Literature DB >> 17409274

Development of a Transcreener kinase assay for protein kinase A and demonstration of concordance of data with a filter-binding assay format.

Karen L Huss1, Pauline E Blonigen, Robert M Campbell.   

Abstract

A Transcreener kinase fluorescence polarization (FP) assay has been developed for the serine/threonine kinase protein kinase A (PKA). The PKA Transcreener kinase assay is an homogenous, competitive antibody-based FP assay that uses Far Red Alexa Fluor 633-labeled adenosine 5' disphosphate (ADP) tracer and mouse monoclonal anti-ADP antibody. The Transcreener PKA assay was validated with both known PKA inhibitors and library compounds. The Transcreener PKA assay is resistant to low-wavelength (or common) fluorescent interference from small-molecule library compounds and generates IC50 results comparable with current radioactive filter-binding assay.

Entities:  

Mesh：

Substances：

Year:  2007        PMID： 17409274     DOI： 10.1177/1087057107300221

Source DB:  PubMed          Journal:  J Biomol Screen        ISSN： 1087-0571


  14 in total

1.  A basis for reduced chemical library inhibition of firefly luciferase obtained from directed evolution.

Authors:  Douglas S Auld; Ya-Qin Zhang; Noel T Southall; Ganesha Rai; Marc Landsman; Jennifer MacLure; Daniel Langevin; Craig J Thomas; Christopher P Austin; James Inglese
Journal:  J Med Chem       Date:  2009-03-12       Impact factor: 7.446

2.  Characterization and optimization of a red-shifted fluorescence polarization ADP detection assay.

Authors:  Karen M Kleman-Leyer; Tony A Klink; Andrew L Kopp; Thane A Westermeyer; Mark D Koeff; Brad R Larson; Tracy J Worzella; Cori A Pinchard; Sebastianus A T van de Kar; Guido J R Zaman; Jorrit J Hornberg; Robert G Lowery
Journal:  Assay Drug Dev Technol       Date:  2009-02       Impact factor: 1.738

3.  Comparison of bioluminescent kinase assays using substrate depletion and product formation.

Authors:  Cordelle Tanega; Min Shen; Bryan T Mott; Craig J Thomas; Ryan MacArthur; James Inglese; Douglas S Auld
Journal:  Assay Drug Dev Technol       Date:  2009-12       Impact factor: 1.738

Review 4.  Regulators of G-protein signaling and their Gα substrates: promises and challenges in their use as drug discovery targets.

Authors:  Adam J Kimple; Dustin E Bosch; Patrick M Giguère; David P Siderovski
Journal:  Pharmacol Rev       Date:  2011-07-07       Impact factor: 25.468

5.  Discovery of LY2457546: a multi-targeted anti-angiogenic kinase inhibitor with a novel spectrum of activity and exquisite potency in the acute myelogenous leukemia-Flt-3-internal tandem duplication mutant human tumor xenograft model.

Authors:  Timothy P Burkholder; Joshua R Clayton; Mark E Rempala; James R Henry; John M Knobeloch; David Mendel; Johnathan A McLean; Yan Hao; David A Barda; Eileen L Considine; Mark T Uhlik; Yuefeng Chen; Liandong Ma; Laura J Bloem; Jacqueline K Akunda; Denis J McCann; Manuel Sanchez-Felix; David K Clawson; Michael M Lahn; James J Starling
Journal:  Invest New Drugs       Date:  2011-03-01       Impact factor: 3.850

6.  High-throughput screening for RecA inhibitors using a transcreener adenosine 5'-O-diphosphate assay.

Authors:  Eliza J R Peterson; William P Janzen; Dmitri Kireev; Scott F Singleton
Journal:  Assay Drug Dev Technol       Date:  2011-12-22       Impact factor: 1.738

7.  Evaluating PI3 kinase isoforms using Transcreener ADP assays.

Authors:  Tony A Klink; Karen M Kleman-Leyer; Andrew Kopp; Thane A Westermeyer; Robert G Lowery
Journal:  J Biomol Screen       Date:  2008-06-19

8.  The human kinome and kinase inhibition.

Authors:  Krisna C Duong-Ly; Jeffrey R Peterson
Journal:  Curr Protoc Pharmacol       Date:  2013-03

9.  Development and validation of a high-density fluorescence polarization-based assay for the trypanosoma RNA triphosphatase TbCet1.

Authors:  Christophe Antczak; David Shum; Constantin Radu; Venkatraman E Seshan; Hakim Djaballah
Journal:  Comb Chem High Throughput Screen       Date:  2009-03       Impact factor: 1.339

10.  Two Galpha(i1) rate-modifying mutations act in concert to allow receptor-independent, steady-state measurements of RGS protein activity.

Authors:  Thomas Zielinski; Adam J Kimple; Stephanie Q Hutsell; Mark D Koeff; David P Siderovski; Robert G Lowery
Journal:  J Biomol Screen       Date:  2009-12
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.