کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1361620 981468 2008 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Profiling Protein Arginine Deiminase 4 (PAD4): A novel screen to identify PAD4 inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Profiling Protein Arginine Deiminase 4 (PAD4): A novel screen to identify PAD4 inhibitors
چکیده انگلیسی

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.

Herein we describe a novel screen for PAD4 inhibitors that is based on an Activity-Based Protein Profiling Reagent that covalently modifies PAD4 and renders it fluorescent.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 16, Issue 2, 15 January 2008, Pages 739–745
نویسندگان
, , ,