scholarly journals A biotechnological approach for the development of new antifungal compounds to protect the environment and the human health

2015 ◽  
Vol 4 (3) ◽  
Author(s):  
Claudia Zani ◽  
Francesco Maria Restivo ◽  
Mauro Carcelli ◽  
Donatella Feretti ◽  
Giorgio Pelosi ◽  
...  
Keyword(s):  
Human Health ◽  
High Throughput ◽  
High Throughput Screening ◽  
Animal Feed ◽  
Po Valley ◽  
Biotechnological Approach ◽  
Relevant Role ◽  
Food Economy ◽  
Set Up ◽  
New Compounds

<em>Background</em>. In the Po Valley aflatoxins play a relevant role: the local food economy is heavily based on cereal cultivations for animal feed and human nutrition. Aims of this project are the identification of new compounds that inhibit <em>Aspergillus</em> proliferation, the development of new inhibitors of aflatoxins production, and the set-up a practical screening procedure to identify the most effective and safe compounds. <br /><em>Design and Methods.</em> New compounds will be synthetized with natural origin molecules as ligands and endogenous metal ions to increase their bioavailability for the fungi as metal complexes. A biotechnological high-throughput screening will be set up to identify efficiently the most powerful substances. The newly synthesized compounds with effective antifungal activities, will be evaluated with battery of tests with different end-points to assess the toxic potential risk for environmental and human health. <br /><em>Expected impact of the study for public health.</em> The fundamental step in the project will be the synthesis of new compounds and the study of their capability to inhibit aflatoxin biosynthesis. A new, simple, inexpensive and high-throughput method to screen the anti-fungine and anti-mycotoxin activity of the new synthesised compounds will be applied. The evaluation of possible risks for humans due to toxic and genotoxic activities of the molecules will be made with a new approach using different types of cells (bacteria, plants and human cells).

A high‐throughput screening method for determination of multi‐antibiotics in animal feed

2019 ◽  
Vol 42 (18) ◽  
pp. 2968-2976 ◽  
Author(s):  
Mingrong Qian ◽  
Xiaoming Zhang ◽  
Huiyu Zhao ◽  
Xiaofeng Ji ◽  
Xiaodan Li ◽  
...  
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Animal Feed ◽  
Screening Method

scholarly journals Assay Concordance between SPA and TR-FRET in High-Throughput Screening

2006 ◽  
Vol 11 (6) ◽  
pp. 606-616 ◽  
Author(s):  
Oliver Von Ahsen ◽  
Anne Schmidt ◽  
Monika Klotz ◽  
Karsten Parczyk
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Statistical Significance ◽  
Resonance Energy Transfer ◽  
Resonance Energy ◽  
Time Resolved ◽  
Detection Technology ◽  
Significant Difference ◽  
Set Up ◽  
Detection Technologies

High-throughput screening (HTS) of large chemical libraries has become the main source of new lead compounds for drug development. Several specialized detection technologies have been developed to facilitate the cost- and time-efficient screening of millions of compounds. However, concerns have been raised, claiming that different HTS technologies may produce different hits, thus limiting trust in the reliability of HTS data. This study was aimed to investigate the reliability of the authors most frequently used assay techniques: scintillation proximity assay (SPA) and homogeneous time-resolved fluorescence resonance energy transfer (TR-FRET). To investigate the data concordance between these 2 detection technologies, the authors screened a large subset of the Schering compound library consisting of 300,000 compounds for inhibitors of a nonreceptor tyrosine kinase. They chose to set up this study in realistic HTS scale to ensure statistical significance of the results. The findings clearly demonstrate that the choice of detection technology has no significant impact on hit finding, provided that assays are biochemically equivalent. Data concordance is up to 90%. The little differences in hit findings are caused by threshold setting but not by systematic differences between the technologies. The most significant difference between the compared techniques is that in the SPA format, more false-positive primary hits were obtained.

High throughput screening to identify new compounds with proapoptotic activity in resistant lung cancer cells

2015 ◽  
Vol 32 (3) ◽  
pp. 324
Author(s):  
P. Gilson ◽  
L. Vanwonterghem ◽  
F. Mahuteau ◽  
S. Piguel ◽  
J.L. Coll ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Cancer Cells ◽  
High Throughput ◽  
High Throughput Screening ◽  
Lung Cancer Cells ◽  
New Compounds

scholarly journals Using In Vitro High-Throughput Screening Data for Predicting Benzo[k]Fluoranthene Human Health Hazards

Risk Analysis ◽  
2016 ◽  
Vol 37 (2) ◽  
pp. 280-290 ◽  
Author(s):  
Lyle D. Burgoon ◽  
Ingrid L. Druwe ◽  
Kyle Painter ◽  
Erin E. Yost
Keyword(s):  
Human Health ◽  
High Throughput ◽  
High Throughput Screening ◽  
Health Hazards

scholarly journals PubChem BioAssay: A Decade’s Development toward Open High-Throughput Screening Data Sharing

2017 ◽  
Vol 22 (6) ◽  
pp. 655-666 ◽  
Author(s):  
Yanli Wang ◽  
Tiejun Cheng ◽  
Stephen H. Bryant
Keyword(s):  
Data Sharing ◽  
High Throughput ◽  
High Throughput Screening ◽  
Technology Development ◽  
Information Access ◽  
Biological Data ◽  
Information Platform ◽  
Chemical Structures ◽  
Data Content ◽  
Set Up

High-throughput screening (HTS) is now routinely conducted for drug discovery by both pharmaceutical companies and screening centers at academic institutions and universities. Rapid advance in assay development, robot automation, and computer technology has led to the generation of terabytes of data in screening laboratories. Despite the technology development toward HTS productivity, fewer efforts were devoted to HTS data integration and sharing. As a result, the huge amount of HTS data was rarely made available to the public. To fill this gap, the PubChem BioAssay database ( https://www.ncbi.nlm.nih.gov/pcassay/ ) was set up in 2004 to provide open access to the screening results tested on chemicals and RNAi reagents. With more than 10 years’ development and contributions from the community, PubChem has now become the largest public repository for chemical structures and biological data, which provides an information platform to worldwide researchers supporting drug development, medicinal chemistry study, and chemical biology research. This work presents a review of the HTS data content in the PubChem BioAssay database and the progress of data deposition to stimulate knowledge discovery and data sharing. It also provides a description of the database’s data standard and basic utilities facilitating information access and use for new users.

The Future of High-Throughput Screening

2008 ◽  
Vol 13 (6) ◽  
pp. 443-448 ◽  
Author(s):  
Lorenz M. Mayr ◽  
Peter Fuerst
Keyword(s):  
Drug Discovery ◽  
High Throughput ◽  
High Throughput Screening ◽  
Biological Data ◽  
Steady Increase ◽  
Continuous Change ◽  
Lead Discovery ◽  
The Past ◽  
Basic And Applied Research ◽  
Set Up

High-throughput screening (HTS) is a well-established process in lead discovery for pharma and biotech companies and is now also being set up for basic and applied research in academia and some research hospitals. Since its first advent in the early to mid-1990s, the field of HTS has seen not only a continuous change in technology and processes but also an adaptation to various needs in lead discovery. HTS has now evolved into a quite mature discipline of modern drug discovery. Whereas in previous years, much emphasis has been put toward a steady increase in capacity (“quantitative increase”) via various strategies in the fields of automation and miniaturization, the past years have seen a steady shift toward higher content and quality (“quality increase”) for these biological test systems. Today, many experts in the field see HTS at the crossroads with the need to decide either toward further increase in throughput or more focus toward relevance of biological data. In this article, the authors describe the development of HTS over the past decade and point out their own ideas for future directions of HTS in biomedical research. They predict that the trend toward further miniaturization will slow down with the implementation of 384-well, 1536-well, and 384 low-volume-well plates. The authors predict that, ultimately, each hit-finding strategy will be much more project related, tailor-made, and better integrated into the broader drug discovery efforts. ( Journal of Biomolecular Screening 2008:443-448)

scholarly journals Discovery of New Compounds Active against Plasmodium falciparum by High Throughput Screening of Microbial Natural Products

PLoS ONE ◽  
2016 ◽  
Vol 11 (1) ◽  
pp. e0145812 ◽  
Author(s):  
Guiomar Pérez-Moreno ◽  
Juan Cantizani ◽  
Paula Sánchez-Carrasco ◽  
Luis Miguel Ruiz-Pérez ◽  
Jesús Martín ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Natural Products ◽  
High Throughput ◽  
High Throughput Screening ◽  
New Compounds ◽  
Microbial Natural Products

scholarly journals Set-Up and Validation of a High Throughput Screening Method for Human Monoacylglycerol Lipase (MAGL) Based on a New Red Fluorescent Probe

Molecules ◽  
2019 ◽  
Vol 24 (12) ◽  
pp. 2241 ◽  
Author(s):  
Matteo Miceli ◽  
Silvana Casati ◽  
Roberta Ottria ◽  
Simone Di Leo ◽  
Ivano Eberini ◽  
...  
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Low Cost ◽  
Screening Method ◽  
Endocannabinoid System ◽  
Accurate Method ◽  
Monoacylglycerol Lipase ◽  
Serine Hydrolase ◽  
Lead Compounds ◽  
Set Up

Monoacylglycerol lipase (MAGL) is a serine hydrolase that has a key regulatory role in controlling the levels of 2-arachidonoylglycerol (2-AG), the main signaling molecule in the endocannabinoid system. Identification of selective modulators of MAGL enables both to provide new tools for investigating pathophysiological roles of 2-AG, and to discover new lead compounds for drug design. The development of sensitive and reliable methods is crucial to evaluate this modulatory activity. In the current study, we report readily synthesized long-wavelength putative fluorogenic substrates with different acylic side chains to find a new probe for MAGL activity. 7-Hydroxyresorufinyl octanoate proved to be the best substrate thanks to the highest rate of hydrolysis and the best Km and Vmax values. In addition, in silico evaluation of substrates interaction with the active site of MAGL confirms octanoate resorufine derivative as the molecule of choice. The well-known MAGL inhibitors URB602 and methyl arachidonylfluorophosphonate (MAFP) were used for the assay validation. The assay was highly reproducible with an overall average Z′ value of 0.86. The fast, sensitive and accurate method described in this study is suitable for low-cost high-throughput screening (HTS) of MAGL modulators and is a powerful new tool for studying MAGL activity.

scholarly journals High-Throughput Screening for Ion Channel Modulators

2002 ◽  
Vol 7 (5) ◽  
pp. 460-465 ◽  
Author(s):  
Margaret Falconer ◽  
Fiona Smith ◽  
Sandha Surah-Narwal ◽  
Gill Congrave ◽  
Zhen Liu ◽  
...  
Keyword(s):  
Ion Channels ◽  
Ion Channel ◽  
High Throughput ◽  
High Throughput Screening ◽  
Resonance Energy Transfer ◽  
Resonance Energy ◽  
Pharmacological Characterization ◽  
Core System ◽  
Set Up ◽  
Ion Channel Modulators

Ion channels present a group of targets for major clinical indications, which have been difficult to address due to the lack of suitable rapid but biologically significant methodologies. To address the need for increased throughput in primary screening, the authors have set up a Beckman/Sagian core system to fully automate functional fluorescence-based assays that measure ion channel function. They apply voltage-sensitive fluorescent probes, and the activity of channels is monitored using Aurora's Voltage/Ion Probe Reader (VIPR). The system provides a platform for fully automated high-throughput screening as well as pharmacological characterization of ion channel modulators. The application of voltage-sensitive fluorescence dyes coupled with fluorescence resonance energy transfer is the basis of robust assays, which can be adapted to the study of a variety of ion channels to screen for both inhibitors and activators of voltage-gated and other ion channels.

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