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https://www.readbyqxmd.com/read/29044549/effects-of-clioquinol-on-the-scuticociliatosis-causing-protozoan-miamiensis-avidus-in-olive-flounder-paralichthys-olivaceus
#1
J-H Lee, J-J Park, J-H Choi, S-Y Kang, Y-J Kang, K H Park
Scuticociliatosis is a devastating and intractable protozoal disease in olive flounder, leading to a significant loss throughout the year. This study aimed to investigate a systemically effective antiscuticociliatosis agent for olive flounder for better absorption into the infected internal organs. The in vitro and in vivo antiscuticociliatosis effects of clioquinol (CQ) were examined after screening 30 biocidal agents against the highly pathogenic scuticociliate Miamiensis avidus. CQ was the most potent in vitro drug of those tested against cultured M...
October 17, 2017: Journal of Fish Diseases
https://www.readbyqxmd.com/read/28979759/mass-spectrometric-directed-system-for-the-continuous-flow-synthesis-and-purification-of-diphenhydramine
#2
Bradley P Loren, Michael Wleklinski, Andy Koswara, Kathryn Yammine, Yanyang Hu, Zoltan K Nagy, David H Thompson, R Graham Cooks
A highly integrated approach to the development of a process for the continuous synthesis and purification of diphenhydramine is reported. Mass spectrometry (MS) is utilized throughout the system for on-line reaction monitoring, off-line yield quantitation, and as a reaction screening module that exploits reaction acceleration in charged microdroplets for high throughput route screening. This effort has enabled the discovery and optimization of multiple routes to diphenhydramine in glass microreactors using MS as a process analytical tool (PAT)...
June 1, 2017: Chemical Science
https://www.readbyqxmd.com/read/28951824/intraocular-in%C3%A2-vivo-imaging-of-pancreatic-islet-cell-physiology-pathology
#3
REVIEW
Ingo B Leibiger, Per-Olof Berggren
BACKGROUND: Diabetes mellitus has reached epidemic proportions and requires new strategies for treatment. Unfortunately, the efficacy of treatment regimens on maintaining/re-gaining functional beta cell mass can, at the present, only be determined indirectly. Direct monitoring of beta cell mass is complicated by the anatomy of the endocrine pancreas, which consists of thousands to a million of discrete micro-organs, i.e. islets of Langerhans, which are scattered throughout the pancreas...
September 2017: Molecular Metabolism
https://www.readbyqxmd.com/read/28889384/spheroid-cultures-of-primary-urothelial-cancer-cells-cancer-tissue-originated-spheroid-ctos-method
#4
Takahiro Yoshida, Hiroaki Okuyama, Hiroko Endo, Masahiro Inoue
Increasingly, it has been recognized that studying cancer samples from individual patients is important for the development of effective therapeutic strategies and in endeavors to overcome therapy resistance. Primary cultures of cancer cells acutely dissected from individual patients can provide a platform that enables the study and characterization of individual tumors. To that end, we have developed a method for preparing cancer cells in the form of multi-cellular spheroids. The cells can be derived from patient tumors (primary cells), from patient-derived xenografts, or from genetically- or chemically induced animal tumors...
2018: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28835636/potential-inhibitors-designed-against-ndm-1-type-metallo-%C3%AE-lactamases-an-attempt-to-enhance-efficacies-of-antibiotics-against-multi-drug-resistant-bacteria
#5
Asad U Khan, Abid Ali, Danishuddin, Gaurava Srivastava, Ashok Sharma
NDM-1 and its variants are the most prevalent types of metallo-β-lactamases, hydrolyze almost all antibiotics of β-lactam group leading to multiple-drug resistance in bacteria. No inhibitor has yet been obtained for NDM-1 or other class of metallo-β-lactamases. Therefore, strategies to identify novel anti-β-lactamase agents with specific mechanisms of action are the need of an hour. In this study, we have reported the discovery of novel non-β-lactam inhibitors against NDM-1 by multi-step virtual screening approach...
August 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28685162/in-vivo-indicators-of-cytoplasmic-vacuolar-and-extracellular-ph-using-phluorin2-in-candida-albicans
#6
Hélène Tournu, Arturo Luna-Tapia, Brian M Peters, Glen E Palmer
Environmental or chemically induced stresses often trigger physiological responses that regulate intracellular pH. As such, the capacity to detect pH changes in real time and within live cells is of fundamental importance to essentially all aspects of biology. In this respect, pHluorin, a pH-sensitive variant of green fluorescent protein, has provided an invaluable tool to detect such responses. Here, we report the adaptation of pHluorin2 (PHL2), a substantially brighter variant of pHluorin, for use with the human fungal pathogen Candida albicans...
July 2017: MSphere
https://www.readbyqxmd.com/read/28669605/industrial-medicinal-chemistry-insights-neuroscience-hit-generation-at-janssen
#7
REVIEW
Gary Tresadern, Frederik J R Rombouts, Daniel Oehlrich, Gregor Macdonald, Andres A Trabanco
The role of medicinal chemistry has changed over the past 10 years. Chemistry had become one step in a process; funneling the output of high-throughput screening (HTS) on to the next stage. The goal to identify the ideal clinical compound remains, but the means to achieve this have changed. Modern medicinal chemistry is responsible for integrating innovation throughout early drug discovery, including new screening paradigms, computational approaches, novel synthetic chemistry, gene-family screening, investigating routes of delivery, and so on...
June 29, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28590392/pilot-studies-examining-feasibility-of-substance-use-disorder-screening-and-treatment-linkage-at-urban-sexually-transmitted-disease-clinics
#8
Jan Gryczynski, Courtney D Nordeck, Shannon Gwin Mitchell, Kathleen R Page, Luke L Johnsen, Kevin E O'Grady, Robert P Schwartz
BACKGROUND: Sexually transmitted disease (STD) clinics provide critical public health services for screening and treatment of sexually transmitted infections throughout the United States. These settings serve high-risk populations, often on a walk-in basis, and may be promising venues for integrating substance use disorder (SUD) services. METHODS: We report findings from 2 pilot studies conducted at Baltimore City Health Department's STD clinics. The screening study characterized rates of SUDs among STD clinic patients...
September 2017: Journal of Addiction Medicine
https://www.readbyqxmd.com/read/28573153/optical-imaging-of-the-rat-brain-suggests-a-previously-missing-link-between-top-down-and-bottom-up-nervous-system-function
#9
Susan A Greenfield, Antoine-Scott Badin, Giovanni Ferrati, Ian M Devonshire
Optical imaging with voltage-sensitive dyes enables the visualization of extensive yet highly transient coalitions of neurons (assemblies) operating throughout the brain on a subsecond time scale. We suggest that operating at the mesoscale level of brain organization, neuronal assemblies may provide a functional link between "bottom-up" cellular mechanisms and "top-down" cognitive ones within anatomically defined regions. We demonstrate in ex vivo rat brain slices how varying spatiotemporal dynamics of assemblies reveal differences not previously appreciated between: different stages of development in cortical versus subcortical brain areas, different sensory modalities (hearing versus vision), different classes of psychoactive drugs (anesthetics versus analgesics), different effects of anesthesia linked to hyperbaric conditions and, in vivo, depths of anesthesia...
July 2017: Neurophotonics
https://www.readbyqxmd.com/read/28566227/boosted-protease-inhibitor-monotherapy-versus-boosted-protease-inhibitor-plus-lamivudine-dual-therapy-as-second-line-maintenance-treatment-for-hiv-1-infected-patients-in-sub-saharan-africa-anrs12-286-mobidip-a-multicentre-randomised-parallel-open-label-superiority
#10
Laura Ciaffi, Sinata Koulla-Shiro, Adrien Bruno Sawadogo, Cheik Tidiane Ndour, Sabrina Eymard-Duvernay, Pretty Rosereine Mbouyap, Liliane Ayangma, Jacques Zoungrana, Ndeye Fatou Ngom Gueye, Mohamadou Diallo, Suzanne Izard, Guillaume Bado, Coumba Toure Kane, Avelin Fobang Aghokeng, Martine Peeters, Pierre Marie Girard, Vincent Le Moing, Jacques Reynes, Eric Delaporte
BACKGROUND: Despite satisfactory efficacy of WHO-recommended second-line antiretroviral treatment for patients with HIV in low-income countries, the need for simplified, low-cost, and less-toxic maintenance strategies remains high. We compared boosted protease inhibitor monotherapy with dual therapy with boosted protease inhibitor plus lamivudine in patients on second-line antiretrovial therapy (ART). METHODS: We did a multicentre, randomised, parallel, open-label, superiority, trial in the HIV services of five hospitals in sub-Saharan Africa (Yaoundé, Cameroon; Dakar, Senegal; and Bobo Dioulasso, Burkina Faso)...
September 2017: Lancet HIV
https://www.readbyqxmd.com/read/28545327/designing-of-inhibitors-against-ctx-m-15-type-%C3%AE-lactamase-potential-drug-candidate-against-%C3%AE-lactamases-producing-multi-drug-resistant-bacteria
#11
Abid Ali, Danishuddin, Lubna Maryam, Gaurava Srivastava, Ashok Sharma, Asad U Khan
CTX-M-15 are the most prevalent types of β-lactamases that hydrolyze almost all antibiotics of β-lactam group lead to multiple-antibiotic resistance in bacteria. Three β-lactam inhibitors are available for use in combination with different antibiotics of cephalosporine group against the CTX-M-15-producing strains. Therefore, strategies to identify novel anti β-lactamase agents with specific mechanisms of action are the need of an hour. In this study, we screened three novel non-β-lactam inhibitors against CTX-M-15 by multi-step virtual screening approach...
June 8, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28515725/application-of-zebrafish-models-in-inflammatory-bowel-disease
#12
REVIEW
Li Hanyang, Liu Xuanzhe, Chen Xuyang, Qiu Yujia, Fu Jiarong, Shen Jun, Ran Zhihua
Inflammatory bowel disease (IBD) is a chronic, recurrent, and remitting inflammatory disease with unclear etiology. As a clinically frequent disease, it can affect individuals throughout their lives, with multiple complications. Unfortunately, traditional murine models are not efficient for the further study of IBD. Thus, effective and convenient animal models are needed. Zebrafish have been used as model organisms to investigate IBD because of their suggested highly genetic similarity to humans and their superiority as laboratory models...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/28514994/active-syphilis-and-its-association-with-hiv-and-sexual-risk-behaviours-in-a-multicity-sample-of-men-who-have-sex-with-men-and-transgender-women-in-peru
#13
Lia N Pizzicato, Panagiotis Vagenas, Pedro Gonzales, Javier R Lama, Monica Pun, Jorge Sanchez, Frederick L Altice
Background: Syphilis in Peru is heavily concentrated in men who have sex with men (MSM) and transgender women (TGW). The aim of the present study was to understand the risk factors for active syphilis infection among MSM and TGW in Peru. Methods: Independent correlates suggestive of active syphilis infection were examined to better understand risk factors for syphilis in MSM and TGW, with separate analyses conducted based on location and among TGW. In 2011, 5101 MSM and TGW completed both self-report surveys and HIV and syphilis testing in five Peruvian cities...
May 18, 2017: Sexual Health
https://www.readbyqxmd.com/read/28500978/novel-polyglycerol-dioleate-based-cubosomal-dispersion-with-tailored-physical-characteristics-for-controlled-delivery-of-ondansetron
#14
M Mansour, A O Kamel, S Mansour, N D Mortada
In this study different amphiphilic lipids viz. glycerylmonooleate (GMO), Glycerylmonolinoleate (GML), Plurol(®) (polyglycerol 3-dioleate), Soya phosphatidylcholine (Soya PC), Dipalmitoyl-phosphatidylcholine (DPPC) and Dipalmitoyl- phosphatidylglycerol (DPPG) were screened for their ability to form cubosomes and the formed particles were optimized for controlled delivery using ondansetron as a model drug. Polarized optical microscopy and high resolution transmission electron microscopy were performed to investigate the morphology of the prepared particles...
April 26, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28409029/biophysical-approaches-facilitate-computational-drug-discovery-for-atp-binding-cassette-proteins
#15
REVIEW
Steven V Molinski, Zoltán Bozóky, Surtaj H Iram, Saumel Ahmadi
Although membrane proteins represent most therapeutically relevant drug targets, the availability of atomic resolution structures for this class of proteins has been limited. Structural characterization has been hampered by the biophysical nature of these polytopic transporters, receptors, and channels, and recent innovations to in vitro techniques aim to mitigate these challenges. One such class of membrane proteins, the ATP-binding cassette (ABC) superfamily, are broadly expressed throughout the human body, required for normal physiology and disease-causing when mutated, yet lacks sufficient structural representation in the Protein Data Bank...
2017: International Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28342321/improvement-of-paracellular-transport-in-the-caco-2-drug-screening-model-using-protein-engineered-substrates
#16
Rebecca L DiMarco, Daniel R Hunt, Ruby E Dewi, Sarah C Heilshorn
The Caco-2 assay has achieved wide popularity among pharmaceutical companies in the past two decades as an in vitro method for estimation of in vivo oral bioavailability of pharmaceutical compounds during preclinical characterization. Despite its popularity, this assay suffers from a severe underprediction of the transport of drugs which are absorbed paracellularly, that is, which pass through the cell-cell tight junctions of the absorptive cells of the small intestine. Here, we propose that simply replacing the collagen I matrix employed in the standard Caco-2 assay with an engineered matrix, we can control cell morphology and hence regulate the cell-cell junctions that dictate paracellular transport...
June 2017: Biomaterials
https://www.readbyqxmd.com/read/28335860/-muscling-throughout-life-integrating-studies-of-muscle-development-homeostasis-and-disease-in-zebrafish
#17
REVIEW
Michelle F Goody, Erin V Carter, Elisabeth A Kilroy, Lisa Maves, Clarissa A Henry
The proper development and function of skeletal muscle is vital for health throughout the lifespan. Skeletal muscle function enables posture, breathing, and locomotion; and also impacts systemic processes-such as metabolism, thermoregulation, and immunity. Diseases of skeletal muscle (myopathies, muscular dystrophies) and even some neurological, age-related, and metabolic diseases compromise muscle function and negatively affect health span and quality of life. There have been numerous, recent examples of studies on skeletal muscle development with exciting, therapeutic implications for muscle diseases...
2017: Current Topics in Developmental Biology
https://www.readbyqxmd.com/read/28317879/a-novel-method-for-screening-adenosine-receptor-specific-agonists-for-use-in-adenosine-drug-development
#18
Karlie R Jones, Uimook Choi, Ji-Liang Gao, Robert D Thompson, Larry E Rodman, Harry L Malech, Elizabeth M Kang
Agonists that target the A1, A2A, A2B and A3 adenosine receptors have potential to be potent treatment options for a number of diseases, including autoimmune diseases, cardiovascular disease and cancer. Because each of these adenosine receptors plays a distinct role throughout the body, obtaining highly specific receptor agonists is essential. Of these receptors, the adenosine A2AR and A2BR share many sequence and structural similarities but highly differ in their responses to inflammatory stimuli. Our laboratory, using a combination of specially developed cell lines and calcium release analysis hardware, has created a new and faster method for determining specificity of synthetic adenosine agonist compounds for the A2A and A2B receptors in human cells...
March 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28116998/exploration-of-new-and-potent-lead-molecules-against-caax-prenyl-protease-i-of-leishmania-donovani-through-pharmacophore-based-virtual-screening-approach
#19
Sitrarasu Vijaya Prabhu, Kartikeya Tiwari, Venkatesan Suryanarayanan, Vikash Kumar Dubey, Sanjeev Kumar Singh
AIM AND OBJECTIVE: Visceral leishmaniasis is a deadly disease left untreated in over 95% of cases. It is characterized by irregular bouts of fever, weight loss, enlargement of the spleen and liver, and anemia. It is highly endemic in the Indian subcontinent. CAAX prenyl protease I of Leishmania donovani is one of the important targets regulating the post translational modification process. Hence identifying potent drug candidate against the target is essential. This study mainly focuses on developing new and potent inhibitors against CAXX prenyl protease I of Leishmania donovani...
2017: Combinatorial Chemistry & High Throughput Screening
https://www.readbyqxmd.com/read/28070873/animal-models-of-ptsd-a-critical-review
#20
Elizabeth I Flandreau, Mate Toth
The goals of animal research in post-traumatic stress disorder (PTSD) include better understanding the neurophysiological etiology of PTSD, identifying potential targets for novel pharmacotherapies, and screening drugs for their potential use as PTSD treatment in humans. Diagnosis of PTSD relies on a patient interview and, as evidenced by changes to the diagnostic criteria in the DSM-5, an adequate description of this disorder in humans is a moving target. Therefore, it may seem insurmountable to model the construct of PTSD in animals such as rodents...
January 10, 2017: Current Topics in Behavioral Neurosciences
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