A high-throughput assay for the determination of acyltransferase activity of lipase CAL-A

2013 ◽  
Vol 116 (2) ◽  
pp. 232-236 ◽  
Author(s):  
Janett Müller ◽  
Birte Fredrich ◽  
Christina Kohlmann ◽  
Lukas Maksym ◽  
Uwe T. Bornscheuer
Keyword(s):  
High Throughput ◽  
Acyltransferase Activity ◽  
High Throughput Assay

High throughput assay for the determination of piperaquine in plasma

2005 ◽  
Vol 39 (3-4) ◽  
pp. 601-605 ◽  
Author(s):  
N. Lindegårdh ◽  
N.J. White ◽  
N.P.J. Day
Keyword(s):  
High Throughput ◽  
High Throughput Assay

High throughput assay for the determination of lumefantrine in plasma

2005 ◽  
Vol 822 (1-2) ◽  
pp. 330-333 ◽  
Author(s):  
A. Annerberg ◽  
T. Singtoroj ◽  
P. Tipmanee ◽  
N.J. White ◽  
N.P.J. Day ◽  
...  
Keyword(s):  
High Throughput ◽  
High Throughput Assay

scholarly journals A fluorescence-based high throughput assay for the determination of small molecule−human serum albumin protein binding

2014 ◽  
Vol 406 (7) ◽  
pp. 1867-1875 ◽  
Author(s):  
Megan M. McCallum ◽  
Alan J. Pawlak ◽  
William R. Shadrick ◽  
Anton Simeonov ◽  
Ajit Jadhav ◽  
...  
Keyword(s):  
Human Serum Albumin ◽  
Serum Albumin ◽  
Protein Binding ◽  
Human Serum ◽  
Small Molecule ◽  
High Throughput ◽  
High Throughput Assay

scholarly journals Development of a High-Throughput Screening Assay to Identify Inhibitors of the SARS-CoV-2 Guanine-N7-Methyltransferase Using RapidFire Mass Spectrometry

2021 ◽  
pp. 247255522110006
Author(s):  
Lesley-Anne Pearson ◽  
Charlotte J. Green ◽  
De Lin ◽  
Alain-Pierre Petit ◽  
David W. Gray ◽  
...  
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Mutational Analysis ◽  
Nonstructural Protein ◽  
Translation Efficiency ◽  
Screening Assay ◽  
High Throughput Screening Assay ◽  
Starting Point ◽  
Approved Drugs ◽  
High Throughput Assay

Severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) represents a significant threat to human health. Despite its similarity to related coronaviruses, there are currently no specific treatments for COVID-19 infection, and therefore there is an urgent need to develop therapies for this and future coronavirus outbreaks. Formation of the cap at the 5′ end of viral RNA has been shown to help coronaviruses evade host defenses. Nonstructural protein 14 (nsp14) is responsible for N7-methylation of the cap guanosine in coronaviruses. This enzyme is highly conserved among coronaviruses and is a bifunctional protein with both N7-methyltransferase and 3′-5′ exonuclease activities that distinguish nsp14 from its human equivalent. Mutational analysis of SARS-CoV nsp14 highlighted its role in viral replication and translation efficiency of the viral genome. In this paper, we describe the characterization and development of a high-throughput assay for nsp14 utilizing RapidFire technology. The assay has been used to screen a library of 1771 Food and Drug Administration (FDA)-approved drugs. From this, we have validated nitazoxanide as a selective inhibitor of the methyltransferase activity of nsp14. Although modestly active, this compound could serve as a starting point for further optimization.

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