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https://www.readbyqxmd.com/read/28340413/design-synthesis-and-biological-evaluation-of-novel-coumarin-based-benzamides-as-potent-histone-deacetylase-inhibitors-and-anticancer-agents
#1
Tooba Abdizadeh, Mohammad Reza Kalani, Khalil Abnous, Zahra Tayarani-Najaran, Bibi Zahra Khashyarmanesh, Rahman Abdizadeh, Razieh Ghodsi, Farzin Hadizadeh
Histone deacetylases (HDACs) are attractive therapeutic targets for the treatment of cancer and other diseases. It has four classes (I-IV), among them especially class I isozyme are involved in promoting tumor cells proliferation, angiogenesis, differentiation, invasion and metastasis and also viable targets for cancer therapeutics. A novel series of coumarin-based benzamides was designed and synthesized as HDAC inhibitors. The cytotoxic activity of the synthesized compounds (8a-u) was evaluated against six human cancer cell lines including HCT116, A2780, MCF7, PC3, HL60 and A549 and a single normal cell line (Huvec)...
March 18, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28340300/synthesis-of-3-o-sulfated-oligosaccharides-to-understand-the-relationship-between-structures-and-functions-of-heparan-sulfate
#2
Zhangjie Wang, Po-Hung Hsieh, Yongmei Xu, David Thieker, Evangeline Juan En Chai, Shaoshuai Xie, Brian Cooley, Robert Woods, Lianli Chi, Jian Liu
The sulfation at the 3-OH position of glucosamine is an important modification in forming structural domains for heparan sulfate to enable its biological functions. Seven 3-O-sulfotransferase isoforms in the human genome are involved in the biosynthesis of 3-O-sulfated heparan sulfate. As a rare modification present in heparan sulfate, the availability of 3-O-sulfated oligosaccharides is very limited. Here, we report the use of a chemoenzymatic synthetic approach to synthesize six 3-O-sulfated oligosaccharides, including three hexasaccharides and three octasaccharides...
March 24, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28340006/benefit-of-biologics-initiation-in-moderate-versus-severe-rheumatoid-arthritis-evidence-from-a-united-states-registry
#3
Arthur Kavanaugh, Edward Keystone, Jeffrey D Greenberg, George W Reed, Jenny M Griffith, Alan W Friedman, Katherine C Saunders, Arijit Ganguli
Objectives.: To compare clinical outcomes and treatment patterns among patients with moderate vs severe RA following biologic DMARD initiation. Methods.: Biologics-naive patients with moderate to severe RA [Clinical Disease Activity Index (CDAI) >10] who initiated a biologic DMARD were selected from the Corrona registry (2001-13). CDAI, functional status [modified HAQ (mHAQ)] and patterns of drug use were compared at 1 and 2 years post-initiation between patients with moderate (CDAI >10⩽22) vs severe (CDAI >22) baseline disease activity...
March 8, 2017: Rheumatology
https://www.readbyqxmd.com/read/28339817/bsr-and-bhpr-guideline-for-the-prescription-and-monitoring-of-non-biologic-disease-modifying-anti-rheumatic-drugs
#4
Jo Ledingham, Nicola Gullick, Katherine Irving, Rachel Gorodkin, Melissa Aris, Jean Burke, Patrick Gordon, Dimitrios Christidis, Sarah Galloway, Eranga Hayes, Andrew Jeffries, Scott Mercer, Janice Mooney, Sander van Leuven, James Galloway
No abstract text is available yet for this article.
February 27, 2017: Rheumatology
https://www.readbyqxmd.com/read/28339791/bridg-a-domain-information-model-for-translational-and-clinical-protocol-driven-research
#5
Lauren B Becnel, Smita Hastak, Wendy Ver Hoef, Robert P Milius, MaryAnn Slack, Diane Wold, Michael L Glickman, Boris Brodsky, Charles Jaffe, Rebecca Kush, Edward Helton
Background: It is critical to integrate and analyze data from biological, translational, and clinical studies with data from health systems; however, electronic artifacts are stored in thousands of disparate systems that are often unable to readily exchange data. Objective: To facilitate meaningful data exchange, a model that presents a common understanding of biomedical research concepts and their relationships with health care semantics is required. The Biomedical Research Integrated Domain Group (BRIDG) domain information model fulfills this need...
February 26, 2017: Journal of the American Medical Informatics Association: JAMIA
https://www.readbyqxmd.com/read/28339737/a-novel-chronic-opioid-monitoring-tool-to-assess-prescription-drug-steady-state-levels-in-oral-fluid
#6
Naum Shaparin, Neel Mehta, Frank Kunkel, Richard Stripp, Damon Borg, Elizabeth Kolb
Objective. : Interpretation limitations of urine drug testing and the invasiveness of blood toxicology have motivated the desire for the development of simpler methods to assess biologically active drug levels on an individualized patient basis. Oral fluid is a matrix well-suited for the challenge because collections are based on simple noninvasive procedures and drug concentrations better correlate to blood drug levels as oral fluid is a filtrate of the blood. Well-established pharmacokinetic models were utilized to generate oral fluid steady state concentration ranges to assess the interpretive value of the alternative matrix to monitor steady state plasma oxycodone levels...
February 23, 2017: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
https://www.readbyqxmd.com/read/28339468/pbmda-a-novel-and-effective-path-based-computational-model-for-mirna-disease-association-prediction
#7
Zhu-Hong You, Zhi-An Huang, Zexuan Zhu, Gui-Ying Yan, Zheng-Wei Li, Zhenkun Wen, Xing Chen
In the recent few years, an increasing number of studies have shown that microRNAs (miRNAs) play critical roles in many fundamental and important biological processes. As one of pathogenetic factors, the molecular mechanisms underlying human complex diseases still have not been completely understood from the perspective of miRNA. Predicting potential miRNA-disease associations makes important contributions to understanding the pathogenesis of diseases, developing new drugs, and formulating individualized diagnosis and treatment for diverse human complex diseases...
March 24, 2017: PLoS Computational Biology
https://www.readbyqxmd.com/read/28335462/therapeutic-potentials-of-microalgae-in-the-treatment-of-alzheimer-s-disease
#8
REVIEW
Tosin A Olasehinde, Ademola O Olaniran, Anthony I Okoh
Current research is geared towards the discovery of new compounds with strong neuroprotective potential and few or no side effects compared to synthetic drugs. This review focuses on the potentials of extracts and biologically active compounds derived from microalgal biomass for the treatment and management of Alzheimer's disease (AD). Microalgal research has gained much attention recently due to its contribution to the production of renewable fuels and the ability of alga cells to produce several secondary metabolites such as carotenoids, polyphenols, sterols, polyunsaturated fatty acids and polysaccharides...
March 18, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28335308/probe-microscopic-studies-of-dna-molecules-on-carbon-nanotubes
#9
REVIEW
Kazuo Umemura, Katsuki Izumi, Shusuke Oura
Hybrids of DNA and carbon nanotubes (CNTs) are promising nanobioconjugates for nanobiosensors, carriers for drug delivery, and other biological applications. In this review, nanoscopic characterization of DNA-CNT hybrids, in particular, characterization by scanning probe microscopy (SPM), is summarized. In many studies, topographical imaging by atomic force microscopy has been performed. However, some researchers have demonstrated advanced SPM operations in order to maximize its unique and valuable functions...
October 8, 2016: Nanomaterials
https://www.readbyqxmd.com/read/28335253/soft-interaction-in-liposome-nanocarriers-for-therapeutic-drug-delivery
#10
REVIEW
Domenico Lombardo, Pietro Calandra, Davide Barreca, Salvatore Magazù, Mikhail A Kiselev
The development of smart nanocarriers for the delivery of therapeutic drugs has experienced considerable expansion in recent decades, with the development of new medicines devoted to cancer treatment. In this respect a wide range of strategies can be developed by employing liposome nanocarriers with desired physico-chemical properties that, by exploiting a combination of a number of suitable soft interactions, can facilitate the transit through the biological barriers from the point of administration up to the site of drug action...
June 25, 2016: Nanomaterials
https://www.readbyqxmd.com/read/28335215/rapamycin-loaded-solid-lipid-nanoparticles-as-a-new-tool-to-deliver-mtor-inhibitors-formulation-and-in-vitro-characterization
#11
Alice Polchi, Alessandro Magini, Jarosław Mazuryk, Brunella Tancini, Jacek Gapiński, Adam Patkowski, Stefano Giovagnoli, Carla Emiliani
Recently, the use of mammalian target of rapamycin (mTOR) inhibitors, in particular rapamycin (Rp), has been suggested to improve the treatment of neurodegenerative diseases. However, as Rp is a strong immunosuppressant, specific delivery to the brain has been postulated to avoid systemic exposure. In this work, we fabricated new Rp loaded solid lipid nanoparticles (Rp-SLN) stabilized with polysorbate 80 (PS80), comparing two different methods and lipids. The formulations were characterized by differential scanning calorimetry (DSC), nuclear magnetic resonance (NMR), wide angle X-ray scattering (WAXS), cryo-transmission electron microscopy (cryo-TEM), dynamic light scattering (DLS) and particle tracking...
May 9, 2016: Nanomaterials
https://www.readbyqxmd.com/read/28334805/hair-testing-for-drugs-of-abuse-and-new-psychoactive-substances-in-a-high-risk-population
#12
Alberto Salomone, Joseph J Palamar, Enrico Gerace, Daniele Di Corcia, Marco Vincenti
Hundreds of new psychoactive substances (NPS) have emerged in the drug market over the last decade. Few drug surveys in the USA, however, ask about use of NPS, so prevalence and correlates of use are largely unknown. A large portion of NPS use is unintentional or unknown as NPS are common adulterants in drugs like ecstasy/Molly, and most NPS are rapidly eliminated from the body, limiting efficacy of urine, blood and saliva testing. We utilized a novel method of examining prevalence of NPS use in a high-risk population utilizing hair-testing...
March 4, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/28334528/why-prodrugs-and-propesticides-succeed
#13
John E Casida
What are the advantages of bioactivation in optimizing drugs and pesticides? Why are there so many prodrugs and propesticides? These questions are examined here by considering compounds selected on the basis of economic value or market success. The 100 major drugs and 90 major pesticides are divided into ones acting directly and those definitely or possibly requiring bioactivation. Established or candidate prodrugs accounted for 19% of the total drug sales with corresponding values of 20, 37 and 17% for proinsecticides, proherbicides and profungicides...
March 23, 2017: Chemical Research in Toxicology
https://www.readbyqxmd.com/read/28334136/a-review-of-network-based-approaches-to-drug-repositioning
#14
Maryam Lotfi Shahreza, Nasser Ghadiri, Sayed Rasoul Mousavi, Jaleh Varshosaz, James R Green
Experimental drug development is time-consuming, expensive and limited to a relatively small number of targets. However, recent studies show that repositioning of existing drugs can function more efficiently than de novo experimental drug development to minimize costs and risks. Previous studies have proven that network analysis is a versatile platform for this purpose, as the biological networks are used to model interactions between many different biological concepts. The present study is an attempt to review network-based methods in predicting drug targets for drug repositioning...
February 27, 2017: Briefings in Bioinformatics
https://www.readbyqxmd.com/read/28333338/drug-discovery-for-male-subfertility-using-high-throughput-screening-a-new-approach-to-an-unsolved-problem
#15
Sarah J Martins da Silva, Sean G Brown, Keith Sutton, Louise V King, Halil Ruso, David W Gray, Paul G Wyatt, Mark C Kelly, Christopher L R Barratt, Anthony G Hope
STUDY QUESTION: Can pharma drug discovery approaches be utilized to transform investigation into novel therapeutics for male infertility? SUMMARY ANSWER: High-throughput screening (HTS) is a viable approach to much-needed drug discovery for male factor infertility. WHAT IS KNOWN ALREADY: There is both huge demand and a genuine clinical need for new treatment options for infertile men. However, the time, effort and resources required for drug discovery are currently exorbitant, due to the unique challenges of the cellular, physical and functional properties of human spermatozoa and a lack of appropriate assay platform...
March 16, 2017: Human Reproduction
https://www.readbyqxmd.com/read/28333111/solanesol-biosynthesis-in-plants
#16
REVIEW
Ning Yan, Yanhua Liu, Hongbo Zhang, Yongmei Du, Xinmin Liu, Zhongfeng Zhang
Solanesol is a non-cyclic terpene alcohol composed of nine isoprene units that mainly accumulates in solanaceous plants. Solanesol plays an important role in the interactions between plants and environmental factors such as pathogen infections and moderate-to-high temperatures. Additionally, it is a key intermediate for the pharmaceutical synthesis of ubiquinone-based drugs such as coenzyme Q10 and vitamin K2, and anti-cancer agent synergizers such as N-solanesyl-N,N'-bis(3,4-dimethoxybenzyl) ethylenediamine (SDB)...
March 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28333042/minocycline-releasing-pmma-system-as-a-space-maintainer-for-staged-bone-reconstructions-in-vitro-antibacterial-cytocompatibility-and-anti-inflammatory-characterization
#17
Tiago Silva, Liliana Grenho, Joana Barros, José Silva, Rosana Pinto, Ana Matos, Bruno Colaço, Helena Fernandes, Ana Bettencourt, Pedro S Gomes
In the present work, it is aimed the development and biological characterization of a poly methyl methacrylate (PMMA)-based minocycline delivery system, to be used as a space maintainer within craniofacial staged regenerative interventions. Developed delivery systems were characterized regarding solid state characteristics and assayed in vitro for anti-bacterial and anti-inflammatory activity, and cytocompatibility with human bone cells. Drug release profile allowed for an initial burst release and a more sustained and controlled release over time, with minimum inhibitory concentrations for the assayed and relevant pathogenic bacteria (i...
March 23, 2017: Biomedical Materials
https://www.readbyqxmd.com/read/28332820/kinetic-landscape-of-a-peptide-bond-forming-prolyl-oligopeptidase
#18
Clarissa Melo Czekster, James H Naismith
Prolyl oligopeptidase B from Galerina marginata (GmPOPB) has recently been discovered as a peptidase capable of breaking and forming peptide bonds to yield a cyclic peptide. Despite the relevance of prolyl oligopeptidases in human biology and disease, a kinetic analysis pinpointing rate-limiting steps for a member of this enzyme family is not available. Macrocyclase enzymes are currently exploited to produce cyclic peptides with potential therapeutic applications. Cyclic peptides are promising drug-like molecules due to their stability and conformational rigidity...
March 23, 2017: Biochemistry
https://www.readbyqxmd.com/read/28331550/experiences-of-mobility-for-people-living-with-rheumatoid-arthritis-who-are-receiving-biologic-drug-therapy-implications-for-podiatry-services
#19
Lucy Sanders, Margaret Donovan-Hall, Alan Borthwick, Catherine J Bowen
BACKGROUND: Despite significant advancements in new treatment modalities for rheumatoid arthritis with biological therapies, foot complications remain a disabling and common feature of the disease. In this study the aim was to explore and describe the personal experiences of people with rheumatoid arthritis in receipt of biologic treatments in a bid to understand the impact of this form of medication on their mobility. METHODS: An interpretative phenomenological analysis (IPA) was undertaken to explore in depth the individual experience of rheumatoid disease through personal accounts of the patient journey spanning both 'before' and 'after' the instigation of biologic therapy...
2017: Journal of Foot and Ankle Research
https://www.readbyqxmd.com/read/28331534/ford-and-edison-in-a-modern-regulatory-environment-the-first-in-human-trial-of-night-work-and-artificial-light
#20
EDITORIAL
Thomas C Erren, David M Shaw, Ursula Wild, J Valérie Groß
A thought experiment places Henry Ford and Thomas Alva Edison in a modern regulatory environment. In a utopian occupational world devoid of night-shifts or artificial light, Ford wants to experiment with "working through the night". To support Ford's project, Edison offers his patented electric lamps to "turn nights into days". An ethics committee [EC] does not approve the night-work experiment and Utopia's Food and Drug Administration [FDA] does not approve the potential medical device as safe for use by humans...
2017: Journal of Occupational Medicine and Toxicology
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