Application | Comment | Organism |
---|---|---|
pharmacology | PAD4 inhibitors F-and Cl-amidine represent potential lead compounds for the treatment of rheumatoid arthritis because a growing body of evidence supports a role for PAD4 in the onset and progression of this chronic autoimmune disorder | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
expression of PAD4 | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
additional information | IC50 values for amidine derivatives, overview, inhibition mechanism and structure-activity relationships, overview | Homo sapiens | |
N-alpha-benzoyl-N5-(2-chloro-1-iminoethyl)-L-ornithine amide | i.e. Cl-amidine, a PAD4 inactivator with enhanced potency | Homo sapiens | |
N-alpha-benzoyl-N5-(2-fluoro-1-iminoethyl)-L-ornithine amide | i.e. F-amidine, a potent and bioavailable irreversible inactivator of PAD4, structure of the PAD4-F-amidine-calcium complex, overview | Homo sapiens |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Ca2+ | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
protein-L-arginine + H2O | Homo sapiens | PAD4 is a transcriptional coregulator that catalyzes the calcium-dependent conversion of specific arginine residues in proteins to citrulline and plays a role in the onset and progression of the chronic autoimmune disorder rheumatoid arthritis | protein-L-citrulline + NH3 | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q9UM07 | isozyme PAD4 | - |
Purification (Comment) | Organism |
---|---|
recombinant Pad4 | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
N-alpha-benzoyl-L-arginine ethyl ester + H2O | - |
Homo sapiens | N-alpha-benzoyl-L-citrulline ethyl ester + NH3 | - |
? | |
protein-L-arginine + H2O | - |
Homo sapiens | protein-L-citrulline + NH3 | - |
? | |
protein-L-arginine + H2O | PAD4 is a transcriptional coregulator that catalyzes the calcium-dependent conversion of specific arginine residues in proteins to citrulline and plays a role in the onset and progression of the chronic autoimmune disorder rheumatoid arthritis | Homo sapiens | protein-L-citrulline + NH3 | - |
? |
Synonyms | Comment | Organism |
---|---|---|
PAD4 | - |
Homo sapiens |
protein arginine deiminase 4 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
8 | - |
assay at | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | inhibition kinetics | Homo sapiens | |
0.0059 | - |
N-alpha-benzoyl-N5-(2-chloro-1-iminoethyl)-L-ornithine amide | - |
Homo sapiens | |
0.0216 | - |
N-alpha-benzoyl-N5-(2-fluoro-1-iminoethyl)-L-ornithine amide | - |
Homo sapiens |