Title

A fluopol-ABPP HTS assay to identify PAD inhibitors

UMMS Affiliation

Department of Biochemistry and Molecular Pharmacology

Date

10-14-2010

Document Type

Article

Medical Subject Headings

Arthritis, Rheumatoid; Cell Line, Tumor; Drug Evaluation, Preclinical; Enzyme Inhibitors; Fluorescence Polarization; Fluorescent Dyes; High-Throughput Screening Assays; Humans; Hydrolases; Inhibitory Concentration 50; Streptonigrin

Disciplines

Biochemistry | Enzymes and Coenzymes | Medicinal-Pharmaceutical Chemistry | Therapeutics

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.

Rights and Permissions

Citation: Chem Commun (Camb). 2010 Oct 14;46(38):7175-7. doi: 10.1039/c0cc02634d. Link to article on publisher's site. Epub 2010 Aug 25.

Comments

At the time of publication, Paul Thompson was not yet affiliated with UMass Medical School.

Related Resources

Link to Article in PubMed