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Assay and Drug Development Technologies

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https://www.readbyqxmd.com/read/30106594/multiple-condition-analysis-in-a-retrievable-subcutaneous-animal-model-for-drug-screening-on-full-pancreatic-tissue-digest
#1
Tim W G M Spitters, Parker L Andersen, Chloé Martel, Patrick Vermette
The lack of understanding on how to treat pancreas-related diseases and develop new therapeutics is partly due to the unavailability of appropriate models. In vitro models fail to provide a physiological environment. Testing new drug targets in these models can give rise to bias and misleading results. Therefore, we developed an in vivo model for drug testing on full pancreatic digests, which maintains the interactions between endo- and exocrine tissues and allows retrieving the samples for further analyses...
August 14, 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/30106307/rational-druggability-investigation-toward-selection-of-lead-molecules-impact-of-the-commonly-used-spices-on-inflammatory-diseases
#2
Tara Zakerali, Sajad Shahbazi
Herbal remedies and phytochemicals have been used in traditional medicine. Most of the herbs used in human diet have some major effective elements that can affect various pathways in the human body and play a therapeutic role in healing disorders or diseases. Among the inflammatory diseases, worldwide common disorders possess well-known pathways that can be controlled by diet and behavior. There are some well-established targets that are used for anti-inflammatory drugs like cyclooxygenase type 1 and 2 (COX-1 and COX-2), lipoxygenase, prostaglandin D2 receptor, DP1, CRTH2, and so on...
August 14, 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29985634/interference-potential-of-tannins-and-chlorophylls-in-zebrafish-phenotypic-based-assays
#3
Norazwana Samat, Mei Fong Ng, Nur Faizah Ruslan, Kazuhide Shaun Okuda, Pei Jean Tan, Vyomesh Patel
Natural products are prolific producers of diverse chemical scaffolds, which have yielded several clinically useful drugs. However, the complex features of natural products present challenges for identifying bioactive molecules using high-throughput screens. For most assays, measured endpoints are either colorimetric or luminescence based. Thus, the presence of the major metabolites, tannins, and chlorophylls, in natural products could potentially interfere with these measurements to give either false-positive or false-negative hits...
July 9, 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/30148666/society-of-biomolecular-imaging-and-informatics-5-th-annual-meeting-program-september-18-20-2018
#4
(no author information available yet)
No abstract text is available yet for this article.
August 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/30148665/know-when-you-don-t-know-a-robust-deep-learning-approach-in-the-presence-of-unknown-phenotypes
#5
Oliver Dürr, Elvis Murina, Daniel Siegismund, Vasily Tolkachev, Stephan Steigele, Beate Sick
Deep convolutional neural networks show outstanding performance in image-based phenotype classification given that all existing phenotypes are presented during the training of the network. However, in real-world high-content screening (HCS) experiments, it is often impossible to know all phenotypes in advance. Moreover, novel phenotype discovery itself can be an HCS outcome of interest. This aspect of HCS is not yet covered by classical deep learning approaches. When presenting an image with a novel phenotype to a trained network, it fails to indicate a novelty discovery but assigns the image to a wrong phenotype...
August 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/30148664/high-content-imaging-approaches-to-quantitate-stress-induced-changes-in-nucleolar-morphology
#6
Jin-Shu He, Priscilla Soo, Maurits Evers, Kate M Parsons, Nadine Hein, Katherine M Hannan, Ross D Hannan, Amee J George
The nucleolus is a dynamic subnuclear compartment that has a number of different functions, but its primary role is to coordinate the production and assembly of ribosomes. For well over 100 years, pathologists have used changes in nucleolar number and size to stage diseases such as cancer. New information about the nucleolus' broader role within the cell is leading to the development of drugs which directly target its structure as therapies for disease. Traditionally, it has been difficult to develop high-throughput image analysis pipelines to measure nucleolar changes due to the broad range of morphologies observed...
August 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/30148663/society-of-biomolecular-imaging-and-informatics-special-issue
#7
Myles Fennell, Kaylene J Simpson
No abstract text is available yet for this article.
August 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/30109944/high-content-screening-campaign-to-identify-compounds-that-inhibit-or-disrupt-androgen-receptor-transcriptional-intermediary-factor-2-protein-protein-interactions-for-the-treatment-of-prostate-cancer
#8
Ashley T Fancher, Yun Hua, Daniel P Camarco, David A Close, Christopher J Strock, Paul A Johnston
Twenty percent of prostate cancer (PCa) patients develop a noncurable drug-resistant form of the disease termed castration-resistant prostate cancer (CRPC). Overexpression of Androgen Receptor (AR) coactivators such as transcriptional intermediary factor 2 (TIF2) is associated with poor CRPC patient outcomes. We describe the implementation of the AR-TIF2 protein-protein interaction biosensor (PPIB) assay in a high-content screening (HCS) campaign of 143,535 compounds. The assay performed robustly and reproducibly and enabled us to identify compounds that inhibited dihydrotestosterone (DHT)-induced AR-TIF2 protein-protein interaction (PPI) formation or disrupted preexisting AR-TIF2 PPIs...
August 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/30109941/perspective-sbi-2-at-its-fifth-annual-meeting
#9
Steven A Haney
No abstract text is available yet for this article.
August 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/30088945/improved-ire1-and-perk-pathway-sensors-for-multiplex-endoplasmic-reticulum-stress-assay-reveal-stress-response-to-nuclear-dyes-used-for-image-segmentation
#10
Adrien Nougarède, Chloé Tesnière, Jarkko Ylanko, Ruth Rimokh, Germain Gillet, David W Andrews
In response to a variety of insults the unfolded protein response (UPR) is a major cell program quickly engaged to promote either cell survival or if stress levels cannot be relieved, apoptosis. UPR relies on three major pathways, named from the endoplasmic reticulum (ER) resident proteins IRE1α, PERK, and ATF6 that mediate response. Current tools to measure the activation of these ER stress response pathways in mammalian cells are cumbersome and not compatible with high-throughput imaging. In this study, we present IRE1α and PERK sensors with improved sensitivity, based on the canonical events of xbp1 splicing and ATF4 translation at ORF3...
August 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/30070899/high-content-assay-multiplexing-for-muscle-toxicity-screening-in-human-induced-pluripotent-stem-cell-derived-skeletal-myoblasts
#11
William D Klaren, Ivan Rusyn
Skeletal muscle-associated toxicity is an underresearched area in the field of high-throughput toxicity screening; hence, the potential adverse effects of drugs and chemicals on skeletal muscle are largely unknown. Novel organotypic microphysiological in vitro models are being developed to replicate the contractile function of skeletal muscle; however, the throughput and a need for specialized equipment may limit the utility of these tissue chip models for screening. In addition, recent developments in stem cell biology have resulted in the generation of induced pluripotent stem cell (iPSC)-derived skeletal myoblasts that enable high-throughput in vitro screening...
August 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/30019946/identification-of-novel-structurally-diverse-small-molecule-modulators-of-gpr119
#12
Ainhoa Nieto, Virneliz Fernández-Vega, Timothy P Spicer, Emmanuel Sturchler, Pramisha Adhikari, Nicole Kennedy, Sean Mandat, Peter Chase, Louis Scampavia, Thomas Bannister, Peter Hodder, Patricia H McDonald
GPR119 drug discovery efforts in the pharmaceutical industry for the treatment of type 2 diabetes mellitus (T2DM) and obesity, were initiated based on its restricted distribution in pancreas and GI tract, and its possible role in glucose homeostasis. While a number of lead series have emerged, the pharmacological endpoints they provide have not been clear. In particular, many lead series have demonstrated loss of efficacy and significant toxic side effects. Thus, we sought to identify novel, potent, positive modulators of GPR119...
July 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/30019945/literature-search-and-review
#13
Aaron Wilson, John Concannon, Doug Auld
No abstract text is available yet for this article.
July 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/30019944/a-computational-study-on-the-blocking-ability-of-selected-commercially-available-anticancer-drugs-and-their-hypothetic-derivatives-on-the-ccr5
#14
Rahim Ghadari, Yousef Mohammadzadeh
Computational studies were done on the complexes between some commercially available anticancer drugs and their hypothetic derivatives and the CCR5 protein. At first step, the docking studies were done to obtain the best ligand that can inhibit the CCR5 protein. Based on the binding energy results obtained from the docking studies, 16 complexes were selected. Molecular dynamic studies were carried out on these structures and then molecular mechanics-generalized Born surface area calculations were done to find the binding energies of the ligands to the CCR5 protein...
July 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/30019943/drug-repurposing-and-artificial-intelligence-from-liaison-to-marriage
#15
Hermann A M Mucke
No abstract text is available yet for this article.
July 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/30019942/drug-repurposing-patent-applications-january-march-2018
#16
Hermann A M Mucke
No abstract text is available yet for this article.
July 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/30019941/drug-repurposing-patent-applications-october-december-2017
#17
Hermann A M Mucke
No abstract text is available yet for this article.
July 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29446984/anticancer-drugs-as-antibiofilm-agents-in-candida-albicans-potential-targets
#18
Archana Anandrao Wakharde, Shivkrupa Devrao Halbandge, Datta Baburao Phule, Sankunny Mohan Karuppayil
The human pathogen Candida albicans can grow as a biofilm on host tissues and on the surfaces of different prosthetic devices in a patient's body. Various studies have reported that biofilms formed by C. albicans are resistant to most of the currently used antibiotics including the widely prescribed drug, fluconazole. As such, novel strategies for the treatment of drug-resistant biofilms are required. Drug repositioning or the use of drugs outside their unique indication has the potential to radically change drug development...
July 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29878843/discovery-of-a-tin-piperonal-entecavir-schiff-base-compound-that-overcomes-multidrug-resistance-by-inhibiting-p-glycoprotein
#19
Rehmat Zaman, Ghazanfar Ali, Zeeshan Anjum, Muhammad Sajid, Muhammad Mumtaz Khan, Aziz Ahmad, Syed Rizwan Abbas, Wajid Rehman
The presence of P-glycoprotein in the human intestine represents a significant barrier to effective drug therapy. These proteins form a multidrug-resistant barrier to most drugs, especially those administered orally. Thus, strategies are needed to prepare molecules to combat these resistant proteins and enable an increase in drug efficacy. We developed a novel tin-Schiff base complex using an ultrasonic bath, a new technique in small molecule synthesis. New bond formation was confirmed using ultraviolet and Fourier transform spectroscopies...
May 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29874096/cholesterol-unbound-ror%C3%AE-t-protein-enables-a-sensitive-inverse-agonist-screening
#20
Ryokichi Koyama, Yasunori Fukuda, Yusuke Kamada, Hideyuki Nakagawa, Darbi Witmer, Geza Ambrus-Aikelin, Bi-Ching Sang, Masaharu Nakayama, Hidehisa Iwata
The retinoic acid-related orphan receptor gamma T (RORγt) plays an important role in Th17 cell proliferation and functionality. Thus, RORγt inverse agonists are thought to be potent therapeutic agents for Th17-mediated autoimmune diseases, such as rheumatoid arthritis, asthma, inflammatory bowel disease, and psoriasis. Although RORγt has constitutive activity, it is recognized that the receptor is physiologically regulated by various cholesterol derivatives. In this study, we sought to identify RORγt inverse agonists through a high-throughput screening campaign...
May 2018: Assay and Drug Development Technologies
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