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https://www.readbyqxmd.com/read/28441781/dengue-virus-non-structural-protein-5
#1
REVIEW
Abbas El Sahili, Julien Lescar
The World Health Organization estimates that the yearly number of dengue cases averages 390 million. This mosquito-borne virus disease is endemic in over 100 countries and will probably continue spreading, given the observed trend in global warming. So far, there is no antiviral drug available against dengue, but a vaccine has been recently marketed. Dengue virus also serves as a prototype for the study of other pathogenic flaviviruses that are emerging, like West Nile virus and Zika virus. Upon viral entry into the host cell and fusion of the viral lipid membrane with the endosomal membrane, the viral RNA is released and expressed as a polyprotein, that is then matured into three structural and seven non-structural (NS) proteins...
April 24, 2017: Viruses
https://www.readbyqxmd.com/read/28441616/core-shell-hierarchical-mesostructured-silica-nanoparticles-for-gene-chemo-synergetic-stepwise-therapy-of-multidrug-resistant-cancer
#2
Lijun Sun, Dangge Wang, Yu Chen, Liying Wang, Ping Huang, Yaping Li, Ziwei Liu, Heliang Yao, Jianlin Shi
The design and synthesis of hierarchically nanoporous structures for the co-encapsulation and sequential releases of different cargos are still great challenges in biomedical applications. In this work, we report on the elaborate design and controlled synthesis of a unique core-shell hierarchical mesoporous silica/organosilica nanosystem, in which there are large and small mesopores separately present in the shell and core, facilitating the independent encapsulations of large (siRNA) and small (doxorubicin) molecules, respectively...
April 18, 2017: Biomaterials
https://www.readbyqxmd.com/read/28441501/hooked-on-cryogels-a-carbamate-linker-based-depot-for-slow-drug-release
#3
Duygu Aydin, Mehmet Arslan, Amitav Sanyal, Rana Sanyal
Poly(ethylene glycol) (PEG) based bulk hydrogels and cryogels containing activated carbonate groups as amine reactive handles to facilitate drug conjugations through carbamate linkages were fabricated and evaluated as slow releasing drug reservoirs. As an initial approach, photopolymerization of N-hydroxysuccinimide (NHS)-activated carbonate functional group containing monomer and PEG-methacrylate in the presence of a crosslinker was utilized to obtain bulk hydrogels with high gel conversions. The resultant hydrogels possessed moderate water uptake (170-340 %) which was dependent on the monomer ratios...
April 25, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28441481/best-practices-of-computer-aided-drug-discovery-cadd-lessons-learned-from-the-development-of-a-preclinical-candidate-for-prostate-cancer-with-a-new-mechanism-of-action
#4
Fuqiang Ban, Kush Dalal, Huifang Li, Eric LeBlanc, Paul S Rennie, Artem Cherkasov
Small-molecule drug design is a complex and iterative decision-making process relying on pre-existing knowledge and driven by experimental data. Low molecular weight chemicals represent an attractive therapeutic option as they are readily accessible to organic synthesis and can easily be characterized.1 Their potency, as well as pharmacokinetic and pharmacodynamic properties can be systematically and rationally investigated, and ultimately optimized via expert science behind medicinal chemistry and methods of computer-aided drug design (CADD)...
April 25, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28441471/gemcitabine-integrated-nano-prodrug-carrier-system
#5
Seren Hamsici, Melis Sardan Ekiz, Goksu Cinar Ciftci, Ayse Begum Tekinay, Mustafa O Guler
Peptide nanomaterials have received a great deal of interest in drug delivery applications due to their biodegradability, biocompatibility, suitability for large scale synthesis, high drug loading capacities, targeting ability and ordered structural organization. The covalent conjugation of drugs to peptide backbone results in prolonged circulation time and improved stability of drugs. Therapeutic efficacy of gemcitabine, which is used for breast cancer treatment, is severely compromised due to its rapid plasma degradation...
April 25, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28441023/hydrophobic-nanoparticles-modify-the-thermal-release-behavior-of-liposomes
#6
Matthew Ryan Preiss, Ashley E Hart, Christopher L Kitchens, Geoffrey D Bothun
Understanding the effect of embedded nanoparticles on the characteristics and behavior of lipid bilayers is critical to the development of lipid-nanoparticle assemblies (LNAs) for biomedical applications. In this work we investigate the effect of hydrophobic nanoparticle size and concentration on liposomal thermal release behavior. Decorated LNAs (D-LNAs) were formed by embedding 2 nm (GNP2) and 4 nm (GNP4) dodecanethiol-capped gold nanoparticles into DPPC liposomes at lipid to nanoparticle ratios (L:N) of 25,000:1, 10,000:1, and 5,000:1...
April 25, 2017: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/28440835/the-generation-of-compartmentalized-nanoparticles-containing-sirna-and-cisplatin-using-a-multi-needle-electrohydrodynamic-strategy
#7
Maria F Pina, Wai Lau, Kathrin Scherer, Maryam Parhizkar, Mohan Edirisinghe, Duncan Craig
This study outlines a novel manufacturing technique for the generation of compartmentalized trilayered nanoparticles loaded with an anti-cancer agent and siRNA as a platform for the combination treatment of cancers. More specifically, we describe the use of a multi-needle electrohydrodynamic approach to produce nanoparticles with high size specificity and scalable output, while allowing suitable environments for each therapeutic agent. The inner polylactic-glycolic-acid (PLGA) layer was loaded with cisplatin while the middle chitosan layer was loaded with siRNA...
April 25, 2017: Nanoscale
https://www.readbyqxmd.com/read/28440827/molecular-dynamics-investigations-of-membrane-bound-cyp2c19-polymorphisms-reveal-distinct-mechanisms-for-peripheral-variants-by-long-range-effects-on-the-enzymatic-activity
#8
Ying-Lu Cui, Rong-Ling Wu
Increasing sophistication in methods used to account for human polymorphisms in susceptibility to drug metabolism has been one of the success stories in the prevention of adverse drug reactions. Genetic polymorphisms in drug-metabolizing enzymes can affect enzyme activity and cause differences in treatment response or drug toxicity. CYP2C19 is one of the most highly polymorphic CYP enzymes and acts on 10-15% of drugs in current clinical use. Despite the number of experimental analyses carried out for this system, the detailed structural basis for altered catalytic properties of polymorphic CYP2C19 variants remains unexplained at the atomic level...
April 25, 2017: Molecular BioSystems
https://www.readbyqxmd.com/read/28440819/amphiphilic-carbon-dots-as-versatile-vectors-for-nucleic-acid-and-drug-delivery
#9
Hai-Jiao Wang, Xi He, Tian-Ying Luo, Ji Zhang, Yan-Hong Liu, Xiao-Qi Yu
Carbon dot (CD)-based multifunctional delivery systems have shown great potential in both drug/gene delivery and bio-imaging. In this work, we present a strategy to simply construct amphiphilic CDs (ACDs) by conjugating hydrophobic alkyl epoxide to the surface amino groups of PEI 600-derived CDs. ACDs could well dissolve in water or organic solvents and emit bright fluorescence both in solutions and cells. (1)HNMR also suggested that ACDs may form micelle-like structures in water, and their CMC could be determined...
April 25, 2017: Nanoscale
https://www.readbyqxmd.com/read/28440736/levistilide-a-inhibits-angiogenesis-in-liver-fibrosis-via-vascular-endothelial-growth-factor-signaling-pathway
#10
Zhi-Min Zhao, Hong-Liang Liu, Xin Sun, Tao Guo, Li Shen, Yan-Yan Tao, Cheng-Hai Liu
Levistilide A (C24H28O4, molecular weight = 380.48) derived from Angelica sinensis (Danggui) has been reported to inhibit hepatic stellate cell proliferation. This study investigated the effects of levistilide A on liver fibrosis relating to angiogenesis, particularly on the characteristic change in liver sinusoidal endothelial cells. LX-2 cells were activated by TGF-β1, and the human hepatic sinusoidal endothelial cells (HHSECs) were induced by endothelial cell growth supplement. Cell viability was detected using a methylthiazoldiphenyl-tetrazolium bromide assay; F-actin was visualized through the fluorescence probe method; cell proliferation was examined using the EdU kit; antiangiogenesis activity was assessed using the tube formation assay and transgenic zebrafish model...
May 2017: Experimental Biology and Medicine
https://www.readbyqxmd.com/read/28440570/mass-spectrometric-characterization-of-the-selective-androgen-receptor-modulator-sarm-yk-11-for-doping-control-purposes
#11
Mario Thevis, Thomas Piper, Josef Dib, Andreas Lagojda, Dirk Kuehne, Lars Packschies, Hans Geyer, Wilhelm Schaenzer
RATIONALE: Selective androgen receptor modulators (SARMs) represent an emerging class of therapeutics targeting inter alia conditions referred to as cachexia and sarcopenia. Due to their anabolic properties, the use of SARMs is prohibited in sports as regulated by the World Anti-Doping Agency (WADA), and doping control laboratories test for these anabolic agents in blood and urine. In order to accomplish and maintain comprehensive test methods, the characterization of new drug candidates is critical for efficient sports drug testing...
April 25, 2017: Rapid Communications in Mass Spectrometry: RCM
https://www.readbyqxmd.com/read/28440467/structural-and-evolutionary-divergence-of-aquaporins-in-parasites-review
#12
Zi-Xin Ni, Jian-Min Cui, Nian-Zhang Zhang, Bao-Quan Fu
Aquaporins are ubiquitous proteins that belong to the major intrinsic protein family. Previous studies have indicated that aquaporins are involved in multiple physiological processes in parasites, such as nutrient absorption and end product efflux, and thus, would be promising pharmacological agents in the fight against parasite infection. In the present paper, the authors analyzed the evolutionary relationship of parasitic aquaporins by re‑constructing of a phylogenic tree using neighbor‑joining and maximum likelihood methods...
April 25, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28440193/neurocognitive-correlates-in-driving-under-the-influence-of-cannabis
#13
Francesco Paolo Busardò, Manuela Pellegrini, Julia Klein, Natale Mario di Luca
Delta (9)-tetrahydrocannabinol is the main psychoactive compound in cannabis and is commonly identified in blood samples from arrested drivers assumed to drive under the influence of drugs. Changing social norms towards cannabis and higher acceptability towards the drug emphasize the need for comprehensive understanding of the severe neurocognitive and psychomotor effects caused by cannabis and how these effects are correlated to driving skills and performance. In this review, PubMed, Cochrane Central, Scopus, Web of Science, Science Direct and EMBASE databases were used to identify and select publications up to January 2017 dealing with acute and chronic neurocognitive effects induced by cannabis and ability to drive...
April 23, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/28440185/a-therapeutic-potential-of-animal-%C3%AE-hairpin-antimicrobial-peptides
#14
Tatiana V Ovchinnikova, Pavel V Panteleev, Sergey V Balandin, Vadim T Ivanov
Endogenous antimicrobial peptides (AMPs) are evolutionary ancient molecular factors of innate immunity that play the key role in host defense. Because of the low resistance rate, AMPs have caught extensive attention as possible alternatives to conventional antibiotics. Over the last years, it has become evident that biological functions of AMPs are beyond direct killing of microbial cells. This review focuses on a relatively small family of animal host defense peptides with the β-hairpin structure stabilized by disulfide bridges...
April 24, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28440084/prevalence-and-co-occurrence-of-addictive-behaviors-among-russian-and-spanish-youth
#15
Jennifer Tsai, Jimi Huh, Bulat Idrisov, Artur Galimov, Jose P Espada, María T Gonzálvez, Steve Sussman
Recently, an addiction matrix measure was assessed among U.S. former alternative high school youth. This presentation seeks to examine the generalizability of findings using this measure among Russian and Spanish high school adolescents. Latent class analysis was used to explore addiction subgroups among adolescents in Russia (average age = 16.27; n = 715) and Spain (average age = 14.9; n = 811). Last 30-day prevalence of one or more of 11 addictions reviewed in the previous work was the primary focus (i...
January 1, 2017: Journal of Drug Education
https://www.readbyqxmd.com/read/28439794/the-effectiveness-of-voriconazole-in-therapy-of-candida-glabrata-s-biofilms-oral-infections-and-its-influence-on-the-matrix-composition-and-gene-expression
#16
Célia F Rodrigues, Bruna Gonçalves, Maria Elisa Rodrigues, Sónia Silva, Joana Azeredo, Mariana Henriques
Candida glabrata is one of most prevalent yeast in fungal infections, especially in immunocompromised patients. Its azole resistance results in a low therapeutic response, particularly when associated with biofilms. The main goal of this work was to study the effectiveness of voriconazole (Vcz) against C. glabrata biofilms oral pathologies, as esophageal or oropharyngeal candidiasis. Antifungal susceptibilities were determined in pre-formed 24-h-biofilms and ERG genes expression was determined by qRT-PCR. Protein quantification was performed using BCA(®) Kit, carbohydrate was estimated according to the Dubois assay and β-1,3 glucans concentration were determined using Glucatell(®) kit...
April 24, 2017: Mycopathologia
https://www.readbyqxmd.com/read/28439100/ventral-striatal-regulation-of-crem-mediates-impulsive-action-and-drug-addiction-vulnerability
#17
M L Miller, Y Ren, H Szutorisz, N A Warren, C Tessereau, G Egervari, A Mlodnicka, M Kapoor, B Chaarani, C V Morris, G Schumann, H Garavan, A M Goate, M J Bannon, J M Halperin, Y L Hurd
Impulsivity, a multifaceted behavioral hallmark of attention-deficit/hyperactivity disorder (ADHD), strongly influences addiction vulnerability and other psychiatric disorders that incur enormous medical and societal burdens yet the neurobiological underpinnings linking impulsivity to disease remain poorly understood. Here we report the critical role of ventral striatal cAMP-response element modulator (CREM) in mediating impulsivity relevant to drug abuse vulnerability. Using an ADHD rat model, we demonstrate that impulsive animals are neurochemically and behaviorally more sensitive to heroin and exhibit reduced Crem expression in the nucleus accumbens core...
April 25, 2017: Molecular Psychiatry
https://www.readbyqxmd.com/read/28439010/cyclops-reveals-human-transcriptional-rhythms-in-health-and-disease
#18
Ron C Anafi, Lauren J Francey, John B Hogenesch, Junhyong Kim
Circadian rhythms modulate many aspects of physiology. Knowledge of the molecular basis of these rhythms has exploded in the last 20 years. However, most of these data are from model organisms, and translation to clinical practice has been limited. Here, we present an approach to identify molecular rhythms in humans from thousands of unordered expression measurements. Our algorithm, cyclic ordering by periodic structure (CYCLOPS), uses evolutionary conservation and machine learning to identify elliptical structure in high-dimensional data...
April 24, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28438929/molecular-profile-of-malaria-drug-resistance-markers-of-plasmodium-falciparum-in-suriname
#19
Stella M Chenet, Sheila Akinyi Okoth, Julia Kelley, Naomi Lucchi, Curtis S Huber, Stephen Vreden, Alexandre Macedo de Oliveira, John W Barnwell, Venkatachalam Udhayakumar, Malti R Adhin
In Suriname, an artesunate monotherapy therapeutic efficacy trial was recently conducted to evaluate partial artemisinin resistance emerging in Plasmodium falciparum We genotyped the PfK13 propeller domain of P. falciparum in forty samples as well as other mutations proposed to be associated with artemisinin resistant mutants. We did not find any mutations previously associated with artemisinin resistance in Southeast Asia but we found fixed resistance mutations for chloroquine and sulfadoxine-pyrimethamine...
April 24, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28438697/predicting-drug-loading-in-pla-peg-nanoparticles
#20
M Meunier, A Goupil, P Lienard
Polymer nanoparticles present advantageous physical and biopharmaceutical properties as drug delivery systems compared to conventional liquid formulations. Active pharmaceutical ingredients (APIs) are often hydrophobic, thus not soluble in conventional liquid delivery. Encapsulating the drugs in polymer nanoparticles can improve their pharmacological and bio-distribution properties, preventing rapid clearance from the bloodstream. Such nanoparticles are commonly made of non-toxic amphiphilic self-assembling block copolymers where the core (poly-[D,L-lactic acid] or PLA) serves as a reservoir for the API and the external part (Poly-(Ethylene-Glycol) or PEG) serves as a stealth corona to avoid capture by macrophage...
April 21, 2017: International Journal of Pharmaceutics
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