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Assay and Drug Development Technologies

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https://read.qxmd.com/read/30624955/repositioning-tacrolimus-evaluation-of-the-effect-of-short-term-tacrolimus-treatment-on-osteoprogenitor-cells-and-primary-cells-for-bone-regenerative-engineering
#1
Edward O'Neill, Komal Rajpura, Erica J Carbone, Guleid Awale, Ho-Man Kan, Kevin W-H Lo
Small-molecule-based bone regenerative engineering is an encouraging strategy for repair and regeneration of skeletal tissue. Using osteogenic small molecules for engineering bone tissue has several potential benefits over polypeptide-based approaches. Interestingly, hundreds of such small molecules possess the capability to promote osteogenesis, and several of these are already approved by the FDA for use in other applications, indicating their safety for human use. However, the need for their use at a high frequency and/or duration, due to their short half-life and nonspecificity, is still problematic...
January 9, 2019: Assay and Drug Development Technologies
https://read.qxmd.com/read/30592624/high-content-screening-characterization-of-head-and-neck-squamous-cell-carcinoma-multicellular-tumor-spheroid-cultures-generated-in-384-well-ultra-low-attachment-plates-to-screen-for-better-cancer-drug-leads
#2
Stanton J Kochanek, David A Close, Paul A Johnston
Multicellular tumor spheroid (MCTS) cultures represent more physiologically relevant in vitro cell tumor models that recapitulate the microenvironments and cell-cell or cell-extracellular matrix interactions which occur in solid tumors. We characterized the morphologies, viability, and growth behaviors of MCTSs produced by 11 different head and neck squamous cell carcinoma (HNSCC) cell lines seeded into and cultured in ultra-low attachment microtiter plates (ULA-plates) over extended periods of time. HNSCC MCTS cultures developed microenvironments, which resulted in differences in proliferation rates, metabolic activity, and mitochondrial functional activity between cells located in the outer layers of the MCTS and cells in the interior...
December 28, 2018: Assay and Drug Development Technologies
https://read.qxmd.com/read/30575417/discovery-of-natural-steroid-5-alpha-reductase-inhibitors
#3
Jukkarin Srivilai, Genet Minale, C Norman Scholfield, Kornkanok Ingkaninan
Human steroid 5 alpha-reductases (S5αRs) and NADPH irreversibly reduce testosterone to the more potent dihydrotestosterone (DHT). S5αR inhibitors are useful treatments for DHT-dependent diseases, including benign prostatic hyperplasia, androgenic alopecia and hair growth, and acne. There are three S5αR isozymes, and there is a need for safer and more isozyme selective inhibitors than finasteride and dutasteride currently licensed. In this study, we review the methods used to screen for S5αR inhibitory activity and describe studies that characterize the ability of herbal preparations and their constituents to inhibit S5αRs...
December 21, 2018: Assay and Drug Development Technologies
https://read.qxmd.com/read/30481043/probing-mitochondrial-permeability-transition-pore-activity-in-nucleated-cells-and-platelets-by-high-throughput-screening-assays-suggests-involvement-of-protein-phosphatase-2b-in-mitochondrial-dynamics
#4
Mao Xiang Chen, Emma Ward, Matilde Caivano, Sandy Toh, Kirsten Searle, Sumitra Ramachandran, Yannick Lacroix, Mahmood Ahmed, A Richard Rutter
Mitochondrial permeability transition pore (mPTP) formation is well documented in isolated mitochondria. However, convincing detection of mPTP in whole cells remains elusive. In this study, we describe a high-throughput assay for Ca2+ -activated mPTP opening in platelets using HyperCyt flow cytometry. In addition, we demonstrate that in several nucleated cells, using multiple approaches, the detection of cyclophilin D-dependent mPTP opening is highly challenging. Results with the mitochondrial-targeted Ca2+ -sensing green fluorescent protein (mito-Case12) suggest the involvement of protein phosphatase 2B (PP2B; calcineurin) in regulating mitochondrial dynamics...
November 27, 2018: Assay and Drug Development Technologies
https://read.qxmd.com/read/30657704/society-of-biomolecular-imaging-and-informatics-special-issue
#5
Myles Fennell, Kaylene J Simpson
No abstract text is available yet for this article.
January 2019: Assay and Drug Development Technologies
https://read.qxmd.com/read/30657703/society-of-biomolecular-imaging-and-informatics-high-content-screening-high-content-analysis-preclinical-translational-imaging-colloquium-how-emerging-technologies-in-disease-models-high-content-imaging-and-data-analytics-are-changing-our-approach-to-drug-discovery
#6
https://read.qxmd.com/read/30657702/high-content-and-high-throughput-in-vivo-drug-screening-platforms-using-microfluidics
#7
Adela Ben-Yakar
The drug-discovery process is expensive and lengthy, and has been causing a rapid increase in the global health care cost. Despite extensive efforts, many human diseases still lack a cure. To improve the outcomes, there is a growing need to implement novel approaches into the early stages of the drug-discovery pipeline. A specific such effort has focused on the development of novel disease models such as cellular models (genetically modified cell lines, spheroids, and organoids) and whole-animal models (small animal models and genetically modified large animal models)...
January 2019: Assay and Drug Development Technologies
https://read.qxmd.com/read/30657701/macrophage-cytological-profiling-and-anti-inflammatory-drug-discovery
#8
Tannia A Lau, Walter M Bray, R Scott Lokey
Millions of people are affected by diseases and conditions related to the immune system. Unfortunately, our current supply of approved anti-inflammatory medicine is very limited and only treats a small fraction of inflammatory diseases. Nearly half of the drugs on the market today are natural products and natural product derivatives. The long-term objective of my research is to continue efforts toward the discovery of diverse chemical compounds and their mechanism of action (MOA) to inspire the next generation of novel therapeutics...
January 2019: Assay and Drug Development Technologies
https://read.qxmd.com/read/30427697/autism-spectrum-disorders-potential-neuro-psychopharmacotherapeutic-plant-based-drugs
#9
Kendy Eduardo Urdaneta, María Andrea Castillo, Nola Montiel, Neomar Semprún-Hernández, Nicola Antonucci, Dario Siniscalco
Over the years, scientific researches have validated the healing benefits of many psychopharmacotherapeutic plant-based drugs to ameliorate psychiatric disorders. In contrast, the use of chemical procedures to isolate and purify specific compounds from plants that have been used to treat autism spectrum disorders (ASDs) and its clinical features may contribute to improve the quality of life of many patients. Also, herbal pharmacological treatments could improve the core symptoms of autism with fewer side effects...
November 14, 2018: Assay and Drug Development Technologies
https://read.qxmd.com/read/30362814/drug-repurposing-patent-applications-july-september-2018
#10
Hermann A M Mucke
No abstract text is available yet for this article.
October 26, 2018: Assay and Drug Development Technologies
https://read.qxmd.com/read/30325673/alternative-pharmaceutical-formulation-for-oral-administration-of-rifampicin
#11
Priscila Cristina Bartolomeu Halicki, Gabriela Hädrich, Raphael Boschero, Laís Andrade Ferreira, Andrea von Groll, Pedro Eduardo Almeida da Silva, Cristiana Lima Dora, Daniela Fernandes Ramos
Tuberculosis (TB) is considered an emergency global public health, mainly due to the TB-HIV co-infection, bacillus dormancy stage, and emergence of resistant strains. In addition, the therapeutic toxicity and its pharmacokinetic interactions with other drugs may influence treatment non-compliance, low serum concentration of drugs, and, consequently, treatment failure. Strategies using nanotechnology represent a new tool for the therapy, since they are effective delivery systems due to the possibility of solubilization of hydrophobic compounds, enable the production of formulations for oral use, and, in addition, increase bioavailability of drugs...
October 16, 2018: Assay and Drug Development Technologies
https://read.qxmd.com/read/30339090/literature-search-and-review
#12
Anton Simeonov, Mindy I Davis, Doug Auld
No abstract text is available yet for this article.
October 2018: Assay and Drug Development Technologies
https://read.qxmd.com/read/30339089/drug-repurposing-patent-applications-april-june-2018
#13
Hermann A M Mucke
No abstract text is available yet for this article.
October 2018: Assay and Drug Development Technologies
https://read.qxmd.com/read/30307314/a-comparative-study-of-fluorescence-assays-in-screening-for-brd4
#14
Pia Hansson, Helen Boyd, Ian L Dale, Göran Dahl, Felix Nicolaus, Wayne Bowen, Klaus Doering, Colin Dunsmore, Graham Cotton, Helena Lindmark
Fluorescence assay technologies are commonly used in high-throughput screening because of their sensitivity and ease of use. Different technologies have their characteristics and the rationale for choosing one over the other can differ between projects because of factors such as availability of reagents, assay performance, and cost. Another important factor to consider is the assay susceptibility to artifacts, which is almost as important as the ability of the assay to pick up active compounds. Spending time and money on false positives or missing the opportunity to build chemistry around false negatives is something that every drug project tries to avoid...
October 2018: Assay and Drug Development Technologies
https://read.qxmd.com/read/30251873/a-pharmacochaperone-based-high-throughput-screening-assay-for-the-discovery-of-chemical-probes-of-orphan-receptors
#15
Camilo J Morfa, Daniel Bassoni, Andras Szabo, Danielle McAnally, Haleli Sharir, Becky L Hood, Stefan Vasile, Tom Wehrman, Jane Lamerdin, Layton H Smith
G-protein-coupled receptors (GPCRs) have varying and diverse physiological roles, transmitting signals from a range of stimuli, including light, chemicals, peptides, and mechanical forces. More than 130 GPCRs are orphan receptors (i.e., their endogenous ligands are unknown), representing a large untapped reservoir of potential therapeutic targets for pharmaceutical intervention in a variety of diseases. Current deorphanization approaches are slow, laborious, and usually require some in-depth knowledge about the receptor pharmacology...
October 2018: Assay and Drug Development Technologies
https://read.qxmd.com/read/30106594/multiple-condition-analysis-in-a-retrievable-subcutaneous-animal-model-for-drug-screening-on-full-pancreatic-tissue-digest
#16
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://read.qxmd.com/read/30106307/rational-druggability-investigation-toward-selection-of-lead-molecules-impact-of-the-commonly-used-spices-on-inflammatory-diseases
#17
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://read.qxmd.com/read/30148666/society-of-biomolecular-imaging-and-informatics-5-th-annual-meeting-program-september-18-20-2018
#18
(no author information available yet)
No abstract text is available yet for this article.
August 2018: Assay and Drug Development Technologies
https://read.qxmd.com/read/30148665/know-when-you-don-t-know-a-robust-deep-learning-approach-in-the-presence-of-unknown-phenotypes
#19
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://read.qxmd.com/read/30148664/high-content-imaging-approaches-to-quantitate-stress-induced-changes-in-nucleolar-morphology
#20
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
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