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https://www.readbyqxmd.com/read/28685162/in-vivo-indicators-of-cytoplasmic-vacuolar-and-extracellular-ph-using-phluorin2-in-candida-albicans
#1
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
#2
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
#3
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...
June 5, 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
#4
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
#5
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)...
May 26, 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
#6
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
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
https://www.readbyqxmd.com/read/28034363/the-screening-of-novel-inhibitors-against-leishmania-donovani-calcium-ion-channel-to-fight-leishmaniasis
#16
Mohammad Kashif, Partha Pratim Manna, Yusuf Akhter, Mohammed Alaidarous, Abdur Rub
Leishmania is an intracellular protozoan parasite which causes Leishmaniasis, a global health problem affecting millions of people throughout 89 different countries in the world. The current treatment which includes use of amphotericin B, antimonials, and others has major drawbacks due to toxicity, resistance, and extraordinary high cost. So there is an urgent need of development of new drug targets to fight against leishmaniasis. In this regard we have selected Leishmania donovani Ca2+ ion channel (Ld-CC) as potential drug target...
December 30, 2016: Infectious Disorders Drug Targets
https://www.readbyqxmd.com/read/28018175/progressive-seizure-aggravation-in-the-repeated-6-hz-corneal-stimulation-model-is-accompanied-by-marked-increase-in-hippocampal-p-erk1-2-immunoreactivity-in-neurons
#17
Carmela Giordano, Anna M Costa, Chiara Lucchi, Giuseppina Leo, Luc Brunel, Jean-Alain Fehrentz, Jean Martinez, Antonio Torsello, Giuseppe Biagini
The 6-Hz corneal stimulation test is used to screen novel antiepileptic molecules to overcome the problem of drug refractoriness. Although recognized as a standard test, it has been evaluated only recently in the attempt to characterize the putative neuronal networks involved in seizures caused by corneal stimulation. In particular, by recording from the CA1 region we previously established that the hippocampus participates to propagation of seizure activity. However, these findings were not corroborated by using markers of neuronal activation such as FosB/ΔFosB antigens...
2016: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/27964869/relapse-to-opioid-use-in-opioid-dependent-individuals-released-from-compulsory-drug-detention-centres-compared-with-those-from-voluntary-methadone-treatment-centres-in-malaysia-a-two-arm-prospective-observational-study
#18
Martin P Wegman, Frederick L Altice, Sangeeth Kaur, Vanesa Rajandaran, Sutayut Osornprasop, David Wilson, David P Wilson, Adeeba Kamarulzaman
BACKGROUND: Detention of people who use drugs into compulsory drug detention centres (CDDCs) is common throughout East and Southeast Asia. Evidence-based pharmacological therapies for treating substance use disorders, such as opioid agonist treatments with methadone, are generally unavailable in these settings. We used a unique opportunity where CDDCs coexisted with voluntary drug treatment centres (VTCs) providing methadone in Malaysia to compare the timing and occurrence of opioid relapse (measured using urine drug testing) in individuals transitioning from CDDCs versus methadone maintenance in VTCs...
February 2017: Lancet Global Health
https://www.readbyqxmd.com/read/27920558/monitoring-the-effects-of-doxorubicin-on-3d-spheroid-tumor-cells-in-real-time
#19
NamHuk Baek, Ok Won Seo, MinSung Kim, John Hulme, Seong Soo A An
Recently, increasing numbers of cell culture experiments with 3D spheroids presented better correlating results in vivo than traditional 2D cell culture systems. 3D spheroids could offer a simple and highly reproducible model that would exhibit many characteristics of natural tissue, such as the production of extracellular matrix. In this paper numerous cell lines were screened and selected depending on their ability to form and maintain a spherical shape. The effects of increasing concentrations of doxorubicin (DXR) on the integrity and viability of the selected spheroids were then measured at regular intervals and in real-time...
2016: OncoTargets and Therapy
https://www.readbyqxmd.com/read/27920535/prevalence-of-alcohol-use-disorders-and-associated-factors-among-people-with-epilepsy-attending-amanuel-mental-specialized-hospital-addis-ababa-ethiopia
#20
Tsegereda Waja, Jemal Ebrahim, Zegeye Yohannis, Asres Bedaso
INTRODUCTION: Alcohol use disorders represent one of the leading causes of preventable death, illness, and injury in many societies throughout the world. Heavy alcohol consumption has multiple negative consequences for people with epilepsy such as precipitation of seizure, exacerbation of seizure, poor seizure control, increased side effects of antiepileptic drugs, noncompliance to antiepileptic drugs, alcohol withdrawal seizures, long-term hospital admission, status epilepticus, sudden unexpected death, and premature mortality...
2016: Neuropsychiatric Disease and Treatment
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