Issue 38, 2010
From the journal:

Chemical Communications

A fluopol-ABPP HTS assay to identify PADinhibitors†‡

Bryan Knuckley,ab   Justin E. Jones,ab   Daniel A. Bachovchin,c   Jessica Slack,ab   Corey P. Causey,b   Steven J. Brown,c   Hugh Rosen,c   Benjamin F. Cravattc  and  Paul R. Thompson*ab  

* Corresponding authors

a Department of Chemistry, The Scripps Research Institute, Scripps Florida, 120 Scripps Way, Jupiter, Florida, USA
E-mail: Pthompso@scripps.edu
Fax: +1 561-228-3050
Tel: +1 561-228-2860

b Department of Chemistry & Biochemistry, University of South Carolina, 631 Sumter Street, Columbia, SC, USA

c Department of Chemical Physiology, The Scripps Research Institute, 10550 N. Torrey Pines Rd., La Jolla, CA, USA

Abstract

Protein Arginine Deiminase (PAD) activity is dysregulated in numerous diseases, e.g., Rheumatoid Arthritis. Herein we describe the development of a fluorescence polarization-Activity Based Protein Profiling (fluopol-ABPP) based high throughput screening assay that can be used to identify PAD-selective inhibitors. Using this assay, streptonigrin was identified as a potent, selective, and irreversible PAD4 inactivator.

Graphical abstract: A fluopol-ABPP HTS assay to identify PAD inhibitors

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Article information

DOI
https://doi.org/10.1039/C0CC02634D
Article type
Communication
Submitted
17 jul 2010
Accepted
30 jul 2010
First published
25 aug 2010

Chem. Commun., 2010,46, 7175-7177

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A fluopol-ABPP HTS assay to identify PAD inhibitors

B. Knuckley, J. E. Jones, D. A. Bachovchin, J. Slack, C. P. Causey, S. J. Brown, H. Rosen, B. F. Cravatt and P. R. Thompson, Chem. Commun., 2010, 46, 7175 DOI: 10.1039/C0CC02634D

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