Profiling Protein Arginine Deiminase 4 (PAD4): a novel screen to identify PAD4 inhibitors.
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 on 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.
Mesh Terms:
Arthritis, Rheumatoid, Chlortetracycline, Combinatorial Chemistry Techniques, Enzyme Inhibitors, Fluorescent Dyes, Hydrolases, Minocycline, Models, Biological, Molecular Structure, Streptomycin, Tetracycline
Arthritis, Rheumatoid, Chlortetracycline, Combinatorial Chemistry Techniques, Enzyme Inhibitors, Fluorescent Dyes, Hydrolases, Minocycline, Models, Biological, Molecular Structure, Streptomycin, Tetracycline
Bioorg. Med. Chem.
Date: Jan. 15, 2008
PubMed ID: 17964793
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