scholarly journals Deploying Fluorescent Nucleoside Analogues for High‐Throughput Inhibitor Screening

ChemBioChem ◽  
2019 ◽  
Vol 21 (1-2) ◽  
pp. 108-112 ◽  
Author(s):  
Leah Seebald ◽  
Amaël G. E. Madec ◽  
Barbara Imperiali
2010 ◽  
Vol 15 (8) ◽  
pp. 1001-1007 ◽  
Author(s):  
Rakesh Rathore ◽  
Patrick Pribil ◽  
Jay J. Corr ◽  
William L. Seibel ◽  
Artem Evdokimov ◽  
...  

Current methods for high-throughput screening (HTS) use a serial process to evaluate compounds as inhibitors toward a single therapeutic target, but as the demand to reduce screening time and cost continues to grow, one solution is the development of multiplex technology. In this communication, the multiplex assay capability of a mass spectrometry (MS)–based readout system is verified using a kinase and esterase reaction simultaneously. Furthermore, the MS-based readout is shown to be compatible with a typical HTS workflow by identifying and validating several new inhibitors for each enzyme from a small library of compounds. These data confirm that it is possible to monitor inhibition of multiple therapeutic targets with one pass through the compound repository, thus demonstrating the potential for MS-based methods to become a method of choice for HTS of isolated enzymes.


Author(s):  
Hye Seon Kim ◽  
Bok-Kyu Shin ◽  
Jaehong Han

1997 ◽  
Vol 248 (3) ◽  
pp. 930-937 ◽  
Author(s):  
Helene Pelicano ◽  
Georges Maury ◽  
Abdelaziz Elalaoui ◽  
Manijeh Shafiee ◽  
Jean-Louis Imbach ◽  
...  

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