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

Bozdag, Murat; Dreker, Tobias; Henry, Christophe; Tosco, Paolo; Vallaro, Maura; Fruttero, Roberta; Scozzafava, Andrea; Carta, Fabrizio; Supuran, Claudiu T.

Affiliation

Bozdag M; Università degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy.

Bioorg Med Chem Lett ; 23(3): 715-9, 2013 Feb 01.

Article in En | MEDLINE | ID: mdl-23265898

ABSTRACT

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.

Subject(s)

Enzyme Inhibitors/chemical synthesis; Enzyme Inhibitors/pharmacology; Hydrolases/antagonists & inhibitors; Enzyme Activation/drug effects; Enzyme Inhibitors/chemistry; Guanine/chemistry; Humans; Inhibitory Concentration 50; Models, Molecular; Molecular Structure; Protein-Arginine Deiminase Type 4; Protein-Arginine Deiminases

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Enzyme Inhibitors / Hydrolases Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2013 Type: Article Affiliation country: Italy

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