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Literature summary for 3.5.3.15 extracted from

  • Subramanian, V.; Knight, J.S.; Parelkar, S.; Anguish, L.; Coonrod, S.A.; Kaplan, M.J.; Thompson, P.R.
    Design, synthesis, and biological evaluation of tetrazole analogs of Cl-amidine as protein arginine deiminase inhibitors (2015), J. Med. Chem., 58, 1337-1344 .
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
N-[(1S)-1-(2-tert-butyl-2H-tetrazol-5-yl)-4-[(2-fluoroethanimidoyl)amino]butyl]benzamide preferentially inhibits protein-arginine deiminase 2 by 3fold with the highest selectivity being observed for PAD2 over PAD4. Highly selective protein-arginine deiminase 2 inhibitor relative to the other protein-arginine deiminases Homo sapiens
N-[(1S)-1-(2-tert-butyl-2H-tetrazol-5-yl)-4-[(2-fluoroethanimidoyl)amino]butyl][1,1'-biphenyl]-4-carboxamide preferentially inhibits protein-arginine deiminase 2 by 25fold with the highest selectivity being observed for PAD2 over PAD4. Highly selective protein-arginine deiminase 2 inhibitor relative to the other protein-arginine deiminases Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9UM07
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-
Homo sapiens Q9Y2J8
-
-

Source Tissue

Source Tissue Comment Organism Textmining
additional information PAD2 is expressed in most tissues and cell types Homo sapiens
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neutrophil PAD4 is primarily expressed in neutrophils Homo sapiens
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Synonyms

Synonyms Comment Organism
PAD2
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Homo sapiens
PAD4
-
Homo sapiens

General Information

General Information Comment Organism
metabolism the enzyme mediates histone hypercitrullination induces heterochromatin decondensation and chromatin unfolding to form neutrophil extracellular traps Homo sapiens