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Bioorg Med Chem Lett. 2013 Feb 1;23(3):715-9. doi: 10.1016/j.bmcl.2012.11.102. Epub 2012 Dec 2.

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

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  • 1Universit√† degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy.

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.

Copyright © 2012 Elsevier Ltd. All rights reserved.

PMID:
23265898
[PubMed - indexed for MEDLINE]
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