The protein arginine deiminase 4 (PAD4) is a calcium-dependent enzyme, which catalyses the irreversible conversion of peptidyl-arginines into peptidyl-citrullines and plays an important role in several diseases such as in the rheumatoid arthritis, multiple sclerosis, Alzheimer's disease, Creutzfeldt-Jacob's disease and cancer. In this study, we report the inhibition profiles and computational docking toward the PAD4 enzyme of a series of 1,2,3-triazole peptidomimetic-based derivatives incorporating the beta-phenylalanine and guanidine scaffolds. Several effective, low micromolar PAD4 inhibitors are reported in this study.
Peptidomimetics as protein arginine deiminase 4 (PAD4) inhibitors / Trabocchi, A.; Pala, N.; Krimmelbein, I.; Menchi, G.; Guarna, A.; Sechi, M.; Dreker, T.; Scozzafava, A.; Supuran, C.T.; Carta, F.. - In: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY. - ISSN 1475-6374. - ELETTRONICO. - 30:(2015), pp. 466-471. [10.3109/14756366.2014.947976]
Peptidomimetics as protein arginine deiminase 4 (PAD4) inhibitors
Trabocchi, A.;Menchi, G.;Supuran, C. T.;Carta, F.
2015
Abstract
The protein arginine deiminase 4 (PAD4) is a calcium-dependent enzyme, which catalyses the irreversible conversion of peptidyl-arginines into peptidyl-citrullines and plays an important role in several diseases such as in the rheumatoid arthritis, multiple sclerosis, Alzheimer's disease, Creutzfeldt-Jacob's disease and cancer. In this study, we report the inhibition profiles and computational docking toward the PAD4 enzyme of a series of 1,2,3-triazole peptidomimetic-based derivatives incorporating the beta-phenylalanine and guanidine scaffolds. Several effective, low micromolar PAD4 inhibitors are reported in this study.
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