A Generic High-Throughput Screening Assay for Kinases: Protein Kinase A as an Example-Reference-Cited by-同舟云学术

A Generic High-Throughput Screening Assay for Kinases: Protein Kinase A as an Example

Published:2003-04 Issue:2 Volume:8 Page:198-204
ISSN:1087-0571
Container-title:Journal of Biomolecular Screening
language:en
Short-container-title:J Biomol Screen

Author:

Mallari Rommel,Swearingen Elissa,Liu Wei,Ow Arnold,Young Stephen W.,Huang Shu-Gui¹

Affiliation:

1. Lead Discovery Department, AGY Therapeutics, Inc., 290 Utah Ave., South San Francisco, CA 94080. fhuang@agyinc.com

Abstract

A generic high-throughput screening assay based on the scintillation proximity assay technology has been developed for protein kinases. In this assay, the biotinylated33P-peptide product is captured onto polylysine Ysi bead via avidin. The scintillation signal measuring the product formation increases linearly with avidin concentration due to effective capture of the product on the bead surface via strong coulombic interactions. This novel assay has been optimized and validated in 384-well microplates. In a pilot screen, a signal-to-noise ratio of 5-to 9-fold and a Z′ factor ranging from 0.6 to 0.8 were observed, demonstrating the suitability of this assay for high-throughput screening of random chemical libraries for kinase inhibitors. ( Journal of Biomolecular Screening 2003:198-204)

Publisher

Elsevier BV

Link

http://journals.sagepub.com/doi/pdf/10.1177/1087057103252306

Reference26 articles.

1. Structural biology in drug design: selective protein kinase inhibitors

2. Gene-regulating protein kinases as important anti-inflammatory targets

3. Histidine Phosphorylation and Two-Component Signaling in Eukaryotic Cells

4. Growth factor signaling by receptor tyrosine kinases

5. Protein tyrosine phosphatases in signal transduction

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