Work

A fluopol-ABPP HTS assay to identify PAD inhibitors

Year: 2010

Type: article

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.

Source: Chemical Communications

DOI: 10.1039/c0cc02634d

Authors: Bryan Knuckley, Justin E. Jones, Daniel A. Bachovchin, Jessica Slack, Corey P. Causey, Steven J. Brown, Hugh Rosen, Benjamin F. Cravatt, Paul R. Thompson

Institutions: Scripps Research Institute, University of South Carolina

Language: English

Topic: Cancer-related gene regulation

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: green

Funders: National Cancer Institute, National Institute of General Medical Sciences

Awards: Chemical Probes Targeting the Protein Arginine Deiminases, G3510558551, G4749479223

OpenAlex ID: W2070324798

FWCI: 2.481

Cites: 25

Cited by: 89

Related to: 10