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Merck
CN

Novel small molecule protein arginine deiminase 4 (PAD4) inhibitors.

Bioorganic & medicinal chemistry letters (2012-12-26)
Murat Bozdag, Tobias Dreker, Christophe Henry, Paolo Tosco, Maura Vallaro, Roberta Fruttero, Andrea Scozzafava, Fabrizio Carta, Claudiu T Supuran
摘要

Protein arginin deaminase 4 (PAD4) is a calcium dependent enzyme which catalyses the conversion of peptidyl-arginine into peptidyl-citrulline and is implicated in several diseases such as rheumatoid arthritis (RA) and cancer. Herein we report the discovery of novel small-molecule, non peptidic PAD4 inhibitors incorporating primary/secondary guanidine moieties.

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Sigma-Aldrich
肽基精氨酸脱亚胺酶 来源于兔骨骼肌, buffered aqueous glycerol solution, ≥200 units/mg protein (Bradford)