Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 16, Issue 2, Pages 739-745Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2007.10.021
Keywords
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Funding
- NIGMS NIH HHS [R01 GM079357-01A1, R01 GM079357] Funding Source: Medline
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Protein Arginine Deiminase 4 (PAD4) has emerged as a leading target for the development of a Rheumatoid Arthritis (RA) pharmaceutical. Herein, we describe the development of a novel screen for PAD4 inhibitors that is based oil a PAD4-targeted Activity-Based Protein Profiling reagent, denoted Rhodamine-conjugated F-Amidine (RFA), This screen was validated by screening 10 Disease Modifying Anti-Rheumatic Drugs (DMARDs) and identified streptomycin, minocycline, and chlortetracycline as micromolar inhibitors of PAD4 activity. (c) 2007 Elsevier Ltd. All rights reserved.
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