894 results match your criteria Assay and drug development technologies[Journal]


Quantitative Size-Based Analysis of Tumor Spheroids and Responses to Therapeutics.

Assay Drug Dev Technol 2019 Apr;17(3):140-149

1 Department of Biomedical Engineering and The University of Akron, Akron, Ohio.

Drug resistance remains a major clinical problem despite advances in targeted therapies. In recent years, methods to culture cancer cells in three-dimensional (3D) environments to better mimic native tumors have gained increasing popularity. Nevertheless, unlike traditional two-dimensional (2D) cell cultures, analysis of 3D cultures is not straightforward. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.895DOI Listing
April 2019
1 Read
2.075 Impact Factor

High-Throughput Three-Dimensional Hydrogel Cell Encapsulation Assay for Measuring Matrix Metalloproteinase Activity.

Assay Drug Dev Technol 2019 Apr;17(3):100-115

1 Department of Biomedical Engineering, The Ohio State University, Columbus, Ohio.

Three-dimensional (3D) cell culture systems more closely mimic the in vivo cellular microenvironment than traditional two-dimensional cell culture methods, making them a valuable tool in drug screening assays. However, 3D environments often make analysis of cellular responses more difficult, so most high-throughput (HT) 3D assays have been limited to measurements of cell viability. Yet, many other cell functions contribute to disease and are important pharmacological targets. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.877DOI Listing
April 2019
3 Reads

High-Throughput Zika Viral Titer Assay for Rapid Screening of Antiviral Drugs.

Assay Drug Dev Technol 2019 Apr;17(3):128-139

2 National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, Maryland.

Zika virus has recently emerged as a worldwide pathogen and public health burden due to its rapid spread and identification as a causative agent for multiple neurological defects, including congenital microcephaly. While there has been a flurry of recent research to address this emerging pathogen, there are currently no approved drug treatments for ZIKV infection. The gold standard for testing antiviral activity is to quantify infectious virion production. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.881DOI Listing
April 2019
1 Read

Technology for Discovery of Antifibrotic Drugs: Phenotypic Screening for LARP6 Inhibitors Using Inverted Yeast Three Hybrid System.

Assay Drug Dev Technol 2019 Apr 22;17(3):116-127. Epub 2019 Mar 22.

1 Department of Biomedical Sciences, College of Medicine, Florida State University, Tallahassee, Florida.

Fibrosis is defined by excessive production of type I collagen in various organs. Excessive type I collagen production in fibrosis is stimulated by binding of RNA protein LARP6 to the structural element of collagen mRNAs, the 5' stem loop (5'SL). The LARP6-dependent regulation is specific for type I collagen and critical for fibrosis development. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.904DOI Listing
April 2019
1 Read

Literature Search and Review.

Assay Drug Dev Technol 2019 Feb/Mar;17(2):37-43

2 Novartis Institutes for BioMedical Research, Cambridge, Massachusetts.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2019.29087.litDOI Listing

In Silico Screening to Identify Inhibitors of Growth Factor Receptor 2-Focal Adhesion Kinase Interaction for Therapeutic Treatment of Pathological Cardiac Hypertrophy.

Assay Drug Dev Technol 2019 Feb/Mar;17(2):58-67

Computational and Structural Biology Laboratory, Division of Biological Sciences and Engineering, Netaji Subhas University of Technology, Dwarka, India.

The focal adhesion kinase-growth factor receptor 2 (FAK-Grb2) protein-protein interaction is implicated in pathogenesis of stress-induced cardiac hypertrophy. The focal adhesion targeting (FAT) domain of FAK unfolds to form a structural intermediate that interacts with a multibinding hot spot in the SH2 domain of Grb2. Disruption of the Grb2-FAT interaction is a therapeutic strategy for prevention of pathological cardiac hypertrophy. Read More

View Article

Download full-text PDF

Source
https://www.liebertpub.com/doi/10.1089/adt.2018.887
Publisher Site
http://dx.doi.org/10.1089/adt.2018.887DOI Listing
March 2019
3 Reads

Possible Antidiabetic and Antioxidative Activity of Hydro-Methanolic Extract of Musa balbisiana (Colla) Flower in Streptozotocin-Induced Diabetic Male Albino Wistar Strain Rat: A Genomic Approach.

Assay Drug Dev Technol 2019 Feb/Mar;17(2):68-76

Molecular Medicine and Nutrigenomics Research Laboratory, Department of Bio-Medical Laboratory Science and Management, Vidyasagar University, Midnapore, India.

The aim of the investigation was to search out the possible corrective effect of hydro-methanolic extract:: 3:2 of Musa balbisiana flower on streptozotocin (STZ)-induced diabetic male rat. In this concern, glycemic profile, oxidative stress profile, lipid profile, and toxicity profile were studied where a genomic approach has been taken to explain the mechanism of action of the said extract for such recovery. Such enzyme kinetics domain and genomic domain of concerned profile were not covered till now to explore the mechanism of diabetes management by this plant part. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.889DOI Listing

Electrophysiological and Pharmacological Characterization of Human Inwardly Rectifying K2.1 Channels on an Automated Patch-Clamp Platform.

Assay Drug Dev Technol 2019 Apr 5;17(3):89-99. Epub 2019 Mar 5.

1 Integrated Drug Discovery, High-Content Biology, Sanofi Research and Development, Vitry-sur-Seine, France.

Inwardly rectifying I potassium currents of the heart control the resting membrane potential of ventricular cardiomyocytes during diastole and contribute to their repolarization after each action potential. Mutations in the gene encoding K2.1 channels, which primarily conduct ventricular I, are associated with inheritable forms of arrhythmias and sudden cardiac death. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.882DOI Listing
April 2019
3 Reads

Repositioning of Itraconazole for the Management of Ocular Neovascularization Through Surface-Modified Nanostructured Lipid Carriers.

Assay Drug Dev Technol 2019 Mar 5. Epub 2019 Mar 5.

4 School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, India.

Retinopathy is one of the most common complications of diabetes. Approximately 80% of patients with diabetes history for over 10 years suffer from some degree of diabetic retinopathy (DR). Currently available treatments include use of antivascular endothelial growth factor-165 (VEGF) agents or steroids. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.898DOI Listing
March 2019
1 Read

Society of Biomolecular Imaging and Informatics Special Issue.

Assay Drug Dev Technol 2019 Jan;17(1):1-2

2 Peter MacCallum Cancer Centre, Melbourne, Australia.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.29086.sbi2DOI Listing
January 2019
1 Read

High-Content and High-Throughput In Vivo Drug Screening Platforms Using Microfluidics.

Authors:
Adela Ben-Yakar

Assay Drug Dev Technol 2019 Jan;17(1):8-13

Department of Mechanical Engineering, The University of Texas at Austin, Austin, Texas.

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.908DOI Listing
January 2019
20 Reads

Macrophage Cytological Profiling and Anti-Inflammatory Drug Discovery.

Assay Drug Dev Technol 2019 Jan;17(1):14-16

Department of Chemistry and Biochemistry, University of California Santa Cruz, Santa Cruz, California.

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. Read More

View Article

Download full-text PDF

Source
https://www.liebertpub.com/doi/10.1089/adt.2018.894
Publisher Site
http://dx.doi.org/10.1089/adt.2018.894DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6352509PMC
January 2019
10 Reads

Repositioning Tacrolimus: Evaluation of the Effect of Short-Term Tacrolimus Treatment on Osteoprogenitor Cells and Primary Cells for Bone Regenerative Engineering.

Assay Drug Dev Technol 2019 Feb/Mar;17(2):77-88. Epub 2019 Jan 9.

1 Institute for Regenerative Engineering, University of Connecticut Health Center, School of Medicine, Farmington, Connecticut.

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.876DOI Listing
January 2019
1 Read

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.

Assay Drug Dev Technol 2019 Jan 28;17(1):17-36. Epub 2018 Dec 28.

1 Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh, Pittsburgh, Pennsylvania.

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. Read More

View Article

Download full-text PDF

Source
https://www.liebertpub.com/doi/10.1089/adt.2018.896
Publisher Site
http://dx.doi.org/10.1089/adt.2018.896DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6352515PMC
January 2019
8 Reads

Discovery of Natural Steroid 5 Alpha-Reductase Inhibitors.

Assay Drug Dev Technol 2019 Feb/Mar;17(2):44-57. Epub 2018 Dec 21.

2 Bioscreening Unit, Department of Pharmaceutical Chemistry and Pharmacognosy, Faculty of Pharmaceutical Sciences and Center of Excellence for Innovation in Chemistry, Naresuan University, Phitsanulok, Thailand.

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.870DOI Listing
December 2018
1 Read

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.

Assay Drug Dev Technol 2018 Dec 27;16(8):445-455. Epub 2018 Nov 27.

GlaxoSmithKline R&D , Stevenage, United Kingdom .

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 Ca-activated mPTP opening in platelets using HyperCyt flow cytometry. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.872DOI Listing
December 2018
2 Reads
2.075 Impact Factor

Autism Spectrum Disorders: Potential Neuro-Psychopharmacotherapeutic Plant-Based Drugs.

Assay Drug Dev Technol 2018 Nov 14. Epub 2018 Nov 14.

4 Department of Experimental Medicine, University of Campania , Naples, Italy .

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. Read More

View Article

Download full-text PDF

Source
https://www.liebertpub.com/doi/10.1089/adt.2018.848
Publisher Site
http://dx.doi.org/10.1089/adt.2018.848DOI Listing
November 2018
19 Reads

Drug Repurposing Patent Applications July-September 2018.

Assay Drug Dev Technol 2018 Oct 26. Epub 2018 Oct 26.

H.M. Pharma Consultancy , Wien, Austria .

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.29083.pq3DOI Listing
October 2018
1 Read

Literature Search and Review.

Assay Drug Dev Technol 2018 Oct;16(7):365-371

2 Novartis Institutes for BioMedical Research , Cambridge, Massachusetts.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.29082.litDOI Listing
October 2018
1 Read

Drug Repurposing Patent Applications April-June 2018.

Assay Drug Dev Technol 2018 Oct;16(7):420-426

H.M. Pharma Consultancy , Wien, Austria .

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.29081.pq2DOI Listing
October 2018
1 Read

Alternative Pharmaceutical Formulation for Oral Administration of Rifampicin.

Assay Drug Dev Technol 2018 Oct 16. Epub 2018 Oct 16.

1 Núcleo de Pesquisa em Microbiologia Médica, Faculdade de Medicina, Universidade Federal do Rio Grande-FURG , Rio Grande, Brazil .

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. Read More

View Article

Download full-text PDF

Source
https://www.liebertpub.com/doi/10.1089/adt.2018.874
Publisher Site
http://dx.doi.org/10.1089/adt.2018.874DOI Listing
October 2018
9 Reads

A Comparative Study of Fluorescence Assays in Screening for BRD4.

Assay Drug Dev Technol 2018 Oct 9;16(7):372-383. Epub 2018 Oct 9.

1 AstraZeneca R&D, Discovery Biology , Discovery Sciences, IMED Biotech Unit, AstraZeneca, Gothenburg, Sweden .

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. Read More

View Article

Download full-text PDF

Source
https://www.liebertpub.com/doi/10.1089/adt.2018.850
Publisher Site
http://dx.doi.org/10.1089/adt.2018.850DOI Listing
October 2018
3 Reads

A Pharmacochaperone-Based High-Throughput Screening Assay for the Discovery of Chemical Probes of Orphan Receptors.

Assay Drug Dev Technol 2018 Oct 22;16(7):384-396. Epub 2018 Sep 22.

1 Conrad Prebys Center for Chemical Genomics, Sanford Burnham Prebys Medical Discovery Institute at Lake Nona, Orlando, Florida.

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.868DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6207161PMC
October 2018
3 Reads

Society of Biomolecular Imaging and Informatics 5 Annual Meeting Program September 18-20, 2018.

Authors:

Assay Drug Dev Technol 2018 Aug/Sep;16(6):361-363

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.29079.programDOI Listing
August 2018
2 Reads

Know When You Don't Know: A Robust Deep Learning Approach in the Presence of Unknown Phenotypes.

Assay Drug Dev Technol 2018 Aug/Sep;16(6):343-349

1 Institute of Data Analysis and Process Design, ZHAW Winterthur , Winterthur, Switzerland .

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.859DOI Listing
August 2018
7 Reads

High-Content Imaging Approaches to Quantitate Stress-Induced Changes in Nucleolar Morphology.

Assay Drug Dev Technol 2018 Aug/Sep;16(6):320-332

1 ANU Centre for Therapeutic Discovery, The Australian National University , Acton, Australia .

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. Read More

View Article

Download full-text PDF

Source
https://www.liebertpub.com/doi/10.1089/adt.2018.861
Publisher Site
http://dx.doi.org/10.1089/adt.2018.861DOI Listing
August 2018
5 Reads

Society of Biomolecular Imaging and Informatics Special Issue.

Assay Drug Dev Technol 2018 Aug/Sep;16(6):289-290

2 Peter MacCallum Cancer Centre , Melbourne, Australia .

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.29080.ediDOI Listing
August 2018
2 Reads

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.

Assay Drug Dev Technol 2018 Aug/Sep;16(6):297-319. Epub 2018 Aug 15.

1 Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh , Pittsburgh, Pennsylvania.

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.858DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6114076PMC
August 2018
5 Reads

Perspective: SBI at Its Fifth Annual Meeting.

Authors:
Steven A Haney

Assay Drug Dev Technol 2018 Aug/Sep;16(6):291-296. Epub 2018 Aug 15.

Pharmaceutical Biotechnology Center, Indiana Biosciences Research Institute , Indianapolis, Indiana.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.878DOI Listing
August 2018
2 Reads

Multiple-Condition Analysis in a Retrievable Subcutaneous Animal Model for Drug Screening on Full Pancreatic Tissue Digest.

Assay Drug Dev Technol 2018 Aug 14. Epub 2018 Aug 14.

1 Laboratoire de bio-ingénierie et de biophysique de l'Université de Sherbrooke, Department of Chemical and Biotechnological Engineering, Université de Sherbrooke , Sherbrooke, Canada .

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.846DOI Listing
August 2018
2 Reads

Rational Druggability Investigation Toward Selection of Lead Molecules: Impact of the Commonly Used Spices on Inflammatory Diseases.

Assay Drug Dev Technol 2018 Oct 14;16(7):397-407. Epub 2018 Aug 14.

2 Department of Biotechnology, Panjab University , Chandigarh, India .

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.853DOI Listing
October 2018
3 Reads

Improved IRE1 and PERK Pathway Sensors for Multiplex Endoplasmic Reticulum Stress Assay Reveal Stress Response to Nuclear Dyes Used for Image Segmentation.

Assay Drug Dev Technol 2018 Aug/Sep;16(6):350-360. Epub 2018 Aug 8.

1 Biological Sciences Platform, Sunnybrook Research Institute , Sunnybrook Health Science Centre, Toronto, Ontario, Canada .

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. Read More

View Article

Download full-text PDF

Source
https://www.liebertpub.com/doi/10.1089/adt.2018.862
Publisher Site
http://dx.doi.org/10.1089/adt.2018.862DOI Listing
August 2018
25 Reads

High-Content Assay Multiplexing for Muscle Toxicity Screening in Human-Induced Pluripotent Stem Cell-Derived Skeletal Myoblasts.

Assay Drug Dev Technol 2018 Aug/Sep;16(6):333-342. Epub 2018 Aug 2.

Department of Veterinary Integrative Biosciences, Texas A&M University , College Station, Texas.

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.860DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6114077PMC
August 2018
5 Reads

Identification of Novel, Structurally Diverse, Small Molecule Modulators of GPR119.

Assay Drug Dev Technol 2018 Jul;16(5):278-288

1 Department of Molecular Medicine, The Scripps Research Institute , Jupiter, Florida.

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.849DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6065524PMC
July 2018
20 Reads
2.080 Impact Factor

Literature Search and Review.

Assay Drug Dev Technol 2018 Jul;16(5):260-265

Novartis Institutes for BioMedical Research , Cambridge, Massachusetts.

View Article

Download full-text PDF

Source
http://www.liebertpub.com/doi/10.1089/adt.2018.29075.lit
Publisher Site
http://dx.doi.org/10.1089/adt.2018.29075.litDOI Listing
July 2018
15 Reads

A Computational Study on the Blocking Ability of Selected Commercially Available Anticancer Drugs and Their Hypothetic Derivatives on the CCR5.

Assay Drug Dev Technol 2018 Jul;16(5):266-277

Computational Chemistry Laboratory, Department of Organic and Biochemistry, Faculty of Chemistry, University of Tabriz , Tabriz, Iran .

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2017.836DOI Listing
July 2018
4 Reads

Drug Repurposing and Artificial Intelligence: From Liaison to Marriage.

Assay Drug Dev Technol 2018 Jul;16(5):231

Editor, Drug Repurposing, Rescue, and Repositioning (DRRR) Advisory Board.

View Article

Download full-text PDF

Source
http://www.liebertpub.com/doi/10.1089/adt.2018.29078.edi
Publisher Site
http://dx.doi.org/10.1089/adt.2018.29078.ediDOI Listing
July 2018
7 Reads

Drug Repurposing Patent Applications January-March 2018.

Assay Drug Dev Technol 2018 Jul;16(5):253-259

H.M. Pharma Consultancy , Wien, Austria .

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.29077.pq1DOI Listing
July 2018
3 Reads

Drug Repurposing Patent Applications October-December 2017.

Assay Drug Dev Technol 2018 Jul;16(5):247-252

H.M. Pharma Consultancy , Wien, Austria .

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.29076.pq4DOI Listing
July 2018
3 Reads

Interference Potential of Tannins and Chlorophylls in Zebrafish Phenotypic-Based Assays.

Assay Drug Dev Technol 2018 Oct 9;16(7):408-419. Epub 2018 Jul 9.

Cancer Research Malaysia , Subang Jaya, Selangor, Malaysia .

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. Read More

View Article

Download full-text PDF

Source
https://www.liebertpub.com/doi/10.1089/adt.2017.833
Publisher Site
http://dx.doi.org/10.1089/adt.2017.833DOI Listing
October 2018
7 Reads

Discovery of a Tin-Piperonal-Entecavir Schiff Base Compound That Overcomes Multidrug Resistance by Inhibiting P-Glycoprotein.

Assay Drug Dev Technol 2018 May/Jun;16(4):205-211. Epub 2018 Jun 7.

4 Department of Chemistry, Hazara University , Mansehra, Pakistan .

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.844DOI Listing
June 2018
4 Reads
2.075 Impact Factor

Cholesterol Unbound RORγt Protein Enables a Sensitive Inverse Agonist Screening.

Assay Drug Dev Technol 2018 May/Jun;16(4):194-204. Epub 2018 Jun 6.

1 Biomolecular Research Laboratories, Pharmaceutical Research Division, Takeda Pharmaceutical Company Limited , Fujisawa, Japan .

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. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.852DOI Listing
June 2018
9 Reads

Engineered EF-Tu and tRNA-Based FRET Screening Assay to Find Inhibitors of Protein Synthesis in Bacteria.

Assay Drug Dev Technol 2018 May/Jun;16(4):212-221. Epub 2018 Jun 5.

Department of Microbiology, Biochemistry and Molecular Genetics, Rutgers New Jersey Medical School , Newark, New Jersey.

Antibiotic-resistant infections that do not respond to available drugs are becoming more common. Methicillin-resistant Staphylococcus aureus, carbapenem-resistant enterobacteria ("superbugs"), and many others pose a continuous threat to public health. To provide tools to combat such deadly infections, we present in this study a homogeneous assay focused on an insufficiently addressed molecular interaction linked to ribosomal translation. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.843DOI Listing
June 2018
3 Reads
2.080 Impact Factor

Changes on the Horizon for Drug Repurposing, Rescue, and Repositioning at ASSAY.

Assay Drug Dev Technol 2018 May/Jun;16(4):193. Epub 2018 Jun 5.

2 Editor, Drug Repurposing, Rescue, and Repositioning (DRRR) Advisory Board.

View Article

Download full-text PDF

Source
http://www.liebertpub.com/doi/10.1089/adt.2018.29074.edi
Publisher Site
http://dx.doi.org/10.1089/adt.2018.29074.ediDOI Listing
June 2018
8 Reads

Human Induced Pluripotent Stem Cell-Derived Cardiomyocytes Reveal Bradycardiac Effects Caused by Co-Administration of Sofosbuvir and Amiodarone.

Assay Drug Dev Technol 2018 May/Jun;16(4):222-229. Epub 2018 May 30.

1 Guangdong-Hongkong-Macau Institute of CNS Regeneration, Ministry of Education CNS Regeneration Collaborative Joint Laboratory, Jinan University , Guangzhou, China .

Co-administration of sofosbuvir, an anti-hepatitis C virus medication, and antiarrhythmic amiodarone causes symptomatic severe bradycardia in patients and animal models. However, in a few in vitro studies, the combination of sofosbuvir and amiodarone resulted in tachycardiac effects in human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs). This discrepancy may be attributable to the use of immature hiPSC-CMs in the in vitro studies. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2017.834DOI Listing
May 2018
8 Reads

High-Throughput Gene Expression Profiles to Define Drug Similarity and Predict Compound Activity.

Assay Drug Dev Technol 2018 Apr;16(3):162-176

1 Janssen Research & Development , A Division of Janssen Pharmaceutica NV, Computational Sciences, Discovery Sciences, Beerse, Belgium .

By adding biological information, beyond the chemical properties and desired effect of a compound, uncharted compound areas and connections can be explored. In this study, we add transcriptional information for 31K compounds of Janssen's primary screening deck, using the HT L1000 platform and assess (a) the transcriptional connection score for generating compound similarities, (b) machine learning algorithms for generating target activity predictions, and (c) the scaffold hopping potential of the resulting hits. We demonstrate that the transcriptional connection score is best computed from the significant genes only and should be interpreted within its confidence interval for which we provide the stats. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.845DOI Listing
April 2018
8 Reads

A High-Throughput Time-Resolved Fluorescence Energy Transfer Assay to Screen for Modulators of RGS7/Gβ5/R7BP Complex.

Assay Drug Dev Technol 2018 Apr;16(3):150-161

1 Department of Neuroscience, The Scripps Research Institute , Jupiter, Florida.

G protein-coupled receptors (GPCRs) are excellent drug targets exploited by majority of the Food and Drug Administration-approved medications, but when modulated, are often accompanied by significant adverse effects. Targeting of other elements in GPCR pathways for improved safety and efficacy is thus an unmet need. The strength of GPCR signaling is tightly regulated by regulators of G protein signaling (RGS) proteins, making them attractive drug targets. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2017.839DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5906730PMC
April 2018
7 Reads

Effect of 2-Phenylethanol as Antifungal Agent and Common Antifungals (Amphotericin B, Fluconazole, and Itraconazole) on Candida Species Isolated from Chronic and Recurrent Cases of Candidal Vulvovaginitis.

Assay Drug Dev Technol 2018 Apr;16(3):141-149

2 Department of Medical Parasitology and Mycology, School of Medicine, Iran University of Medical Sciences , Tehran, Iran .

The antifungal effects of 2-phenylethanol are clearly visible through its intervention in Candida morphogenesis. Chronic and recurrent vulvovaginitis, however, does not respond to this standard experimental therapy; therefore, the study presented in this article investigated the effect of common antifungal drugs (amphotericin B [AMB], fluconazole [FLU], and itraconazole [ITC]), in combination with 2-phenylethanol, on the Candida species isolated from cases of chronic and recurrent vulvovaginitis, thereby allowing the recommendation of a more appropriate treatment option. Forty isolates from patients with chronic and recurrent vaginal candidiasis were investigated in this experimental study. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2017.837DOI Listing
April 2018
7 Reads

Literature Search and Review.

Assay Drug Dev Technol 2018 Apr;16(3):133-140

2 Novartis Institutes for BioMedical Research , Cambridge, Massachusetts.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/adt.2018.29073.litDOI Listing
April 2018
4 Reads