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

About
Cited by
Related
Download options Please wait...

Supplementary files

Article information

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

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

Permissions

Request permissions

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

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements