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Literature summary extracted from

  • Knuckley, B.; Luo, Y.; Thompson, P.R.
    Profiling protein arginine deiminase 4 (PAD4): a novel screen to identify PAD4 inhibitors (2008), Bioorg. Med. Chem., 16, 739-745.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
3.5.3.15 drug development PAD4 is a leading target for the development of a rheumatoid arthritis pharmaceutical Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.5.3.15 5-aminosalicylic acid
-
 Homo sapiens
3.5.3.15 Azathioprine
-
 Homo sapiens
3.5.3.15 azithromycin
-
 Homo sapiens
3.5.3.15 clindamycin
-
 Homo sapiens
3.5.3.15 leflunomide
-
 Homo sapiens
3.5.3.15 methotrexate
-
 Homo sapiens
3.5.3.15 minocycline a mixed type inhibitor Homo sapiens
3.5.3.15 additional information PAD4 inhibitor screening based on a PAD4-targeted activity-based protein profiling reagent, denoted rhodamine-conjugated F-amidine, RFA, rapid competitive assay method development, overview Homo sapiens
3.5.3.15 streptomycin a competitive inhibitor of PAD4 Homo sapiens
3.5.3.15 sulfamethoxazole
-
 Homo sapiens
3.5.3.15 sulfapyridine
-
 Homo sapiens
3.5.3.15 trimethoprim
-
 Homo sapiens

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
3.5.3.15 Ca2+
-
 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
-
-
-

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 PAD4
-
 Homo sapiens
3.5.3.15 protein arginine deiminase 4
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.5.3.15 37
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.5.3.15 7.6
-
 assay at Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.5.3.15 additional information
-
 additional information inhibition kinetics Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.5.3.15 1.8
-
 pH 7.6, 37°C, recombinant PAD4 Homo sapiens streptomycin
3.5.3.15 2.4
-
 pH 7.6, 37°C, recombinant PAD4 Homo sapiens leflunomide
3.5.3.15 5.1
-
 pH 7.6, 37°C, recombinant PAD4 Homo sapiens clindamycin
3.5.3.15 7.5
-
 pH 7.6, 37°C, recombinant PAD4 Homo sapiens trimethoprim
3.5.3.15 8.1
-
 pH 7.6, 37°C, recombinant PAD4 Homo sapiens Azathioprine
3.5.3.15 10
-
 above, pH 7.6, 37°C, recombinant PAD4 Homo sapiens methotrexate
3.5.3.15 10
-
 above, pH 7.6, 37°C, recombinant PAD4 Homo sapiens 5-aminosalicylic acid
3.5.3.15 10
-
 above, pH 7.6, 37°C, recombinant PAD4 Homo sapiens sulfamethoxazole
3.5.3.15 10
-
 above, pH 7.6, 37°C, recombinant PAD4 Homo sapiens sulfapyridine
3.5.3.15 10
-
 above, pH 7.6, 37°C, recombinant PAD4 Homo sapiens azithromycin