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https://www.readbyqxmd.com/read/28813681/uncoupling-the-mitogenic-and-metabolic-functions-of-fgf1-by-tuning-fgf1-fgf-receptor-dimer-stability
#1
Zhifeng Huang, Yi Tan, Junlian Gu, Yang Liu, Lintao Song, Jianlou Niu, Longwei Zhao, Lakshmi Srinivasan, Qian Lin, Jingjing Deng, Yang Li, Daniel J Conklin, Thomas A Neubert, Lu Cai, Xiaokun Li, Moosa Mohammadi
The recent discovery of metabolic roles for fibroblast growth factor 1 (FGF1) in glucose homeostasis has expanded the functions of this classically known mitogen. To dissect the molecular basis for this functional pleiotropy, we engineered an FGF1 partial agonist carrying triple mutations (FGF1(ΔHBS)) that diminished its ability to induce heparan sulfate (HS)-assisted FGF receptor (FGFR) dimerization and activation. FGF1(ΔHBS) exhibited a severely reduced proliferative potential, while preserving the full metabolic activity of wild-type FGF1 in vitro and in vivo...
August 15, 2017: Cell Reports
https://www.readbyqxmd.com/read/28813474/binge-like-sucrose-consumption-reduces-the-dendritic-length-and-complexity-of-principal-neurons-in-the-adolescent-rat-basolateral-amygdala
#2
Masroor Shariff, Paul Klenowski, Michael Morgan, Omkar Patkar, Erica Mu, Mark Bellingham, Arnauld Belmer, Selena E Bartlett
A compelling body of evidence suggests that the worldwide obesity epidemic is underpinned by excessive sugar consumption, typified by the modern western diet. Furthermore, evidence is beginning to emerge of maladaptive changes in the mesolimbic reward pathway of the brain in relation to excess sugar consumption that highlights the importance of examining this neural circuitry in an attempt to understand and subsequently mitigate the associated morbidities with obesity. While the basolateral amygdala (BLA) has been shown to mediate the reinforcing properties of drugs of abuse, it has also been shown to play an important role in affective and motivated behaviours and has been shown to undergo maladaptive changes in response to drugs of abuse and stress...
2017: PloS One
https://www.readbyqxmd.com/read/28813419/vaccine-driven-pharmacodynamic-dissection-and-mitigation-of-fenethylline-psychoactivity
#3
Cody J Wenthur, Bin Zhou, Kim D Janda
Fenethylline, also known by the trade name Captagon, is a synthetic psychoactive stimulant that has recently been linked to a substance-use disorder and 'pharmacoterrorism' in the Middle East. Although fenethylline shares a common phenethylamine core with other amphetamine-type stimulants, it also incorporates a covalently linked xanthine moiety into its parent structure. These independently active pharmacophores are liberated during metabolism, resulting in the release of a structurally diverse chemical mixture into the central nervous system...
August 16, 2017: Nature
https://www.readbyqxmd.com/read/28813027/sulfonamide-linked-ciprofloxacin-sulfadiazine-and-amantadine-derivatives-as-a-novel-class-of-inhibitors-of-jack-bean-urease-synthesis-kinetic-mechanism-and-molecular-docking
#4
Pervaiz Ali Channar, Aamer Saeed, Fernando Albericio, Fayaz Ali Larik, Qamar Abbas, Mubashir Hassan, Hussain Raza, Sung-Yum Seo
Sulfonamide derivatives serve as an important building blocks in the drug design discovery and development (4D) process. Ciprofloxacin-, sulfadiazine- and amantadine-based sulfonamides were synthesized as potent inhibitors of jack bean urease and free radical scavengers. Molecular diversity was explored and electronic factors were also examined. All 24 synthesized compounds exhibited excellent potential against urease enzyme. Compound 3e (IC50 = 0.081 ± 0.003 µM), 6a (IC50 = 0.0022 ± 0.0002 µM), 9e (IC50 = 0...
August 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28812556/coupling-phenotypic-persistence-to-dna-damage-increases-genetic-diversity-in-severe-stress
#5
Gilad Yaakov, David Lerner, Kajetan Bentele, Joseph Steinberger, Naama Barkai
Mutation rate balances the need to protect genome integrity with the advantage of evolutionary innovations. Microorganisms increase their mutation rate when stressed, perhaps addressing the growing need for evolutionary innovation. Such a strategy, however, is only beneficial under moderate stresses that allow cells to divide and realize their mutagenic potential. In contrast, severe stresses rapidly kill the majority of the population with the exception of a small minority of cells that are in a phenotypically distinct state termed persistence...
January 4, 2017: Nature ecology & evolution
https://www.readbyqxmd.com/read/28812229/economics-and-cost-effectiveness-of-multiple-sclerosis-therapies-in-the-usa
#6
REVIEW
Daniel M Hartung
Multiple sclerosis (MS) is a disabling, chronic disease that imposes a significant economic burden on patients and the US healthcare system. The largest cost component for individuals with MS are prescription drugs, specifically disease-modifying therapies (DMTs). Despite an increase in the number and diversity of DMTs over the past 10 years, acquisition costs for all DMTs have escalated dramatically at rates substantially higher than medical inflation. Currently, costs for most DMTs exceed $70,000 a year. Recent cost-effectiveness studies suggest the cost for nearly all DMTs exceeds generally accepted thresholds for what is considered a good value in the USA, even after factoring expected rebates...
August 15, 2017: Neurotherapeutics: the Journal of the American Society for Experimental NeuroTherapeutics
https://www.readbyqxmd.com/read/28812060/reolysin-and-histone-deacetylase-inhibition-in-the-treatment-of-head-and-neck-squamous-cell-carcinoma
#7
Alena C Jaime-Ramirez, Jun-Ge Yu, Enrico Caserta, Ji Young Yoo, Jianying Zhang, Tae Jin Lee, Craig Hofmeister, John H Lee, Bhavna Kumar, Quintin Pan, Pawan Kumar, Robert Baiocchi, Theodoros Teknos, Flavia Pichiorri, Balveen Kaur, Matthew Old
Oncolytic viruses (OVs) are emerging as powerful anti-cancer agents and are currently being tested for their safety and efficacy in patients. Reovirus (Reolysin), a naturally occurring non-pathogenic, double-stranded RNA virus, has natural oncolytic activity and is being tested in phase I-III clinical trials in a variety of tumor types. With its recent US Food and Drug Administration (FDA) orphan drug designation for several tumor types, Reolysin is a potential therapeutic agent for various cancers, including head and neck squamous cell carcinomas (HNSCCs), which have a 5-year survival of ∼55%...
June 16, 2017: Molecular Therapy Oncolytics
https://www.readbyqxmd.com/read/28811184/experimental-cocrystal-screening-and-solution-based-scale-up-cocrystallization-methods
#8
REVIEW
Maria Malamatari, Steven A Ross, Dennis Douroumis, Sitaram P Velaga
Cocrystals are crystalline single phase materials composed of two or more different molecular and/or ionic compounds generally in a stoichiometric ratio which are neither solvates nor simple salts. If one of the components is an active pharmaceutical ingredient (API), the term pharmaceutical cocrystal is often used. There is a growing interest among drug development scientists in exploring cocrystals, as means to address physicochemical, biopharmaceutical and mechanical properties and expand solid form diversity of the API...
August 12, 2017: Advanced Drug Delivery Reviews
https://www.readbyqxmd.com/read/28809666/biomolecular-network-controllability-with-drug-binding-information
#9
Lin Wu, Lingkai Tang, Min Li, Jianxin Wang, Fang-Xiang Wu
Complex networks are ubiquitous in nature. In biological systems, biomolecules interact with each other to form so-called biomolecular networks, which determine the cellular behaviors of living organisms. Controlling the cellular behaviors by regulating certain biomolecules in the network is one of the most concerned problems in systems biology. Recently, the connections between biological networks and structural control theory have been explored, uncovering some interesting biological phenomena. Some researchers have paid attentions to the structural controllability of networks in notion of the minimum steering sets (MSSs)...
July 2017: IEEE Transactions on Nanobioscience
https://www.readbyqxmd.com/read/28808971/high-throughput-screening-for-identification-of-novel-innate-immune-activators
#10
Bryan J Gall, Victor R DeFilippis
Modern drug discovery has embraced in vitro platforms that enable investigation of large numbers of compounds within tractable timeframes and for feasible costs. These endeavors have been greatly aided in recent years by advances in molecular and cell-based methods such as gene delivery and editing technology, advanced imaging, robotics, and quantitative analysis. As such, the examination of phenotypic impacts of novel molecules may only be limited by the size of the compound collection. Innate immune signaling processes in mammalian cells are especially amenable to high-throughput screening platforms since the cellular responses elicited by their activation often result in high level transcription that can be harnessed in the form of bioluminescent or fluorescent signal...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28808688/adaptive-mistranslation-accelerates-the-evolution-of-fluconazole-resistance-and-induces-major-genomic-and-gene-expression-alterations-in-candida-albicans
#11
Tobias Weil, Rodrigo Santamaría, Wanseon Lee, Johan Rung, Noemi Tocci, Darren Abbey, Ana R Bezerra, Laura Carreto, Gabriela R Moura, Mónica Bayés, Ivo G Gut, Attila Csikasz-Nagy, Duccio Cavalieri, Judith Berman, Manuel A S Santos
Regulated erroneous protein translation (adaptive mistranslation) increases proteome diversity and produces advantageous phenotypic variability in the human pathogen Candida albicans. It also increases fitness in the presence of fluconazole, but the underlying molecular mechanism is not understood. To address this question, we evolved hypermistranslating and wild-type strains in the absence and presence of fluconazole and compared their fluconazole tolerance and resistance trajectories during evolution. The data show that mistranslation increases tolerance and accelerates the acquisition of resistance to fluconazole...
July 2017: MSphere
https://www.readbyqxmd.com/read/28807936/genomic-alterations-in-circulating-tumor-dna-from-diverse-cancer-patients-identified-by-next-generation-sequencing
#12
Maria Schwaederle, Ranajoy Chattopadhyay, Shumei Kato, Paul T Fanta, Kimberly C Banks, In Sil Choi, David E Piccioni, Sadakatsu Ikeda, AmirAli Talasaz, Richard B Lanman, Lyudmila Bazhenova, Razelle Kurzrock
Non-invasive genomic profiling of tumors may be possible with next-generation sequencing (NGS) of blood-derived circulating tumor DNA (ctDNA), but proof of concept in a large cohort <p>of patients with diverse cancers has yet to be reported. Here we report the results of an analysis of plasma-derived ctDNA from 670 patients with diverse cancers.</p> The tumors represented in the patient cohort were mainly gastrointestinal (31.8%), brain (22.7%) or lung (20.7%). ctDNA obtained from most patients (N = 423 (63%)) displayed at least 1 alteration...
August 14, 2017: Cancer Research
https://www.readbyqxmd.com/read/28807683/nano-sized-drug-carriers-extravasation-intratumoral-distribution-and-their-modeling
#13
Joseph W Nichols, Yu Sakurai, Hideyoshi Harashima, You Han Bae
Navigating intratumoral drug distribution has proven to be one of the most challenging aspects of drug delivery. The barriers are significant and varied; increased diffusional distances, elevated interstitial fluid pressure, regions of dense extracellular matrix and high cell density, and overall heterogeneity. Such a long list imposes significant requirements on nano-sized carriers. Unfortunately, other capabilities are eclipsed by the distribution requirements. A drug can do no good until it reaches its target...
August 11, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28807368/membrane-interactions-and-antimicrobial-effects-of-inorganic-nanoparticles
#14
REVIEW
Sara Malekkhaiat Häffner, Martin Malmsten
Interactions between nanoparticles and biological membranes are attracting increasing attention in current nanomedicine, and play a key role both for nanotoxicology and for utilizing nanomaterials in diagnostics, drug delivery, functional biomaterials, as well as combinations of these, e.g., in theranostics. In addition, there is considerable current interest in the use of nanomaterials as antimicrobial agents, motivated by increasing resistance development against conventional antibiotics. Here, various nanomaterials offer opportunities for triggered functionalites to combat challenging infections...
July 27, 2017: Advances in Colloid and Interface Science
https://www.readbyqxmd.com/read/28807159/herb-drug-interactions-of-commonly-used-chinese-medicinal-herbs
#15
Amrinder Singh, Kaicun Zhao
With more and more popular use of traditional herbal medicines, in particular Chinese herbal medicines, herb-drug interactions have become a more and more important safety issue in the clinical applications of the conventional drugs. Researches in this area are increasing very rapidly. Herb-drug interactions are complicated due to the fact that multiple chemical components are involved, and these compounds may possess diverse pharmacological activities. Interactions can be in both pharmacokinetics and pharmacodynamics...
2017: International Review of Neurobiology
https://www.readbyqxmd.com/read/28807097/genotypic-characterization-of-methicillin-resistant-staphylococcus-aureus-isolated-from-pigs-and-retail-foods-in-china
#16
Wei Wang, Feng Liu, Zulqarnain Baloch, Cun Shan Zhang, Ke Ma, Zi Xin Peng, Shao Fei Yan, Yu Jie Hu, Xin Gan, Yin Ping Dong, Yao Bai, Feng Qin Li, Xiao Mein Yan, Ai Guo Ma, Jin Xu
OBJECTIVE: To investigate the genotypic diversity of Methicillin-resistant Staphylococcus aureus (MRSA) isolated from pigs and retail foods from different geographical areas in China and further to study the routes and rates of transmission of this pathogen from animals to food. METHODS: Seventy-one MRSA isolates were obtained from pigs and retail foods and then characterized by multi-locus sequencing typing (MLST), spa typing, multiple-locus variable number of tandem repeat analysis (MLVA), pulsed-field gel electrophoresis (PFGE), and antimicrobial susceptibility testing...
August 2017: Biomedical and Environmental Sciences: BES
https://www.readbyqxmd.com/read/28806076/structure-affinity-relationships-and-structure-kinetics-relationships-of-pyrido-2-1-f-purine-2-4-dione-derivatives-as-human-adenosine-a3-receptor-antagonists
#17
Lizi Xia, Wessel A C Burger, Jacobus P D van Veldhoven, Boaz J Kuiper, Tirsa T van Duijl, Eelke B Lenselink, Ellen Paasman, Laura H Heitman, Adriaan P IJzerman
We expanded on a series of pyrido[2,1-f]purine-2,4-dione derivatives as human adenosine A3 receptor (hA3R) antagonists to determine their kinetic profiles and affinities. Many compounds showed high affinities and a diverse range of kinetic profiles. We found hA3R antagonists with very short residence time at the receptor (RT of 2.2 min for 5) and much longer RTs (e.g. 376 min for 27, or 391 min for 31). Two representative antagonists (5 and 27) were tested in [(35)S]GTPγS binding assays, and their RTs appeared correlated to their (in)surmountable antagonism...
August 14, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28805740/adp-ribosyl-n%C3%A2-a-versatile-precursor-for-divergent-syntheses-of-adp-ribosylated-compounds
#18
Lingjun Li, Qianqian Li, Shengqiang Ding, Pengyang Xin, Yuqin Zhang, Shenlong Huang, Guisheng Zhang
Adenosine diphosphate-ribose (ADP-ribose) and its derivatives play important roles in a series of complex physiological procedures. The design and synthesis of artificial ADP-ribosylated compounds is an efficient way to develop valuable chemical biology tools and discover new drug candidates. However, the synthesis of ADP-ribosylated compounds is currently difficult due to structural complexity, easily broken pyrophosphate bond and high hydrophilicity. In this paper, ADP-ribosyl-N₃ was designed and synthesized for the first time...
August 14, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28805687/a-review-of-the-antiviral-role-of-green-tea-catechins
#19
REVIEW
Jun Xu, Zhao Xu, Wenming Zheng
Over the centuries, infectious diseases caused by viruses have seriously threatened human health globally. Viruses are responsible not only for acute infections but also many chronic infectious diseases. To prevent diseases caused by viruses, the discovery of effective antiviral drugs, in addition to vaccine development, is important. Green tea catechins (GTCs) are polyphenolic compounds from the leaves of Camelliasinensis. In recent decades, GTCs have been reported to provide various health benefits against numerous diseases...
August 12, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28803883/the-provision-of-emergency-contraception-in-kinshasa-s-private-sector-pharmacies-experiences-of-mystery-clients
#20
Julie H Hernandez, Mbadu Muanda Fidèle, Mélissa Garcia, Annie Glover
OBJECTIVES: Recent programmatic and research efforts on addressing gaps in health systems of low-income countries increasingly see task shifting, i.e. the provision of healthcare by non-medically trained personnel, as a possible solution to increase the availability of specific services and commodities. In Kinshasa, private-sector pharmacies are the primary and preferred provider of family planning (FP) methods, and thus constitute a potential resource for expanding access to specific contraceptives...
August 10, 2017: Contraception
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