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.
Novel small molecule protein arginine deiminase 4 (PAD4) inhibitors / Bozdag, Murat; Dreker, Tobias; Henry, Christophe; Tosco, Paolo; Vallaro, Maura; Fruttero, Roberta; Scozzafava, Andrea; Carta, Fabrizio*; Supuran, Claudiu T.. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - ELETTRONICO. - 23:(2013), pp. 715-719. [10.1016/j.bmcl.2012.11.102]
Novel small molecule protein arginine deiminase 4 (PAD4) inhibitors
Bozdag, Murat;Scozzafava, Andrea;Carta, Fabrizio;Supuran, Claudiu T.
2013
Abstract
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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