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

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Bozdag M, Dreker T, Henry C, Tosco P, Vallaro M, Fruttero R, Scozzafava A, Carta F, Supuran CT

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

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

PubMed ID

23265898 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Acetazolamide	Carbonic anhydrase 1	Ki (nM)	250	N/A	N/A	Details
Acetazolamide	Carbonic anhydrase 12	Ki (nM)	5.7	N/A	N/A	Details
Acetazolamide	Carbonic anhydrase 2	Ki (nM)	12	N/A	N/A	Details