• Protein citrullination plays a role in several autoimmune diseases. (figshare.com)
  • Protein citrullination is a post-translational modification of arginine that controls a diverse array of cellular processes, including gene regulation, protein stability, and neutrophil extracellular trap (NET) formation. (umassmed.edu)
  • PADs cause post-translational deimination of proteins by converting arginine into citrulline (citrullination/deimination), resulting in structural and functional changes in target proteins. (westminster.ac.uk)
  • Peptidylarginine Deiminase Inhibitor Application, Using Cl-Amidine, PAD2, PAD3 and PAD4 Isozyme-Specific Inhibitors in Pancreatic Cancer Cells, Reveals Roles for PAD2 and PAD3 in Cancer Invasion and Modulation of Extracellular Vesicle Signatures. (open.ac.uk)
  • In the current study, we demonstrate that systemic inhibition of peptidylarginine deiminases (PADs), the enzymes mediating citrullination, through BB-Cl-amidine treatment, prevents diabetes development in NOD mice. (figshare.com)
  • Our results point to a role of citrullination in the pathogenesis of autoimmune diabetes, with PAD inhibition leading to disease prevention through modulation of immune pathways. (figshare.com)
  • Altogether, we are the first to demonstrate that NETs inhibition with Cl-amidine ameliorated neuroinflammation, neuronal apoptosis, and neurological deficits via STING-dependent IRE1α/ASK1/JNK signaling pathway after TBI. (biomedcentral.com)
  • Since PADs epigenetically regulate gene expression, we hypothesized that histone citrullination alters Dgcr8 expression thereby affecting miRNA biogenesis. (umassmed.edu)
  • Here, we used Cl-amidine, a selective inhibitor of NETs to investigate the role of NETs in neural damage after TBI. (biomedcentral.com)
  • In the pancreas, BB-Cl-amidine treatment preserved insulin production and was associated with a less destructive immune infiltrate, characterized by reduced frequencies of effector memory CD4 + T cells and a modest reduction in the frequency of IFNγ-producing CD4 + and CD8 + T cells. (figshare.com)
  • NETs inhibitor Cl-amidine treatment improved short-term neurological functions, reduced cerebral lesion volume, reduced brain edema, and restored cerebral blood flow (CBF) after TBI. (biomedcentral.com)
  • Thus, Cl-amidine treatment may provide a promising therapeutic approach for the early management of TBI. (biomedcentral.com)
  • To address the canonical pathway of NET formation-which involves generation of reactive oxygen species (ROS) and chromatin decondensation via histone citrullination by peptidyl arginine deiminase 4 (PAD4)-PMNs exposed to the medications were incubated with DPI (NADPH inhibitor), BB-Cl-amidine (PAD4 inhibitor) and muscarinic receptors antagonists. (nih.gov)
  • 7. GnRH Stimulates Peptidylarginine Deiminase Catalyzed Histone Citrullination in Gonadotrope Cells. (nih.gov)
  • They are using a novel, selective pharmacologic inhibitor of PAD2 (AFM30a), as well as a pan PAD inhibitor (BB-Cl-amidine) to evaluate whether this leads to inhibition of citrullination of vimentin. (nih.gov)
  • 1. Inducement of ER Stress by PAD Inhibitor BB-Cl-Amidine to Effectively Kill AML Cells. (nih.gov)
  • 2. Peptidylarginine Deiminase Inhibitor Application, Using Cl-Amidine, PAD2, PAD3 and PAD4 Isozyme-Specific Inhibitors in Pancreatic Cancer Cells, Reveals Roles for PAD2 and PAD3 in Cancer Invasion and Modulation of Extracellular Vesicle Signatures. (nih.gov)
  • 8. Suppression of colitis in mice by Cl-amidine: a novel peptidylarginine deiminase inhibitor. (nih.gov)
  • 9. The Peptidylarginine Deiminase Inhibitor Cl-Amidine Suppresses Inducible Nitric Oxide Synthase Expression in Dendritic Cells. (nih.gov)
  • 13. Controlled Delivery of Pan-PAD-Inhibitor Cl-Amidine Using Poly(3-Hydroxybutyrate) Microspheres. (nih.gov)
  • 11. Inhibition of PAD4-mediated NET formation by cl-amidine prevents diabetes development in nonobese diabetic mice. (nih.gov)
  • 2008). Specifically, citrullination happens during NETosis, a proinflammatory form of cell death that is aberrantly upregulated in numerous autoimmune diseases including RA, atherosclerosis, and lupus (Khandpur et al. (oscars2019info.com)
  • Hydralazine, but not procainamide, induced significant release of hydrogen peroxide in PMNs, and NET formation was inhibited by DPI and BB-Cl-amidine. (nih.gov)