High-throughput screening

Cronk, David

doi:10.1016/b978-0-7020-4299-7.00008-1

Cited by 13 publications

(35 citation statements)

References 88 publications

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“…In the high-throughput screening process, large numbers of samples are screened, microplates having up to 3456 wells are generally used to hold the samples. Primarily, automation plays an essential role in the high-throughput screening process enabling millions of compounds to be rapidly screened in shorter time periods, as opposed to laboratory benchtop investigation of compounds by researchers in the same period [2,17].…”

Section: Breakthrough Technologies 41 Automation and Roboticsmentioning

confidence: 99%

Design and Implementation of High Throughput Screening Assays for Drug Discoveries

Bokhari¹,

Albukhari²

2022

High-Throughput Screening for Drug Discovery

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The process of drug discovery is challenging and a costly affair. It takes about 12 to 15 years and costs over $1 billion dollars to develop a new drug and introduce the finished product in the market. With the increase in diseases, virus spread, and patients, it has become essential to invent new medicines. Consequently, today researchers are becoming interested in inventing new medicines faster by adopting higher throughput screening methods. One avenue of approach to discovering drugs faster is the High-Throughput Screening (HTS) method, which has gained a lot of attention in the previous few years. Today, High-Throughput Screening (HTS) has become a standard method for discovering drugs in various pharmaceutical industries. This review focuses on the advancement of technologies in High-Throughput Screening (HTS) methods, namely fluorescence resonance energy transfer (FRET), biochemical assay, fluorescence polarization (FP), homogeneous time resolved fluorescence (HTRF), Fluorescence correlation spectroscopy (FCS), Fluorescence intensity distribution analysis (FIDA), Nuclear magnetic resonance (NMR), and research advances in three major technology areas including miniaturization, automation and robotics, and artificial intelligence, which promises to help speed up the discovery of medicines and its development process.

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Section: Breakthrough Technologies 41 Automation and Roboticsmentioning

confidence: 99%

Design and Implementation of High Throughput Screening Assays for Drug Discoveries

Bokhari¹,

Albukhari²

2022

High-Throughput Screening for Drug Discovery

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“…This enhances the process of gathering information, for example Rational Drug Design protocols (Rishton, 2003). Coupled with the current high performance of computational resources, High-throughput in silico methods for the study of interactions between several proteins and a single receptor paves the road for the development of pharmacological leads more efficiently (Cronk, 2013). Nevertheless, the problem resides when this study is performed on polyproteins.…”

Section: Introductionmentioning

confidence: 99%

Application of PolyPRep tools on HIV protease polyproteins using molecular docking

et al. 2024

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In recent years, the development of high-throughput technologies for obtaining sequence data leveraged the possibility of analysis of protein data in silico. However, when it comes to viral polyprotein interaction studies, there is a gap in the representation of those proteins, given their size and length. The prepare for studies using state-of-the-art techniques such as Machine Learning, a good representation of such proteins is a must. We present an alternative to this problem, implementing a fragmentation and modeling protocol to prepare those polyproteins in the form of peptide fragments. Such procedure is made by several scripts, implemented together on the workflow we call PolyPRep, a tool written in Python script and available in GitHub. This software is freely available only for noncommercial users.

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“…Therefore, screening and detection of glycosylation reactions is crucial in employing further applications. Moreover, screening that is prone to high-throughput involves miniaturization, automation, and rapid readouts of a specific question under study [23]. However, due to the lack of high-throughput and reliable assays available for plant UGTs further and additional applications remain elusive.…”

Section: Introductionmentioning

confidence: 99%

Comparative Analysis of High-Throughput Assays of Family-1 Plant Glycosyltransferases

McGraphery¹,

Schwab²

2020

IJMS

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The ability of glycosyltransferases (GTs) to reduce volatility, increase solubility, and thus alter the bioavailability of small molecules through glycosylation has attracted immense attention in pharmaceutical, nutraceutical, and cosmeceutical industries. The lack of GTs known and the scarcity of high-throughput (HTP) available methods, hinders the extrapolation of further novel applications. In this study, the applicability of new GT-assays suitable for HTP screening was tested and compared with regard to harmlessness, robustness, cost-effectiveness and reproducibility. The UDP-Glo GT-assay, Phosphate GT Activity assay, pH-sensitive GT-assay, and UDP2-TR-FRET assay were applied and tailored to plant UDP GTs (UGTs). Vitis vinifera (UGT72B27) GT was subjected to glycosylation reaction with various phenolics. Substrate screening and kinetic parameters were evaluated. The pH-sensitive assay and the UDP2-TR-FRET assay were incomparable and unsuitable for HTP plant GT-1 family UGT screening. Furthermore, the UDP-Glo GT-assay and the Phosphate GT Activity assay yielded closely similar and reproducible KM, vmax, and kcat values. Therefore, with the easy experimental set-up and rapid readout, the two assays are suitable for HTP screening and quantitative kinetic analysis of plant UGTs. This research sheds light on new and emerging HTP assays, which will allow for analysis of novel family-1 plant GTs and will uncover further applications.

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High-throughput screening

Cited by 13 publications

References 88 publications

Design and Implementation of High Throughput Screening Assays for Drug Discoveries

Design and Implementation of High Throughput Screening Assays for Drug Discoveries

Application of PolyPRep tools on HIV protease polyproteins using molecular docking

Comparative Analysis of High-Throughput Assays of Family-1 Plant Glycosyltransferases

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