Profiling Protein Arginine Deiminase 4 (PAD4): A novel screen to identify PAD4 inhibitors

Bioorganic & Medicinal Chemistry
2008.0

Abstract

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.

Knowledge Graph

Similar Paper

Profiling Protein Arginine Deiminase 4 (PAD4): A novel screen to identify PAD4 inhibitors
Bioorganic & Medicinal Chemistry 2008.0
Novel small molecule protein arginine deiminase 4 (PAD4) inhibitors
Bioorganic & Medicinal Chemistry Letters 2013.0
The Development of N-α-(2-Carboxyl)benzoyl-N<sup>5</sup>-(2-fluoro-1-iminoethyl)-<scp>l</scp>-ornithine Amide (o-F-amidine) and N-α-(2-Carboxyl)benzoyl-N<sup>5</sup>-(2-chloro-1-iminoethyl)-<scp>l</scp>-ornithine Amide (o-Cl-amidine) As Second Generation Protein Arginine Deiminase (PAD) Inhibitors
Journal of Medicinal Chemistry 2011.0
Peptidylarginine deiminases 4 as a promising target in drug discovery
European Journal of Medicinal Chemistry 2021.0
Novel Inhibitors of Protein Arginine Deiminase with Potential Activity in Multiple Sclerosis Animal Model
Journal of Medicinal Chemistry 2013.0
Insights into the mechanism of streptonigrin-induced protein arginine deiminase inactivation
Bioorganic &amp; Medicinal Chemistry 2014.0
Rhodanine derivatives as novel inhibitors of PDE4
Bioorganic &amp; Medicinal Chemistry Letters 2008.0
Mining biologically-active molecules for inhibitors of fatty acid amide hydrolase (FAAH): Identification of phenmedipham and amperozide as FAAH inhibitors
Bioorganic &amp; Medicinal Chemistry Letters 2009.0
Thalidomide analogs and PDE4 inhibition
Bioorganic &amp; Medicinal Chemistry Letters 1998.0
A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis
Bioorganic &amp; Medicinal Chemistry Letters 2004.0