scholarly journals A High‐Throughput Mass Spectrometric Enzyme Activity Assay Enabling the Discovery of Cytochrome P450 Biocatalysts

2019 ◽  
Vol 131 (30) ◽  
pp. 10220-10225 ◽  
Author(s):  
Tristan de Rond ◽  
Jian Gao ◽  
Amin Zargar ◽  
Markus de Raad ◽  
Jack Cunha ◽  
...  
Keyword(s):  
Enzyme Activity ◽  
Cytochrome P450 ◽  
High Throughput ◽  
Mass Spectrometric ◽  
Activity Assay ◽  
Enzyme Activity Assay

scholarly journals A High‐Throughput Mass Spectrometric Enzyme Activity Assay Enabling the Discovery of Cytochrome P450 Biocatalysts

2019 ◽  
Vol 58 (30) ◽  
pp. 10114-10119 ◽  
Author(s):  
Tristan de Rond ◽  
Jian Gao ◽  
Amin Zargar ◽  
Markus de Raad ◽  
Jack Cunha ◽  
...  
Keyword(s):  
Enzyme Activity ◽  
Cytochrome P450 ◽  
High Throughput ◽  
Mass Spectrometric ◽  
Activity Assay ◽  
Enzyme Activity Assay

scholarly journals High-Throughput Scintillation Proximity Assay for Stearoyl-CoA Desaturase-1

2011 ◽  
Vol 16 (5) ◽  
pp. 506-517 ◽  
Author(s):  
Paul Tawa ◽  
Jean-Pierre Falgueyret ◽  
Sebastien Guiral ◽  
Elise Isabel ◽  
David A. Powell ◽  
...  
Keyword(s):  
Enzyme Activity ◽  
High Throughput ◽  
High Throughput Screening ◽  
Activity Assay ◽  
Enzyme Activity Assay ◽  
Scintillation Proximity Assay ◽  
Binding Characteristics ◽  
Obesity And Diabetes ◽  
High Throughput Screening Assay ◽  
Stearoyl Coa Desaturase

Stearoyl-CoA desaturase (SCD) catalyzes the synthesis of monounsaturated fatty acids and has been implicated in a number of disease states, including obesity and diabetes. To find small-molecule inhibitor leads, a high-throughput scintillation proximity assay (SPA) was developed using the hydrophobic binding characteristics of a glass microsphere scintillant bead to capture SCD1 from a crude lysate of recombinant SCD1 in Sf9 lysate coupled with the strong binding characteristics of an azetidine compound ([3H]AZE). The SPA assay was stable over 24 h and could detect compounds with micromolar to nanomolar potencies. A robust 1536-well high-throughput screening assay was developed with good signal-to-noise ratio (10:1) and excellent Z′ factor (0.8). A screening collection of 1.6 million compounds was screened at 11 µM, and approximately 7700 compounds were identified as initial hits, exhibiting at least 35% inhibition of [3H]AZE binding. Further screening and confirmation with an SCD enzyme activity assay led to a number of new structural leads for inhibition of the enzyme. The SPA assay complements the enzyme activity assay for SCD1 as a tool for the discovery of novel leads in drug discovery.

scholarly journals Acoustic deposition with NIMS as a high-throughput enzyme activity assay

2012 ◽  
Vol 403 (3) ◽  
pp. 707-711 ◽  
Author(s):  
Matthew Greving ◽  
Xiaoliang Cheng ◽  
Wolfgang Reindl ◽  
Benjamin Bowen ◽  
Kai Deng ◽  
...  
Keyword(s):  
Enzyme Activity ◽  
High Throughput ◽  
Activity Assay ◽  
Enzyme Activity Assay

Expression and Enzyme Activity Assay of pfu with Molecular Chaperone

2010 ◽  
Vol 31 (6) ◽  
pp. 499-503
Author(s):  
Hai-Jun ZHANG ◽  
Jun YANG ◽  
Xiao-Guang LIU ◽  
Xiang-Yang HU
Keyword(s):  
Enzyme Activity ◽  
Molecular Chaperone ◽  
Activity Assay ◽  
Enzyme Activity Assay

Impact of enzyme activity assay on indication in liver transplantation for ornithine transcarbamylase deficiency

2012 ◽  
Vol 105 (3) ◽  
pp. 404-407 ◽  
Author(s):  
Taiichi Wakiya ◽  
Yukihiro Sanada ◽  
Taizen Urahashi ◽  
Yoshiyuki Ihara ◽  
Naoya Yamada ◽  
...  
Keyword(s):  
Liver Transplantation ◽  
Enzyme Activity ◽  
Ornithine Transcarbamylase ◽  
Ornithine Transcarbamylase Deficiency ◽  
Activity Assay ◽  
Enzyme Activity Assay
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