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Literature summary 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

EC Number Inhibitors Comment Organism Structure
3.5.3.15 2-({(1S)-1-(2-tert-butyl-2H-tetrazol-5-yl)-4-[(2-chloroethanimidoyl)amino]butyl}carbamoyl)benzoic acid
-
 Homo sapiens
3.5.3.15 2-({(1S)-1-(2-tert-butyl-2H-tetrazol-5-yl)-4-[(2-fluoroethanimidoyl)amino]butyl}carbamoyl)benzoic acid
-
 Homo sapiens
3.5.3.15 2-{[(1S)-4-[(2-chloroethanimidoyl)amino]-1-(2H-tetrazol-5-yl)butyl]carbamoyl}benzoic acid 15fold selectivity versus PAD2 and PAD3; 15fold selectivity versus PAD2 and PAD3; 15fold selectivity versus PAD2 and PAD3; 15fold selectivity versus PAD2 and PAD3 Homo sapiens
3.5.3.15 2-{[(1S)-4-[(2-fluoroethanimidoyl)amino]-1-(2H-tetrazol-5-yl)butyl]carbamoyl}benzoic acid exhibits 20 to 30fold selectivity over isoform PAD2 and PAD3 when compared to PAD1; exhibits 20 to 30fold selectivity over isoform PAD2 and PAD3 when compared to PAD1; exhibits 20 to 30fold selectivity over isoform PAD2 and PAD3 when compared to PAD1; exhibits 20 to 30fold selectivity over isoform PAD2 and PAD3 when compared to PAD1 Homo sapiens
3.5.3.15 chloroamidine
-
 Homo sapiens
3.5.3.15 N-[(1S)-4-[(2-chloroethanimidoyl)amino]-1-(2H-tetrazol-5-yl)butyl]benzamide
-
 Homo sapiens
3.5.3.15 N-[(1S)-4-[(2-chloroethanimidoyl)amino]-1-(2H-tetrazol-5-yl)butyl][1,1'-biphenyl]-4-carboxamide
-
 Homo sapiens
3.5.3.15 N-[(1S)-4-[(2-fluoroethanimidoyl)amino]-1-(2H-tetrazol-5-yl)butyl]benzamide
-
 Homo sapiens
3.5.3.15 N-[(1S)-4-[(2-fluoroethanimidoyl)amino]-1-(2H-tetrazol-5-yl)butyl][1,1'-biphenyl]-4-carboxamide
-
 Homo sapiens
3.5.3.15 N-{(1S)-1-(2-tert-butyl-2H-tetrazol-5-yl)-4-[(2-chloroethanimidoyl)amino]butyl}benzamide
-
 Homo sapiens
3.5.3.15 N-{(1S)-1-(2-tert-butyl-2H-tetrazol-5-yl)-4-[(2-chloroethanimidoyl)amino]butyl}[1,1'-biphenyl]-4-carboxamide
-
 Homo sapiens
3.5.3.15 N-{(1S)-1-(2-tert-butyl-2H-tetrazol-5-yl)-4-[(2-fluoroethanimidoyl)amino]butyl}benzamide highly selective isoform PAD2 inhibitor; highly selective isoform PAD2 inhibitor; highly selective isoform PAD2 inhibitor; highly selective isoform PAD2 inhibitor Homo sapiens
3.5.3.15 N-{(1S)-1-(2-tert-butyl-2H-tetrazol-5-yl)-4-[(2-fluoroethanimidoyl)amino]butyl}[1,1'-biphenyl]-4-carboxamide preferentially inhibits isoform PAD2 by 3 to 25fold with the highest selectivity being observed for PAD2 over PAD4; preferentially inhibits isoform PAD2 by 3 to 25fold with the highest selectivity being observed for PAD2 over PAD4; preferentially inhibits isoform PAD2 by 3 to 25fold with the highest selectivity being observed for PAD2 over PAD4; preferentially inhibits isoform PAD2 by 3 to 25fold with the highest selectivity being observed for PAD2 over PAD4 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.5.3.15 protein L-arginine + H2O Homo sapiens
-
 protein L-citrulline + NH3
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
3.5.3.15 Homo sapiens Q9ULC6
-
-
3.5.3.15 Homo sapiens Q9ULW8
-
-
3.5.3.15 Homo sapiens Q9UM07
-
-
3.5.3.15 Homo sapiens Q9Y2J8
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.5.3.15 protein L-arginine + H2O
-
 Homo sapiens protein L-citrulline + NH3
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.5.3.15 PAD1 isoform Homo sapiens
3.5.3.15 PAD2 isoform Homo sapiens
3.5.3.15 PAD3 isoform Homo sapiens
3.5.3.15 PAD4 isoform Homo sapiens