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drug screening

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BACKGROUND: A body of empirical work demonstrates that wide fluctuations in a person's blood pressure across consecutive measures, known as blood pressure variability (BPV), hold prognostic value to predict stroke and transient ischemic attack. However, the magnitude of association between BPV and other neurological outcomes remains less clear. This systematic review aims to pool together data regarding BPV with respect to incident dementia, cognitive impairment, and cognitive function...
October 15, 2018: Systematic Reviews
Bremansu Osa-Andrews, Kee W Tan, Angelina Sampson, Surtaj H Iram
Multidrug resistance protein 1 (MRP1) can efflux a wide variety of molecules including toxic chemicals, drugs, and their derivatives out of cells. Substrates of MRP1 include anti-cancer agents, antibiotics, anti-virals, anti-human immunodeficiency virus (HIV), and many other drugs. To identify novel substrates and modulators of MRP1 by exploiting intramolecular fluorescence resonance energy transfer (FRET), we genetically engineered six different two-color MRP1 proteins by changing green fluorescent protein (GFP) insertion sites, while keeping the red fluorescent protein (RFP) at the C-terminal of MRP1...
October 13, 2018: Pharmaceutics
Pankaj Pandey, Kuldeep K Roy, Haining Liu, Guoyi Ma, Sara Pettaway, Walid F Alsharif, Rama S Gadepalli, John M Rimoldi, Christopher R McCurdy, Stephen J Cutler, Robert J Doerksen
Natural products are an abundant source of potential drugs, and their diversity makes them a rich and viable prospective source of bioactive cannabinoid ligands. Cannabinoid receptor 1 (CB1) antagonists are clinically established and well documented as potential therapeutics for treating obesity, obesity-related cardiometabolic disorders, pain, and drug/substance abuse, but their associated CNS-mediated adverse effects hinder the development of potential new drugs and no such drug is currently on the market...
October 13, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Farman Ali, Zujie Yao, Wanxin Li, Lina Sun, Wenxiong Lin, Xiangmin Lin
luxS is conserved in several bacterial species, including A. hydrophila, which causes infections in prawn, fish, and shrimp, and is consequently a great risk to the aquaculture industry and public health. luxS plays a critical role in the biosynthesis of the autoinducer-2 (AI-2), which performs wide-ranging functions in bacterial communication, and especially in quorum sensing (QS). The prediction of a 3D structure of the QS-associated LuxS protein is thus essential to better understand and control A. hydrophila pathogenecity...
October 12, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
T K Shameera Ahamed, Vijisha K Rajan, K Sabira, K Muraleedharan
Developments of novel inhibitors to prevent the function of 5-lipoxygenase (5-LOX) proteins that are responsible for a variety of inflammatory and allergic disease are a major challenge in the scientific community. In this study, robust QSAR classification models for predicting 5-LOX activity were developed using machine learning algorithms. The Support Vector Machines (SVM), Logistic Regression, k-Nearest Neighbour (NN) and Decision Trees were adopted to improve the prediction ability of the classification models...
October 5, 2018: Computational Biology and Chemistry
Constantinos Potamitis, Dimitra Siakouli, Konstantinos D Papavasileiou, Athina Boulaka, Vassiliki Ganou, Marina Roussaki, Theodora Calogeropoulou, Panagiotis Zoumpoulakis, Michael N Alexis, Maria Zervou, Dimitra J Mitsiou
Glucocorticoids (GCs) are widely used as potent anti-inflammatory drugs; however, GC therapy is often accompanied by adverse side effects. The anti-inflammatory action of GCs is exerted through the glucocorticoid receptor (GR) in part by antagonizing the pro-inflammatory nuclear factor k B (NF-kB) whereas the majority of side effects are assumed to be mediated by transactivation of GR target genes. We set out to identify novel non-steroidal selective GR agonists (SEGRA) favoring transrepression of NF-kB target genes over transactivation of genes associated with undesirable effects...
October 12, 2018: Journal of Steroid Biochemistry and Molecular Biology
Satish Chandra Pandey, Anubhuti Jha, Awanish Kumar, Mukesh Samant
Visceral leishmaniasis (VL) is one of the most devastating diseases of the tropical region caused by protozoan parasite Leishmania donovani. So far, there is no effective drug and vaccine available against this fatal disease. The DEAD-box RNA helicase is quite essential for the RNA processing, amastigote differentiation and infectivity in Leishmania. In this study, L. donovani DEAD-box RNA helicase (LdHel-67) was evaluated as a potential drug target against VL. Using in-silico approach we have identified ligands that can specifically bind to this protein by using various application of Schrodinger (Maestro, version 10...
October 12, 2018: International Journal of Biological Macromolecules
Nathiya Ranganathan, Gayathri Mahalingam
Endophytic fungi, especially from mangrove plants, are rich source of secondary metabolites, which plays a major role in various pharmacological actions preferably in cancer and bacterial infections. To perceive its role in antidiabetic activity we isolated and tested the metabolites derived from a novel strain Alternaria longipes strain VITN14G obtained from mangrove plant Avicennia officinalis. The crude extract was analyzed for antidiabetic activity and subjected to column chromatography. The isolated fractions were screened in vitro for α-glucosidase and α-amylase inhibitory activities...
October 15, 2018: Journal of Cellular Biochemistry
B V Siva Prasad, Vishal Khatri, P Suresh Yadav, M Subhosh Chandra, D Vijaya Lakshmi, Kalyan Goswami
Background: After mass drug administration to eliminate human lymphatic filariasis, there is a need for surveillance to detect the measurable endpoint of the program. Methods: An immunodominant seroreactive clone, WbL1, was identified through immunoscreening of a Wuchereria bancrofti L3 complementary DNA expression library. Recombinant WbL1 (rWbL1) was analysed with sera from W. bancrofti patients. Diagnostic evaluation was carried out by developing an enzyme-linked immunosorbent assay (ELISA) to detect the filarial-specific antibodies in various categories of filarial sera samples against recombinant WbL1 (rWbL1) protein...
October 15, 2018: Transactions of the Royal Society of Tropical Medicine and Hygiene
Jane Harper, Katherine J Adams, Giovanna Bossi, Debbie E Wright, Andrea R Stacey, Nicole Bedke, Ruth Martinez-Hague, Dan Blat, Laure Humbert, Hazel Buchanan, Gabrielle S Le Provost, Zoe Donnellan, Ricardo J Carreira, Samantha J Paston, Luise U Weigand, Martina Canestraro, Joseph P Sanderson, Sophie Botta Gordon-Smith, Kate L Lowe, Karolina A Rygiel, Alex S Powlesland, Annelise Vuidepot, Namir J Hassan, Brian J Cameron, Bent K Jakobsen, Joseph Dukes
Robust preclinical testing is essential to predict clinical safety and efficacy and provide data to determine safe dose for first-in-man studies. There are a growing number of examples where the preclinical development of drugs failed to adequately predict clinical adverse events in part due to their assessment with inappropriate preclinical models. Preclinical investigations of T cell receptor (TCR)-based immunotherapies prove particularly challenging as these biologics are human-specific and thus the conventional testing in animal models is inadequate...
2018: PloS One
Ya Chen, Xia Yuan, Zhangping Xiao, Hongwei Jin, Liangren Zhang, Zhenming Liu
Multidrug resistance protein 4 (MRP4/ABCC4) is an ATP-binding cassette (ABC) transporter. It is associated with multidrug resistance (MDR), which is becoming a growing challenge to the treatment of cancer and infections. In the context of several types of cancer in which MRP4 is overexpressed, MRP4 inhibition manifests striking effects against cancer progression and drug resistance. In this study, we combined ligand-based and structure-based drug design strategy, by searching the SPECS chemical library to find compounds that are most likely to bind to MRP4...
2018: PloS One
Kamila Anna Meissner, Thales Kronenberger, Vinícius Gonçalves Maltarollo, Gustavo Henrique Goulart Trossini, Carsten Wrenger
Malaria is a devastating disease depending only on chemotherapy as treatment. However, medication is losing efficacy and therefore there is an urgent need for the discovery of novel pharmaceutics. Recently plasmepsin V, an aspartic protease anchored in the endoplasmatic reticulum, was demonstrated as responsible for the trafficking of parasite-derived proteins to the erythrocytic surface and further validated as a drug target. In this sense, ligand-based virtual screening has been applied to design inhibitors that target plasmepsin V of P...
October 15, 2018: Chemical Biology & Drug Design
Michael Ronzetti, Bolormaa Baljinnyam, Adam Yasgar, Anton Simeonov
Drug plasma protein binding remains highly relevant to research and drug development, making the assessment and profiling of compound affinity to plasma proteins essential to drug discovery efforts. Although there are a number of fully-characterized methods, they lack the throughput to handle large numbers of compounds. As the evaluation of adsorption, distribution, metabolism, and excretion is addressed earlier in the drug development timeline, the need for higher-throughput methods has grown. Areas Covered: This review will highlight recent developments on methods for profiling drug plasma binding, with an emphasis on fluorescent probes and emerging high-throughput methodologies...
October 15, 2018: Expert Opinion on Drug Discovery
Bijan Pirnia, Ali Akbar Soleimani, Parastoo Malekanmehr, Kambiz Pirnia, Alireza Zahiroddin
Background: Topiramate facilitates gamma aminobutyric acid (GABA) transference and an ideal candidate for reducing cocaine use in methadone patients. The present study evaluated topiramate in Dual dependence on opiate and cocaine. Methods: This placebo-controlled study (Clinical Trial Registration Code: TCTR20170201001) conducted during the period 2013-2014, Cocaine-dependent individuals maintained on methadone (n=50) were randomized to receive topiramate or identical placebo capsules...
September 2018: Iranian Journal of Public Health
Ismet Sahin, Yu Zhang, Florencia McAllister
Tumor sphere quantification plays an important role in cancer research and drugs screening. Even though the number and size of tumor spheres can be found manually, this process is time-consuming, prone to making errors, and may not be viable when the number of images is very large. This manuscript presents a method for automated quantification of spheres with a novel segmentation technique. The segmentation method relies on initial watershed algorithm which detects the minima of the distance transform and finds a tumor sphere for each minimum...
2018: Journal of Molecular Imaging & Dynamics
Anjana Radhakrishnan, Christopher M Furze, Mohd Syed Ahangar, Elizabeth Fullam
One of the major obstacles to obtaining a complete structural and functional understanding of proteins encoded by the Mycobacterium tuberculosis ( Mtb ) pathogen is due to significant difficulties in producing recombinant mycobacterial proteins. Recent advances that have utilised the closely related Mycobacterium smegmatis species as a native host have been effective. Here we have developed a method for the rapid screening of both protein production and purification strategies of mycobacterial proteins in whole M...
September 27, 2018: RSC Advances
Weiwei Liu, Yajie Zhang, Weina Zhu, Chunhua Ma, Jie Ruan, Hongyan Long, Yue Wang
Rheumatoid arthritis (RA) is a chronic autoimmune inflammatory arthropathy associated with articular damage and attendant comorbidities. Even although RA treatment has advanced remarkably over the last decade, a significant proportion of patients still do not achieve sustained remission. The cause of RA is not yet known despite the many potential mechanisms proposed. It has been confirmed that RA is associated with dysregulated immune system and persistent inflammation. Therefore, management of inflammation is always the target of therapy...
2018: Frontiers in Immunology
Sara Castagnola, Sébastien Delhaye, Alessandra Folci, Agnès Paquet, Frédéric Brau, Fabrice Duprat, Marielle Jarjat, Mauro Grossi, Méline Béal, Stéphane Martin, Massimo Mantegazza, Barbara Bardoni, Thomas Maurin
Fragile X syndrome (FXS), the most common form of inherited intellectual disability (ID) and a leading cause of autism, results from the loss of expression of the Fmr1 gene which encodes the RNA-binding protein Fragile X Mental Retardation Protein (FMRP). Among the thousands mRNA targets of FMRP, numerous encode regulators of ion homeostasis. It has also been described that FMRP directly interacts with Ca2+ channels modulating their activity. Collectively these findings suggest that FMRP plays critical roles in Ca2+ homeostasis during nervous system development...
2018: Frontiers in Molecular Neuroscience
Brandy Henry
Despite the widespread use of the drug court model, standardized performance measures for drug courts are not uniformly utilized, and rarely include process measures. To ensure that drug courts are being implemented in the most effective manner, the use of performance measurement tools should be considered for wide scale adoption. Drug court effectiveness is moderated by participant characteristics, and is most effective for individuals with the highest substance use needs. Therefore, having quality clinical screening processes is crucial to ensuring that drug courts are serving the population for which they are effective...
2018: Criminal Justice Studies (Abingdon, England)
Jiyong Jian, Xinyu Yang, Jun Yang, Liang Chen
Background: The incidence of tuberculosis (TB), especially multidrug-resistant TB (MDR-TB) and extensively drug-resistant TB (XDR-TB), continues to increase alarmingly worldwide. Molecular line probe assays (LPAs) are endorsed by the World Health Organization for the fast detection of MDR-TB and XDR-TB. The aim of this study was to evaluate the performance of LPAs in China. Methods: We analyzed MDR-TB and XDR-TB in 96 isolates from Beijing by using culture-based drug susceptibility testing (DST) and LPAs to compare the detection rate of the two methods...
2018: Infection and Drug Resistance
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