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Drug interaction

Ju Hui Jeong, Yong Jin Oh, Yunmee Lho, Sun You Park, Kwang-Hyeon Liu, Eunyoung Ha, Young Ho Seo
The molecular chaperone Hsp90 plays an important role in cancer cell survival and proliferation by regulating the maturation and stabilization of numerous oncogenic proteins. Due to its potential to simultaneously disable multiple signaling pathways, Hsp90 has emerged as an attractive therapeutic target for cancer treatment. In this study, the design, synthesis, and biological evaluation of a series of Hsp90 inhibitors are described. Among the synthetic compounds, 6,7-dihydrothieno [3,2-c]pyridin-5(4H)-yl amide 19 exhibits a remarkable binding affinity to the N-terminus of Hsp90 in a fluorescence polarization (FP) binding assay (IC50 = 50...
October 18, 2016: European Journal of Medicinal Chemistry
Min Ma, Fuwei Pi, Jiasheng Wang, Jian Ji, Xiulan Sun
Humans are most likely to be exposed to microcystins (MCs) combined with other water pollutants rather than to individual compounds through the consumption of contaminated drinking water or through recreational activities, such as swimming. However, the combined effects of MC-LR, estradiol (EST), and ractopamine (RAC) have not been extensively researched. The goal of this study was to investigate the combined effects of these compounds. For this purpose, cytotoxicity was evaluated in HepG2 cells treated with single or combined doses of MC-LR, EST, and RAC based on concentration addition (CA), independent action (IA), and Chou-Talalay's combination-index (CI) methods...
October 23, 2016: Chemosphere
Amy E B Packard, Ann E Egan, Yvonne M Ulrich-Lai
Perhaps the most salient behaviors that individuals engage in involve the avoidance of aversive experiences and the pursuit of pleasurable experiences. Engagement in these behaviors is regulated to a significant extent by an individual's hormonal milieu. For example, glucocorticoid hormones are produced by the hypothalamic-pituitary-adrenocortical (HPA) axis, and influence most aspects of behavior. In turn, many behaviors can influence HPA axis activity. These bidirectional interactions not only coordinate an individual's physiological and behavioral states to each other, but can also tune them to environmental conditions thereby optimizing survival...
September 15, 2016: Comprehensive Physiology
Michele Fernanda Borges da Silva, Patrícia Dias de Brito, Lusiele Guaraldo
Objective: to describe the profile of standardized oral drugs at a hospital unit and assess their adequacy for use via enteral feeding tubes, according to recommendations from the literature. Method: descriptive study, with data on drugs collected from the Pharmacy Service Dispensing System. Specific recommendations for the use of these drugs via enteral feeding tubes were found after searches in literary databases, books, manuals, guidelines and package insert collections...
September 2016: Revista Brasileira de Enfermagem
Daniella Kovacsics, Izabel Patik, Csilla Özvegy-Laczka
The in vivo fate and effectiveness of a drug depends highly on its absorption, distribution, metabolism, excretion and toxicity (ADME-Tox). Organic anion transporting polypeptides (OATPs) are membrane proteins involved in the cellular uptake of various organic compounds, including clinically used drugs. Since OATPs are significant players in drug absorption and distribution, modulation of OATP function via pharmacotherapy with OATP substrates/inhibitors, or modulation of their expression, affects drug pharmacokinetics...
October 26, 2016: Expert Opinion on Drug Metabolism & Toxicology
Svenja Winzen, James Ciro Schwabacher, Julius Mueller, Katharina Landfester, Kristin Mohr
Surfactants, even in miniscule amounts, are often used for the synthesis and especially the stabilization of nanomaterials, which is essential for in vivo applications. In this study, we show that the interaction between nanoparticles and proteins strongly depends on the type of stabilizing surfactants and their (small) concentration changes. The reaction between human serum albumin (HSA) and polystyrene nanoparticles (PS-NPs) stabilized by an ionic or nonionic surfactant - sodium dodecyl sulfate (SDS) or Lutensol AT50, respectively - was monitored using isothermal titration calorimetry (ITC)...
October 26, 2016: Biomacromolecules
Anders Lundgren, Björn Agnarsson, Ronald Zirbs, Vladimir P Zhdanov, Erik Reimhult, Fredrik Höök
Emerging biomedical applications such as molecular imaging and drug delivery often require directed binding of nanoparticles to cell-membrane receptors. The specific apparent affinity of such ligand-functionalized particles is size-dependent, an observation so far solely attributed to multivalent receptor-ligand interaction. We question the universality of this explanation by demonstrating that the binding kinetics also depends on weak, attractive colloidal-type interaction between nanoparticles and a lipid membrane...
October 26, 2016: ACS Nano
Claudia Greißing, Katharina Kössler, Johanna Freyer, Lucie Hüter, Peter Buchal, Susanne Schiek, Thilo Bertsche
Background Pharmacist-led medication reviews have shown to prevent drug-related problems (DRPs). So far, data is rare about the implementation in routine care, the conditions for intensifying this service and the practical skills of community pharmacists to perform medication reviews. Objective To assess the current status of medication review implementation in German community pharmacies and the performance of identifying DRPs in a ficticious patient example. Setting German community pharmacies. Method An online survey was conducted from July to September 2015 including questions about medication reviews currently performed in routine care of community pharmacies and hidden DRPs in a ficticious patient example...
October 25, 2016: International Journal of Clinical Pharmacy
Remigijus Didziapetris, Kiril Lanevskij
A large and chemically diverse hERG inhibition data set comprised of 6690 compounds was constructed on the basis of ChEMBL bioactivity database and original publications dealing with experimental determination of hERG activities using patch-clamp and competitive displacement assays. The collected data were converted to binary format at 10 µM activity threshold and subjected to gradient boosting machine classification analysis using a minimal set of physicochemical and topological descriptors. The tested parameters involved lipophilicity (log P), ionization (pK a ), polar surface area, aromaticity, molecular size and flexibility...
October 25, 2016: Journal of Computer-aided Molecular Design
Feng Q He, Markus Ollert
Identification of key genes for a given physiological or pathological process is an essential but still very challenging task for the entire biomedical research community. Statistics-based approaches, such as genome-wide association study (GWAS)- or quantitative trait locus (QTL)-related analysis have already made enormous contributions to identifying key genes associated with a given disease or phenotype, the success of which is however very much dependent on a huge number of samples. Recent advances in network biology, especially network inference directly from genome-scale data and the following-up network analysis, opens up new avenues to predict key genes driving a given biological process or cellular function...
October 26, 2016: Advances in Biochemical Engineering/biotechnology
Naomi Nitschke, Kalina Atkovska, Jochen S Hub
Molecular dynamics simulations are capable of predicting the permeability of lipid membranes for drug-like solutes, but the calculations have remained prohibitively expensive for high-throughput studies. Here, we analyze simple measures for accelerating potential of mean force (PMF) calculations of membrane permeation, namely, (i) using smaller simulation systems, (ii) simulating multiple solutes per system, and (iii) using shorter cutoffs for the Lennard-Jones interactions. We find that PMFs for membrane permeation are remarkably robust against alterations of such parameters, suggesting that accurate PMF calculations are possible at strongly reduced computational cost...
September 28, 2016: Journal of Chemical Physics
Vaibhav Jain, Prabal K Maiti, Prasad V Bharatam
Computational studies performed on dendrimer-drug complexes usually consider 1:1 stoichiometry, which is far from reality, since in experiments more number of drug molecules get encapsulated inside a dendrimer. In the present study, molecular dynamic (MD) simulations were implemented to characterize the more realistic molecular models of dendrimer-drug complexes (1:n stoichiometry) in order to understand the effect of high drug loading on the structural properties and also to unveil the atomistic level details...
September 28, 2016: Journal of Chemical Physics
Robert G Nichols, Nicole E Hume, Philip B Smith, Jeffrey M Peters, Andrew D Patterson
The drug metabolism field has long recognized the beneficial and sometimes deleterious influence of microbiota in the absorption, distribution, metabolism, and excretion of drugs. Early pioneering work with the sulfanilamide precursor prontosil pointed toward the necessity not only to better understand the metabolic capabilities of the microbiota but also, importantly, to identify the specific microbiota involved in the generation and metabolism of drugs. However, technological limitations important for cataloging the microbiota community as well as for understanding and/or predicting their metabolic capabilities hindered progress...
October 26, 2016: Chemical Research in Toxicology
Subhajit Ghosh, Saswat Mohapatra, Anisha Thomas, Debmalya Bhunia, Abhijit Saha, Gaurav Das, Batakrishna Jana, Surajit Ghosh
An ideal nano drug delivery agent must be potent enough to carry high dose of therapeutics, competent enough in targeting specific cell of interest, having adequate optimized physiochemical properties and biocompatibility. Carrying differentially polar therapeutics simultaneously will make them superior in their class. However, it is of enormous challenge to the researchers to find out such a unique nanocarrier and engineer all the above-mentioned features into it. In this manuscript, we have shown for the first time that Apoferritin (Apf) can carry and deliver high dose of doxorubicin (Dox), docetaxel (Doc) and combination of both Dox and Doc specifically into the cancer cell and enhances killing compared to free drug without any functionalization or property modulation...
October 26, 2016: ACS Applied Materials & Interfaces
T L Rodgers, J E Magee, T Amure, F R Siperstein
The dynamics of co-polymer systems play an important role in the preparation and stability of formulations, as well as on their capability to function in drug delivery systems. Micelle inversion can occur as a result of a change in concentration when a solvent is very volatile and evaporates, or as a result of a change in solvent quality upon addition of another solvent to the original solution, or upon changes in pH. In this work, dissipative particle dynamics (DPD) is used to examine the dynamics of micelle inversion in concentrated systems of diblock and triblock amphiphiles, where interactions between neighboring aggregates are observed...
October 26, 2016: Soft Matter
Ki-Young Lee, Bong-Jin Lee
Bacterial toxin-antitoxin (TA) systems have received increasing attention for their diverse identities, structures, and functional implications in cell cycle arrest and survival against environmental stresses such as nutrient deficiency, antibiotic treatments, and immune system attacks. In this review, we describe the biological functions and the auto-regulatory mechanisms of six different types of TA systems, among which the type II TA system has been most extensively studied. The functions of type II toxins include mRNA/tRNA cleavage, gyrase/ribosome poison, and protein phosphorylation, which can be neutralized by their cognate antitoxins...
October 22, 2016: Toxins
Heidi Barth, Morgane Solis, Wallys Kack-Kack, Eric Soulier, Aurélie Velay, Samira Fafi-Kremer
Developments of genome amplification techniques have rapidly expanded the family of human polyomaviruses (PyV). Following infection early in life, PyV persist in their hosts and are generally of no clinical consequence. High-level replication of PyV can occur in patients under immunosuppressive or immunomodulatory therapy and causes severe clinical entities, such as progressive multifocal leukoencephalopathy, polyomavirus-associated nephropathy or Merkel cell carcinoma. The characterization of known and newly-discovered human PyV, their relationship to human health, and the mechanisms underlying pathogenesis remain to be elucidated...
October 22, 2016: Viruses
Rita Turnaturi, Giuseppina Aricò, Giuseppe Ronsisvalle, Lorella Pasquinucci, Carmela Parenti
Polypharmacology, or the associations between two or more drugs producing biological effects on two or more different sites of action could represent a possible therapeutic approach for the clinical management of acute and chronic pain. The multitude and complexity of neuronal mechanisms that contribute to pain transmission provide several possible targets for pharmacological intervention. Thus, multitarget ligands possessing opioid-opioid or non-opioid-opioid mechanisms of action are potential drug candidates for pain relief...
October 24, 2016: Current Medicinal Chemistry
M Drozdzik, S Oswald
Orally administered drugs must pass through the intestinal wall and then through the liver before reaching systemic circulation. During this process drugs are subjected to different processes that may determine the therapeutic value. The intestinal barrier with active drug metabolizing enzymes and drug transporters in enterocytes plays an important role in the determination of drug bioavailability. Accumulating information demonstrates variable distribution of drug metabolizing enzymes and transporters along the human gastrointestinal tract (GI), that creates specific barrier characteristics in different segments of the GI...
October 24, 2016: Current Medicinal Chemistry
Saket Kumar Singh, Bibhas Kumar Bhunia, Nandana Bhardwaj, Sween Gilotra, Biman B Mandal
Tunable repeated drug administration is often inevitable in number of pathological cases. Reloadable 3D matrices for sustained drug delivery are predicted as a prospective avenue to realize this objective. This study was directed towards sonication-induced fabrication of novel reloadable Bombyx mori silk fibroin (SF) (4, 6 and 8 wt%) hydrogel, injected within 3D porous (8 wt%) scaffolds. The focus was to develop a dual-barrier reloadable depot system for sustained molecular cargo-release. Both the varying SF concentration (4, 6 and 8 wt%) and the sonication time (30, 45 and 60 s) dictated the extent of cross-linking, β-sheet content and porosity (1-10 µm) influencing the release behavior of model molecules...
October 26, 2016: Molecular Pharmaceutics
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