods evaluation of its effect on students' attitudes towards substance abuse research and treatment...
February 8, 2017: Substance Abuse
https://www.readbyqxmd.com/read/28328191/enhancing-tumor-penetration-of-nanomedicines
#6
Qingxue Sun, Tarun Ojha, Fabian Kiessling, Twan Lammers, Yang Shi
Tumor-targeted nanomedicines have been extensively applied to alter the drawbacks and enhance the efficacy of chemotherapeutics. Despite the large number of preclinical nanomedicine studies showing initial success, their therapeutic benefit in the clinic has been rather modest, which is partially due to the inefficient tumor penetration caused by tumor microenvironment (high density of cells and extracellular matrix, increased interstitial fluid pressure). Furthermore, tumor penetration of nanomedicines is significantly influenced by physicochemical characteristics such as size, surface chemistry and shape...
March 22, 2017: Biomacromolecules
https://www.readbyqxmd.com/read/28328150/yolk-shell-nanostructure-an-ideal-architecture-to-achieve-harmonious-integration-of-magnetic-plasmonic-hybrid-theranostic-platform
#7
Li-Sen Lin, Xiangyu Yang, Zijian Zhou, Zhen Yang, Orit Jacobson, Yijing Liu, Angela Yang, Gang Niu, Jibin Song, Huang-Hao Yang, Xiaoyuan Chen
Magnetic-plasmonic hybrid nanoparticles (MPHNs) have attracted great interest in cancer theranostics. However, the relaxivity of the magnetic component is typically reduced by the plasmonic component in conventional core-shell structured MPHNs, due to the presence of a water-impenetrable coating which severely restricts the proximity of protons to the magnetic portion. To circumvent this issue, yolk-shell structured MPHNs comprising a Fe3 O4 core within a hollow cavity encircled by a porous Au outer shell are designed...
March 22, 2017: Advanced Materials
https://www.readbyqxmd.com/read/28327793/insights-into-cytochrome-bc1-complex-binding-mode-of-antimalarial-2-hydroxy-1-4-naphthoquinones-through-molecular-modelling
#8
Ana Carolina Rennó Sodero, Bárbara Abrahim-Vieira, Pedro Henrique Monteiro Torres, Pedro Geraldo Pascutti, Célia Rs Garcia, Vitor Francisco Ferreira, David Rodrigues da Rocha, Sabrina Baptista Ferreira, Floriano Paes Silva
BACKGROUND: Malaria persists as a major public health problem. Atovaquone is a drug that inhibits the respiratory chain of Plasmodium falciparum, but with serious limitations like known resistance, low bioavailability and high plasma protein binding. OBJECTIVES: The aim of this work was to perform molecular modelling studies of 2-hydroxy-1,4-naphthoquinones analogues of atovaquone on the Qo site of P. falciparum cytochrome bc1 complex (Pfbc1) to suggest structural modifications that could improve their antimalarial activity...
April 2017: Memórias do Instituto Oswaldo Cruz
https://www.readbyqxmd.com/read/28327716/chemo-photodynamic-combined-gene-therapy-and-dual-modal-cancer-imaging-achieved-by-ph-responsive-alginate-chitosan-multilayer-modified-magnetic-mesoporous-silica-nanocomposites
#9
Hong Yang, Yin Chen, Zhongyuan Chen, Yue Geng, Xiaoxue Xie, Xue Shen, Tingting Li, Shun Li, Chunhui Wu, Yiyao Liu
Multifunctional theranostics have offered some interesting new opportunities for cancer therapy and diagnosis in the last decade. Herein, magnetic mesoporous silica nanoparticles (M-MSNs) were designed and synthesized, then the photosensitizer chlorin e6 (Ce6) and antitumor drug doxorubicin (Dox) were adsorbed onto the M-MSNs. Biocompatible alginate/chitosan polyelectrolyte multilayers (PEM) were assembled on the M-MSNs to achieve a pH-responsive drug delivery system and adsorb P-gp shRNA for reversing the multidrug resistance...
March 22, 2017: Biomaterials Science
https://www.readbyqxmd.com/read/28327677/access-to-drugs-and-out-of-pocket-expenditure-in-primary-health-facilities
#10
A K Thapa, N Ghimire, S R Adhikari
BACKGROUND: The Government of Nepal promulgated health as a human right via Interim constitution and implemented Free Health Service Program in 2008 as a commitment to universalize basic health care services. So, the aim of this study was to understand reported access to medicine and health care services received by outpatients in public primary facilities. METHODS: The study followed cross sectional study design. Two hundred and thirty-four For data 234 out patients were interviewed on the day of the field visit in March and October 2014 across 28 primary health facilities of seven purposively selected districts representing three ecological belts and five development regions of the country...
September 2016: Journal of Nepal Health Research Council
https://www.readbyqxmd.com/read/28327083/the-effect-of-an-interactive-cycling-training-on-cognitive-functioning-in-older-adults-with-mild-dementia-study-protocol-for-a-randomized-controlled-trial
#11
E G A Karssemeijer, W J R Bossers, J A Aaronson, R P C Kessels, M G M Olde Rikkert
BACKGROUND: To date there is no cure or an effective disease-modifying drug to treat dementia. Available acetylcholine-esterase inhibiting drugs or memantine only produce small benefits on cognitive and behavioural functioning and their clinical relevance remains controversial. Combined cognitive-aerobic interventions are an appealing alternative or add-on to current pharmacological treatments. The primary aim of this study is to investigate the efficacy of a combined cognitive-aerobic training and a single aerobic training compared to an active control group in older adults with mild dementia...
March 21, 2017: BMC Geriatrics
https://www.readbyqxmd.com/read/28327075/magnetic-nanobubbles-with-potential-for-targeted-drug-delivery-and-trimodal-imaging-in-breast-cancer-an-in-vitro-study
#12
Weixiang Song, Yindeng Luo, Yajing Zhao, Xinjie Liu, Jiannong Zhao, Jie Luo, Qunxia Zhang, Haitao Ran, Zhigang Wang, Dajing Guo
AIM: The aim of this study was to improve tumor-targeted therapy for breast cancer by designing magnetic nanobubbles with the potential for targeted drug delivery and multimodal imaging. MATERIALS & METHODS: Herceptin-decorated and ultrasmall superparamagnetic iron oxide (USPIO)/paclitaxel (PTX)-embedded nanobubbles (PTX-USPIO-HER-NBs) were manufactured by combining a modified double-emulsion evaporation process with carbodiimide technique. PTX-USPIO-HER-NBs were examined for characterization, specific cell-targeting ability and multimodal imaging...
March 13, 2017: Nanomedicine
https://www.readbyqxmd.com/read/28326907/skin-sensitizers-in-cosmetics-and-beyond-potential-multiple-mechanisms-of-action-and-importance-of-t-cell-assays-for-in-vitro-screening
#13
Stanislav Vukmanović, Nakissa Sadrieh
Allergic contact dermatitis (ACD) is a delayed-type hypersensitivity (DTH) reaction induced by repeated contact with sensitizers. The ability of a chemical to act as a sensitizer has most frequently been tested in animals. As the use of animals for these purposes is gradually and globally being phased out, there is a need for reliable in vitro surrogate assays. Currently proposed in vitro assays are designed to test four key events of the adverse outcome pathway (AOP) involving covalent modification of self-proteins by sensitizers (haptenation) and presentation of new antigens (hapten/carrier complexes) to the immune system...
March 22, 2017: Critical Reviews in Toxicology
https://www.readbyqxmd.com/read/28326681/population-pharmacokinetics-of-selumetinib-and-its-metabolite-n-desmethyl-selumetinib-in-adult-patients-with-advanced-solid-tumors-and-children-with-low-grade-gliomas
#14
Y T Patel, V M Daryani, P Patel, D Zhou, J Fangusaro, D J Carlile, P D Martin, L Aarons, C F Stewart
Selumetinib (AZD6244, ARRY-142886), a mitogen activated protein kinases (MEK1 and 2) inhibitor, has been granted orphan drug designation for differentiated thyroid cancer. The primary aim of this analysis was to characterize the population pharmacokinetics of selumetinib and its active metabolite N-desmethyl-selumetinib in patients with cancer. Concentration-time data from adult and pediatric clinical trials were pooled to develop a population pharmacokinetic model using a sequential approach where selumetinib and N-desmethyl-selumetinib data were modeled separately...
March 22, 2017: CPT: Pharmacometrics & Systems Pharmacology
https://www.readbyqxmd.com/read/28326432/harnessing-scientific-literature-reports-for-pharmacovigilance-prototype-software-analytical-tool-development-and-usability-testing
#15
Alfred Sorbello, Anna Ripple, Joseph Tonning, Monica Munoz, Rashedul Hasan, Thomas Ly, Henry Francis, Olivier Bodenreider
OBJECTIVES: We seek to develop a prototype software analytical tool to augment FDA regulatory reviewers' capacity to harness scientific literature reports in PubMed/MEDLINE for pharmacovigilance and adverse drug event (ADE) safety signal detection. We also aim to gather feedback through usability testing to assess design, performance, and user satisfaction with the tool. METHODS: A prototype, open source, web-based, software analytical tool generated statistical disproportionality data mining signal scores and dynamic visual analytics for ADE safety signal detection and management...
March 22, 2017: Applied Clinical Informatics
https://www.readbyqxmd.com/read/28325895/simulation-assisted-design-of-microfluidic-sample-traps-for-optimal-trapping-and-culture-of-non-adherent-single-cells-tissues-and-spheroids
#16
Nassim Rousset, Frédéric Monet, Thomas Gervais
This work focuses on modelling design and operation of "microfluidic sample traps" (MSTs). MSTs regroup a widely used class of microdevices that incorporate wells, recesses or chambers adjacent to a channel to individually trap, culture and/or release submicroliter 3D tissue samples ranging from simple cell aggregates and spheroids, to ex vivo tissue samples and other submillimetre-scale tissue models. Numerous MST designs employing various trapping mechanisms have been proposed in the literature, spurring the development of 3D tissue models for drug discovery and personalized medicine...
March 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28325790/dopamine-terminals-from-the-ventral-tegmental-area-gate-intrinsic-inhibition-in-the-prefrontal-cortex
#17
William C Buchta, Stephen V Mahler, Benjamin Harlan, Gary S Aston-Jones, Arthur C Riegel
Spike frequency adaptation (SFA or accommodation) and calcium-activated potassium channels that underlie after-hyperpolarization potentials (AHP) regulate repetitive firing of neurons. Precisely how neuromodulators such as dopamine from the ventral tegmental area (VTA) regulate SFA and AHP (together referred to as intrinsic inhibition) in the prefrontal cortex (PFC) remains unclear. Using whole cell electrophysiology, we measured intrinsic inhibition in prelimbic (PL) layer 5 pyramidal cells of male adult rats...
March 2017: Physiological Reports
https://www.readbyqxmd.com/read/28325505/clinical-interpretation-of-urine-drug-tests-what-clinicians-need-to-know-about-urine-drug-screens
#18
REVIEW
Karen E Moeller, Julie C Kissack, Rabia S Atayee, Kelly C Lee
Urine drug testing is frequently used in clinical, employment, educational, and legal settings and misinterpretation of test results can result in significant adverse consequences for the individual who is being tested. Advances in drug testing technology combined with a rise in the number of novel misused substances present challenges to clinicians to appropriately interpret urine drug test results. Authors searched PubMed and Google Scholar to identify published literature written in English between 1946 and 2016, using urine drug test, screen, false-positive, false-negative, abuse, and individual drugs of abuse as key words...
March 18, 2017: Mayo Clinic Proceedings
https://www.readbyqxmd.com/read/28325450/classification-of-nervous-system-withdrawn-and-approved-drugs-with-toxprint-features-via-machine-learning-strategies
#19
Aytun Onay, Melih Onay, Osman Abul
BACKGROUND AND OBJECTIVES: Early-phase virtual screening of candidate drug molecules plays a key role in pharmaceutical industry from data mining and machine learning to prevent adverse effects of the drugs. Computational classification methods can distinguish approved drugs from withdrawn ones. We focused on 6 data sets including maximum 110 approved and 110 withdrawn drugs for all and nervous system diseases to distinguish approved drugs from withdrawn ones. METHODS: In this study, we used support vector machines (SVMs) and ensemble methods (EMs) such as boosted and bagged trees to classify drugs into approved and withdrawn categories...
April 2017: Computer Methods and Programs in Biomedicine
https://www.readbyqxmd.com/read/28325287/cholesterol-containing-nuclease-resistant-sirna-accumulates-in-tumors-in-a-carrier-free-mode-and-silences-mdr1-gene
#20
Ivan V Chernikov, Daniil V Gladkikh, Mariya I Meschaninova, Alya G Ven'yaminova, Marina A Zenkova, Valentin V Vlassov, Elena L Chernolovskaya
Chemical modifications are an effective way to improve the therapeutic properties of small interfering RNAs (siRNAs), making them more resistant to degradation in serum and ensuring their delivery to target cells and tissues. Here, we studied the carrier-free biodistribution and biological activity of a nuclease-resistant anti-MDR1 cholesterol-siRNA conjugate in healthy and tumor-bearing severe combined immune deficiency (SCID) mice. The attachment of cholesterol to siRNA provided its efficient accumulation in the liver and in tumors, and reduced its retention in the kidneys after intravenous and intraperitoneal injection...
March 17, 2017: Molecular Therapy. Nucleic Acids
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